United States
               Environmental Protection
               Agency
               Environmental Criteria and
               Assessment Office
               Cincinnati OH 45268
EPA/600/8-86/018A
June 1986
Review Draft
               Research and Development
&ERA
Health Assessment
Document for
Polychlorinated
Dibenzofurans
 Review
 Draft
 (Do Not
 Cite or Quote)
                            NOTICE

               This document is a preliminary draft. It has not been formally
               released by the U.S. Environmental Protection Agency and
               should not at this stage be construed to represent Agency policy.
               It is being circulated for comments on its technical accuracy and
               policy implications.

-------
(Do Not                                       EPA/600/8-86/018A
Cite or Quote)                                          June 1986
                                                   Review Draft
     Health Assessment  Document for
       Polychlorinated  Dibenzofurans
                            NOTICE

           This document is a preliminary draft It has not been formally
           released by the U S Environmental Protection Agency and
           should not atthis stage be construed to represent Agency policy
           It is being circulated for comment son its technical accuracy and
           policy implications
             Environmental Criteria and Assessment Office
             Office of Health and Environmental Assessment
                 Office of Research and Development
                U.S. Environmental Protection Agency
                      Cincinnati, OH 45268

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                                  DISCLAIMER







    This report  1s  an external draft  for  review purposes only and  does not



constitute  Agency  policy.   Mention of  trade names  or  commercial  products



does not constitute endorsement or recommendation for use.
                                       11

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                                   PREFACE

    The  Office of  Health  and  Environmental  Assessment  has  prepared  this
Health Assessment  Document  on polychloHnated  dlbenzofurans  at the  request
of the Office of Air Quality Planning and Standards.

    In the  development  of  this assessment  document,  the  scientific  litera-
ture has been  Inventoried,  key  studies have been evaluated, and summary  and
conclusions  have  been  prepared  such  that  the  toxldty of polychlorlnated
dlbenzofurans  1s  qualitatively  and,  where  possible,  quantitatively  Identi-
fied.  Observed effect  levels and dose-response relationships are  discussed
where  appropriate  In order  to  Identify the  critical  effect and  to  place
adverse health responses 1n  perspective with observed  environmental  levels.

    This  document  was  reviewed by  a panel of  expert scientists during  the
peer review  workshop held  at U.S.  EPA,  Cincinnati,  OH, on May  29 and  30,
1986.
                                     111

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                             DOCUMENT DEVELOPMENT
Debdas Mukerjee, Ph.D., Document Manager and Project Officer
Environmental Criteria and Assessment Office,  Cincinnati
U.S. Environmental Protection Agency
Authors

Chapter 1:  Introduction, D. Mukerjee,  Ph.D.

Chapter 2:  Physical and Chemical Properties,  S.S.  Que Hee,  Ph.D.

Chapter 3:  Sampling and Analysis, S.S. Que Hee,  Ph.D.

Chapter 4:  Sources 1n the Environment, S.S.  Que  Hee, Ph.D.,
            S. Garattlnl, M.D. and A.  JoM, Ph.D.

Chapter 5:  Environmental Fate, Transport and Distribution,
            S. Garattlnl, M.D., A. Jor1, Ph.D. and  S.S. Que  Hee, Ph.D.

Chapter 6:  Environmental Levels and Exposure, S.S. Que Hee, Ph.D.,
            S. Garattlnl, M.D. and A.  Jorl, Ph.D.

Chapter 7:  Toxlcologlcal Effects 1n Man and Animals

            Sections 7.1. through 7.4.  and 7.8. —  S. Garattlnl, M.D.
                                                  A. JoM, Ph.D.

            Section 7.5. —                       G.L. Klmmel, Ph.D.

            Section 7.6. --                       S. Rosenthal, Ph.D.

            Section 7.7.1. —                     S. Garattlnl, M.D.
                                                  A. JoM, Ph.D.
                                                  C. Hlremath, Ph.D.

            Section 7.7.2. —                     D. Bayllss, M.S.

Chapter 8:  Effects of Major Concern and Health Risk Assessment,
            D. Mukerjee, Ph.D.
                                      1v

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           PolychloMnated Dlbenzofurans Peer Review Panel Members
                             May 29 and 30,  1986
                               Cincinnati,  Ohio
Co-chairmen:
Dr. Jerry F.  Stara
Environmental Criteria and Assessment Office
U.S. Environmental Protection Agency
Cincinnati, Ohio

Dr. Debdas Mukerjee
Environmental Criteria and Assessment Office
U.S. Environmental Protection Agency
Cincinnati, Ohio
                                    Members
Dr. Linda Blrnbaum
Systemic Toxicology Branch
Natl. Institute of Environmental Health
  Sciences
Research Triangle Park, NC

Mr. David L. Bayllss
Carcinogen Assessment Group
Office of Health and Environmental
  Assessment
U.S. Environmental Protection Agency
Washington, DC

Dr. G. Choudhary
Division of Physical Sciences and
  Engineering
National Institute for Occupational
  Safety and Health
Cincinnati, OH

Dr. Thomas A. Gas1ew1cz
Dept. of Radiation Biology and
  Biophysics
University of Rochester
Rochester, NY

Dr. AUstalr W.M. Hay
Department of Chemical Pathology
Old Medical School
The University of Leeds
Leeds, United Kingdom

Dr. Charallngayya B. Hlremath
Carcinogen Assessment Group
Office of Health and Environmental
  Assessment
U.S. Environmental Protection Agency
Washington, DC
                           Dr. Otto Hutzlnger
                           Lehrstuhl fur Okologlsche Chemle
                             und Geochemle
                           Un1vers1tat Bayreuth
                           Bayreuth, Federal Republic of
                             Germany

                           Dr. Armanda Jor1
                           InstHut d1 Rlcerche Farmaco-
                             loglche "Mario Negrl"
                           Mllano, Italy

                           Dr. Gary Klmmel
                           Reproductive Effects Assessment
                             Group
                           Office of Health and Environmental
                             Assessment
                           U.S. Environmental Protection Agency
                           Washington, DC

                           Dr. Edo D. PelHzzaM
                           Analytical and Chemical Sciences
                           Research Triangle Institute
                           Research Triangle Park, NC

                           Dr. Shane S. Que Hee
                           Ketterlng Laboratory
                           Department of Environmental Health
                           University of Cincinnati Medical
                             Center
                           Cincinnati, OH

                           Dr. Chrlstoffer Rappe
                           Department of Organic Chemistry
                           Umea Un1vers1tet
                           Umea, Sweden

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                               Members  (cont.)
Dr. John J. Ryan
Health Protection Branch/Food Division
Health and Welfare — Canada
Ottawa, Ontario, Canada

Dr. Steven H. Safe
Department of Veterinary Physiology
  and Pharmacology
College of Veterinary Medicine
Texas A&M University
College Station, TX

Dr. Arnold J. Schecter
Department of Preventive Medicine
Upstate Medical Center, College of
  Medicine
Blnghamton, NY
Dr. RHa Schoeny
Environmental Criteria and
  Assessment Office
U.S. Environmental Protection Agency
Cincinnati, OH

Dr. Stanlslaw Tarkowskl
World Health Organ1zat1on/EMRO
Copenhagen, Denmark

Dr. Michael L. Taylor
Brehm Laboratory
Wright State University
Dayton, OH
          Only  written  comments were  sent  by  the  following  reviewers:
Dr. Jerry N. Blancato
Exposure Assessment Group
Office of Health and Environmental
  Assessment
U.S. Environmental Protection Agency
Washington, DC

Dr. David H. Cleverly
Office of A1r Quality Planning and
  Standards
U.S. Environmental Protection Agency
Washington, DC

Mr. William G. Ewald
Environmental Criteria and Assessment
  Office
U.S. Environmental Protection Agency
Research Triangle Park, NC

Dr. Fred Hlleman
Monsanto Company
St. Louis, MO
Dr. Charles H. Nauman
Exposure Assessment Group
Office of Health and Environmental
  Assessment
U.S. Environmental Protection Agency
Washington, DC

Dr. Ellen Sllbergeld
Environmental Defense Fund
Washington, DC

Dr. David Stalling
Columbia National Fisheries Research
  Laboratory
U.S. Fish and Wildlife Service
Columbia, MO
                                      vl

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                             TABLE OF CONTENTS

                                                                       Page
1.  INTRODUCTION	   1-1

2.  PHYSICAL AND CHEMICAL PROPERTIES	2-1

    2.1.   SUMMARY	;	2-1
    2.2.   INTRODUCTION	2-2
    2.3.   PHYSICAL PROPERTIES	2-3

           2.3.1.   Molecular Structure 	  2-3
           2.3.2.   Melting Points	2-3
           2.3.3.   Solubility	2-15
           2.3.4.   Partition Coefficients	2-15
           2.3.5.   Boiling Points and Vapor Pressures	2-15
           2.3.6.   Adsorption and Desorptlon 	  2-15
           2.3.7.   Miscellaneous Properties	2-19
           2.3.8.   Spectroscoplc Properties	2-19

    2.4.   CHEMICAL REACTIONS 	  2-22

           2.4.1.   General 	  2-22
           2.4.2.   PhotodecomposHlon	2-28
           2.4.3.   Pyrolysls 	  2-33

    2.5.   SYNTHESIS	2-37

           2.5.1.   General Methods 	  2-37
           2.5.2.   Methods for PHDFs 	  2-38

3.  SAMPLING AND ANALYTICAL METHODS 	  3-1

    3.1.   SUMMARY	3-1
    3.2.   SAMPLING METHODS 	  3-2

           3.2.1.   Incinerators	3-2

    3.3.   GC METHODS FOR THE PCDFs	3-4

           3.3.1.   Packed Column GC	  3-4
           3.3.2.   Representative Sample Preparations and
                    Methods of Analysis	3-9

    3.4.   GC/MS METHODS FOR PBDFs	3-44
    3.5.   OTHER METHODS FOR PCDFs	3-46
                                     vll

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                          TABLE  OF  CONTENTS  (cont.)

                                                                       Page
4.  SOURCES IN THE ENVIRONMENT	4-1

    4.1.   SUMMARY	      4-1
    4.2.   SOURCES OF PCDFs FROM CHEMICALS	4-1

           4.2.1.   Chlorinated Phenols 	  4-2
           4.2.2.   PCDFs 1n Polychlorlnated Blphenyls	4-10
           4.2.3.   PCDFs In Phenoxy Herbicides 	  4-19
           4.2.4.   PCDFs In Chlorodlphenyl Ether Herbicides
                    (PCDPE)	4-23
           4.2.5.   PCDFs 1n Hexachlorobenzene	4-25
           4.2.6.   PCDFs 1n Hexachlorophene	4-25
           4.2.7.   PCDFs In PBBs	4-25
           4.2.8.   PCDFs 1n Metal Salts	4-26

    4.3.   PHOTOCHEMICAL PRODUCTION 	  4-26
    4.4.   SOURCES OF PCDF FROM BURNING AND OTHER HIGH
           TEMPERATURE PROCESSES	4-29

           4.4.1.   Thermal Degradation of Technical Products ....  4-29
           4.4.2.   Incineration of Municipal  Waste 	  4-37
           4.4.3.   Sewage Sludge Combustion	4-50
           4.4.4.   Electrical Equipment Fires	4-51
           4.4.5.   Incineration of Hazardous  Waste 	  4-51
           4.4.6.   Car Exhaust	4-54
           4.4.7.   Other Sources 	  4-54

5.  ENVIRONMENTAL FATE, TRANSPORT AND DISTRIBUTION	5-1

    5.1.   SUMMARY	5-1
    5.2.   INTRODUCTION	5-1
    5.3.   ENVIRONMENTAL TRANSPORT	5-2

           5.3.1.   Air	5-2
           5.3.2.   Water 	  5-4
           5.3.3.   Soil	5-4

    5.4.   ENVIRONMENTAL TRANSFORMATION 	  5-5

           5.4.1.   Abiotic Transformation	5-5
           5.4.2.   Blotransformatlon 	  5-5

    5.5.   BIOACCUMULATION	5-6

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                         TABLE OF CONTENTS  (cont.)

                                                                       Page
6.  ENVIRONMENTAL LEVELS AND EXPOSURE 	   6-1

    6.1.   SUMMARY	6-1
    6.2.   ENVIRONMENTAL LEVELS 	   6-1

           6.2.1.   Introduction.	   6-1
           6.2.2.   In Soil and Sediments	6-2
           6.2.3.   In Plants	6-5
           6.2.4.   In Aquatic Organisms	6-8
           6.2.5.   In Birds	6-16
           6.2.6.   In Terrestrial Animals	6-17

    6.3.   EXPOSURE	6-18

           6.3.1.   Food	6-18
           6.3.2.   Air	6-20
           6.3.3.   Other Exposure Routes 	   6-20

7.  TOXICOLOGICAL EFFECTS IN MAN AND EXPERIMENTAL ANIMALS 	   7-1

    7.1.   SUMMARY OF  EFFECTS OF POLYCHLORINATED DIBENZOFURANS.  ...   7-1

           7.1.1.   Tox1cok1net1cs	7-1
           7.1.2.   Toxlclty	7-3
           7.1.3.   Epidemiology	7-5

    7.2.   INTRODUCTION	7-6
    7.3.   TOXICOKINETICS	7-7

           7.3.1.   Introduction	7-7
           7.3.2.   Absorption	7-7
           7.3.3.   Distribution,  Metabolism and Excretion	7-8
           7.3.4.   Metabolic Fate	7-42

    7.4.   ACUTE, SUBACUTE AND CHRONIC TOXICITY 	   7-47

           7.4.1.   Acute Toxlclty	7-47
           7.4.2.   Subacute Toxlclty 	   7-49
           7.4.3.   Chronic Toxlclty	7-53
           7.4.4.   Contribution of PCDF to the Toxlclty of
                    Industrial Products and Environmental
                    Contaminants	7-53
           7.4.5.   Some Particular Aspects of the Toxic Reactions.  .   7-59
                                     1x

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                         TABLE OF CONTENTS (cont.)

                                                                       Page
    7.5.    REPRODUCTIVE/DEVELOPMENTAL  TOXICITY	7-78

           7.5.1.    Introduction	7-78
           7.5.2.    Development  	   7-78
           7.5.3.    Reproductive  Function/Fertility  	   7-84
           7.5.4.    Summary 	   7-85

    7.6.    MUTAGENICITY	7-86
    7.7.    CARCINOGENICITY	7-87

           7.7.1.    Animal	7-87
           7.7.2.    Human 	   7-88

    7.8.    EPIDEMIOLOGY -- SYSTEHIC TOXIC EFFECTS 	   7-89

           7.8.1.    The Japanese  Incident (Yusho disease)  	   7-90
           7.8.2.    The Taiwan Incident ("Yu-Cheng"  disease)	   7-93
           7.8.3.    The Blrmlnghamton, NY Transformer  Accident.  .  .  .   7-95

8.  EFFECTS OF MAJOR CONCERN AND  HEALTH HAZARD  ASSESSMENT  	   8-1

    8.1.    EXISTING GUIDELINES AND STANDARDS	8-1
    8.2.    CURRENT LEVELS OF EXPOSURE  	   8-1
    8.3.    HIGH RISK POPULATIONS	8-2
    8.4.    BASIS AND DETERMINATION OF  RISK	8-3

           8.4.1.    Estimation of LOAELs	8-4
           8.4.2.    Derivation of Reference Dose (RfD)	8-6

9.  REFERENCES	9-1

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                               LIST OF TABLES

No.                               Title                                Page

2-1     Chemical Abstracts System Registry Numbers (CAS-RN) for
        PHDFs	2-4

2-2     X-Ray Crystallographlc Indices of Some Selected PHDFs ....  2-9

2-3     Melting and Boiling Points of Some PHDFs	2-10

2-4     The Logarithm of Octanol/Water Partition Coefficients (Kow)
        of Some PHDFs from HPLC Methods 	  2-16

2-5     Vapor Densities and Pressures of PCDFs as Estimated from
        a Gas Chromatographlc Method	2-17

2-6     Ultraviolet Absorption Maxima and Molar Absorptlvltles
        for Some Substituted PBDFs	2-20

2-7     Absorption Maxima of Some  PCDFs In Chloroform  	  2-21

2-8     Proton NMR Data for Some PCDFs	2-23

2-9     FMedel-Crafts Acetylatlon of Substituted PHDFs	2-29

2-10    ChloMnatlon of TrCDF with Antimony Pentachlor1de/CCl4
        Reagent to Produce TCDFs	2-30

2-11    Photodegradatlon of TCDFs  (1  yg/ml) at 254 nm  After
        4 Hours of Irradiation In  Hexane or Tetradecane 	  2-34

2-12    Photodecomposltlon of PeCDFs  In Hexane at 254  nm	2-35

2-13    Formation of PCDFs from  the  Pyrolysls of Specific  PCBs.  .  .  .  2-40

2-14    Formation of PCDFs from  Pyrolysls of Chlorobenzenes  	  2-44

2-15    Synthetic Methods for PCDFs  using Chlorinated  Dlphenyl
        Ethers  (CDPEs) as Substrates	2-46

3-1     Relative Intensities of  Ions  Containing from One  to  Eight
        Chlorine Atoms	3-11

3-2     Percent Intensities of the Major Ions In the Mass  Spectra
        of  Isomerlc PCDFs	3-14

3-3     Exact Molecular Weights  of the PCDFs	3-16

3-4     Characteristics of Some  Glass Capillary Columns for
        Separating PCDFs	3-22
                                      x1

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                           LIST OF TABLES (cont.)

No.                               Title                                page

3-5     Relative Retention Times of PCDFs and PCDDs on the
        Capillary Columns of Table 3-4	3-24

3-6     Relative Retention Times (RRT) and Relative Response
        Factors (RRF) for PCDFs Synthesized as Reference Standards. .  3-29

3-7     Error 1n Estimation of PCDFs by Six Methods	3-42

4-1     Presence of PCDFs 1n Industrial  Chemicals and
        Their Entry Into the Environment	4-3

4-2     Estimated PCDD and PCDF Release to the Canadian
        Environment from Chemical Sources 	  4-4

4-3     Chemical Analysis of a Typical Pure and Technical
        Pentachlorophenol 	  4-5

4-4     Levels of PCDFs and PCDDs 1n Some Commercial Chlorophenols. .  4-6

4-5     Order of Abundance of PCDFs 1n European Chlorophenols ....  4-9

4-6     PCDF Content 1n Some PCBs and 1n Kaneml 011	4-14

4-7     Suspected Maximum Levels of Toxic PCDFs 1n Various
        PCBs and In Kaneml 011	4-16

4-8     PCDFs 1n Commercial PCBs	4-20

4-9     PCDFs and PCDDs 1n Phenoxy Herbicides 	  4-22

4-10    Levels of PCDDs and PCDFs 1n Commercial Dlphenyl Ether
        Herbicides	4-24

4-11    PCDFs and PCDDs In Several Metal Salts	4-27

4-12    Estimated PCDD and PCDF Releases to the Canadian
        Environment from Combustion Sources 	  4-30

4-13    Pyrolysls Products of Aroclor 1254 1n a Quartz Tube for
        Pyrolysls Time of 3 Seconds	4-32

4-14    Levels of Trapped PCDFs and PCDDs on Charcoal  from
        Burning Chlorophenolate-Impregnated Leaves and Wood Wool.  . .  4-34

4-15    Production of PCDDs and PCDFs after 0.6 to 1.00 Second
        Pyrolysls In Air of 2-Butoxyethyl-2,4,5-TMchloro-
        phenoxyacetate	4-36

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                           LIST OF TABLES (cont.)

No.                               Title                                Page

4-16    PCDF Composition of Municipal Incinerator Fly Ash
        Resulting from Electrostatic Precipitation	4-39

4-17    PCDF Composition of Stack Effluent of Municipal
        Incinerators	4-41

4-18    Influence of Type of Waste on PCDF Formation	4-43

4-19    Annual Toxic Equivalent of CDBFs Emitted by Netherlands
        Incinerators In Terms of 2,3,7,8-TCDD Toxic Equivalents .  .  .  4-47

4-20    Levels of PCDD and PCDF from MSW Incineration, Umea 	  4-48

4-21    PCDFs Formed During PCB Fires 	  4-52

6-1     Levels of PCDFs 1n Environmental Media	6-3

6-2     Ranges of 2,3,7,8-TCDD and PCDFs 1n Top Soil and
        Biological Samples In ppt fresh weight In a Dutch
        Hazardous Waste Dump	6-6

6-3     PCDF Residues In Wildlife	6-10

6-4     PCDF Distribution In Pond Known to be Contaminated
        by Aroclor 1260	6-12

6-5     Levels of Toxic PCDF Isomers 1n Wild Animals	6-14

7-1     Percentages of the Total Intake of Original PCDF Isomers
        Found 1n the Livers of Monkeys and Rats	7-10

7-2     Concentration of "C-2.3.7.8-TCDF 1n Tissues of Male
        Fisher 344 Rats	7-11

7-3     Distribution of Radioactivity 3 Days After Administration
        of 14C-2,3,7,8-TCDF to 200-250 g Male Fisher 344 Rats  ....  7-13

7-4     Components for the Elimination of Radioactivity from
        Tissues of Fisher 344 Rats	7-14

7-5     Excretion of 2,3,7,8-TCDF-Der1ved Radioactivity by
        Three Mice	7-17

7-6     Distribution of 2,3,7,8-TCDF-Derlved Radioactivity 1n
        Three Rhesus Monkeys 21 Days After Treatment	7-19

7-7     Distribution of 2,3,7,8-TCDF-Der1ved Radioactivity During
        the First 24 Hours 1n Liver, Fat and Skin of Bulnea P1gs. .   .  7-21

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                           LIST OF  TABLES (cont.)

No.                               Title                                Page

7-8     2,3,7,8-TCDF Pharmacoklnetlc Parameters for Physiological
        Model	7-24

7-9     Concentrations of PCBs, PCDFs and PCQs 1n  the Rice 011s
        from Japan and Taiwan	7-26

7-10    Concentrations of PCDF Congeners 1n the Tissues of the
        Deceased Patient with Yu-Cheng 1n Taiwan	7-28

7-11    Structural Assignments by PCDF Congeners 1n the Toxic
        Rice-Bran 011 Ingested by the Deceased Yu-Cheng Patient . .  .  7-29

7-12    PCB and PCDF Concentrations In Liver and Adipose Tissue
        of Deceased Yusho Patients	7-30

7-13    Levels of PCDF (pg/g) and PCB (ng/g) 1n Tissue Samples of a
        Baby from a Woman from Taiwan Suffering from Yusho Disease.  .  7-31

7-14    Relationship Between the Amount of R1ce 011 Used by Yusho
        Patients, Amounts of PCBs and PCDFs Ingested, and Clinical
        Severity	7-32

7-15    Concentrations of PCBs, PCDFs and PCQs 1n  the Tissues of
        Yusho Patients, Unexposed Individuals and  in the M1lk Fat
        of a Worker Occupatlonally Exposed to PCBs	7-34

7-16    Levels of PCDD and PCDF 1n Blood Samples from Workers 1n
        the Saw Mill Industry After Exposure to 2,3,4,6-Tetra-
        chlorophenolate 	  7-36

7-17    Levels of PCDD and PCDF 1n Blood Samples from Workers In
        the Textile and Leather Industry After Exosure to
        Pentachlorophenol (PCP) or  PCP Derivatives	7-37

7-18    Levels of PCDF In Tissue Samples of a Worker Exposed to
        Phenoxy Herbicides	7-38

7-19    Half-lives and Contents of  PCDDs and PCDFs 1n
        Human Adipose Tissue	7-40

7-20    PCDD and PCDF Levels 1n Blnghamton, New York Adipose
        Tissue Levels (ppt) 1n Exposed and Unexposed Subjects ....  7-41

7-21    Levels (pg/g) of PCDDs and PCDFs 1n Human  Samples from
        Sweden, U.S.A. and Vietnam Subjects 	  7-43

7-22    2,3,7,8-ChloMne-Substltuted PCDDs and PCDFs 1n Human
        Unexposed Subject 	  7-44
                                     xlv

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                           LIST OF TABLES (cont.)

No.                               Title                                Page

7-23    Total PCDD and PCDF Levels (pg/g) 1n Tissue Samples from
        an Unexposed Subject	7-45

7-24    Levels of PCDDs and PCDFs In Breast M1lk	7-46

7-25    Summary of Pathologic Effects of 2,3,7,8-Tetra-CDBF
        1n Rhesus Monkeys	7-50

7-26    Acute Tox1c1ty of 2,3,7,8-TCDF 1n Several Animal Species. .  .  7-51

7-27    Subacute Tox1c1ty of PCDFs 1n Laboratory Animals	7-54

7-28    Probable Contributions of PCDF In Aroclor 1260 and Pure
        2,4,5,2',4',5'-Hexachlorob1phenyl to the Toxlclty 1n
        Rabbits of PCBs Applied at 120 mg/50 cm2	7-57

7-29    Effects of Different PCDF Congeners on Rat Hepatic
        Cytosollc Receptor Binding Avidities, AHH and EROD
        Induction 1n Rat Hepatoma H-4-II E Cells	7-72

7-30    Signs and Symptoms of Yusho Disease In Adult Japanese ....  7-91
                                     xv

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                               LIST  OF  FIGURES

No.                               Title                                Page

2-1     Possible Reaction Schemes to Produce PCDFs from the
        Pyrolysls of 2,2' ,4,4' ,5,5'-Hexachlorob1phenyl ........  2-42

3-1     Mass Spectral Behavior of PCOFs ...............  3-12

3-2     Low Resolution Mass Spectra of (A) TrCDF, (B) TCOF,
        (C) PeCDF, (D) HxCDF and (E) OCDF ..............  3-17

3-3     Mass Chromatograms of (A) 2,3,4,6-Tetrachlorophenol and
        (B) Pentachlorophenol Showing the Elutlon of PCDF ......  3-19

3-4     Mass Chromatograms (OV-101 Glass Capillary Column at
        197°C) of "Yusho" 011 Showing Elutlon of PCDF ........  3-25

4-1     Comparison of Specific Ion Current Profiles after
        Chromatography of "Yusho" 011 ................   4-18
7-1     A plot of the -log ECso Values for AHH Induction 1n Rat
        Hepatoma H-4-IIE Cells vs. the jm vivo -log £059 Values
        for Thymlc Atrophy (top) and Body Weight Loss (bottom)
        for Several PCDFs, 2,3,7,8-TCDD and a Reconstituted PCDF
        Mixture ...........................  7-74
                                     xv1

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                               1.  INTRODUCTION

    Polychlorlnated  dlbenzofurans   (PCDFs)  are  members  of  a  group  of  the
widespread and  environmentally  stable halogenated tMcycHc  aromatic  hydro-
carbons.   This  group  1s  structurally  similar  to polychlorlnated  blphenys
(PCBs), polychlorlnated  napthalenes  (PCNs),  polychlorlnated  d1benzo-£d1ox1ns
(PCDDs),  polybromlnated  blphenyls   (PBBs)  and polychlorlnated  blphenylenes.
PCDFs are not deliberately disseminated In  the environment as primary  Indus-
trial products, but  enter  the environment as  unintentional  trace Impurities
1n PCBs,  chlorinated  phenols,  PCNs, 2,4,5-T formulations and as  a  result of
diverse combustion  processes.   PCDFs have  been  detected  In fly ash and In
flue gas  from municipal  and  Industrial  Incinerators, and have  been  found to
bloaccumulate 1n  seal,  fish, turtle  and  human adipose tissue.   Residues of
PCDFs have  also been  detected  In   human  breast  milk.  As  a result of  PCDF
detection  1n  milk from  Swedish  mothers  1t  has  been suggested  that  primary
PCDF exposure  to  this population  1s occurring  from  municipal  Incinerators.
Consequently, 1n  1985 the  National  Swedish  Environmental   Protection  Board
decided on a moratorium for new municipal  Incinerators.
    PCDFs are extremely  toxic  to animals  and humans.  Signs  and symptoms of
toxlclty  are  very similar to  those  caused  by  2,3,7,8-tetrachlorod1benzo-p_-
dloxln.   Of  the total 135  possible  Isomer  congeners so far determined  for
PCDFs,  2,3,7,8-TCDF and  2,3,4,7,8-PeCDF seem  to  be the most  toxic.   However,
the relative toxlclty  of all the congeners have not  yet been fully  studied.
The guinea pig  Is the  most sensitive species  to  toxic effects of PCDF.   Mice
and rats  are  less sensitive than  guinea  pigs.  Like PCDDs,  these  compounds
are  strong Inducers  of  aryl  hydrocarbon  hydroxylase  (AHH) and  the  most
acutely toxic Isomers are also the  most  potent Inducers  of  AHH activity.


1925A                               1-1                               06/23/86

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    Mutagenlclty  data   on  PCDFs  are  extremely  limited  and  three  Isomers
studied gave negative responses In short-term mlcroblal  mutagenesls assay.
    Recent  observations  Indicate that  2,3,7,8-TCDF  1s  teratogenlc  1n  mice
resulting  1n  dose-related  Increases  1n  both  Isolated  cleft  palates  and
hydronephrosls  1n  the  fetus.   Animal  experimentation data  Indicate  that
PCOFs  are  capable  of  being  transferred  to  the  developing offspring,  pre-
natally through transplacental migration and  postnatally  through  the nursing
mother's milk.  When these two rates  of  transfer  were compared,  1t was found
that  PCDF  transported  through nursing  mother's milk  appeared to  be higher
than transplacental migration  to  the fetus.
    Information on  adverse  health effects  1n  humans  has been observed  from
the  Japanese and  Taiwanese  population who  consumed PCB-  and  PCDF-contam1-
nated  rice  oil  In 1968  and   1979,  respectively.   Severe  adverse  toxic
effects,  many of  which  are  similar  to those  caused by 2,3,7,8-TCDD,  were
observed 1n  the affected population.
    Though  PCOFs  have been detected  1n  a  number of chemicals as  contaminants
and  1n the emissions from waste Incinerators, a  chronic toxldty data  base
for  this  class of  compounds  1s   not  available.  Primarily  because of their
prevalence  In the environment and structural  similarities  between PCDFs and
PCDDs,  there Is  concern as  to the public  health  Impact  of  their  presence 1n
the environment.
1925A                               1-2                              06/30/86

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                     2.   PHYSICAL AND CHEMICAL  PROPERTIES
2.1.   SUMMARY
    The dlbenzofurans (DBFs)  are a  group  of  organic compounds that  contain
two benzene rings annulated  to  a central furan ring.  The  benzene  rings  can
be  substituted  at  the 1,2,3,4,6,7,8,9  positions.   For  a single  substHuent
like chlorine  there  are  135  congeners  over  the substitution  range  mono- to
octa-:   these  Include 4 mono-,  16  dl-,  28  tr1-,   38  tetra-,  28 penta-,  16
hexa-,  4 hepta- and 1 octa-.
    The crystal  structure of the  2,3,7,8-tetrachlorodlbenzofuran  (2,3,7,8-
TCDF)  Is  monocllnlc.  The  latter  1s  a  structural analogue  of  the  highly
toxic  2,3,7,8-TCDD.   The  two  benzene  rings  are  coplanar except  for  the
1,2- and  1,9-subst1tuted  derivatives.   Most  polyhalogenated  dlbenzofurans
(PHDFs), Including the polychlorlnated  dlbenzofurans (PCDFs),  polyfluoMnat-
ed  dlbenzofurans (PFDFs),  polybromlnated  dlbenzofurans  (PBDFs) and  the poly-
lodlnated  dlbenzofurans   (PIDFs)  are  solids   at  room  temperature  and  have
relatively high  boiling  points, which  Increase with degree of substitution.
PHDFs  are  generally  quite soluble  In organic  solvents  but  water  solubility
decreases  with chlorlnatlon.   The  octanol/water  partition coefficients  of
PCDFs  Increase with   chlorine number; log K    values  for 2,8-d1chlorod1ben-
zofuran  (2,8-DCDF),  2,3,7,8-TCDF, and  the octachlorodlbenzofuran  (OCDF)  are
5.30,  5.82i0.02, and  8.78, respectively.   Vapor  pressure data  for  some PCDFs
are  available.   The  less polar  the  PHDF,  the  more  readily  1t  will  adsorb to
organic matter.
    The  PHDFs  are  aromatic  compounds,  and thus there are  at  least two dis-
tinct  UV absorption  maxima  near  217  nm (o* *=• a  transition) and  near  280
nm  (tr*^-ir  transition).  The   effect  of  ring  substitution  on  absorption
maxima  tends   to  be   minor.   The proton  and   13C-nuclear magnetic  resonance


1926A                                2-1                              06/23/86

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(NMR)  spectra  are  characteristic of  aromatic  molecules.   As  expected  of
aromatic molecules, the parent  Ions  In  the mass spectra are Intense and  are
suitable for  specific Ion  monitoring.   The  major  fragment Ions  are  M-C1,
M-Clp,  M-C1-CO,  and  M-C1--CO.   The  major cleavage  patterns  are  determin-
ed by the great stability of the  ring system  so that  the  fragmentations tend
to be directed by the substUuents.
    The  PHDFs  exhibit reactions  directed  by  the  substUuents  of  the  most
substituted ring towards  the least substituted ring.
    Higher  PCDFs can be degraded by ultraviolet  (UV)  light.  These  reactions
are dependent on solvent and wavelength.   Degradation  Is  slow  at  310 nm,  but
rapid at 254 nm or at 310 nm 1n the presence  of suitable triplet  sensltlzers.
    PHDF can  also  be produced  by photodecomposltlon  of higher  PHDFs,  by
photocycllzatlon or  pyrolysls  of halogenated  dlphenyl ethers, by  pyrolysls
of  polyhalogenated blphenyls  (PHBs)  and  halobenzenes,  by  halogenatlon  of
lower  PHDFs,  by  palladium  acetate  cycllzatlon   of  substituted   dlphenyl
ethers, and by cycllzatlon  of  substituted  hydroxylated  PHBs, and  substituted
dlazotlzed halophenoxy-o-an1lines.
2.2.   INTRODUCTION
    The accepted system of numbering of  PHDFs 1s now as follows:
The  ring  that 1s  most  substituted has  priority 1n numbering.   For  equally
substituted  rings, the  numbering that  allows  the  lowest sum  of the  sub-
stituted positions 1s the correct one.


1926A                               2-2                              06/21/86

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    There are 135 positional  Isomers  for  a single substltuent:  4  mono-,  16
dl-, 28  tr1-,  38 tetra-, 28  penta-,  16  hexa-,  4 hepta- and 1  octa-.   There
has  been  IHtle  Investigation  of  the physico-chemical  properties of  such
compounds.
    The Chemical  Abstracts  System  Registry  Numbers  (CAS  RN)  for   the  PHDFs
that have been cited In the literature are provided  1n  Table 2-1.
2.3.   PHYSICAL PROPERTIES
2.3.1.   Holecular  Structure.  The  acutely  toxic  2,3,7,8-TCDF  belongs  to
the  monocl1n1c  space  group C2/c and  the  molecule 1s planar  (Table 2-2).   A
crystallographlc  2-fold  axis  bisects  the  bond  between  the rings and  passes
through the oxygen atom.  The longest  carbon-carbon bond  distance within the
benzenold  rings  joins  the  carbon atoms  to which  the  chlorine   atoms  are
attached  (Hubbard et al., 1978).   Thus, the  compound  1s  very closely related
1n  structure to  the highly  toxic 2,3,7,8-TCDD  (Boer  et  al., 1972).   No X-ray
data for  the other PHDFs are available.
    The electronic  structures of  25  PCDFs  were characterized  by Cheney and
Tolly  (1979).   The  powder  X-ray  diffraction patterns  of 4 PCDFs  have been
reported  by Cantrell et  al.  (1986).   An unspecified  MCDF, 3,6-DCDF, 2,3,7,8-
TCDF,  and OCDF  were  examined.   The  DCDF  1s easily distinguished  from OCDF
and  the  TCDF  by Us  Intense diffraction  at 24.35 2e,  and the TCDF  by Us
strong  line  at  15.20  2e.   The  OCDF can  with  difficulty  be detected  by Us
diffraction at 31.81 2e.
2.3.2.    Heltlng  Points.   Table  2-3  gives  the  melting  points   of  some
PHDFs.  Norstrom et  al. (1979)  showed by  gas  chromatography/mass   spectrome-
try  (GC/MS)  that the  PCDFs  for  which they  determined  melting points were
pure.   Kurokl  et al.  (1984)  have  published  melting points  for other PCDFs
(Table 2-3).


1926A                               2-3                              06/21/86

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                                   TABLE 2-1

                  Chemical Abstracts System Registry Numbers
                              (CAS-RN)  for PHDFs
Chemical Substitution
PCDF
Mono mono
2-
3-
4-
D1 d1
1,2-
1,3-
1,4-
1,6-
1,7-
1,8-
1,9-
2,3-
2,4-
2,6-
2,7-
2,8-
3,4-
3,6-
3,7-
4,6-
Tr1 tr1
1,2,3-
1,2,4-
1,2,6-
1,2,7-
1,2,8-
1,2,9-
1,3,4-
1,3,6-
1,3,7-
1,3,8-
1,3,9-
1,4,6-
1,4,7-
1,4,8-
1,4,9-
CAS-RN

42934-53-2
84761-86-4
25074-67-3
74992-96-4
43047-99-0
64126-85-8
94538-00-8
94538-01-9
74992-97-5
94538-02-0
81638-37-1
70648-14-5
64126-86-9
24478-74-8
60390-27-4
74992-98-6
5409-83-6
94570-83-9
74918-40-4
58802-21-4
64560-13-0
43048-00-6
83636-47-9
24478-73-7
64560-15-2
83704-37-4
83704-34-1
83704-38-5
82911-61-3
83704-39-6
64560-16-3
76621-12-0
83704-40-9
82911-60-2
83704-41-0
64560-14-1
70648-13-4
1926A
2-4
06/21/86

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                              TABLE 2-1 (cont.)
   Chemical
Substitution
CAS-RN
PCDF (cont.)
Tr1 (cont.) 2,3,4-
2,3,6-
2,3,7-
2,3,8-
2,3,9-
2,4,6-
2,4,7-
2,4,8-
2,4,9-
2,6,7-
3,4,6-
3,4,7-
3,4,8-
3,4,9-
Tetra tetra
1,2,3,4-
1,2,3,6-
1,2,3,7-
1,2,3,8-
1,2,3,9-
1,2,4,6-
1,2,4,7-
1,2,4,8-
1,2,4,9-
1,2,6,7-
1,2,6,8-
1,2,6,9-
1,2,7,8-
1,2,7,9-
1,2,8,9-
1,3,4,6-
1,3,4,7-
1,3,4,8-
1,3,4,9-
1,3,6,7-
1,3,6,8-
1,3,6,9-
1,3,7,8-
1,3,7,9-
1,4,6,7-
1,4,6,8-
1,4,6,9-
1,4,7,8-

57H7_34_7
57117-33-6
58802-17-8
57117-32-5
58802-18-9
58802-14-5
83704-42-1
54589-71-8
82911-59-9
83704-43-4
83704-43-2
83704-44-3
83704-45-4
83794-46-5
30402-14-03
24478-72-6
83704-21-6
83704-22-7
62615-08-1
83704-23-8
71998-73-7
83719-40-8
64126-87-0
83704-24-9
83704-25-0
83710-07-0
70648-18-9
58802-20-3
83704-26-1
70648-22-5
83704-27-2
70648-16-7
64126-87-0
83704-28-3
57117-36-9
71998-72-6
83690-98-6
57117-35-8
64560-17-4
66794-59-0
82911-58-8
70648-19-0
83704-29-4
1926A
  2-5
06/21/86

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                               TABLE  2-1  (cont.)
Chemical Substitution
PCDF (cont.)
Tetra (cont.) 2,3,4,6-
2,3,4,7-
2,3,4,8-
2,3,4,9-
2,3,6,7-
2,3,6,8-
2,3,7,8-
2,4,6,7-
2,4,6,8-
3,4,6,7-
Penta penta
1,2,3,4,6-
1,2,3,4,7-
1,2,3,4,8-
1,2,3,4,9-
1,2,3,6,7-
1,2,3,6,8-
1,2,3,6,9-
1,2,3,7,8-
1,2,3,7,9-
1,2,3,8,9-
1,2,3,6,7-
1,2,4,6,8-
1,2,4,6,9-
1,2,4,7,8-
1,2,4,7,9-
1,2,4,8,9-
1,2,6,7,8-
1,3,4,6,7-
1,3,4,6,8-
1,3,4,6,9-
1,3,4,7,8-
1,3,4,7,9-
1,3,4,8,9-
2,3,4,6,7-
2,3,4,6,8-
2,3,4,6,9-
2,3,4,7,8-
2,3,4,7,9-
CAS-RN

83704-30-7
83704-31-8
83704-32-9
83704-33-0
57117-39-2
57117-37-0
51207-31-9
57117-38-1
58802-19-0
57117-40-5
30402-15-4
83704-47-6
83704-48-7
67517-48-0
83704-49-8
57H7_42-7
83704-51-2
83704-52-3
57117-41-6
83704-53-4
83704-54-5
83704-50-1
69698-57-3
70648-24-7
58802-15-6
71998-74-8
70648-23-6
69433-00-7
83704-36-3
83704-55-6
70648-15-6
58802-16-7
70648-20-3
70872-82-1
57117-43-8
67481-22-5
83704-35-2
57H7_31_4
70648-21-4
1926A
2-6
06/21/86

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                               TABLE  2-1  (cont.)
   Chemical
Substitution
CAS-RN
PCDF (cont.)
Hexa
















Hepta




Octa

"C


PBDF
Mono



D1



hexa
1,2,3,4,6,7-
1,2,3,4,6,8-
1,2,3,4,6,9-
1,2,3,4,7,8-
1,2,3,4,7,9-
1 23489-
1 , C , J,t,O ,3-
1,2,3,6,7,8-
1,2,3,6,7,9-
1,2,3,6,8,9-
1,2,3,7,8,9-
1,2,4,6,7,8-
1,2,4,6,7,9-
1,2,4,6,8,9-
1,3,4,6,7,8-
1,3,4,6,7,9-
2,3,4,6,7,8-
hepta
1,2,3,4,6,7,8-
1,2,3,4,6,7,9-
1,2,3,4,6.8,9-
1,2,3,4,7,8,9-
octa
1,2,3,4,6,7,8,9-
1,2,7,8-
2,3,7,8-
2,3,4,7,8-

1-
2-
3-
4-
2,7-
2,8-
3,7-

55684-94-1
79060-60-9
69698-60-8
91538-83-9
70648-26-9
91538-84-0
92341-07-6
57H7_44_9
92341-06-5
75198-38-8
72918-21-9
67562-40-7
75627-02-0
69698-59-5
71998-75-9
92341-05-4
60851-34-5
38998-75-3
67562-39-4
70648-25-8
69698-58-4
55673-89-7
3268-87-9
39001-02-0
78813-10-2
78813-09-9
87665-66-5

50548-45-3
86-76-0
26608-06-0
89827-45-2
65489-80-7
10016-52-1
67019-91-4
1926A
  2-7
06/21/86

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                              TABLE 2-1 (cont.)
Chemical
PBDF (cont.)
TM
Tetra
Penta
Hepta
PFDF
Mono
D1
TM
Tetra
Octa
PIDF
Mono
D1
Nixed halo

Substitution
1,2,8-
2,3,8-
1,2,7,8-
2,3,7,8-
penta
hepta

2-
3-
2,7-
2,8-
1,2,4-
1,2,3,4-
octa
2-
3-
4-
2,7-
2,8-
3,7-
tr1bromo-2,4,8-tr1chloro
tetrabromo-2,4,8-tr1chloro
CAS-RN
84761-81-9
84761-82-0
84761-80-8
67733-57-7
68795-14-2
62994-32-5

391-46-8
391-54-8
71277-77-5
10016-52-1
15950-24-0
15945-39-8
16804-47-0
5408-56-0
5896-29-7
65344-26-5
81050-43-3
5943-11-3
5914_49_8
54605-27-5
54605-26-4
1926A
2-8
06/24/86

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    2,3,7,8-TCDF
                                                      TABLE 2-2

                                X-Ray  Crystallographlc  Indices  of  Some Selected PHDFs*
Dlbenzofuran
Unit Cell Indices (A)
a b c
Density (g/m/i)
(exptl) (calc'd)
Bond Length
(A)
14.702(4)    12.886(4)     6.256(1)
1.72
1.74
(2,8)C-C1(1):1.725(2)
(3,7)C-C1(2):1.732(2)
€-0:1.385(2)

Benz C-C:1.366(2)
to 1.404(2)
    *Source:   Hubbard et  al.,  1978
00

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                                  TABLE 2-3



                   Melting and  Boiling  Points  of  Some  PHDFs
Dlbenzofuran
— , 1-MBOF
— , 2-MBOF
--, 3-HBDF
— , 4-MBDF
--, 2-MCDF
— . 3-MCDF
— , 2-MIDF
— . 3-MIDF
--. 2-MFDF
--, 3-MFDF
--, 2,8-DBDF
--. 2,8-DCDF
— . 3,7-DCDF
— , 2,8-DIDF
--, 2,3,8-
TrCDF
Melting Point Boiling Point
PC) (°C)
67
no
110 220 (40 mm Hg)
120
120 220 (40 mm Hg)
72
67
106
101
101-102
112
142
89
88.5
195
199-200
191.5-192.5
185
184-185
186-188
77
180-181
189-191
Reference
Coffey, 1973
Coffey, 1973
Weast, 1985
Coffey, 1973
Weast, 1985
Coffey, 1973
Weast, 1985
Coffey, 1973
Coffey, 1973
Kurokl et al., 1984
Coffey, 1973
Coffey, 1973
Coffey, 1973
Coffey, 1973
Coffey, 1973
Weast, 1985
Oshlma et al . ,
1968c
Gllman and Young,
1934
Kurokl et al., 1984
Norstrom et al.,
1979
Coffey, 1973
Norstrom et al.,
1979
Gray et al., 1976
1926A
2-10
06/23/86

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                              TABLE 2-3 (cont.)
 Dlbenzofuran
Melting Point     Boiling Point
                                         Reference
-, 2,4,6-
  TrCDF

-,2,4,8-
  TrCDF

--, 1,2,4-
  TrCDF

—,1.3,6,8-
  TCOF

-,1,3,6,7-
  TCOF

-.1,3,7,9-
  TCDF

-.1,4,6,7-
  TCDF

--,2,3,6,8-
  TCDF

-.2,4,6,7-
  TCDF

-,1,2,7,8-
  TCDF

-.1,2,6,7-
  TCDF

-1,2,7,9-
  TCDF

-,2,3,7,8-
  TCDF
-.2,3,6,7-
  TCDF

-.2,4,6,8-
  TCDF
116-117


155-156


100-101


177-178


176.5-177


206.5-207.5


180-181
197-198
202-203

164-164.5
210-211


199-200


184-185


219-221
226-228

227-228

195-196
192-192.5
198-200
                                    Gray et al.,  1976
                                    Kurokl  et al.,  1984
                                    Coffey,  1973
                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Gray et al.,  1976

                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Norstrom et al.,
                                    1979
                                    Gray et al., 1976

                                    Kurokl  et al.,  1984
                                    Kurokl  et  al.,  1984
                                    Gray et al.,  1976
1926A
               2-11
                                                06/21/86

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                             TABLE 2-3  (cent.)
Dibenzofuran
-.1.2,3,7-
TCDF
-.1.2,3,8-
TCDF
-,2,3,4,8-
TCDF
-.2,3,4,7-
TCDF
-.2,3,4,6-
TCDF
-.1.2,4,8-
TCDF
-1.2,3,4-
TCDF
-.1,2,4,6,8-
PeCDF
-,1,2,4,7,8-
PeCDF
-.1,2,4,7,9-
PeCDF
-.1,2,3,7,8-
PeCDF
-.1,2.3,6,7-
PeCDF
-,1,2,6,7,8-
PeCDF
-,2,3.4,7,8-
PeCDF
-.2,3,4,6,7-
PeCDF
Melting Point
167.5-168
197-198
176-177
172.5-173
153-154
191-193
168.5-169
169-170
204-205
236-238
225.5-226.5
234-235
196-197
225-227
205-207
220-221
196-196.5
201.5-202
Boiling Point Reference
Kurokl et al.,
Kurokl et al..
Kurokl et al.,
Kurokl et al.,
Kurokl et al.,
Kurokl et al.,
Kurokl et al.,
Coffey, 1973
Kurokl et al.,

1984
1984
1984
1984
1984
1984
1984
1984
Kurokl et al., 1984
Norstrom et al.,
1979
Gray et al., 1976
Kurokl et al.,
Kurokl et al.,
Kurokl et al.,
Kurokl et al.,
Kurokl et al.,
Kurokl et al..
1984
1984
1984
1984
1984
1984
1926A
2-12
06/21/86

-------
                              TABLE  2-3 (cont.)
 Dlbenzofuran
Melting Point     Boiling Point
      Reference
 -.2,3,4,6,8-
  PeCDF

 -,1,3,4,7,8-
  PeCDF

 -.1,3,4,6,7-
  PeCDF

 -.1,2,3,4,6-
  PeCDF

 -,1,2,4,6,7-
  PeCDF

 -.1,2,3,4,8-
  PeCDF

 -.1,2,4,6,7,8-
  HxCDF

 -,1,3,4,6,7,8-
  HxCDF

 -.1,2,4,6,8,9-
  HxCDF
-,1,2,3,4,6,7-
  HxCDF

-.1,2,3,4,7,8-
  HxCDF

-,1,2,3.6.7.8-
  HxCDF

-,1,2,3,4,6,7,8-
  HxCDF

-,1,2,3,6,8,9-
  HxCDF

-.1,2,4,6,7,9-
  HxCDF
219-220


168-170


195-195.5


194-195


178.5-179.5


177-178


221-222


229-230


247-249

246-248

227-228


225.5-226.5


232-234


239-240


206-207


180-181
Kurokl et al., 1984
Kurokl et al., 1984
Kurokl et al., 1984
Kurokl et al., 1984
Kurokl et al., 1984
Kurokl et al., 1984
Kurokl et al., 1984
Kurokl et al., 1984
Norstrom et al.,
1979
Kurokl et al., 1984

Kurokl et al., 1984
Kurokl et al., 1984
Kurokl et al., 1984
Kurokl et al., 1984
Kurokl et al., 1984
Kurokl et al., 1984
1926A
               2-13
            06/21/86

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                              TABLE 2-3 (cont.)
 Dlbenzofuran
Melting Point     Boiling Point
                                         Reference
-.1,2,3,4.6,8-
  HxCDF

-,1,2,3,4,6,9-
  HxCDF

-,1,2,3,4,7,9-
  HxCDF

-.1,2,3,4,6.7,8-
  HpCDF

-.1,2,3,4,6,8,9-
  HpCDF

-.1,2,3.4,7,8,9-
  HpCDF

—, OFDF
233.5-234


196-197


216-217


236-237


211-212


221-223


100
                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Kurokl  et al.,  1984
                                    Kurokl  et al., 1984
                                    Kurokl et al., 1984
                                    Coffey, 1973
1926A
               2-14
                                                06/21/86

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2.3.3.   Solubility.   PHDFs  are less  polar  than  dlbenzofuran  and  would  be
expected  to  be less soluble  1n water and more  soluble  1n organic solvents.
Research  needs to  be  done 1n  this  area.  No  solubility data even  for  the
PCDFs have been reported.  However,  2,3,7,8-TCOF  1s  said to be slightly more
soluble  In  water  than 1s the  corresponding dloxln,  2,3,7,8-TCDD (Greenlee
and  Poland,  1978),  which  has  a  solubility  of  -0.2  vg/a at  25°C  (Helling
et al., 1973).
2.3.4.   Partition  Coefficients.    Sarna  et  al.  (1984)  and  Burkhard  and
Kuehl  (1986)   have  documented  the  octanol/water  partition  coefficients  for
some  PCDFs  (Table  2-4).   The disagreement for OCDF  arises because of uncer-
tainties  1n  the K    values   of  reference compounds  of  high K   .   The par-
                  ow                         r            3   ow        K
tHIonlng  of  organic  chemicals  between  Upld  and  water  1s  an  Important
determinant  of the  bloconcentratlon  potential  of a  toxicant and has  some-
times been effectively used  as  an Indicator  of  the  preferred degradatlve in
vivo pathways.
2.3.5.   Boiling Points  and  Vapor Pressures.  No  vapor  pressures of  any  of
the PHDFs at 25°C have been measured directly.
    The vapor  pressures  for  a series of  PCDFs have  been estimated by a gas-
chromatographlc method (Firestone,  1977a; Berg  et al.,   1985a)  (Table  2-5).
Unfortunately, different  Investigators  have  obtained  different  pressures  by
this  method  for  the  esters  of  2,4-d1chlorophenoxyacet1c  acid  (Jensen  and
Schall,  1966;  Flint et  al., 1968).   The vapor  pressures,  however, of  the
PCDFs  will  certainly  not be  lower  than the  values In Table  2-5,  and  a
decrease In vapor  pressure with  Increasing chlorlnatlon 1s expected.
2.3.6.   Adsorption  and  Desorptlon.    It  would be  expected  that  the  PHDFs
would  adsorb  very  strongly  to  organic  matter  and  nonpolar   nonorganlc
material such  as  charcoal, but not  so strongly to  polar  Inorganic  material


1926A                               2-15                             06/21/86

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                                  TABLE 2-4
       The Logarithm of the Octanol/Water Partition Coefficients (Kow)
                       of  Some  PHDFs  Using HPLC  Methods
PCDF
2,8-d1chloro-
2,3,7,8-tetrachloro-
octachloro-
log Kow
5.95
5.30°
5.82+0.02
13.37
8.78
Reference
Sarna et al., 1984a
Burkhard and Kuehl, 1986C
Burkhard and Kuehl, 1986C
Sarna et al., 1984a
Burkhard and Kuehl, 1986C
aQuadrat1c equation treatment:   Blorad B1os1l  (10 ym)  data
bQuadrat1c equation treatment:   Unspecified "mlcrobore" HPLC column
cSarna et al. (1984) data recalculated from experimental data
1926A                               2-16                             06/23/86

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                                   TABLE  2-5

          Vapor Densities and Pressures of PCDFs as Estimated from a
                          Gas  Chromatographic  Method*
   PCDF Isomer
  Estimated
Vapor Pressure

(mm Hg x 10~«
   at 25°C)
Estimated Vapor
Density at 25°C

    (yg/m3)
D1-
2,4-
3,7-
2,8-
Tr1-
2,4,6-
2,3,8-
Tetra-
1,4,6,8-
2,4,6,8-
2,3,4,8-
2,4,6,7-
1,2,7,8-
2,3,7,8-
2,3,6,7-
3,4,6,7-
Penta-
1,3,4,7,8-
1,2,4,7,8-
1,2,3,6,7-
2,3,4,7,8-
Hepta-
unspedfled
unspecified
unspecified
Octa-

7.3
7.0
6.8

4.0
3.7

2.5
2.5
2.2
2.1
2.0
2.0
1.9
1.8

1.3
1.3
1.1
1.1

0.44
0.36
0.30
0.19

82
79
77

52
48

38
38
33
32
30
30
29
27

22
22
18
18

9.0
7.4
6.2
4.3
*Source:  Firestone, 1977a
1926A
      2-17
         06/21/86

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such as alumina.  The predicted behavior 1s borne out  by  the  fact  that  alum-
ina  1s  used  generally  for  the  column chromatography  of PCDDs  and  PCDFs
(O'Keefe,  1978a).  Strong binding  1s  expected  to soils of  high  organic con-
tent as observed  for 2,3,7,8-TCOD (Isensee, 1978).   This has been  observed
for  2,3,7,8-TCDD  In  South Vietnam and  northwestern Florida  soils  (Westing,
1978).   Although  both  2,3,7,8-TCDD and -TCDF  are comparatively  Insoluble  In
water,  the 2,3,7,8-TCDF appears to be slightly more  water soluble.   There  1s
a  possibility  that  the  TCDF  will be  more readily  leached from soils  than
TCDD.  Experiments should  be  performed to  test  this hypothesis.  The  rela-
tion, Equation  2-1,  has  been shown to  hold by Karlckhoff et al.  (1979)  for
nonpolar compounds.
                           log Koc =  log Kow -  0.21                   (2-1)
where
    Koc  1s  a  constant  that  1s  characteristic  of   the  compound under  con-
    sideration and
    Kow Is the octanol/water coefficient
    If  the  K    values  of  Burkhard   and  Kuehl  (1986)  (see  Table  2-4)  are
             ow
assumed,  the  log K    values  for  2,8-DCDF, 2,3,7,8-TCDF,  and OCDF  are  5.09,
                   \)\f
5.61 and 8.57, respectively.
     If  the  PHDFs  are adsorbed  1n the same  manner as  dibenzothlophene  by
soils  (Hassett  et  al.,  1980),  the  FreundUch  adsorption  Isotherm  should
apply as follows:
                                 Cs =  KdCw  1/n                        (2-2)
where
     Cs Is the amount sorbed 1n yg/g of  soil
     Cw 1s the equilibrium solution concentration (yg/s.)
     n  Is an Integer  characteristic of the process and
     K(j Is the FreundUch constant

 1926A                               2-18                             06/21/86

-------
If n = 1,  as for dlbenzothlophene (Hassett  et  al.,  1980),
                                  Cs = KdCw                          (2-3)
Since
                               Kd = 100KOC/%OC                       (2-4)
where XOC 1s the percentage of son organic content.   For  an organic content
of  1%,  K   =  100  K   .   Thus,  log  Kd  for  2,8-DCBF,   2,3,7,8-TCDF,   and
OCDF are then 7.09, 7.61 and  10.57,  respectively.
2.3.7.   Miscellaneous   Properties.   The  molar  refractions  of  the  DCDFs,
TrCDFs, TCDFs,  PeCDFs,   HpCDFs and OCOF have been  estimated to be 60.2, 65.0,
69.8, 74.6, 84.2 and 89.0, respectively (Firestone, 1977a).
2.3.8.   Spectroscoplc  Properties.
    2.3.8.1.   ULTRAVIOLET ABSORPTION  SPECTRA — There are  few  studies  of
the UV absorption  spectra  of  PHDFs.  The existing  data for MBOFs are provid-
ed  by  Weast (1985) In  Table  2-6 and for PCOFs by  Firestone (1977a)  and  Gray
et al., (1976)  1n Table 2-7.
    The UV  spectra  of  some 2-MHDFs  have  been  reported by  Kurokl (1968).   The
Hammett  p  value  for  the  2-substltuted  derivatives  was  1.44.  Thus,  there
was  not  much  effect   on  \     of  substitution  at  this   position  (Kurokl,
1968).
    Chloro-substltutlon  does  not  affect  the x   „   of  the  parent  compound
                                                max
very  much for  the  2-MCDF  and 3-MCDF  (Cern1an1  et al., 1954).   The  UV spec-
trum  of  2,8-DCDF  Is also similar  to  that of unsubstltuted OF with  a  \max
at  290 nm 1n  methanol  (Crosby et al.,  1973).   Firestone (1977a) reported the
UV  absorptions  of  several  PCDFs  and found  the red shift on Increasing chlor-
1nat1on was small as shown In Table 2-7.
    2.3.8.2.    FLUORESCENCE -- No fluorescence  data  for  the PHDFs  have  yet
been  published.
 1926A                               2-19                             06/21/86

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                                  TABLE 2-6

          Ultraviolet  Absorption Maxima and Molar AbsorptlvHIes for
                           Some Substituted PBDFs*
  MBDF
   Solvent
     Absorption Peak  In nm
    [log(molar absorptivity)]
  2-Bromo
  3-Bromo
Acetic acid
Ethanol
222(4.58),  251(4.19),  288(4.25),
310(3.67)

219(4.55),  254(4.31),  290(4.31),
300(4.22)
*Source:   Weast,  1985
1926A
               2-20
                        06/21/86

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                                   TABLE  2-7

                Absorption Maxima of Some PCDFs In Chloroform3
                                               UV Absorption
            PCDF                           Maxima Wavelengths (nm)
           2,3,8-TrCDF                    256, 302, 313

           2,3,6,8-TCDF                   250, 260, 285, 297, 314b

           2,3,7,8-TCDF                   257, 294, 310, 323

           2,4,6,8-TCDF                   259, 309, 316

           1,2,4,7,8-PeCDF                256, 266, 297

           1,3,4,7,8-PeCDF                263, 272, 297, 320


aSource:  Firestone, 1977a

bGray et al., 1976
1926A                               2-21                             06/21/86

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    2.3.8.3.    PHOSPHORESCENCE  —  Few   studies   have  been   reported  on  the
phosphorescence of the PHDFs.  Teplyakov  et  al. (1970) noted an Increase  In
quantum efficiency on substitution of dlbenzofuran with chlorine atoms.  The
use of  phosphorescence  techniques  to  determine PCDFs  has  been suggested  by
Brownrlgg et al.  (1972).  The difficulties of  low-temperature  technology and
the Interference by Impurities  are substantial.
    2.3.8.4.    NMR AND  EPR  SPECTROSCOPY  —The proton  and  "F  spectra  of
1,2,3,4-TFDF  and  1,2,4-TrFDF  Implied  that there was a large para F-F coup-
ling (Brown and  Mooney,  1967).   The  proton NMR data of some PCDFs are given
In Table 2-8.
    The  13C-NMR  chemical shifts  and  assignments  of  carbon-proton  coupling
constants have  been  reported for the  2-MBDF  and  2,8-DBDF.  Long range  sub-
stltuent effects were observed In unsymmetMcal  compounds  (Huckerby,  1979).
    2.3.8.5.    MASS  SPECTROSCOPY  -- The   spectra  for  the  2,3,7,8-TCDF  and
OCDF (Curley  et  al., 1974) attest to  the great stability of the parent  1on
since the latter 1s the largest peak  1n the spectrum.
    The  mass  spectra of the PHDFs will  be discussed more  thoroughly  1n  the
section  on  GC/MS  (Section  3.4.2.2.2).   The  major fragment  Ions  are M-C1,
M-C12, M-C1-CO and M-C12-CO.
2.4.   CHEMICAL REACTIONS
2.4.1.   General.   PHDF  reactions  have  been  reviewed  by  Coffey  (1973);
Gllman's  group  was  largely  responsible   for  much  of the  early  chemistry
(GUman  et  al.,  1934a,b,  1935a,b,  1939a,b,c,d, 1940a,b,c, 1944; GUman  and
Young,  1934,  1935; GUman and  Ess, 1939;  GUman and  Abbott, 1943;  Oilman and
Thlrtle,  1944;  Gllman  and  Swiss, 1944;  Gllman and Avaklan,  1945a,b;  Gllman
and Esmay, 1953, 1954).
 1926A                               2-22                             06/21/86

-------
                                                                               TABLE 2-8
lO
ro
Proton NMR Data for Some PCDFs
PCDF
1-
2-
3-
4-
2.3-d1-
2,6-d1-
2
2
i
B 3
1
1
2
2
2
2
1
,7-dl-
,8-d1-
,7-d1-
,3,6-tr1-
,3,8-tM-
,3.4-trl-
,3.8-trl-
,4.8-tr1-
,6,7-trl-
,2.3,4-tetra-
Chemlcal Shifts
(ppm downMeld from tetramethylsllane)
Coupling Constants (J)
(Hertz)
ra, 7.20-8.10
m. 7.20-8.10
m, 7.20-8.10
m, 7.20-8.10
m. 7.20-8.10
m. 7.20-8.20
in, 7.20-8
m, 7.20-8
m- H3.4,6
HT = 7.98
H2 = 7.55
H2 = 7.55
m. H6 to
HT = 8.27
HT = 8.07
HI = 7.77
H! = 8.08
H6 = 7.65
.20
.10
.7 = 1
; H2 =
; H4 =
; H4 =
Hg = 7
; H4 =
; "6.7
;H3 =
; H3 =
; H7 =

.45-7.47; H-\
7.38; H4 =
7.85; H7 =
7.79; H6 =
.25-8.25; H-\
7.82; H6 =
= 7.54 (m);
7.49; H6 =
7.46; H4 =
7.58; H8 =

,9 =
7.68
7.68;
7.76;
= 8.
7.56;
Hg .
7.56;
7.63;
7.44;

7.87
H8 = 7.50; Hg = 8.27
H7 = 7.64; Hg = 8.27
39
H7 = 7.45; Hg = 8.09
8.24
H7 = 7.48; Hg = 7.87
H8 = 7.48; Hg = 7.99
Hg = 8.34

Jl,9
J1.2
J2.4
J8.9
J2.4
J7.9

J6.7
J1.3
J7.9
Jl,3
J8.9
J7.8

= 1.1;
= 8.30
= 1.6;
= 8.1;
= 1.6;
= 2.2

= 8.6;
= 2.0;
= 1.8
- 2.4;
= 8.4
; 6.7;

1.8
; J2>4 = 1.40
J7.8 • 8.1;
J7.g = 1.2
J&.7 • 8.4;

J7.9 • 2.2
36.7 • 8.8;
H3.4 • 8-2;
7.8= 7.0;
Reference
Safe and Safe,
Safe and Safe,
Safe and Safe,
Safe and Safe,
Safe and Safe,
Safe and Safe.
Safe and Safe,
Safe and Safe,
Kurokl et al..
Nor strom et al
Safe and Safe,
Safe and Safe,
Safe and Safe,
Safe and Safe,
Norstrom et al
Kurokl et al.,
Safe and Safe,
Bell and Gara,
1984
1984
1984
1984
1984
1984
1984
1984
1984
. . 1979
1984
1984
1984
1984
., 1979
1984
1984
1985
            1,2,3,7-tetra-
CO
m, 8.29-8.40 for  Hg
ro. 7.33-7.76 for  H&>7>8

H4 = 7.63; He =  7.57;  H8 7.38;  Hg  =  8.23
H4 = 7.65; H6 =  7.60;  H8 =  7.41; Hg  =  8.25
                                                                                                    J6.8/7.9 = 2.0
J8.9 • 8.4;  H6(8
                                                                                                                                  Kurokl et al., 1984
Kurokl et al., 1984

-------
V0
ro
3*
PCDF
1.2,3,8-tetra-
1.2.4.7-tetra-
1,2.4.8-tetra-

1,2,6,7-tetra-

1.2.7,8-tetra-
1,2.7.9-tetra-
1,3.4.7-tetra-
ro 1.3,6.7-tetra-
i
£ 1.3.6,8-tetra-

1.3,7.9-tetra-
1.4,6.7-tetra-
2.3.4.6-tetra-



2,3.4,7-tetra-

2.3,4,8-tetra-


2,3,6.7-tetra-
-5 2.3,6.8-tetra-
r
(ppm
H4 =
H3 *
H3 •
«3 •
H3 •
H3 =
H3 •
H3 •
H2 =
H2 -

H2 =
H2 =
H2.8
H2 =
Hl =

H] =

Hl =
Hi -
»1 -

H] -
Hi -
H] =
Hi -
Chemical Shifts
downfleld from tetramethylsllane)
7.64;
7.59;
7.60;
7.76;
7.50;
7.52;
7.43;
7.43;
7.45;
7.36;

7.39;
7.39;
= 7.41
7.30;
7.95;

8.39;

7.91;
7.88;
7.92;
7.87;
8.39;
7.99;
7.98;
8.44;
H6>7 * 7.50; H9
H& = 7.67;
H6.7 = ">•
H6 = 7.71;
H4 = 7.57;
H4 = 8.20;
H4 = 7.57;
H4 = 7.61;
H6 = 7.64;
H4 = 7.54;

H4 = 7.56;
H4 = 7.56;
; H4>6 - 7
H3 = 7.43;
H7 = 7.55;

H7 = 7.69;

H6 = 7.64;
H6 = 7.62;
H6 = 7.57;
H6 = 7.54;
H6 . 7.78;
H4 = 7.77;
H4 = 7.76;
H4 = 8.06;
HB •
7.45-7
H7 .
H8 =
H8 =
H6 •
H6 •
H8 .
H8 =

H7 =
H7 =
.48
H8 =
HB -

H8 -

H8 =
HB •
H7 .
H7 =
H7 =
H8 -
H7 =
H7 =
= 8.
7.43
.56;
7.58
7.50
7.62
7.71
7.49
7.40
7.46

7.52
7.52

7.51
7.33

7.51

7.39
7.36
7.50
7.46
7.64
7.47
7.51
7.70
29
; H9
H9
; H9
; H9
; H9
; H9
; H8
: H9
; H9

; H9


: H9
; H9

; H9

; H9

; H9
; H9
; H9
; H9
; H9
; H9

- 8.28
= 8.31
= 8.25
= 8.17
= 7.49
- 8.44
= 7.43
= 8.19
- 8.06

= 8.16
- 8.16

= 8.14
= 7.79

= 8.18

= 7.79
= 7.77
= 7.87
= 7.82
= 8.18
= 7.71
= 7.77
= 8.23
Coupling Constants (J)
(Hertz)
'7.9 =
J8,9 =
J7,9 =

J3,4 *

'3.4 •
J3.4 •
J8.9 =
J8.9 =

'2.4 •

J2,4 -
J2.3 =
J8.9 '
J7,9 =
J8.9 =
J7,9 =
J8,9 =
Jfl.9 =
J6.7 -
J&.7 -

•>8,9 =
J7,9 =
^7,9 =
1.3
8.3;
1.1
9.0;
8.8;
8.7;
8.8;
8.8;
8.9;
8.5;

1.5;
1.8;
2.0;
8.4;
7.4;
1.5
7.8;
1.2
8.3;
7.9;
8.8;
8.8;
8.8;
8.5
1.65
2.0

'6.8 •

J7.9 -
J8,9 -
J8,9 =
J6,9 =
J6.8 -
J6,8 =
'2.4 -

J7,9 =
J7,9 =
J&.8 *
J8,9 =
J7.8 -

J7.8 =

J6.8 =
'6.8 =
J7.9 =
J7,9 =
J7.9 -




1.8

2.3
8.5
8.7
0.4
1.9
2.0
1.65

1.5
2.0
2.0
8.5
7.6

7.8

1.6
2.0
1.8
2.0
2.2



Reference
Kurokl et al..
Bell and Gara,
Kurokl et al..
Safe and Safe.
Kurokl et al.,
Bell and Gara.
Kurokl et al..
Kurokl et al..
Bell and Gara.
Kurokl et al..

Kurokl et al..
Bell and Gara,
Kurokl et al..
Kurokl et al..
Kurokl et al..

Safe and Safe,

Kurokl et al..
Bell and Gara,
Kurokl et al..
Bell and Gara,
Safe and Safe,
Kurokl et al..
Kurokl et al..
Bell and Gara,
1984
1985
1984
1984
1984
1985
1984
1984
1985
1984

1984
1985
1984
1984
1984

1984

1984
1985
1984
1985
1984
1984
1984
1985
              2,3.7.8-tetra-
CO
cr>
H! 9 = 7.90;  H4 6 = 7.70
Hi'9 = 7.94;  H4'fc = 7.67
Hi'9 = 7.89;  H4'fc = ?
Kurokl et al.. 1984
Bell and Gara. 1985
Norstrom et al.. 1979

-------
INJ
                                                                              TABLE 2-8 (cont.)


PCOF
2,4.6-7-tetra-
2.4,6.8-tetra-
3,4.6,7-tetra-



i
tn








o
CP
2
CO
1,2,3,4
1,2.3.4
1.2,3,6
1.2,3,6
1.2,3,7
1.2.3,8
1.2.4,6
1.2.4.6
1.2.4,6
1.2,4.7
1,2,4.7
1.2,4.8
1.2.6,7
1.3.4.6
1.3.4.6
1.3.4,6
,6-penta-
,8-penta-
,7-penta-
,9-penta-
,8-penta-
,9-penta-
,7-penta-
,8-penta-
,9-penta-
,8-penta-
,9-penta-
,9-penta-
,8-penta-
,7-penta-
,8-penta-
,9-penta-
(ppm
Hi -
Hi -
Hi. 9
Hi. 9
H7 .
H6.7
H4 =
H4 =
H4 .
H4 =
H4 =
H4 .
H4 =
H3 =
H3 =
H3 =
H3 =
H3 =
H3 =
H3 =
H3 =
H2 =
H2 =
H2 =
Chemical Shifts
downfleld from tetramethylsllane)
7.79; H3 = 7.51;
8.23; H3 = 7.73;
= 7.77; H3j * '
1 H8
L53
= 7.48; H9 = 7.72
= 7.70; H9 = 8.18
= 7.70; H2?8 = 7.46
7.58;
= m;
7.89;
7.72;
7.71;
7.71;
7.65;
8.06;
7.69;
7.65;
7.63;
7.60;
7.65;
7.69;
7.63;
7.68;
7.69;
7.52;
7.51;
7.48;
7.51;
H8 = 7.38;
7.55-7.56;
H7 = 7.74;
HB = 7.52;
H8 = 7.45;
H7 = 7.43;
H6 = 7.71;
H6 = 8.08;
H6 = 7.64;
H6 = 7.64;
H8 = 7.54;
HB = 7.51;
H7 = 7.59;
H7 = 7.46;
H6 = 7.79;
Hj = 7.58;
H6 = 7.67;
H4 = 7.61;
H8 = 7.53;
H7 = 7.54;
H7 = 7.44;
;«4
H9 =
; H9
; H9
; H9
; H8
; H9
; H9
; H9
! H7
; H9
; H9
; H9
; H8
; H9
; H8
I **~J
| no
; H9
; H9
;H8
* 8.24
8.27
= 8.37
= 8.15
= 8.13
= 7.34
= 8.40
= 8.52
= 8.39
= 7.43
= 8.19
= 8.15
= 8.25
= 7.37
= 8.45
= 7.47
- 7.52
= 8.38
= 8.11
- 8.14
= 7.34
Coupling Constants (J)
(Hertz)
J8,9 °
J8,9 =
Jl.3; ;
J8.9; 1
^7.8 =
J7.9 =
J7.9 -
J6.7 •
J8,9 =
J8,9 =
J7.8 •

J&.7 •
Ja!9 =
J7,9 =
-"7.8 •

J6.8 -
J&.7 =
J3.4 •
J8,9 «
J7.9 =
J7.8 -
8.45; J] 3 = 2.1
8.3; Ji>3 = 1.9
f,9 = 1-8
1.2 = 8.7
7.75; J8 9 = 7.55;
1.4
1.3
8.6; J7>9 = 2.2
8.6
8.5
8.5

8.6
8.7
8.6
2.1
8.5

2.0
8.B
8.85
8.4
2.0
8.9
Reference
Kurokl et al..
Bell and Gara,
Kurokl et al..
Bell and Gara,
Kurokl et al..
Kurokl et al..
Safe and Safe,
Kurokl et al..
Bell and Gara,
Bell and Gara,
Kurokl et al..
Safe and Safe,
Bell and Gara.
Bell and Gara,
Kurokl et al..
Bell and Gara,
Kurokl et al..
Bell and Gara,
Kurokl et al..
Kurokl et al..
Bell and Gara,
Kurokl et al.,
Kurokl et al..
Bell and Gara,
Bell and Gara,
1984
1985
1984
1985
1984
1984
1984
1984
1985
1985
1984
1984
1985
1985
1984
1985
1984
1985
1984
1984
1985
1984
1984
1985
1985

-------
vO
                                                                           TABLE 2-8 (cont.)
«i^











rvj
I
O>













O
\
—1
^

1.3.4,7

1.3.4.7
2,3.4,6

2,3.4.6
2.3,4,6
2.3,4,7


1.2.3.4

1,2.3,4

1,2,3,4

1.2,3,4

1.2.3,4

1.2,3,4
1,2,3.6


1,2.3,6
1,2,3,6

1.2.3.7
1,2.4,6
PCDF
,8-penta-

,9-penta-
,7-penta-

,8-penta-
,9-penta-
,8-penta-


,6.7-hexa-

6 8-hexa-

6 9-hexa-

7 8-hexa-

,7,9-hexa-

,8,9-hexa-
7 8-hexa-


7 9-hexa-
R 9-hexa-

,8,9-hexa-
,7,8-hexa-
Chemlcal Shifts
(ppm downfleld from tetramethylsllane)
H2 = 7.46;
H2 = 7.49;
H2 = 7.51;
H! = 7.89;
H! = 7.93;
H! = 7.92;
H! = 8.32;
H! = 7.91;
HT = 8.43;
HT = 7.93;
H8 = 7.55;
H8 = 7.53;
H7 = 7.59;
1 '
H7 = 7.59;
H7 = 7.50;
H7 = 7.48;
H6 = 7.79;
H6 * 7.77;
H6 = 7.59;
H6 = 7.58;
H6 = 7.68;
H4 = 7.74;
H4 = 7.72;
H4 = 8.16;
Hi = 7.73;
^ •
Hi 7 = 7.71
^ ( 1
H4.6 = 7-65
H3 = 7.65;
H6 =
H& •
H6 •
H8 =
H8 -
H7 .
H7 =
H& •
H& •
H& •
H9 .
H9 .
H9 =
H9 =
HB -
o
HB -
H9 =
H9 .
HB -
HB -
H7 =
H9 =
H9 =
H9 .
HR =
O
or


H9 =
7
7
7
7
7
7
7
7
8
7
8
8
8
8
7
7
8
8
7
7
7
8
8
8
7
7.


8
.73; H9 = 8.31
.77; H9 = 8.36
.56; H8 = 7.44
.47; H9 = 7.68
.50; H9 = 7.71
.54; H9 = 7.77
.45; H8 = 7.30
.77; H9 = 7.97
.09; H9 = 8.46
.73; H9 = 7.87
.16
.14
.22
.21
.40
.38
.41
.40
.48
.47
.52
.35
.34
.51
.55
74


.36
Coupling Constants
(Hertz)


36.8 =
Ja.9 -
Ja.9 =
J7.9 =
J7.8 -



J8.9 =
J8.9 =
J7 9 =
J7|9 •
J7,8 =



J6.8 •
J&.8 =
J6,7 =










1
8
8
2
8



8
8
1
1
8
8


1
1
8










.9
.4
.2
.0
.4



.25
.5
.8
.9
.7
.5


.8
.9
.8








(J) Reference
Bell and Gara,
Kurokl et al.,
Bell and Gara,
Bell and Gara,
Kurokl et al..
Kurokl et al..
Bell and Gara,
Kurokl et al.,
Safe and Safe,
Bell and Gara,
Kurokl et al..
Bell and Gara,
Kurokl et al..
Bell and Gara,
Kurokl et al..
Bell and Gara.
Kurokl et al..
Bell and Gara,
Kurokl et al.,
Bell and Gara,
Bell and Gara,
Kurokl et al..
Bell and Gara,
Safe and Safe,
Bell and Gara,
Kurokl et al..

Bell and Gara,
Kurokl et al..
1985
1984
1985
1985
1984
1984
1985
1984
1984
1985
1984
1985
1984
1985
1984
1985
1984
1985
1984
1985
1985
1984
1985
1984
1985
1984

1985
1984
ca
                                         7.99;  H9  =  8.54
Safe and Safe, 1984

-------
                                                                       TABLE 2-8 (cont.)
 I
ro
               PCDF
            Chemical  Shifts
(ppm downfleld  from  tetramethylsllane)
Coupling Constants (3)
     (Hertz)
Reference
1.2

1.2

1 3

2 3



1.2
1 ?
1.2
.4

.4

4

4



.3
3
.3
.6

.6

f>

f,



.4
4
.4
.7

.8

7

7



.6
f.
.7
,9-hexa-

,9-hexa-

8-hexa-

8-hexa-



,7,8-hepta-
8 9-hepta-
,8,9-hepta-
H3
H3
H3
H3
H2
H2
Hi
1
Hi
Hi
Hi
H9
H7
/
H&
_
=
,7

_
=

.
,9
.9
.9
=
_
=
7
7
-
8
7
7
=
=
=
=
8
7
7
.71
.69
7.
.02
.52
.51
7.
7.
8.
8.
.35
.75
.74
; H8 = 7.57
; H8 = 7.54
73

; Hg = 8.30
; H9 = 7.51
92
91
24
32



Kurokl et al..
Bell and Gara.
Kurokl et al..
Nor strom et al
Kurokl et al..
Bell and Gara.
Kurokl et al..
Be 1-1 and Gara,
Nor strom et al
Safe and Safe,
Kurokl et al.,
Kurokl et al..
Kurokl et al..
1984
1985
1984
., 1979
1984
1985
1984
1985
.. 1979
1984
1984
1984
1984
o

\
ro

\
o>

-------
    The 2-carboxyl1c add of DBF has been made by  the  Grlgnard  reaction  from
2-MBDF.  Since  BDBFs  yield  the llthlo  compounds  by  Interchange,  all  four
Hthlo-DBFs are  accessible and  the lithium  atoms can be  replaced by  car-
boxyl,  methyl   (using  dimethyl  sulfate),   halogen or  amlno  groups  (using
0-methylhydroxylam1ne).
    OFDF reacts with  sodium methoxlde 1n methanol  to  yield the  3-mono- and
3,7-dlether.   Similarly,   1,2,3,4-TFDF  undergoes  nucleophlUc   substitution
reactions with sodium hydrogen  sulflde, sodium methlolate and lithium  tetra-
hydrldoalumlnate,  In which the  3-fluorlne atom 1s  replaced  by SH,  SMe  and H,
respectively.
    The directing effects  of  functional  groups  at the 2-pos1t1on  appear  to
be  mainly  toward the  8-pos1t1on regardless  of  whether  the  group  Is  elec-
tron-attracting or  electron-withdrawing  (Keuml  et  al., 1972a).   This  1s  not
so  for  the 3-pos1t1on  since 3-halo- groups  give substantial  amounts  of  the
7-subst1tuted compounds  (Table 2-9).
    2-MIDF  reacts with  ammonia  over  cuprous bromide  at  200-210°C  to  yield
95% 2-am1no-DF (Brown and  Coleman,  1973a).   3-MBDF directs  the  nltronlum Ion
to  the l-pos1t1on;   1-MBDF 1s  nitrated  at  the  3-pos1t1on  (Grlnev et  al.,
1973);  the TrCDFs  are  monochlorlnated   by  SbCl5/CCl4  reagent  to  produce
TCOFs (Table 2-10).
2.4.2.   Photodecomposltlon.  Irradiation of  various  lower  chlorinated  PCBs
In  aqueous  suspensions  of 1 and 10 mg/ft. at  254 nm  (mercury  arc)  caused no
appearance  of  PCDFs.   Irradiation  at  310 nm  resulted  1n  PCDFs  from 2,5-d1-
chloro- and 2,2',5,5'-tetrachloro-PCB  to  the extent of -0.2% after Irradia-
tion  times  of up to 200  hours.   This  suggests that PCDFs  may  be destroyed at
254 nm  but  only  very slowly at 310 nm (Hutzlnger  et al.,  1973).   The pres-
1926A                               2-28                             06/21/86

-------
                                   TABLE  2-9

                Friedel-Crafts Acetylatlon of Substituted PHOFs*
     PHDF    Conditions             Acetylatlng Agent   Derivative   Percentage
                                                                       Yield
-(2-Br)
-(2-C1)
-(3-Br)

-(3-C1)

8-
8-
N1trobenzene/AlCl3 Benzoyl chloride 8-
(50-60°C/1 hr) 7-
8-
7-
84
84
56
31
60
3
*Source:  Keuml et al., 1972a
1926A                               2-29                             06/23/86

-------
                                                                           TABLE 2-10

                                         Chlorlnatlon of TrCDF with Antimony Pentachlor1de/CCl4 Reagent  to  Produce  TCDFs*
   Produced          	Original  TrCDF
     TCDF
                     123  124  126  127  128   129  134  136  137  138  139  146  147  148  149  234   236   237   238   239   246   247  248  249  346  347  348  349


     1234             XXX                                            X
     1236             X         X                       X                                            X
     1237             XXX                                            X
     1238             X                   X                        X                                            X
     1239             XXX                                            X
     1246                  XX                                           X                                           X
     1247                  XX                                           X                                           X
     1248                  XX                                            X                                            X
     1249                  XX                                            X                                            X
     2346                                                                                       XX                   X                   X
     2347                                                                                       XX                   X                   X
     2348                                                                                       XX                   X                   X
     2349                                                                                       X                    X                   X                   X
     1346                                          XXX                                                               X
7»   1347                                          XXX                                                               X
La   "48                                          XXX                                                                X
<=>   1349                                          XXX                                                                X
     1267                       XX                                                                                                                XX
     1268                       XX                                                                                        XX
     1269                       XX                                       XX
     1278                            XX                                                                     XX
     1279                            XX                   XX
     1289                                 XX
     1367                                               XX                                                                                   XX
     1368                                               XX                                                          XX
     1369                                               X              XXX
     1378                                                    XX                                      XX
     1379                                                    X         X
     1467                                                                   XX                                                           XX
     1468                                                                   XX                                  XX
     1469                                                                   X               X
     1478                                                                        XX              X              X
     2367                                                                                           XX                                       XX

     SB                                                                                           '    ,    !
O   2467                                                                                                               xx               XX
a*   2468                                                                                                               X          x
£   3467                                                                                                                                   XX

CO
        ::   Adapted from Hazer et al.,  1983a,b

-------
ence  of  the   triplet   sensltlzer,   4,4'-d1chlorod1benzophenone,   Increased
photodecomposltlon of 2,8-DCDF (Crosby and Mollanen,  1973).
    Choudhry and  Hutzlnger  (1982a,b)  reviewed  the  photochemical  formation
and degradation of  PCDFs.   PCDFs  could be produced  1n  yields  up  to 10% from
polychlorlnated dlphenyl ethers (0.8 mM  1n methanol)  bearing 2- or  2'-chloro
substHuents  after  88  hours  Irradiation  at  310   nm  {Choudhry   et  a!.,
1977a,b).  The addition  of  the  triplet  sensltlzer  acetone  at 0.45 M markedly
Increased   the   PCDF  yield  while   suppressing   reductive  dechlorlnatlon.
Greater than 50%  yields  of  2-MCDF,  2,3-DCDF  and  2,3,8-TrCDF were obtained 1n
the presence of  acetone at 310 nm after  10-15 hours Irradiation of 2,4'-d1-
chloro-,  2,4,5-trlchloro- and  2,4,4',5-tetrachlorod1phenyl  ether,  respec-
tively.   The  PCDFs  can also be  produced In  solvents  such as  n-hexane  and
ethanol (Choudhry and Hutzlnger, 1982a,b).
    The  photodegradatlon of  OCDF  Irradiated at 310  nm In  n-hexane  1s more
rapid than  that of  2,8-DCDF  similarly  Irradiated  (Hutzlnger et al., 1972a,b,
1973).   The half-lives  were -1.5  and  2.5  hours,  respectively.   There  was
also  a  pronounced  solvent  effect.   The  half-life  for OCDF  In  methanol  was
-15  minutes.   This  1s  the  reverse  of   results  with  OCDD (Crosby  et al.,
1971).  Irradiation  of  both  PCDFs  In  hexane  for  20 hours caused formation of
a  "yellow gum,"  probably  a  polymer, which  showed  no  recognizable chlorine
1sotop1c  patterns  1n the mass spectra.   At shorter Irradiation times, reduc-
tive  dechlorlnatlon  was postulated to be  the  major  photoprocess  although no
photoproducts  were  Identified unambiguously.  When water  was  used  as  a sol-
vent  and  thin  films of the  two  PCDFs were  Irradiated at  310  nm,  the same
products  were  formed although much more  slowly.   The  2,8-DCDF also produced
a  TrCDF,  probably because  the  viscous  film allowed  free  radical  "cages" to
exist  for  comparatively  long  times.   This  proves  that   -Cl  1s  produced


1926A                               2-31                             06/21/86

-------
during the Irradiations.  The OCDF 1n a  thin  film  or  1n solution appeared to
produce PCDFs to HpCDFs.
    Crosby and  Mollanen (1973) confirmed  the previously stated  results  for
2,8-DCDF  (10-100  mg/a)  1n methanol  after  Irradiation  1n  a solar  simulator
and  1n addition,  unambiguously  Identified   2-MCDF  as  the  first  reductive
dechlorlnatlon product.   As expected, the  half-life was  longer  than reported
for  OCDF  above  (-75  hours).   The  2-MCDF  was  almost  unaffected by  further
Irradiation  (the  half-life was  -1  day),  whereas  95% of  the   2,8-DCDF  was
degraded within 48  hours.  The  photodecomposHlon  rate depended  also  on  the
purity of the methanol, technical grade  methanol containing  acetone (a trip-
let  sensltlzer)  decreasing   substrate   half-life  to  near  25  hours.   The
absence of  lower  chlorinated blphenyls  1n   most  environmental   samples  was
thought to Indicate a potential  for  the occurrence of  the  hydroxylatlon  and
PCDF photochemical routes  1n  the environment  (Crosby et al.,  1973).
    Buser (1976b)  reported  that  4 hours of  UV Irradiation  (mercury  arc)  of
25  yg/ml  OCDF   In  95%   hexane/benzene  caused   extensive   dechlorlnatlon,
-90%  of  the  compound  being   degraded.   The  major  products  were HxCDFs  and
HpCDFs with trace  amounts  of  PeCDFs.  After   24 hours  of  Irradiation,  HxCDFs
predominated  (40%)  along  with PeCDFs and  HpCDFs,  and also  trace amounts  of
TCDFs.  Only  2% of OCDF remained.   At  least  13 HxCDFs were formed  from  the
prolonged  Irradiation.   The  dechlorlnatlon  was  not  as  selective  as  for
OCDD.  These  events were  also confirmed by Firestone  (1977b).   Preferential
reductive  dechlorlnatlon   (mostly  to  HpCDFs)  was  Induced  by   4  hours   of
Y-1rrad1at1on  (60Co;  1.4  Mrad/hr).    Unfortunately,   specific   Isomers were
not Identified 1n any  of these experiments.
    Mazer and Hlleman  (1982)  and Mazer  et   al.  (1983a,b)   Irradiated  eight
TCDFs  (2,3,6,8-,  2,4,6,7,  1,2,7,8-,  1,4,6,8-,  1,2,4,8-, 2,4,6,8-,  2,3,7,8-


1926A                               2-32                             06/21/86

-------
and  1,2,3.4-)  at  1  yg/mj.  In  n-tetradecane or  n-hexane with  254 nm  light
for  4  hours.   GS/MS after  HPLC  showed the TrCDFs were  mostly  formed  (Table
2-11).  DCDFs  were also produced  towards  the  end of  the  photolysis  experi-
ments.  The order  of photodegradatlon  for  chlorines  1n 1,2,3,4-TCDF  was 3- >
2- >  1-  = 4-.   For 1,2,4,8-TCOF,  the  1- and 2-pos1t1ons were most reactive.
Thus,  1t  was  found  that  chlorines on  the same aromatic ring  stabilize  the
loss  of  a chlorine  from  that ring,  that  adjacent chlorines around  a  given
chlorine  will  facilitate  preferential  cleavage  of  that chlorine,  and that 1f
there  are an  equal number of vicinal  chlorines,  the 3-chlorlne will  be lost
before the 2-chlor1ne.
     Mazer  and  Hlleman  (1982) and Hlleman  et al.  (1985)  also reported on the
photodegradatlon  of  PeCDFs  (1,2,3,6,7-, 1,2,3,4,8-,  2,3,4,6,9-,  1,3,4,6,7-,
2,3,4,6,8- and  2,3,4,6,7-)  at  254 nm  1n hexane  (Table 2-12).  The same gen-
eral  principles appear to  hold  as for the TCDFs, that  1s,  the most substi-
tuted  ring tends  to  lose  chlorine, especially  1f adjacent chlorines are pre-
sent.  A  quantitative analysis of  the  data  1s not yet  available.
     Ballschmlter  et  al.  (1985)  showed  that the  dechlorlnatlon  of OCDF  by UV
light  favored   expulsion  of the chlorine  In  the 9-pos1t1on  and  to  a  lesser
extent  the  8-pos1t1on.    The  1,8-congeners dominated  among the  HpCDF  and
HxCDFs formed.
2.4.3.    Pyrolysls.   Very few studies  of  pyrolysls  of  pure  PHDFs have been
reported.   Thermal degradation  of OCDF at 400°C for  15 hours  In  a  sealed
silica tube  resulted  1n expulsion  of chlorine  1n  the  9-pos1t1on   (Ball-
schmlter  et  al.,  1985),  and OCDF was  thermally much  less  stable than OCDD.
HpCDFs mainly  resulted with  the 1,2,3,4,6,7,8-HpCDF  dominating.
 1926A                               2-33                             06/21/86

-------
                                  TABLE 2-11
              Photodegradatlon  of  TCDFs (1  pg/mft)  at  254 nm After
               4 Hours of Irradiation  In Hexane or Tetradecane3
TCDF
4:0C
1,2,3,4-
3:1
1,2,4,8-
2:2
2,3,6,8-
1,4,6,8-
2,4,6,8-
2,4,6,7-
2,3,7,8-
1,2,7,8-

Major

1,2,4-
1.0

2,4,8-
1.0

2,4,8-
1.0
2,4,6-
1.0
2,4,8-
1.0
2,4,7-
1.0
2,3,8-
1.0
1,2,8-
1.0
TrCDFs and Their
Formed bv
Second

1,3,4-
0.38

1,4,8-
0.4

2,4,7-
0.59
1,4,6-
0.59
2,4,6-
0.40
2.4,6-
0.45
2,3,7-
0.52
2,3,8-
0.94
Relative Rat1osb
Photolysis
Third

2,3,4-
0.13

1,2,8-
0.1

2,3,8-
0.09
2,4,9-
0.60
-
3,4,8-
0.1
-
1,2,7-
0.75

Fourth

1,2,3-
0.12

1,2,4-
ND

2,3,6-
0.03
1,4,8-
0.21
-
3,4,6-
ND
-
2,3,9-
0.37
 Source:  Mazer and Hlleman, 1982
 Assuming equivalent mass spectrometer responses.
C4:0  Substitution   Indicates  four  chlorines  on  one  aromatic  ring  and  no
 chlorines on the other aromatic ring.
ND = None detected at the point at which DCDFs began to form.
1926A
2-34
06/21/86

-------
                                                      TABLE  2-12


|5                                 PhotodecomposIt Ion of PeCDFs  In Hexane at 254  nm*
rsj
CO
in
o
<3>
ro
_j
-v
00

Produced TCDF


1234
1236
1237
1238
1239
1246
1247
1248
1249
2346
2347
2348
2349
1346
1347
1348
1349
1267
1268
1269
1278
1279
1289
Original PeCDF
*^«o«.,-....o,;SSS|5|ESgS8S!5S8!o8S{5S!5


X X X X
X XXX
X XXX
X XXX
XX XXX
X XXX
X X XX
XXX X
XXX X
X XXX
X XXX
X XXX
X XXX
X XXX
X XXX
X XXX
X XXX
XX XX
XXX X
XXX X
XXX X
X XX X
X X

-------
VO
ro
                                                 TABLE 2-12  (cont.)
                                                             Original  PeCDF
      Produced  TCDF
oo


1367
1368
1369
1378
1379
1467
1468
1469
1478
2367
2368
2378
2467
2468
3467
fXlCUCVJCsJCXlCNjCNJCNJCVICXlCXlCNJCNJeVlC^CVlCOC^COCOCOOCOCOCOCOCOCXl

X XX X
XX X X
XX XX
XX X X
X X
X XXX
X XXX
X X
XX XX
X XXX
XX XX
X X
X XXX
X X
X X
    *Source:   Adapted from Mazer et al., 1983a,b
o
c»
-V
ro
CO
CK

-------
2.5.   SYNTHESIS

    Synthesis  of  all 135  Isomers 1n  large  quantities  1s  still an  Important

research priority.

2.5.1.   General  Methods.   Coffey  (1973)  has    evlewed   the   older  general

synthetic methods leading  to  the  production  of PCDFs.

    PHDFs are  produced  by  the following methods:

    a.  Eliminating  water  or  hydrogen hallde from  substituted 2,2'-d1-
        hydroxy- or  2-halo-2'-hydroxyblphenyls,  respectively:


                                     Zn Clj
                                  48% HBr/CH, COOH
                 OH   OH
                                                    (Rij»90p«l»n end GiiMpmi. 1942)
                                    Futad KOH
                 Cl   OH
                                                    (Schimmelschmidt, 1950)
    b.
Both types of  reactions occur more easily  under  alkaline condi-
tions  when  halogen  groups are  present  ortho- or  para-  to the
hydroxy and halogen  groups to be eliminated  (Alphen,  1932; Case
and Schock, 1943):

Decomposing  blsdlazonlum  salts  of  substituted  2,2'-d1am1nob1-
phenyls, although  phenazones  are frequent  contaminants (Coffey,
1973):
                                                                 O
                                      H20
         D1azot1zat1on of  substituted  o-am1nob1phenyl  ethers  (HcComble
         et  al..  1931):
 1926A
                             2-37
                                                 where Ph = CeHs-
06/21/86

-------
    d. PHDFs have been  prepared 1n  poor  yield by  the pyrolysls of  substi-
       tuted dlphenyl ethers  (Choudhry and  Hutzlnger, 1982a,b) and  chloro-
       phenols   (Bell,  1936).   This  route may  be  of  environmental  signifi-
       cance since  Incineration  Is often  used  to  dispose of  phenol-Impreg-
       nated woods  and  papers  (Chapter 4).  The reaction  of phenol  and  HC1
       at 550°C for  5 minutes  for  an Initial HC1 concentration  >1  mM caused
       the  production of  trace amounts  of PCDFs and  PCDOs  (Eklund  et  al.,
       1986).
2.5.2.   Methods for PHDFs.  Gllman  et  al. (1934a)   reacted  dlbenzofuran  and
chlorine in  carbon  tetrachlorlde to  yield 30% 2,8-DCDF. The 2-MCDF was  pro-
duced  In  a  similar fashion  In ethanol  as  solvent at  60°C.   The  2-MCDF,
3-MCDF-, 2,8-DCDF  and 3,8-DCDF were synthesized by  Shlbata et  al.  (1952)  and
procedures  were reviewed  by Olta  et al.  (1955).   The 1,3-cycloadd1t1on  of
3,4,5,6-tetrachlorobenzene-2-d1azo-l-ox1de In  chlorobenzene  at  130°C  yields
1,2,3,4-TCDF (Hulsgen et al.,  1964).
    The presence of  higher  PCDFs as  reaction by-products was  noted by Clark
(1940) after the chlorlnatlon of dlbenzofuran, and  also by Cox et  al. (1965)
after  vacuum pyrolysls  of  various dlbenzofuran-based  polymers and  copoly-
mers.   Cox  et  al.  (1965)  observed that  the  chlorinated  polymers were  more
stable  than  the bromlnated  ones  except for the tetra-bromlnated ones.   R1ed
and  Eng (1969) found  that o-qu1none  dlazldes added  benzene  with  nitrogen
elimination  to  yield the 1,2,3,4-TCDF,  1,2,3-TrCDF  and 1,3-DCDF.  OCDF  was
produced by pyrolysls of pentachlorophenol (Sanderman et al., 1958).
    Further  Interest In the synthesis of  PCDFs  had  to  await  more Interest In
their toxlcologlcal  properties  and  those of commercial  PCBs.
    Specific PCDFs  have been synthesized  by direct  chlorlnatlon of  unsubstl-
tuted  dlbenzofuran  (Gray  et al.,  1976),  photolysis of chlorinated  dlphenyl


1926A                               2-38                             06/21/86

-------
ethers (Choudhry  et  al.,  1977a,b; Norstrom  et  al.. 1976a, 1977;  Llndahl  et
al.,  1980),  by Ullman reaction  (MorHa  et al.,  1977b),  photodechlorlnatlon
of OCDF  (Buser,  1976b) and  by thermal oxldatlve  cycllzatlon  of  specific  PCB
Isomers  (MorHa et al., 1978; Buser et al.,  1978a,d;  Buser  and Rappe,  1979),
or chlorobenzenes (Buser, 1979).  The mechanisms  Involved  In  the thermochem-
Ical  generation  of  PCDFs  have  been reviewed  by Choudhry  and  Hutzlnger
(1982b).    Nearly all  of  these  methods  result  1n complex  mixtures  which
require  extensive chromatography  and  purification  before pure  compounds  can
be obtained, In general,  with final  yields <10%.
    A  synthetic  route with  environmental  Implications  1s  the  thermal  produc-
tion  of  PCDFs  from  PCBs.   Buser  et al.  (1978a,d)  and  Buser and  Rappe  (1979)
showed that  when  specific  PCBs  were pyrolyzed  1n  quartz  ampules between  500
and  700°C,  PCOF  yields  1n  the  1-10% range could  be  obtained,  though  they
were  accompanied by  many  other  products,  Including  chlorinated  benzenes,
naphthalenes and  hydroxy  PCBs.   Buser et al. (1978a)  described  the products
of  pyrolysls  at 600°C, Identified  by GC/MS.   Yields  were  as high as  a  few
percent  In  favorable  cases.   The  decompositions  are  summarized 1n  Table
2-13.  There appear  to  be  four  major  paths  for  production of  PCDFs  from
PCBs:  loss  of  two ortho  chlorines, loss of  ortho hydrogen as well as  chlor-
ine,  loss  of an ortho hydrogen as well  as chlorine but  Involving a shift of
chlorine  from  the  2- to the 3-pos1t1on  and  loss  of two ortho hydrogens.
These  paths are  summarized  In  Figure  2-1  for 2,2',4,4',5,5'-hexachlorob1-
phenyl.   Such   paths  are  environmentally  Important 1n  the  origin of  toxic
PCDFs  and  PBDFs from various PCB and PBB formulations,  respectively.   Mazer
and  HUeman (1982),  Mazer  et al.  (1983a,b) and  Hlleman et  al.  (1985)  have
utilized  the technique to  produce  110  pure TCDFs  to  act as  chromatographlc
standards after HPLC separation and confirmation by GC/MS and Kovats Indices.


1926A                              2-39                             06/21/86

-------
                                  TABLE  2-13

            Formation of PCDFs from the Pyrolysls of Specific PCBsa
  PCB Pyrolyzed
                   PCDFs Formed
Tetra:

  2,3,4,5-

  2,3,5,6-

  2,6,2',6'-

Penta:

  2,3,4,5,6-


  2,4,5,2',5'-


  2,4,5,3',4'-


  2,4,6,2',4'-


  2,3,6.2'.5'-



Hexa:

  2,4,5,2'.4',5'-


  2,4,6,2',4',6'-

  2,4,5,2',4',6'-


  2,3,4,2',3',4'-

  2,3,5,2',3',5'-

  2,3,6,2',3',6'-


  3,4,5,3',4',5'-
2,3,4-tr1-b; 1.2,3.4-tetra-

l,2,4-tr1-

l,9-d1; 1.4,9-trl-
l,2,3,4-tetra-b; small amounts of 1,2,4-tM-;
2,3,4-trl-;

2,3,8-tr1-b; small amounts of 2,3,6,8-tetra-
plus three other tetra; 1,3,4,6,9-penta-;

2,3,7,8-tetra-b; 2,3,6,7-tetra-;
1,3,4,7,8-penta;

l,3,7-tr1-b; 1,3,6.7-tetra-;  1,3,7,9-tetra-;
1,3,4,7-tetra-;

1,4,8-trl-; 1.2,8-trl-; 1,4,6,8-tetra-;
1,2,6,8-tetra-;  1,2,4,8-tetra-b;
l,2,6,9-tetra-;l,4,6,9-tetra-;
2,3,7,8-tetra-b;  2,3,4,7,8-penta-;
1,3,4,7,8-penta

1,3,7,9-tetra; 1,3,4,7,9-penta-;

l,3,7,8-tetra-b;  1,3,4,7,8-penta-;
1,3,4,7,9-penta

3,4,6,7-tetra-b;  1,2,3,6,7-penta-:

2,4,6,8-tetra-; 1,2,4,6,8-penta-;

l,2,4,8-tetra-b;  1,2,8,9-tetra-b;
l,2,4,6,9-penta(?);  1,2,4,8,9-penta-;

2,3,4,6,7,8-hexa-;  small  penta-
1926A
        2-40
06/21/86

-------
                              TABLE 2-13 (cont.)
  PCB Pyrolyzed                                PCDFs Formed
Hepta:

  2,3,4,5,2',3',4'-        -2,3,4,6,7-penta-;  1,2,3,4,6,7-hexa-b;
                            1,2,3,6,7,8-hexa-; 1,2,3,4,7,8,9-hepta-;
                            1,2,3,4,6,7,8-hepta-;  1,2,3,4,6,7,9-hepta-;

  2,3,4,5,2',4',5'-         2,3,4,7,8-penta-b; 1,2,3,4,7,8-hexa-;
                            l,3,4,6,7,8-hexa-b;  2,3,4,6,7,8-hexa-;
                            1,2,3,4,6,7,9-hepta-;

Octa:

  2,3,4,5,2',3',4',5'-      2,3,4,6,7,8-hexa-b;  1,2,3,4,6,7,8-hepta-b


aSource:  Buser and Rappe, 1979

bMost abundant PCDF
1926A                               2-41                              06/21/86

-------
                            AT
                                    loss of two
                                    Ortho Cl
loss of ortho H
and Cl with
                                    Cl shift
                                    loss of ortho
                                    H and Cl
                                     loss of two
                                     ortho H
                                                          2,3.7.8-tetra-CDBF

                                                         Cl              Cl
                                                         Cl     O
                                                           2.3,4,7,8-penta-CDBF
                                                           1.3.4,6,7,9-hexa-CDBF
                                     FIGURE 2-1

        Possible  Reaction Schemes to  Produce  PCDFs from the Pyrolysls of
                        2,2', 4,4',  5,5'-Hexachlorob1phenyl

                    Source:  Adapted from Buser  and Rappe,  1979
1926A
    2-42
06/21/86

-------
    The  formation  of  PCDFs  by pyrolysls  of  commercial  chlorobenzenes  1s
similarly Important  (Buser,  1979).   PCDDs, chlorinated  naphthalenes,  chlor-
inated  styrenes  and  chlorophenols  are also  produced.   Samples  that  were
pyrolyzed at  620°C 1n  quartz  ampules  1n  the  presence of air  contained  the
PCDF levels shown  1n  Table 2-14.  The PCDF content was  much  higher  than  the
PCDD content  In  all  cases,  especially for  the trlchlorobenzenes for  which
the ratio of  PCDF  to PCDD content  was >40.   The  amounts of  the  toxic  PCDF
Isomers (2,3,7,8-TCDF-;  1,2,3,7,8-PeCDF-;  2,3,4,7,8-PeCDF-) were small.
    Llndahl  et  al.  (1980) reported that  pyrolysls  of  2,2',4,4',5,5'-hexa-
chlorodlphenyl ether  In quartz  ampules  at 500, 600  and 700°C for  1  minute
yielded  0.1,   1.3  and  0.1%,  respectively,  of PCDFs.    The  products  were
1,2,4,6,8,9-HxCDF,  1,2,4,7,8-PeCDF  and some  PCDDs.   More PCDFs   than  PCDDs
were  formed  when  chlorodlphenyl ethers  were  pyrolyzed  under these  condi-
tions.   Between  3.5  and  4.5%  PCDFs  were  produced   when the  3,5,4'-tr1-,
2,4,5,4'-tetra-,    2,4,6,3',5'-penta- and   2,3,4,5,6,2' ,3',4'-octa-chloro-d1-
phenyl  ethers  (CDPEs) were  pyrolyzed  at  600°C  compared  with up  to  0.6% of
PCDDs.   PCDF   production   was  not   so  favored  from  the  hexa-chlorodlphenyl
ethers     (2,3,4,2',3',4'-,     2,3,4,2',3',5'-,     2,3,4,2',4',5'-     and
2,4,5,2',4',5'-),  PCDF  and  PCDD contents  both  ranging from  0.8-1.3%.   The
same  mechanisms  depicted  In Figure 2-1  for  production  of PCDFs from  PCBs
also prevail from  chlorinated  dlphenyl  ethers  except  that loss of 2-ortho-H,
ortho-H and -Cl  are  favored.  Loss  of  two  ortho-H  appears to be  favored for
the  tr1-  and  tetra-CDPEs,  but  loss of  ortho-H and  -Cl  Is  predominant  for
higher  CDPEs.  The octa-CDPE also  yielded  HxCDFs that can be formed  when two
chlorines are  lost by rearrangement, one of which  was the 1,2,3,4,6,7-HxCDF
formed  by loss of  two ortho-Cl.  Buser (1986)  found  that pyrolysls  of three
polybromlnated dlphenyl  ethers  used as  flame retardants  resulted In yields


1926A                               2-43                             06/23/86

-------
1C
no
a*
                                                       TABLE 2-14


                                  Formation of PCDFs from Pyrolysls of Chlorobenzenes*
Total Amount Percentage of PCDFs Formed Relative to Chlorobenzene
Chlorobenzene
Compound
Tri-
ll, 2, 3-; 1,2,4-; 1,3,5-)
Tetra-
Penta-
Mlxture
(tri-; tetra-; penta-)
Pyrolyzed (yg)
(ratio of Isomers) Tetra-
200 0.20
(1:1:1)
200 <10~4
200 <10~4
500 0.040
(1:1:1)

Penta-
0.55

2.5xlO~3
<2.5xlO"3
0.12


Hexa-
0.28

0.080
<2.5xlO~3
0.22


Hepta-
0.025

0.23
<2.5xlO~a
0.12


Octa-
<2.5xl03

0.10
<1.5xlO"3
1.20xlO~4

    *Source:   Recalculated from Buser, 1979
00

-------
of PBDFs and PBDDs of  up  to  10% at  510-630°C 1n quartz ampules.   The mechan-
ism of formation appeared to be  the  same  as  that for the chlorinated deriva-
tives.  The  2,3,7,8-TBDF  was not a  major product from  pyrolysls  of penta-,
octa- or decabromodlphenyl ethers.
    Perchlorlnatlon has also been Investigated  as  a synthetic route  to  the
PCDFs (Williams and Blanchfleld,  1972; Hucklns  et  al.,  1974;  Crist and Hose-
man,  1977;  Ballschmlter  et  al., 1985).   The  perchloMnatlon  of  2-hydroxyb1-
phenyl  with thlonyl  chloride/antimony pentachlorlde/lodlne  produced 8%  of
pure  OCDF  (Gara et al.,  1980).   No lower PCDFs  were formed  from  the reac-
tion.     Perchlorlnatlon    with   BMC    Reagent    (SO  Cl /S  Cl /A1C1     Is
                                                       C  C   C  C.      
-------
10
ro
TABLE 2-15
Synthetic Methods for PCDFs Using Chlorinated Dlphenyl Ethers (CDPEs) as Substrates




i
£






o
NS
CO
a*
Starting COPE PCDF
3',4,4'-Tr1- 2,3,8-TM-
3.3'.4.4'-Tetra- 2,3.7.8-Tetra-
3,3'-D1- 3.7-D1-
2.2',4,4'.5,5'-Hexa- 1 ,2,4,6,8,9-Hexa-
2.2'.3,3',4,41-Hexa- 2,3.4,6.7.8-Hexa-
2.2'.4,4'-Tetra- 2,4,6.8-Tetra-
2,2'.4.4l.5-Penta- 1, 2.4,6, 8-Penta-
2,31,4.4',5-Penta- 1 ,2.4.6, 8-Penta-
2,2',3,4,4'-Penta- 2,3.4,6.8-Penta-
2,2',3,4,4',5-Hexa- 1,2,4,6.7,8-Hexa-
2.2'.3.3',4,4'.5-Hepta- 1 ,2.3,4.6.7,8-Hepta-
aM1th column chromatography
bWHh preparative TLC



Reaction Time
(hours)
0.50
1.0
0.66
14
3.5
2.0
2.0
2.0
2.0
2.0
2.0





Yield Recrystalllzlng
(X) Solvent
46 n-Hexane
43 n-Hexane
47 MeOH
36 Chloroform
55 Chloroform
cci4
67 CCl4a
54 CCl4a
49 CCl4a
84 CCV
33 CC14





Reference
Sanderman et al.,
Sanderman et al..
Norstrom et al..
Norstrom et al..
Norstrom et al.,
Gara et al., 1979
Crist and Moseman
Crist and Moseman
Crist and Hoseman
Crist and Hoseman
Crist and Hoseman






1958
1958
1977
1977
1977

. 1977
. 1977
, 1977
. 1977
. 1977






-------
tography or  preparatlve-TLC.   Bell  and Gara  (1985)  have synthesized all  87
TCDFs, PeCDFs, HxCDFs, HpCDFs and OCTA using this synthetic  route.
    Another method  1s  the  cycllzatlon of  dlazotlzed  chlorophenoxy-o-an1l1nes
(Gray  et  al.,  1976;  Kurokl  et  al.,  1984).   Commonly,  a  nltro-chlorlnated
dlphenyl ether   1s  obtained by  reaction  of the appropriate  potassium  halo-
phenolate and  the  halonltrobenzene  at 120°C  for 15  hours.   The nltro  group
Is  converted  to an amlno  group  (CH-COOH/Fe for  15 hours), dlazotlzed  and
                                     O
cycllzed with  Isoamyl nitrite  1n tetrachloroethylene  (80°C for 15  hours).
The crude product 1s  purified by column chromatography  and  recrystalUzed.
Overall yields are typically -6-10%.
    A  modification  of  the  above   1s  the  base-catalyzed  cycllzatlon   of
hydroxy-PCBs In DMSO/KOH (Safe and Safe,  1984).  The hydroxy-PCB can  be pre-
pared  from coupling of a chlorinated  anlsldlne  and 1-substltuted  symmetrical
benzene at  120°C 1n  Isoamyl  nitrite  for  18 hours  followed  by  purification
and  demethylatlon  (BBrg/CHpCK  at   20°C   for  24   hours).   It   can   also
arise  from coupling of a 2-chloro-an1l1ne with  a chlorinated anlsole  In Iso-
amyl nitrite followed  by purification  and  demethylation.  The yields  Includ-
ing the Initial  coupling  reaction range  from 3-15%.   The major  advantage of
the latter  modification 1s  that  only  single Isomers are  usually produced.
    Bell  (1983)  has   reported   on   the   synthesis  of  uniformly  labeled
13CTCDF, using  the  Ullman  ether  procedure or  by  phenoxlde  displacement  on
an   lodonlum   salt.    Yields    commonly   exceeded   30%.    Synthesis   of
14C-2,3,7,8- TCOF was  first reported  by Gray (1981).
    Pyrolysls of  octafluorodlbenzothlophene-5,51-dioxide affords  perfluoro-
dlbenzofuran (Chambers et  al., 1968).
1926A                               2-47                             06/21/86

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    1,2,3,4-TFDF  1s  prepared  from  hexafluorobenzene  and  o-!1th1oan1sole.
The o-methoxy  blphenyl  was  first formed,  then  the free phenol  (by  reaction
with aluminum  chloride) and  finally  the TFDF by refluxlng  In  with  potassium
carbonate and dimethylformamlde (Brown et al.,  1967).
 1926A                               2-48                             06/21/86

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                     3.  SAMPLING AND ANALYTICAL METHODS
3.1.   SUMMARY
    The major  thrust of  research  In  analytical  methods  for  the PHDFs  has
been  toward  specific synthesis, separation  and sensitive detection  of  cer-
tain  toxic  PCDFs and PBDFs,  especially the  2,3,7,8 derivatives.  One  such
analytical method  Is the  cap1llary-GC/MS  technique developed  by scientific
teams headed by  Buser and  Rappe  (1979);  many groups have now used this tech-
nique.
    Earlier, the lack  of analytical standards  severely  hampered  the  quantl-
tatlon and  Identification  of specific Isomers, though methods  of quantHat-
Ing  the   total  Isomers   containing  a given  number  of  halogens  (GC/MS)  and
total  PCDFs  (by perchlorlnatlon) have been  developed.   Since  many compounds
have  been shown to  co-elute  with  PCDFs on  gas chromatographlc columns,  and
compounds  (for  example,  chlorinated dlphenyl ethers) may  Interfere  with  the
mass  spectral  analysis,  relatively  specific  cleanup  techniques have  been
developed,  often based  on  the use  of  aluminum oxide column  chromatography
and  Judicious  choice of  solvents,  usually  various  combinations  of  n-hexane
and  methylene  dlchlorlde.   Techniques have  been developed to  Identify PHDFs
1n  PCBs,   Yusho oil, chlorophenols,  fly  ash,  Agent  Orange,   2,4,5-T,  wood
dust,  animal tissues,  gelatin,  human  and  fish  tissues,  mothers' milk  and
bovine milk, wastewater  and PBBs.  Other  methods  are  not as sensitive or as
specific  as  caplllary-GC/MS.  Of  some   utility as  a  screening  test before
GC/MS 1s   a  radlolmmunoassay  technique.  A  cytosol receptor  bloassay  also
shows promise.
     Sampling of PHDFs  Is  comparatively underdeveloped.   Charcoal and XAD-2
resin have  been used to  sample vapors  of  PCDFs.  Modified  EPA-5   sampling
trains are used to  sample  stack  emissions.


1927A                               3-1                               06/23/86

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3.2.   SAMPLING METHODS
    Few  sampling  methods have  been developed  specifically  for PHDFs  since
Interest has been  focused on  the analysis of various  environmental  and  com-
mercial  samples  obtained by  the  usual  procedures.  A review has been  pre-
sented by Tlernan  (1983).  The  federal  procedures  governing  custody,  safety,
transportation, data  review,  sampling  and  the  analysis  of  PCDDs and  PCDFs
have been summarized by Elly (1985).
3.2.1.   Incinerators.
    PCDFs and  PCDDs  In  the  vapor  phase have  been  collected  by  adsorption
onto charcoal  (Norlt  Pk,  0.5-1  mm or Amberllte XAD-2,  20/50 mesh)  contained
In  a  glass  filter  (Rappe et  al.,  1978b).  The vapors were drawn through  a
glass funnel Into  the  filter  by  means of  a  vacuum pump.  Both adsorbents had
to  be  cleaned  by  prior  Soxhlet  extraction  with methylene dlchlorlde  for  24
hours.  The PCOFs  and PCDDs  were desorbed by Soxhlet  extraction  with  methy-
lene  dlchlorlde  for  10  hours.   Partlculate PCDD  or PCDF can be  trapped  on
glass wool  filters that  can  be eluted with  toluene  (Ahllng et al.,  1977).
PCDFs and PCDDs  In the vapor phase were  also collected after  this  filter  by
adsorption  onto  Chromosorb  W coated with 30% Aplezon  M; the columns  can  be
eluted with hexane and toluene.  PCDF and PCDD partlculates and  vapors  have
also  been  collected  1n  Implngers   similar  to  a U.S.  EPA method  5  sampling
train  (OHe et al., 1977, 1982; Cavallaro et al., 1980;  G1zz1  et  al., 1982;
Redford  et  al., 1983;  Wang  et  al.,  1983;  Benfenatl  et  al.,  1983;  Chlu  et
al.,  1983;  Taylor  et  al.,  1983; Ballschmlter  et  al., 1984; Brocco  et  al.,
1984; Clement  et  al., 1985a;  Halle et  al.,  1985;  Weeraslnghe et  al.,  1985a;
Scheldl  et  al.,  1985).   Only  three  groups of Investigators  have attempted to
characterize  the  collection  of  PCDFs   In  the  segments of their  sampling
train.   The closest  approximation  to the  EPA-5  sampling train  (Clement  et


1927A                               3-2                              06/23/86

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al.,  1985a)  was  the  addition of  two Flor1s1l  (10  g)  cartridges after  the
third  Implnger.   In general,  95% of  the  total PCDD/PCDF  was  found  In  the
Implngers, -5%  on  the  filter before  the  first  Implnger,  and  0.3%  on  the
FloMsIl  cartridges.   The  backup FloMsIl  cartridge contained  5% of  PCDF
found  In  the front cartridge.  The  volatile PCDFs were  relatively  enriched
on  the  Florlsll  filter  compared  with the prefllter  and  Implngers.   However,
the  extraction  recovery  of spiked 1,2,3,4-TCDD,  2,3,7,8-TCDD,  2,3,7,8-TCDF,
a PeCDD, a HxCDD, a HpCOD and the OCDD averaged only 43%.
     In  another  sampling  train (Ballschmlter  et  al., 1984), the  sequence  of
components was a  glass fiber  filter,  a  condenser  at  15-18°C,  and two Implng-
ers  containing methoxyethanol at  0°C.  The  PCDD/PCDF  ratio  on  the filter and
1n  the  condensate were similar,  but  PCDFs  were much more  concentrated than
PCDDs  1n  the Implngers with  no HpCDD/HpCDF  and OCDD/OCDF present here.  This
confirmed  the vapor phase nature  of  the condensable fraction.   The overall
collection efficiency was not determined.
     The  sampling  train  utilized  by  Tlernan et  al.  (1985)  comprised,  1n
order,  a  heated  sampling  probe,  a heated cyclone, a heated glass fiber fil-
ter,  and  a series of eight  Implngers  at  0°C, the  first  two containing water
and  with  XAD-2  traps  Intervening  between  empty Implngers 3, 4 and 5.  Sodium
arsenlte  solution  was placed  1n  Implngers  5 and 6, Implnger 7 was empty, and
Implnger  8 was  charged  with  silica gel.  Known  amounts  of  1,2,3,4-TCDD (1.3
vg)  and  1,2,4,8-TCDF  (1  yg)  were  vaporized and  collected with 92  and 97%
efficiency,  respectively.   Most  of  the  PCDDs  and   PCDFs  (-62%) were  col-
lected  1n   two  XAD-2  traps.   The   recovery  of  spiked   37Cl4-2,3,7,8-TCDD
was  <80%  for  the  acetone  back   rinse,  the  cyclohexane  back  rinse  and the
front  XAD-2  trap.
 1927A                               3-3                              06/23/86

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    The  sampling  method recommended by  the Swedish EPA  Is  also based  on  a
modified EPA-5  train (Beryvall and  Jansson,  1986).  The  sampling  equipment
Is  fortified  before sampling with  known amounts of 13C-surrogate  compounds
1n the filter, condensate or adsorbent  (XAD-2)  to act as Internal standards.
    Fly  ash  samples have  been  collected from  different  points In  flue gas
streams  by  electrostatic  precipitation  (Buser  et  al.,  1978b).  Since  the
highest  PCDD  and  PCDF   levels were  found from samples  collected at  flue gas
temperatures  of 200-260°C,  gas  stream  temperature  should  be  measured during
sampling.   Procedures   to  assure representative  analysis of  the  collected
samples  have  not   been  developed.   It  1s   obviously desirable, however,  to
analyze  as much of the  sample as possible.  Soot type  samples  are  generally
sampled with Kleenex tissues (Rappe  et  al.,  1983c).
    Liquid  samples  should be  thoroughly  shaken  or  ultrasonlcated  before
cleanup  and  analysis.   If liquid samples contain solid matter. It  1s prob-
ably advisable  to filter the solution  and  perform analysis  on the  filtrate
and retain the dry  solid.  The  choice  of solvent to elute any adsorbed PCDFs
depends  on  the  nature   of  the  solid.  Probably methylene  dlchlorlde will  be
adequate for  most situations;  recovery  tests  should be performed to choose
the correct solvent.
    Organ  and tissue  samples  are  usually preserved  In  4  or  10%  buffered
formalin (Nagayama  et  al., 1977).   Both tissue and formalin  should be ana-
lyzed  for  PCDFs.   Another  much-used alternative 1s  to  freeze the  tissues at
-70°C  (Albro et al., 1985).
3.3.   GC METHODS FOR THE PCDFs
3.3.1.   Packed  Column   GC.   Because  certain  PCDF  Isomers  are  extremely
toxic  to animals   (Chapter  7),  Interest In the analysis  of  these  compounds
has Increased.  Much of the early work  was hampered by losses Incurred dur-

1927A                               3-4                              06/24/86

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ing sample  cleanup  and analysis, and  by  the fact that the PCDF  peaks  often
coincided with the  peaks  of chlorinated dlphenyl ethers containing  two more
chlorine  atoms  (Crummett and  Stehl,  1973).   Thus,  a  confirmative  spectro-
scoplc  technique,  such as  mass  spectroscopy using multiple  1on  monitoring,
must be used to prove  the specificity  of  the separation.   QuantHatlon  with-
out such  confirmation  w1lT  yield maximum possible values  of  the  contaminant
rather than the true value.  The  contaminant  must  be  Identified before  valid
quantification can  occur.   These problems  have been  reduced by the use  of
capillary GC, which gives more specific separation.
    The presence of PCDFs 1n PCBs was  first  deduced  by Vos et al. (1970),  on
the basis of GC/HS  evidence.  A  2 mg sample  of PCB 1n hexane  was  placed on a
Flor1s1l  column and eluted  with  hexane followed by 5% ethyl  ether  1n hexane
until all PCBs were eluted.  The PCDFs were  eluted with 25%  ether  In hexane
and the  eluate was evaporated.   The  residue  was  then chromatographed  on a
Pyrex column  (5  ft x  1/8  1n)  containing 10%  DC  200  on Gas  Chrom  Q (80/100
mesh)  held  at  200°C,  with  nitrogen  as  carrier  gas  at   50  mi/mln  and  the
separated peaks subjected  to mass spectroscopy.   Only the Clophen  A-60 and
Phenoclor  DP-6 PCBs  contained  PCDFs   since  they were the  only ones  that
caused a  toxic  response In  the  chick  edema assay.   The Investigators  could
not separate or Identify the specific  Isomers  Involved.  A similar  procedure
was also  utilized by Bowes  et al. (1973)  to  determine PCDFs 1n PCBs.  Before
GC/MS analysis, however,  the three  eluates  described  1n  Vos et al.  (1970)
were subjected to  further  fractlonatlon on  an aluminum oxide column with  an
Initial elutlon with  1% methylene  chlorlde/hexane to  collect the  PCBs  and
then with 20% methylene chlorlde/hexane  to elute  the PCDFs.  Bowes et  al.
(1973) also analyzed the  eggs,  fat  and liver  of  sea  gulls for PCDF  content.
Samples were freeze-drled, ground with  sodium  sulfate  (2:1) In a  heavy  glass


1927A                               3-5                              06/23/86

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mortar, extracted  using the  Soxhlet procedure with  a hexane/acetone  azeo-
trope,  the  solution concentrated  and cleaned  up by  passing over  sulfurlc
acid-Impregnated CelHe  before  concentrating and  continuing the  cleanup  on
the FloMsIl  column  mentioned 1n  the  Vos  method.  No account of  recoveries
were given.
    The lack  of analytical  standards  for  the  PCDFs  hampered further  analy-
sis,  but  still  did  not prevent  Roach and  Pomerantz  (1974),  Bowes et  al.
(1975a,b),  Nagayama  et  al.  (1975,  1976)  and  Kuratsune  et  al.  (1976)  from
establishing  the presence of  PCDFs 1n many PCBs,  In Kaneml  oil  and  1n  Yusho
patients exposed to  Kaneml  oil,  from the mass spectrum alone, without  stan-
dards.  Morlta  et al.  (1977a) postulated the presence  of  the 2,3,7,8-TCOF  on
the basis of  GC retention-time  data for an authentic  sample, but  the levels
quoted  were maximal because  of  the  relatively  low  resolving  power of  the
packed  GC column used.   Morlta  et al. (1977a) eluted  the activated  Florlsll
column  with hexane  and then 95:5  hexane/acetone  to remove  the  PCBs  and col-
lected  the  PCDFs by elutlng with  pure acetone.   Recoveries  were >90%.   This
procedure had  also  been recommended by Vos  et  al.  (1970).  Morlta et  al.
(1977a) then  used  the  MS technique to quantltate  the  PCDFs  using  the parent
Ions.
    The analysis of PCDFs  In  chlorophenols  also was  similarly  Impeded  by
lack  of authentic   standards.   Nevertheless,  PCDFs were  found  1n  chlorophe-
nols  (Firestone et  al.,  1972; Pllmmer  et al.,  1973;  Schwetz et  al.,  1974a,b;
Buu-Hol et  al., 1972)  1n  the  crude  base-Insoluble  organic extract  of  the
chlorophenol.   Buu-Ho1  et al. (1972)  showed  that  consideration  of  the entire
spectrum  allowed discrimination  from other  Interfering  compounds,  whereas
reliance  on specific Ions  led to  errors.  For  example,  the mass spectrum of
2,2',3,3',4,4',5,5',6-nonachloro-6'-hydroxyd1phenyl ether  showed loss of  two


1927A                              3-6                              06/23/86

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chlorine  atoms  to  give a  peak  that  coincides  with the  molecular  1on  of
HxCDFs  (m/e  372).   The  presence  of such ethers  can  be verified  by methyl-
atlon and  subsequent  GC/MS  (Pllmmer et al., 1973).   Typically  (Firestone  et
al.,  1972),  chlorophenol was  converted  to  the  phenolate  by reaction  with
sodium hydroxide, the  PCOFs  extracted  In petroleum ether,  the organic layer
washed, concentrated and transferred  to an  aluminum  oxide  column,  the PCDFs
being eluted  by the  original  procedure  of  Vos et al.  (1970)  plus  a final
dlethyl  ether  elutlon.  The   concentrates  were  then  partitioned  between
petroleum ether and sulfurlc add,  the  organic  layer  neutralized  with sodium
bicarbonate and the solutions evaporated  and taken up 1n Isooctane for GC/MS
and EC/GC  analysis.   Recovery  of  2,3,7,8-TCDD  was 33%;  omission  of the sul-
furlc acid step  Increased  recovery to  63%.   No  recoveries  were  cited  for
PCDFs.  Firestone et  al. (1972) used a  6 ft x 1/4 Inch Pyrex column packed
with 5% OV-101  on 80/100 mesh  Chromosorb  W  (HP) under temperature programing
at  10°C/m1n  to 250°C.   The  sulfurlc acid  step was   subsequently  eliminated
(PUmmer et al., 1973).  Capillary GC/MS Is  discussed  1n Section  3.4.2.3.
    Vlllanueva  et al.   (1974)  found HpCDFs  and OCDF   1n  hexachlorobenzene  by
using  aluminum  oxide  column   chromatography   before GC/MS  and  using  the
cleanup  technique  of   Firestone   et   al.   (1972).    The   Pyrex   GC  column
(10 ft x 6.3  mm OD) was  packed with  3% SE-30 on 80/100  mesh Chromosorb  W
(AW/DMCS)  at  230°C,   using  a  helium  carrier  (70   mn/mln).   The  Injector
temperature was 230°C.  The  recovery of  the  OCDF  from the  cleanup procedures
was -72%, much lower than for the OCDD.
    Similarly,  PCDFs   were   Identified  In  2,4,5-T and  Agent  Orange.   The
2,4,5-T ester  formulation was  diluted  with  chloroform and  placed  on a PX-21
foam-charcoal  column.   The   nonpolar   components  In the  formulation  were
eluted  with  chloroform.  Moderately  polar  compounds  were  then  eluted  with
1927A                               3-7                              06/23/86

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benzene.   The  PCDDs  and  PCOFs  were  finally  recovered  by elutlon  of  the
column  with  1:1  toluene/benzene  and  then  the eluate  concentrated  before
aluminum oxide  chromatography.   The  aluminum  oxide column  was washed  with
petroleum ether before  the  concentrate  was  placed  on the column.   The PCDOs
and PCDFs were eluted with  1:4 methylene dlchlorlde/petroleum ether.   The GC
column was a 0.91 m  x 4 mm ID Pyrex column packed with OV-7 on Chromosorb W
(HP)  at 200°C.   The temperature  of the  Injector  was  250°C.   The  average
recovery for the  2,3,7,8-TCDD was  >91%.   Although  the presence  of  PCDFs was
Inferred from  the MS data,  again no specific Isomer Identification was  made
and  no  recoveries of  PCDFs found  (Hucklns et  al.,  1978).   AhUng   et  al.
(1977)  used  the  same technique  but  eluted  the  PCDDs and PCDFs  with  toluene
and confirmed  the existence of  PCDFs  using the available  authentic  samples
and standards.
    PCDF standards were probably first used by  Hutzlnger et al.  (1973) and
by Crosby et al.  (1973)  to  Identify  the  reductive dechlorlnatlon products of
2,8-DCDF Irradiated  In  hexane solution  by UV  light.   DCDFs,   TrCDFs,  TCDFs
and OCDF were  not found 1n various tissues of wildlife 1n  the  Bay  of Fundy/
Gulf of Maine area by ZHko (1972).   Tissue samples  were  ground In anhydrous
sodium  sulfate  and   Soxhlet  extracted  with hexane;  the  solution was  evapo-
rated and  applied to an aluminum  oxide  column.   The column was  eluted  with
hexane, the effluent concentrated  and then  applied  to  a  silicic acid  column,
eluted  with  hexane   and  then  with 10%  ether/hexane.   The hexane  eluate was
further chromatographed  on aluminum oxide  and  then  eluted by  20% methylene
dlchlorlde/hexane.   The 6  ft x  4 mm  GC  column  was  packed  with 4% SE-30 on
Chromosorb W (AW; 60/80 mesh)  at  250°C.  The estimated  recoveries  of DCDFs,
TrCDFs  and  TCDFs  were  each  94%,  and that  of OCDF  was 83% over  the  spiking
1927A                               3-8                              06/23/86

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range of 0.23-1.41 ng/g.  These  column  chromatographlc  conditions,  when com-
pared with  those  cited previously,  appear  too  mild  to  produce  such  good
recoveries.
3.3.2.   Representative Sample Preparations and Methods  of Analysis.
    3.3.2.1.   INTRODUCTION — In  this  section,  the  various optimized  ana-
lytical  treatments of  selected  samples  will be presented  with  an Indication
of  how  the  method evolved.   In all  the methods,  the  final step  1s  GO/MS.
Thus, the   mass  spectrometrlc  characteristics of  the  PCOFs  are  discussed
first, ending with the various treatments for selected samples.
    Reviews   of  the  analytical  methodology  to  determine  PCDFs  have  been
authored by Crummett  (1983),  Albro and Parker  (1980),  Tlernan  (1983),  Rappe
et  al.  (1983a),  Buser  (1985) and  Buser et al. (1985).   A step-by-step pro-
cedure  for  extract1on/cleanup/GC-MS  of  a  typical  sample Is  provided  by
Taylor et al.  (1983).   Albro  et  al.  (1985)  have presented a system to ensure
a  valid Interlaboratory  comparison  of  PCDFs  and  PCDDs  1n  human  adipose
tissue.
    3.3.2.2.   MASS  SPECTROMETRY   OF   CHLORODIBENZOFURANS  —Mass   spectro-
metry,  using  an  electron  Impact  source,  Involves  the  fragmentation  of  a
molecule Into positively or negatively  charged Ions  (usually singly charged)
that  are collected  quantitatively so that  the resultant  plot  of  normalized
lon^current versus  mass/charge  ratio Is  an Identifying  fingerprint  for  the
compound.   The  technique  can  be made  quantitative  by  external  and  Internal
standards techniques.
    3.3.2.2.1.   Chlorine  Isotope  Patterns — Before  discussing  the   mass
spectra  of  PCDFs,  It  will  be  helpful to  review the  patterns of  1on Intensi-
ties  that result from  the  two  chlorine  Isotopes at 35  and 37  amu.   Since
these Isotopes  have  natural   abundances of 75.5  and 24.5%, respectively  (a


1927A                               3-9                               06/23/86

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ratio of 3.08), any  Ion  containing one chlorine will give peaks  1n  the  mass
spectrometer at two mass  numbers  separated by two mass units;  If  the  Inten-
sity of  the first peak  is  100%,  the Intensity  of  the  second  (higher)  mass
peak will  be 32%  (100%/3.08).   If more than  one  chlorine atom  Is  present,
the binomial distribution Is  convoluted  with the Isotoplc abundance to  give
the appropriate peak  pattern.  Table 3-1  shows  the relative  intensity  dis-
tributions  for  ions  containing 1-8 chlorines.   Thus,  by  matching a pattern
in an unknown mass spectrum with a  pattern  given 1n  Table 3-1, it is usually
possible  to determine the  number   of  chlorine atoms present  1n an unknown
chlorinated aromatic  compound.
    3.3.2.2.2.    Mass  Spectra of  PCDFs — The  mass  spectra  of  PCDFs  are
dominated by the  presence of  many  chlorine  Isotope patterns and  by  an abun-
dant molecular  1on.   In  fact  the  molecular  1on  1s  the most Intense peak  1n
the mass spectrum.  The only  fragmentation  of  the PCDFs is the loss  of up  to
thr^e chlorine  atoms  and the loss of CO  (Buser,  1975).   The  fragment  ions
are summarized  1n Figure 3-1, which also  gives  the average relative  Inten-
sity of each 1on.  Each  Ion  Is accompanied  by the  Isotoplc cluster of  peaks,
each of which  has a  relative  Intensity dependent on  the  number  of chlorines
in it, their relative intensities given by the values  in Table  3-1.
    The complete mass spectra  of TrCOFs  to  OCDF  have  appeared  In the litera-
ture; they  are given  in  Figure 3-1.  For  example, HxCDF has  an intense mole-
cular 1on  cluster at m/e 372.   By convention the mass of the lightest  mass
peak  In  an  Isotoplc  cluster   Is  referred  to as the  mass of  that  ion.   The
loss of  one and  two  chlorines gives peaks  at  m/e  337 and 302.   The loss  of
CO from  each of  these Ions  gives  peaks  at  m/e 309  and 274, and  the loss  of
another chlorine  from the latter gives  an  ion at 239.  The ion caused  by the
loss of  CO-C1  1s   the daughter ion used in MS-MS (Ryan et a!.,  1985a,b,c).


1927A                               3-10                             06/23/86

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                        TABLE 3-1

              Relative Intensities of Ions
       Containing from One to Eight Chlorine Atoms
(Ions of relative Intensity 1% or  less have been omitted)
Number of Mass of
Chlorines Fragment
1
M
2
M
M
3
M
M
M
4
M
M
M
5
M
M
M
M
6
M
M
M
M
7
M
M
M
M
M
8
M
M
M
M
M
M
4- 2
M
4- 2
4- 4
M
4- 2
4- 4
4- 6
M
4- 2
4- 4
4- 6
M
4- 2
4- 4
4- 6
4- 8
M
4- 2
4- 4
4- 6
4- 8
M
4- 2
4- 4
4- 6
4- 8
4- 10
M
4- 2
4- 4
4- 6
4- 8
4- 10
Relative
Intensity, %
100
32
100
65
10
100
97
31
3
77
100
49
11
62
100
65
21
3
51
100
81
35
8
44
100
97
52
17
3
34
88
100
65
26
7
1927A
3-11
                                                          06/19/86

-------
                         M+
                        (100XJ-
 -e
         •*-(20X)
                           -Cl
                         N-C1.
                         H-35
                         <5X)
                           -Cl
                         M-C12
                         H-70
                         (5X)
 -CO
 -CO
M-COC1
M-63
(25X)
                -Cl
M-COC12
M-98
(10%)
                                                    -Cl
                                                 H-COC13
                                                 M-133
                                                 (25X)
                                  FIGURE 3-1

                       Mass Spectral Behavior of PCDFs
       Percent Relative Intensities of Each Ion Are Given  In  Parentheses

                             Source:   Buser,  1975
1927A
3-12
                    06/23/86

-------
The  Isotoplc  patterns associated  with each  of these  Ions  agrees with  the
expected number  of chlorine  atoms  as given  by the relative  Intensities  of
the  clusters  In  Figure  3-1;   for  example, the  cluster at  m/e  239-245  has
peaks  of  relative Intensities  characteristic  of three chlorines  (see  Table
3-1).   Since  three chlorines   have  been  lost  from a molecule  containing  six
chlorine atoms to form this 1bn, It should Indeed have a 3-chlor1ne pattern.
    The fragment  Ions  of the  MCDFs to OCDF are  summarized  In  Table 3-2.   In
addition,  the  number  of  chlorine  atoms  1n each 1on Is given  In parentheses
so  that  the appropriate  Isotoplc  pattern  can be noted.  Clearly,  mass num-
bers of  Ions  characteristic  of the various PCDFs can  be  specified from data
such as  these.   In addition,  using such data,  PCDFs  can be Identified with
accuracy 1n environmental samples.
    3.3.2.2.3.   Mass  Spectra  of  Isomerlc PCDFs — Characterizing  1somer1c
PCDFs  by  electron Impact  MS   alone  1s  not possible with present technology
(Buser, 1985).   For example,  2,3,8-TrCDF  and  2,4,6-TrCDF  have  Identical mass
spectra  (Gray  et  al., 1976).  This  1s  to be expected 1f  the fragmentation
mechanisms  operating  In  these  two  compounds  are   not  sensitive  to  the
positions  of  the  chlorine atoms.   Table  3-2 summarizes  the  Intensities  of
the  four  major  Ions  of  various  PCDFs  (Gray et al.,  1976).    All  Isomers,
except  2,3,6,8-TCDF,  regardless of  the  position or  number  of chlorine atoms,
have the  same losses of COC1 and COCK from  their molecular  Ions within an
experimental  error of ^20%  of  the observed  peak  Intensity.    For  2,3,6,8-
TCDF,  the  reported   Intensities  of  the  M-COC1  and  M-COC1-  Ions are much
greater  than  for  the  other   compounds.   The  spectrum  should  be remeasured.
Parker  et  al.  (1983)  have shown  that  the  molecular  Ion carries 52*5% of the
total  Ion current  for PeCDFs  to OCDF  1n magnetic sector MS.
1927A                               3-13                             06/23/86

-------
                                  TABLE 3-2

                 Percent Intensities of the Major Ions In the
                        Mass  Spectra  of  Isomerlc  PCOFsa

2,3,8-Cl3
2,4,6-Cl3
2.3.7-Cl3
2,3,9-Cl3
2,3,6,8-Cl4
2,4,6,8-Cl4
2,3,7,8-Cl4
1,2,7,8-014
1,2,4,7,8-C15
1,3,4,7,8-C15
*• J
Average
M+
100
100
100
100
100
100
100
100
100
100
100
M-COC1
23
23
25
25
41b
22
19
17
22
18
22 ± 3
M-COC13
14
14
24
22
56b
22
16
22
26
22
20 ± 4
M++
11
11
22
20
23
22
12
20
-
24
18 i 5
aSource:  Adapted from Gray et al.,  1976

bOut!1ers
1927A                               3-14                             06/23/86

-------
     Even  though MS alone  cannot  distinguish among  Isomers,  GC  can separate
many of them from  one  another.   In fact, many  GC  retention  values for spe-
cific  PCOF  Isomers  have been published  (Section  3.3.2.3.).
     3.3.2.2.4.   High  Resolution  Mass Spectrometry  of  PCDFs  —  Using  double
focusing  mass  spectral Instrumentation,  H  Is  possible  to measure the mass
of  an  1on to 6 or  7  significant  figures.  Because the various Isotopes have
masses  that  differ  slightly from their  nominal  value (I.e.,  chlorlne-35 has
a  mass of 34.9689  amu),  such  high mass  accuracy  permits calculation  of the
exact  elemental  composition of an  1on  from  Us  exact mass.   The exact mole-
cular  weights of the various PCDFs are given 1n Table 3-3.
     Because  of  the  high aromatlcHy and  the  large  number of  chlorine atoms,
these   exact  masses   are   up   to  0.25  amu  below  the  normal  mass  (see
C-^ClgO).   Thus,  these Ions  can  easily be  distinguished   from  an  1on  at
the  same  nominal mass  that may  come  from a relatively  saturated compound.
For  example, at  m/e  440,  a  hydrocarbon 1on may  be  C00H..,,  which  has  an
                                                         •3d DO
exact  mass  of  440.4382;  this  Is 0.6924  amu  higher than the  corresponding
OCDF molecular  Ion.  When  taken  together with  the  chlorine 1sotop1c patterns
and  adequate  chromatographlc  separation  (see Table  3-1),  these  exact  masses
(Table  3-3)  are almost  specific  Indicators of  the  presence  of  PCOFs  1n
samples.  The chlorinated dlphenyl  ethers  lose 2 chlorines  1n the Ion  source
of  a mass spectrometer to  form  a compound with the  same elemental composi-
tion as a PCDF.  The molecular 1on  of  the ether must  be monitored to prove
whether the Interference Is present or not.
    3.3.2.2.5.   Specific  Ion  Monitoring  Mass   Spectrometry  — Buser  (1975)
based  his quantHatlon  of  PCOFs  In commercial chlorophenols  on  selected  1on
monitoring  of  the  molecular  Ions  (304,  338,  372,  406  and  440;   see  Table
3-2).   Figure 3-2 1s an  example  of such data; the  peaks  attributable  to  the


1927A                               3-15                             06/23/86

-------
                                  TABLE  3-3

                    Exact Molecular Weights  of the PCDFs
             (masses used to calculate these molecular weights:
       C = 12.000000, H = 1.007825, Cl = 34.968855 and 0 = 15.994915)
                Compound                           Molecular Weight


              C12H7C10                                 202.0185

              C12H6C120                                235.9796

              C12H5C130                                269.9406

              C12H4Cl40                                303.9016

              C12H3C150                                337.8627

              C12H2C160                                371.8237

              C12HC170                                 405.7847

              C^ClgO                                  439.7458
1927A                               3-16                             06/23/86

-------
           B
 0)
 o

 CO
"O
 c
 3
.£}
I
J2
DC
100


 •0


 ao

 40


 20

 o



100

 •0


 ao

 40


 20


 0



100

 •0
 20


 0



100


 K>
          20


          0




         100


          •0
                                 207
                       ' I  '  ' T 1  I '  '  • ' I  '
                        160       200      260
                                                 300      360       400
                                                                          460

                                       *•'
                                 x»     ||    m
                        160
                                  1  .  .*?    fr    '
                                200
                                        2SO
                                                 300
                                                         360
                                                                  400
                                                                          460
                                 206
                       160
                             1  '  I
                                200
                                     I  ' '  '  ' 1  '
                                    250       300
                                                         350
r I"
 400
"I
 450

                                                   X»
                        I
                       160
                                200
                                        250
                                                 SCO
                                                         350
                                                    1 I  '
                                                    400
                                                                          460


                                                                          I
                                                                        440
                       "1^
                       160
                                                              177
                                                             *70
                                200      260       300
                                      FIGURE  3-2
                                                        ITOJ    4O6
                                                      I  i Fi  i l'i
                                                         360
                                                                  400
     Low  resolution  mass  spectra  of  (A)  TrCDF,   (B)  TCDF,   (C)   PeCDF,  (D)
 HxCDF and  (E)  OCDF.   In all  cases  the  chlorine  substitution pattern Is  not
 known.  The  fragmentation patterns  are explained In  Figure 3-1.

 Source:   (A)  HHes  and  Lopez-Avlla,  1979;  (B.C.D)  Bowes et  al..  1973;  (E)
 Hutzlnger et al., 1972b.
1927A
                                   3-17
                                                                            06/23/86

-------
HxCDF through  OCDF  are  Indicated.   Figure  3-3  shows  that  m/e  372  (Cl&)
gives a  response  for  the OCDF  Isomer  (see  retention  time 12 m1n).  This  Is
because  OCDF  has  an M-C1-  1on  at m/e  370,  which has  a  more Intense  first
Isotope peak of 372. The specific and multiple  1on monitoring modes allow  pg
sensitivity to be attained and  1s the best technique to use  for  quantHatlon
of  PCDFs  after prior  separation on a  capillary GC  column  (Buser  et al.,
1985).  For example, Rappe et al. (1977) showed  that the  2,3,7,8-TCDF  Isomer
was probably present In Yusho oil (see  Figure  3-3 and Chapter  4).
    3.3.2.2.6.   Other   Types of Mass   Spectroscopy  of   PCDFs  — Electron-
Impact  (El)  MS (50-70  eV at 250°C)  1s  the  preferred analytical  mode for
TCDFs with  sensitivity  1-10  pg  by specific  Ion monitoring.   Decreasing sen-
sitivity  occurs  for the  higher  chlorinated  species  (Rappe  et  al.,   1983a;
Buser  et al., 1985).   Negative  chemical  lonlzatlon  (NCI)  with methane  as
reagent  gas  (0.35 torr,  180°C)  1s  very  sensitive  (1-2 orders   of magnitude
more  sensitive than  electron Impact MS)  for  all PCDF  from  tetra- to  octa-,
but  requires  more cleaning  of  the  Ion source,  or  a  specially   designed 1on
source,  and  1s not as  reproducible  as an electron  Impact source (Buser  et
al.,  1985; Rappe  et al.,  1983c;  Mass et  al.,  1981;  Kuehl  et  al., 1981).  The
base  peak  1s  usually  M"   with (M%H«-C1»)   Ions,  both  singly  and mul-
tiply charged.  As  In electron  Impact MS, NCI  spectra of  Isomers are  Identi-
cal  (Buser  et al.,  1985).   The  Ions  used  for  specific  1on monitoring are
M   or  M~+2.   Rappe et  al.  (1983c)  have  reported  that  Isomers have  dif-
ferent  response  factors In   the  NCI mode.   The NCI/El  response  ratios range
from  0.86  for  1,2,7,9-TCDD  to 11 for  2,3,6,8-TCDF.  The  El  response  Is low-
est  for 1,2,6,7-TCDF  being   59%  of  the  highest  response  for  a  tetra-Uomer,
1,3,6,8-.   The NCI response  1s lowest for  1,2,7,9-tetrabelng  6.8%  of  that
for   the  most  responsive  tetrachloro-lsomer,  2,3,6,8-.   For   PeCDF,  the


1927A                               3-18                             06/24/86

-------
                     m/e 440
                     m/e 406
                     m/e 372
                     m/e 338
                                               octa-
                                                 X20
                                             hepta-
                                              X100
                                   hexa-
                                     X50
                     m/e 304
                                      6
                                          minutes
12
                      m/e 304
                                       6
                                         minutes
 12
                                  FIGURE  3-3

    Mass chromatograms of (A) 2,3,4,6-tetrachlorophenol and (B) pentachloro-
phenol showing the elutlon of PCDF  (m/e  304 = tetra-, m/e 338 = penta-, m/e
372 = hexa-,  m/e  406  = hepta-, and m/e  440 =  OCDF).

Source:  Buser,  1975
                                    3-19
            06/23/86

-------
2,3,4,6,8-lsomer has an 81% response relative to  the  most  El  responsive Iso-
mer, 1,2,4,6,8-; and  48%  In  the NCI mode.  For HxCDF,  the 1,2,3,4,7,8- 1so-
mer  Is  65% of the  El  response  of the most responsive  Isomer,  2,3,4,6,7,8-.
The  corresponding  NCI data for  the 1,2,3,4,7,8- Isomer  Is  73% of  the most
responsive 1,2,4,6,7,8-lsomer.  For two hepta-1somers,  the El  responses were
equivalent, but  for  the  NCI  responses, the 1,2,3,4,6,8,9-  Isomer  was  77% of
the  response  of  the 1,2,3,4,6,7,8-lsomer  (Rappe et al., 1983a).   A Townsend
discharge  Ion  source  (negative  oxygen  chemical  1on1zat1on) seems  to allow a
better  discrimination  of  Isomers  1n each  class (Mass et  al.,  1981; Ch1u et
a>.,  1983;  Lao  et  al.,  1985).   Negative methane/oxygen chemical  1on1zat1on
Is  still  being evaluated  (Mass  et al., 1981).  The  negative  1on atmospheric
pressure  lonlzatlon  mass  spectrometry for  2,3,7,8-TCDF  has   been  reported
(Korfmacher et al., 1983).  Though  the detection  limit  was 0.5 pg, there are
no  significant mass spectral  differences  In the TCDF  Isomers  having 4:0, 3:1
or  2:2  chlorine  ring substitution patterns.
     Another technique  of  promise  Is MS/MS (Voyksner  et  al.,  1983; Sakuma et
al.,  1985;  Shushan et  al.,  1985, Ryan et  al., 1985a,b,c).  The  first ana-
lyzer  provides  nominal  mass  separation   of  the  analyte  1on   (usually  the
molecular  Ion)  from the matrix, the selected 1on  1s  then  fragmented by col-
lision  (He,  2xlO~* mm  Hg)  Into  specific  daughter  Ions (M-C1,  M-COC1) thus
eliminating  background noise.  However,  though  cleanup problems  are mini-
mized,  specific Isomers  cannot be distinguished  through  MS/MS  alone, thus
necessitating  prior GC separation.   MS/MS results appear  to  be consistently
high with respect  to  GC/MS  or GC/MS/MS  for  2,3,7,8-TCDF  (Voyksner et al.,
1983).   An MS/MS  arrangement preceded by a short  capillary  column  allows
fast screening of  TCDF congeners  at 20-400 fg  levels (Sakuma  et al.,  1985),
with the  SP-2340 column used  for separating specific  Isomers.


1927A                               3-20                             06/23/86

-------
    3.3.2.3.   CAPILLARY  GAS  CHROMATOGRAPHY -- The  environmental  chemistry
groups  headed  by Buser,  Bosshardt  and Rappe  have been  largely  responsible
for the development of capillary GC techniques  as  applied to PCDFs.
  *. The  GC/MS  analyses noted  1n  Section  3.3.2.1. were  ultimately  deficient
because the various PCDF  Isomers were  not  resolved on  packed GC columns,  and
often only the total  PCOFs  could be  estimated.  Since  certain PCDFs are more
toxic than others, separation of Isomers Is essential.
    In  view  of  the fact  that  each  chlorinated class of  PCDFs  Includes sev-
eral congeners (with  the  exception of  OCDF), the  separation and quantHatlon
of  other  Isomers  constituting  that chlorinated class  (for  example  quantHa-
tlon of 2,3,7,8-TCDF   1n  the presence of  the  37  other TCDFs)  Is  difficult.
Conditions for  Isomer-speclf1c quantHatlon are  developed  using  calibration
standards containing all  of  the Isomers that may  co-elute with  the  Isomer of
Interest.  A  valid  Isomer-speclf1c  analysis will  be  accompanied by data  (a
mass chromatogram)  that  demonstrate  the  appropriate  conditions  that  permit
the separation of  the Isomer of Interest  from all  other  possible co-elut1ng
Isomers.  If  such calibration  data  1s lacking,  the  Identification of  spe-
cific Isomers must be  regarded as tentative.  Concentrations  of  Isomers cal-
culated on the basis  of unvalldated  1somer-spec1f1c data  should  be regarded
as upper limits  and therefore the  concentrations are approximate.
    Buser (1976a)  was the  first  to  use  Pyrex  capillary columns to produce
the desired  separation of  the PCDF  Isomers.  These  columns with  different
stationary  phases  (OV-101,  OV-17  and Sllar  IOC) allowed lower  operating
temperatures (205-225°C)  as  well  as  Increased  resolution  compared  with con-
ventionally   packed  columns.   The  column  characteristics are  provided  1n
Table  3-4.   The  average  film  thicknesses were  0.1  ym.   The  OV-101  Is a
nonpolar methyl  slUcone;  the  OV-17  1s a  semlpolar methyl phenyl  slUcone;


1927A                              3-21                              06/23/86

-------
                                  TABLE 3-4

               Characteristics of Some Glass Capillary Columns
                            for Separating PCDFs*

Characteristic
Length (m)
I.D. (mm)
Temperature (°C)
Retention time

OV-101
22
0.32
225
33.4
Column
OV-17
22
0.34
225
31.8

S1lar IOC
22
0.34
205
26.9
  (OCDD) (m1n)

Retention Index
  (OCDD)
3055
3420
3645
Theoretical plates
HETP (mm)
Carrier (atm)
42,500
0.52
He(0.5-0.6)
43,400
0.51
He(0.5-0.6)
34,000
0.65
He(0.5-0.6)
*Source:  Buser, 1976a
 1927A
          3-22
                       06/19/86

-------
and  the  Sllar  IOC  1s a  highly polar  cyanopropyl  slUcone.  The  capillary
column was  linked  to  the MS  by a  fused  0.15 mm  ID  platinum capillary  at
250°C  leading  directly Into  the Ion source of  the MS.  The  compounds  were
detected by  MS of the molecular  Ions.   Isothermal  conditions were  found  to
be  suitable  for  the  separation  of  the  PCDFs,  and  the reproduclblllty  1n
quantHatlon was  better  than  that  obtained with temperature-programmed  GC.
The chromatography  of  Aroclor  1268 [which contains  the  most  highly  chlorin-
ated  PCBs  (up to  Cl,_)3,  under  the  same  conditions  given In  Table 3-4,
produced complete PCB  elutlon  within  10 minutes  on  the Sllar IOC  column;  the
peaks  were  also better  resolved than they  were with a  support-coated  open
tubular column.  On  this column, however,  there  was some overlapping of PCDD
and  PCDF  Isomers  that did not occur on the others and there was  also some
reversal of elutlon  order.  When the  same  sample of PCDDs/PCDFs was Injected
on all columns,  the OV-101  column always  resolved  more  peaks.  Better  reso-
lution of  the  less  chlorinated Isomers occurred on  the OV-101  column,  but
the  Sllar  IOC  was best  for  the most highly chlorinated  Isomers.   The  OV-17
column  gave  the  best  resolution   of the  Cl,  Isomers.  Relative  retention
times  of  PCDFs and  PCDDs on  these columns are  presented  In  Table  3-5.   All
samples were Introduced by an  Isothermal splltless technique.
    Rappe et al.  (1977)  used  the technique to  analyze  for PCDFs  1n Yusho oil
but  used  22 m x 0.36  mm ID  glass  capillary  columns  with  OV-101 and  OV-17
stationary phases and  specific mass detection  of the  molecular Ions (Figure
3-4).  It was  shown  that  the  toxic  2,3,7,8-TCDF  was probably one  of the main
PCDFs  1n  Kanem!  oil  causing  Yusho  disease,  constituting  30% of  the  total
TQDFs.  The  2,3,4,8-TCDF co-elutes  with  2,3,7,8-TCDF  on this column  (Mazer
et  al.,  1983a)  and  thus the Identification  Is  ambiguous.  Buser et  al.
(1978a) used  OV-17  capillary  columns of  25  and  50  m length  (0.36 mm ID)  to


1927A                               3-23                             06/23/86

-------
                                  TABLE 3-5

                Relative  Retention Times of  PCDFs  and  PCDDs  on
                     the Capillary Columns of Table 3-4*
Compounds
TCDDs
TCDFs
PeCDDs
PeCDFs
HxCDDs
HxCDFs
HpCDDs
HpCDFs
OCDD
OCDF
Relative
OV-101
0.13-0.18
0.10-0.14
0.20-0.27
0.17-0.24
0.32-0.41
0.29-0.42
0.56-0.63
0.51-0.65
1.00
0.978
Retention Times
OV-17
0.10-0.15
0.09-0.12
0.16-0.24
0.14-0.23
0.28-0.38
0.25-0.40
0.52-0.60
0.47-0.66
1.00
0.025
on Column
Sllar IOC
0.12-0.22
0.11-0.19
0.18-0.30
0.15-0.25
0.31-0.43
0.24-0.50
0.54-0.62
0.44-0.66
1.00
0.933
*Source:   Buser,  1976a
1927A
3-24
06/19/86

-------
INJ
                                               2,3,7,8-tetra-CDBF
CO
I
en
           m/e 372
	 1 	
20 min
	 1 	 1 	
10
	 	 l~
0
CO
CO
cr<
                                          FIGURE 3-4


Mass Chromatograms  (OV-101 Glass Capillary Column at 197°C) of "Yusho"  Oil  Showing Elutlon of PCDF
              (m/e  270 = TrCDF, m/e 304  = TCDF, m/e 338 = PeCDF  and m/e 372 = HxCDF)


                                  Source:   Rappe et  al..  1977

-------
resolve the  PCDF  Isomers produced  by PCB  pyrolysls,  quantHating by  GC/MS
(Chapter 4).   To  achieve the  best  resolution,  a  complex  temperature  pro-
gramming scheme to achieve splltless  Injection was  adopted:   100°C,  2-mlnute
Isothermal; 15°C/m1nute  to  145°C;  5°C/m1nute to 230°C  for  the 25 m  column;
100°C,  2-mlnute Isothermal,  20°C/m1nute  to 230°C  for  the 50 m column,  with
helium  carrier at 0.80  and  1.40 atmospheres, respectively.  The samples  were
Introduced splltlessly  at  260°C.  Optimal  separations  were achieved on  the
50 m  column.  Similar  techniques were utilized  to  analyze  for PCDOs 1n  fly
ash (Buser et al., 1978b; Chapter 4).  PCDDs and PCDFs  produced by pyrolysls
of  chlorophenolates  were detected   (Rappe  et  al.,  1978b),  and  In  2,4,5-T
esters  as  well  as Agent Orange  (Rappe et  al.,  1978c).  PCDFs have  been  ana-
lyzed  In  fly  ash  and In pyrolyzed PCBs  (Buser et al.,  1978c;  Chapter 4);  1n
Yusho oil and used Japanese  PCB  (Buser,  et  al.  1978d);  1n commercial  chloro-
phenols  (Rappe  et al.,  1978a);  In  the  pyrolysates of  specific  PCB  Isomers
(Buser  and  Rappe,  1979) and of  chlorobenzenes  (Buser,  1979); In  tissues  of
patients who  suffered  from  Yusho disease (Rappe et al.,  1979b);  1n  the  pro-
ducts  of   the  palladium acetate  synthetic method  for  PCDFs  (Gara et  al.,
1979);  fish  samples  (Rappe  et  al.,  1981); human  adipose  tissue,  mothers'
milk, bovine fat and bovine  milk (Nygren  et al.,  1986).
    Thus,  H  appears  that  optimum  separations  are achieved  with a  50 m x
0.36  mm ID glass capillary  column  coated  with  OV-17,  operated  with  helium
carrier  1n the temperature  programmed  mode given  by  Rappe et al.  (1978c).
Sometimes  a  combination of  capillary columns,  however. Is  necessary.   Rappe
et  al. (1984)  reported that  a  60m  Supelco SP-2330  capillary column  could
separate most PCF Isomers.   The  toxic 1,2,3,7,8-PeCDF does  co-elute with the
1,2,3,4,8-lsomer  as  does the  toxic  1,2,3,4,7,8-HxCDF  with  the  1,2,3,4,7,9-
Vwrnier.  These  Isomers  can be  separated  on  less  polar  columns like OV-17 and
DB-5.

1927A                              3-26                             06/23/86

-------
    Farrell  (1980)  attempted  unsuccessfully to  produce  the  thinly  coated
columns mentioned previously  (Rappe et al.,  1978c).   He did produce  25  m x
0.25 mm  ID columns with  film  thicknesses  of 0.4-0.5  ym OV-17 and  OV-101,
but analyses took 4-5 hours at  220-260°C  and at  34 cm/sec linear  velocity of
nitrogen carrier.  The problem  may  have been that  the  helium carrier  was  not
used,  since when the  hydrogen  carrier  was  used  a mixture of DCDFs,  TrCDFs,
and  TCDFs  was  resolved,  the 2,3,7,8-TCDF  being  eluted  In  6  minutes on  a
50 m x 0.25 mm ID OV-101  column  (0.5  wm  liquid  phase  film)  at 240°C  and
100  cm/sec hydrogen  carrier  average  velocity.    Another  deficiency   of  the
Farrell  (1980)  study  was  that  he  did  not use the  splHless  Injection tech-
nique  recommended  by  Buser  (1976a).   The  splHless  technique  has now  been
successfully used  by  other laboratories  (Mazer  and Hlleman, 1982; Mazer  et
al., 1983a,b;  Hlleman  et  al., 1985).  Sources of  PCOFs 1n the  United States
have been  summarized by Cantrell et al. (1986).
    The  kinds  of Interferences  expected  1n  GC/MS  of   PCDFs are  reviewed 1n
Smith  and  Johnson  (1983), Rappe  (1984)  and Lau et al.  (1985).   The  quality
assurance  and  control  procedures to meet U.S. EPA  requirements  are  embodied
In  RCRA  method 8280  (Donnelly  et  al., 1986).  Here a  SP-2250  or equivalent
column  1s   recommended  with  multiple  1on  monitoring  and  Internal  standard
quantHatlon.   The  peaks  to  be  monitored  Include   the following:   TCDF,
3M.897,  321.894,  327.885,   256.933 and  258.930;  PeCDF, 353.858,  355.855;
HxCDF,  389.816 and  391.813 for  the PCDFs  themselves,  their  (M-CO-C1) Ions,
and  the molecular  Ions  for  the  Interfering chlorinated dlphenylethers  as
well  as   the  molecular  Ions  of   chlorinated   blphenylenes,  PCBs  and  DDE
Isomers.   All  PCDF Isomers should be on hand.
 1927A                               3-27                             06/23/86

-------
    The most comprehensive  recent  11st of retention times,  flame  lonlzatlon
and electron capture sensitivities for  TCDFs  to  OCDF  Is provided  1n  Table
3-6 (Bell  and  Gara, 1985).  Other  lists can be  found  In Hazer and  Hlleman
(1982); Firestone  (1977a),  Mazer  et  al.  (1983a,b);  Kurokl  et al.  (1984);
Safe  and  Safe   (1984)  and  Llgon  and  May  (1984).  Hale  et  al. (1985)  have
explained  the  retention  behavior  of all  PCDFs  In terms of  number  and  posi-
tion  of  chlorines,  relations  between  chlorines,  and  ring  Interactions.
Keith  et  al.  (1983)  have  described a thermally  modulated  electron-capture
detector that has higher  sensitivity,  better linear range and specificity to
PCDFs than the  conventional  electron-capture detector.
    3.3.2.4.   TREATMENT  OF SPECIFIC  SAMPLES  — In  the  following methods,
the methods were generally  validated by  the  spiking of  known amounts of PCDF
and then  measuring  recovery.   Such methodology  does not  necessarily measure
efficiency 1f an Initial  pretreatment  step  1s  necessary to release PCDFs, as
fjw fly ash  samples.  The quality  assurance  and  control necessary  to achieve
valid  results  1n  the cleanup and  column chromatographlc  steps  are provided
at  length  by  Donnelly  et  al.,  (1986)  1n  regard to  an evaluation  of  RCRA
Method 8280.   The experimental  conditions  for  elutlon  of  compounds from the
"open" alumina mlcrocolumn  are critical.  A  60%  methylene dlchlorlde 1n hex-
ane-elut1ng  solvent was  much more reproducible  than  a 10%  when  neutral or
basic  alumina  was used.   Careful  control of the water  content was necessary
since  deactlvatlon  of neutral  alumina caused  weaker  solvents  to  elute the
PCDFs  and  PCDDs thus leading to  losses  and the  presence  of unwanted Inter-
ferences.
    3.3.2.4.1.    PCB  Formulations  —  The PCB  (100  mg)  was  placed  on an
aluminum  oxide mlcrocolumn (basic aluminum oxide,  Woelm,   In  a  disposable
Pasteur  pipette,  15  cm x 5 mm  ID) and the  bulk of  the PCBs eluted  with


1927A                               3-28                             06/23/86

-------
                                  TABLE 3-6

      Relative  Retention  Times  (RRT) and Relative  Response  Factors  (RRF)
               for  PCDFs  Synthesized as Reference  Standards3*".
                 The  gas  chromatographlc detectors were  flame
                 1on1zat1on  (FID)  and  electron  capture  (ECD).
Congener
1,2,3,4-
1,2,3,6-
1,2,3,7-
1,2,3,8-
1,2,3,9-
1,2,4,6-
1,2,4,7-
1,2,4,8-
1,2,4,9-
1,3,4,6-
1,3,4,7-
1,3,4,8-
1,3,4,9-
2,3,4,6-
2,3,4,7-
2,3,4,8-
2,3,4,9-
1,2,6,7-
1,2,6,8-
1,2,6,9-
1,2,7,8-
1,2,7,9-
1,2,8,9-
1,3,6,7-
1,3,6,8-
1,3,6,9-
1,3,7,8-
1,3,7,9-
1.4,6,7-
1,4,6,8-
Gas
SP-2330
RRT
±0.003
1.389
1.415
1.306
1.396
1.794
1.290
1.179
1.258
1.608
1.252
1.150
1.217
1.466
1.949
1.802
1.900
1.382
1.561
1.294
1.854
1.482
1.569
1.198
1.188
1.000
1.314
1.128
1.131
1.401
1.163
Chromatoqraphlc Column and Detector Usedc
ECD
RRF
±0.05
1.79
0.81
1.06
1.00
0.72
0.51
0.96
1.15
0.87
0.70
0.69
0.84
1.22
0.61
0.92
0.97
1.16
0.79
0.55
0.78
0.93
0.83
0.87
0.63
1.00
1.05
0.62
0.84
0.55
0.75
DB-5
RRT
±0.003
1.161
1.150
1.129
1.148
1.280
1.201
1.063
1.100
1.203
1.070
1.063
1.080
1.186
0.201
1.200
1.197
1.153
1.189
1.100
1.258
1.170
1.208
1.363
1.079
1.000
1.123
1.064
1.084
1.108
1.026
FID
RRF
±0.05
1.26
0.70
1.03
0.87
0.48
0.85
1.25
1.12
1.08
1.06
1.10
1.01
0.82
0.85
0.85
0.96
1.84
1.49
0.65
0.85
0.93
0.89
1.21
0.88
1.00
1.13
0.53
0.70
1.08
1.10
SP-2340
RRT
±0.003
1.413
1.452
1.338
1.446
1.870
1.313
1.194
1.283
1.608
1.278
1.165
1.244
1.515
2.074
1.915
2.006
1.444
1.637
1.336
1.953
1.551
1.633
2.420
1.216
1.000
1.345
1.150
1.145
1.459
1.189
ECD
RRF
±0.05
1.58
0.83
1.05
0.99
0.72
0.46
0.95
1.24
0.84
0.68
0.64
0.78
0.87
0.60
0.92
0.93
1.26
0.76
0.52
0.74
0.92
0.93
0.90
0.60
1.00
1.10
0.60
0.82
0.48
0.77
1927A                               3-29                             06/19/86

-------
                              TABLE 3-6  (cont.)
Congener
1,4,6,9-
1,4,7,8-
2,3,6,7-
2,3,6,8-
2,3,7,8-
2,4,6,7-
2,4,6,8-
3,4,6,7-
1,2,3,4,6-
1,2,3,4.7-
1,2,3,4,8-
1,2,3,4,9-
1,2,3,6,7-
1,2,3,6,8-
1,2,3,6,9-
1,2,3,7,8-
1,2,3,7,9-
1,2,3,8,9-
1,2,4,6,7-
1,2,4,6,8-
1,2,4,6,9-
1,2,4,7,8-
1,2,4,7,9-
1,2,4,8,9-
1,3,4,6,7-
1,3,4,6,8-
1,3,4,6,9-
1,3,4,7,8-
1,3,4,7,9-
1,3,4,8,9-
2,3,4,6,7-
2,3,4,6,8-
2,3,4,6,9-
2,3,4,7,8-
2,3,4,7,9-
2,3,4,8,9-
Gas
SP-2330
RRT
±0.003
1.586
1.304
1.978
1.609
1.866
1.706
1.390
2.149
1.997
1.837
1.961
2.524
2.058
1.659
2.394
1.960
2.023
3.017
1.809
1.471
2.111
1.706
1.759
2.330
1.760
1.427
1.923
1.660
1.615
2.327
3.074
2.418
1.843
2.906
1.568
2.127
Chromatographic Column and Detector Usedc
ECD
RRF
±0.05
0.94
0.79
0.72
1.15
1.05
0.73
0.67
0.68
3.94
4.17
7.27
4.03
2.90
5.02
4.31
3.70
2.24
3.99
3.84
3.66
4.77
6.13
4.64
2.72
2.67
2.58
3.76
3.79
5.43
3.28
3.79
4.08
3.10
7.36
3.50
4.36
DB-5
RRT
±0.003
1.152
1.105
1.234
1.071
1.198
1.137
1.035
1.254
1.573
1.569
1.596
1.801
1.636
1.487
1.726
1.612
1.664
1.901
1.493
1.360
1.569
1.490
1.533
1.720
1.491
1.357
1.544
1.493
1.506
1.723
1.746
1.550
1.512
1.716
1.474
1.653
FID
RRF
±0.05
1.30
1.02
0.93
1.09
1.15
1.04
0.86
1.0
0.67
0.68
1.25
0.63
0.54
0.76
0.72
1.20
0.34
0.61
0.87
0.63
0.74
1.07
0.77
0.41
0.81
0.54
0.71
0.71
1.33
0.52
0.81
0.76
0.64
1.09
0.66
0.88
SP-2340
RRT
±0.003
1.643
1.352
2.128
1.686
1.989
1.820
1.447
2.350
1.186
2.104
2.262
2.907
2.391
1.905
2.758
2.278
2.331
3.501
2.087
1.665
2.419
1.963
2.005
2.704
2.041
1.618
2.213
1.914
1.843
2.702
3.709
2.869
2.149
3.477
1.806
2.495
ECD
RRF
±0.05
0.91
0.79
0.73
1.23
1.02
0.68
0.74
0.63
3.87
4.21
7.25
__
3.05
4.10
3.74
—
1.84
3.36
4.12
3.40
4.10
5.86
3.98
2.31
2.94
2.58
3.20
3.66
4.40
2.79
4.04
4.17
3.07
7.27
3.45
4.63
1927A                               3-30                             06/19/86

-------
                               TABLE  3-6 (cont.)
    Congener
                          Gas Chromatographlc Column and Detector Usedc
               SP-2330

                 RRT
               +0.003
           ECD

           RRF
          +0.05
                     DB-5

                     RRT
                    +0.003
                     FID

                     RRF
                    +0.05
                    SP-2340

                      RRT
                    +0.003
                              ECD

                              RRF
                             +0.05
1,2,3
1,2,3
1,2,3
1,2,3
1,2,3
1.2,3
1,2,3
1,2,3
1,2,3
1,2,3
,4,6,7-
,4,6,8-
,4,6,9-
,4,7,8-
,4,7,9-
,4,8,9-
,6,7,8
,6,7,9-
,6,8,9-
,7,8,9
1,2,4,6,7,8-
1,2,4,6,7,9-
1,2,4,6,8,9-
1,3,4,6,7,8-
1,3,4,6,7,9-
2,3,4,6,7,8-

1,2,3,4,6,7,8-
1,2,3,4,6,7,9-
1,2,3,4,6,8,9-
1,2,3,4,7,8,9-

1,2,3,4,6,7,8,9-
 .949
 .320
 .364
 .800
 .814
 .251
 .845
 .039
3.376
4.016
1
2.
3.
2.
2.
4.
2,
3.
                4,
                4,
                4.
                5.
                  434
                  603
                  893
                  355
                  381
                4.499
  025
  699
  699
  640
 .36
 ,42
 .44
 .14
 .20
 .84
3.76
  18
  66
          2.79

          2.72
            95
            69
            57
            76
          5.06
2,
2.
2.
2.
2.
2.
2.
2.
2.
                    3.
                    4.
316
066
426
320
378
771
345
442
488
          2.748
          2.101
          2.174
          2.217
          2.099
          2.140
                    2.500
                    3.333
                    3.440
            507
            002
                7.809
                    5.708
0.18
0.57
0.45
0.54
0.44
0.34
0.34
0.63
0.51
0.33

0,22
0.59
0.53
0.60
0.34
0.46

2.61
0.61
1.35
1.32

0.43
3.
2.
4.
  793
  943
  276
3.592
3.573
5.426
3.670
3.874
4.276
5.112
                       108
                       295
                       631
                       037
                       025
                               5.996
                       708
                       917
                       501
                       849
2.35
                                        11.854
          4.29

          2.64

          2.82



          2.88
                             9.35
                             2.50
                             4.58
                             4.98

                             1.68
aSource: Bell and Gara, 1985

Detention  times and  response  factors all  given  as  ratios  to  those  for
 1,3,6,8-TCDF.

cColumns:   SP-2330  fused  silica  60  m  x  0.25  mm  ID  at  240°C;  DB-5  bonded
 phase fused silica, 60 m  x  0.25  mm ID  at  240°C; SP-2340 bonded fused silica
 50 m at  220°C.   The ECD was a  63N1-electron  capture  detector.  The  FID
 was  a  H2/a1r  flame  lonlzatlon  detector.   The  nitrogen  carrier  flow  rate
 was 1-2 ml/mln.
1927A
                               3-31
                                                06/19/86

-------
10  ml  of  n-hexane.   PCDFs  were  recovered   by   elutlon   with  6  ml  of
methylene chloride; the eluate evaporated and was subjected  again to cleanup
on  a  second   Identical   aluminum  oxide  mlcrocolumn.   To  achieve  optimal
removal of  PCBs,  10  ma  of  4% methylene d1chlor1de/n-hexane was  then  used
as the first eluent; PCDFs,  lower PCBs, chlorinated  tMcyclIc aromatlcs  were
then  eluted  with  10  ml  of  50% methylene  d1chlor1de/n-hexane.   This  final
eluate was  concentrated  and  Injected  Into  the GC/MS.   Recoveries of  both
2,3,7,8-TCDF  and  TCDD  were  90%  at  the  0.1-1  ppm  level   (Buser  et  al.,
l£78d).  This  1s the basis of U.S.  EPA  method  613 except that  3% methylene
dlchlorlde/n-hexane and  20% methylene d1chlor1de/n-hexane  are used  for  the
first and second eluents, respectively.  RCRA Method  8280  also utilizes  this
step.  Either  basic  or  neutral alumina  can  be  used  with  consistent results
being  obtained with a  3% methylene  dlchlorlde/hexane wash  (10 ml), a  20%
methylene dlchlorlde/hexane  wash  (15  ml)  with  elutlon of  PCODs and  PCDFs
with  50%  methylene  dlchlorlde/hexane  (15   ml).    If  further   cleanup  Is
necessary a charcoal cleanup 1s recommended  (Smith  et al.,  1984).
    3.3.2.4.2.   Yusho  011 --  Yusho  oil  (100 mg)  was  applied  to  a  silica
mlcrocolumn (0.5 g silica gel, 70/230 mesh, Merck,  In a 15 cm x 5 mm dispos-
able  Pasteur  plpet).   The PCBs and  PCDFs were  eluted with 6  ml  of  n-hexane
with  almost  complete retention of  rice  oil on  the  column.    The  eluate  was
concentrated  and  applied to  an  aluminum   oxide  mlcrocolumn  (1.0 g  basic
aluminum oxide,  Woelm,  In a disposable  Pasteur  plpet, 15 cm x  5 mm).   Most
of  the  PCBs  were  eluted  with  10  ml of 2% methylene  d1chlor1de/n-hexane and
the  PCDFs  (plus  other  chlorinated trlcycllc aromatlcs  and  lower chlorinated
blphenyls)  collected  by  elutlon with  10 ml  of  50%  methylene dlchlorlde 1n
n-hexane.   The  latter   fraction  was  concentrated   to   50  yi  and  2  pi
Injected for GC/MS analysis.   Recoveries of both 2,3,7,8-TCDF and -PCDD were


1927A                               3-32                              06/23/86

-------
90% at  the 0.1-1  ppm  level (Buser et  al.,  1978d).  This  procedure  differs
slightly from  the  one  quoted by  Rappe  et  al.  (1977) since  the  latter  tech-
nique resulted  In  losses  of  some of the  less  polar PCDFs.   This  technique
has  also  been  used by  Cull  and Dobbs  (1984),  Rappe  et  al.   (1985b)  and
Paaslvlrta et al. (1985).
    PCB with  soot  or on wipes  1s  generally  treated with 1 M  HC1 for  1  hour
by  shaking,  the slurry  filtered  by  suction,  washed with water,  dried  and
then  Soxhlet  extracted  with   toluene  and  further  treated  as  1n  Section
3.3.2.4.4. (Rappe et al., 1983a).
    3.3.2.4.3.   Chlorophenol  Formulations — A  4 g  sample of  the chloro-
phenol  formulation  was added  to 30 ma.  of methanol  1n  a  250 ml separatory
funnel.  Ten  mil of  2.5 M  lithium hydroxide was  added and  then 100 ml  of
water.   The  neutral fraction  was extracted  with  40 mil of  light  petroleum
ether at pH  12.   If the separation was  difficult,  2-5  g of anhydrous  sodium
sulfate was  added  to break the emulsion.  The organic  phase was washed  with
100  ml  of 0.05  M  lithium hydroxide,  and  then  with  50  mil  of  distilled
water,  which  should be neutral  on separation.   The  organic  phase  was  dried
over  anhydrous   sodium  sulfate  and  a  20  ml  aliquot concentrated  to 2  ml
1n  a  stream  of  nitrogen.   The  procedure for PCB  formulations was  followed,
beginning  at  the second aluminum  oxide  column  step, given  above In  Section
3.3.2.4.1.  This method  Is a  combination  of the  published  methods  of  Buser
and  Bosshardt  (1976)  and  Buser  et  al. (1978d).   Recoveries of PCDFs  were
90%.  The  method has been  used  also  by  Paaslvlrta et al. (1982)  and Singh et
al. (1985).
    3.3.2.4.4.   Fly  Ash  Samples — Fly  ash  (25 g)  was  stirred  1n  1 M
hydrochloric add  (200 ml).  After centrlfugatlon  the  residual   fly ash  was
washed  with  delonlzed  water 1n  a Buchner  funnel and dried  at room tempera-


1927A                               3-33                             06/23/86

-------
ture.  The dried  fly  ash  was  then extracted for 35 hours with  toluene  using
a Soxhlet apparatus.  Approximately 98% was extracted  In  the  first  24 hours,
and  1n  the  next 24 hours 1.2-1.6% more  was recovered (Kooke et al.,  1981).
This  Is  the crucial  step since  other  solvents  like methylene dlchlorlde,
acetone/hexane  or  chloroform  are much  less  efficient.    Also,  use  of  HF
Instead of HC1  drastically lowers the extraction efficiency (Lustenhouwer  et
al.,  1980;  Kooke  et  al.,  1981).  Wang et  al.  (1983)  showed that 12N HC1  or
12N  H_SO.  Increases  OCDD extraction  by  a  factor of 2.   The extract  was
then  concentrated  to  1  ma  and  loaded  onto  a  chromatographlc column  con-
sisting  of  4 g  of silica  loaded with  40%  (weight)  concentrated  sulfurlc
acid.   This  column was  connected to  another,  containing  layers  of 2 g  of
sodium hydroxide treated silica gel (1 part by  weight) of 1 M sodium hydrox-
ide  solution on  2  parts  (by weight of silica gel), 2  g of  silver  nitrate  on
silica gel  (10% by weight),  and 1 g of silica  gel.   The  columns were eluted
with  redistilled   n-hexane.   The  eluent  was  concentrated  and  then  chroma-
tographed by the method described 1n Section  3.3.2.4.2.   Recoveries  of  PCDDs
and  PCDFs were  reported to be  100%  (Lustenhouwer et al.,  1980;  Kooke et al.,
1981).   A  quick method  by Shushan  et al.  (1985) has  not been  adequately
evaluated yet, but HPLC cleanup caused  a  large PCDF loss.
     PCDF  recovery  from  EPA-5  type  sampling  trains   1s  extremely  variable
(Clement et al., 1985a; Wang  et al., 1983; Tlernan et al.,  1985);  a multiple
rinse  scheme  Is necessary to  achieve  reasonable  precision (Tlernan  et  al.,
1985).  An  Interlaboratory comparison 1s documented by Brocco et al.  (1984),
the  results sometimes vary by an order  of magnitude.
     3.3.2.4.5.   Agent Orange and 2,4,5-T Ester  Formulations  — Ester  for-
mulation (1 g)  was added  1n n-hexane to a silica  gel  column  (15 cm x 11  mm;
silica  gel, Merck)  and   eluted  with  30   ma  of 5%  methylene  dlchlorlde  In


1927A                               3-34                             06/23/86

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n-hexane.  The eluate was concentrated  1n a  stream  of  nitrogen.   The concen-
trate was subjected to the  technique  given  In  Section  3.3.2.4.1.  starting at
the  second  aluminum  oxide  column  step.   Recoveries  of 20-50  yg  of  added
TPCODs and TCDFs were 90% (Rappe et al., 1978c).
    3.3.2.4.6.   Wood  Dust — A  published  method  by  Levin  and   Nllsson
(1977) recommended that  the wood dust be extracted with ether and the ether
concentrate subjected  to TLC or  silica  gel, and the PCDFs and  PCDDs eluted
with chloroform.
    3.3.2.4.7.   Gelatin Samples  — A  15  g   gelatin sample  was  weighed  Into
a  100 ma  round bottom  flask.   Ethanol  (20 ma) and  40%  aqueous  potassium
hydroxide  (40 ml)  were  added  and the sample  shaken  for  1.5-2 hours  at  180
strokes/minute.   The  solution  was  then  extracted  with   hexane  (1x20  ma;
3x18  ma)  In  a  separatory  funnel.  The  halogenated hexane extract  was  then
extracted  first with  1  M  potassium hydroxide  (40  ma) and  then  with  40 ma
portions  of  concentrated sulfurlc add until  the acid phase was  colorless.
Heavy  emulsions at  this last  step  were broken  by swirling the  separating
funnel.   Moderate  emulsions were  successfully broken by  addition  of  a  few
crystals  of anhydrous  sodium carbonate.  The washed hexane extract  was fur-
ther  washed  with water  (10 ma)  and  saturated aqueous sodium carbonate  (10
ma)  and  filtered through 5 cm (15  g)  of  anhydrous  sodium  carbonate In  a 19
mm ID x 30 cm chromatographlc  tube.   The  hexane eluent  was  concentrated to 3
ma  on a  steam bath,  the  containing  flask  being  filtered  with  a  modified
mlcro-Snyder  column  and also  containing three 20-mesh carborundum boiling
chips.  Although Firestone  (1977b)  then  utilized  a  slightly different method
to achieve separation  of PCDDs  and  PCDFs  from other chlorinated  compounds to
obtain >90%  recoveries  of  PCDDs (tetra- to hepta-)  and  2,3,7,8- TCDF,  the
more  modern   procedure  described  1n  Section  3.3.2.4.4.  should  be  followed
before GC/MS.

1927A                               3-35                             06/23/86

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    3.3.2.4.8.    Tissues  — Four  methods  are  current:   a  Japanese  method
(Nagayama et al.,  1977),  one advocated by  Albro  and Corbett (1977), one  by
Stalling et al.  (1981),  and others  compared  by  Albro  et al.,  (1985).
    The  Japanese  method,  which  was  also  used by Kurokl  and Masuda  (1977,
1978) and  Rappe  et al.  (1979b), Involves  tissue  homogenlzatlon  1n  n-hexane
and  sodium  sulfate In a Waring  blender  followed  by saponlfIcatlon with  1  N
potassium  hydroxide  In  ethanol.   The  alkaline solution  was extracted with
n-hexane, concentrated and then chromatographed on a silica  gel  column  (2 g)
elutlng with n-hexane.  The concentrate was further  fractionated  on  a  column
of aluminum  oxide  (3 g)  using first n-hexane/carbon tetrachloMde  (4:1  v/v)
and  finally  25%  methylene  d1chlor1de/n-hexane  to  elute the  PCDFs and  PCDDs.
The  final eluate was  evaporated, so  It could be  Injected  Into the GC.   Albro
and  Corbett  (1977)  and  Albro (1979)  showed that  there  were  extensive  losses
of OCDD  and  OCDF  (up to 60%) at room temperature and  90% under  reflux,  dur-
ing  the  potassium  hydroxide  saponlfIcatlon  step.  These losses  are  Important
1f all PCDFs are to  be quantltated or  1f  these compounds  take part  In  syner-
glstlc/antagonlstlc  toxic  reactions.   The recovery  of  2,3,7,8- TPCDD  was
88-90% at room temperature.
     Albro and Corbett (1977)  described  methods to extract PCDFs  from  liver,
blood, urine, milk,  serum and adipose  tissues.   Liver samples  were  blended
1n   200  ml  of   chloroform/methanol  (2:1   v/v);   the   solution  was  filtered
under  suction  through a glass fiber  filter paper;  and the  filter  paper  and
cake was then  blended  with  100  ml of  chloroform/methanol   (2:1 v/v).   The
solution was again  filtered  as above and  the  filtrates combined.  A solution
of   1.2%  aqueous  potassium  chloride  (52  ml)  was  added  and  mixed.   The
phases were  allowed  to clear,  the  lower  phase  collected,  and evaporated just
to  dryness  at  40°C  by  rotary evaporation under  reduced pressure.   Blood,


1927A                               3-36                             06/23/86

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urine, milk  and  serum (100 ml)  were  extracted as described by Kates  (1972)
and the  resulting chloroform phase was  concentrated by rotary evaporation.
Adipose tissues were ground In a mortar and  pestle with  8  times their  weight
of anhydrous sodium  sulfate.  The  powder  was extracted with chloroform  In  a
Soxhlet,  allowing at  least  eight cycles.   The chloroform extracts were  con-
centrated by  rotary  evaporation.  All  the chloroform concentrates  obtained
above were  then  further  treated by  the  same  cleanup procedure.   The  llpld
residue  from  10  g of  liver,  100 ml  of  biological   fluid  or  1 g of adipose
tissue was  leached  Into  15  ml   of carbon tetrachlorlde.  Concentrated  sul-
fuMc add  (15 ml)  was  added,   the mixture  shaken  and  centrlfuged  at  2000
rpm for 30 minutes.  The  organic layer was removed,  the  volume noted and the
layer dried  by passing H through  anhydrous  sodium  carbonate  In  a glasswool
plugged  funnel.   The  sodium  carbonate  was  then   rinsed  with  fresh  CC1.
(2 ml).   The  filtrate was  concentrated  just to  dryness  by rotary  evapora-
tion  at  40°C.  The  residue was  leached  with  1.5  ml of  n-hexane/methylene
dlchlorlde (97:3 v/v).  The  leachate  was  loaded onto a  dry-packed column  of
Fisher A-540  aluminum oxide  (3 g) of  diameter 0.5-0.7 cm.   The flask  was
rinsed with  1  ml  of  n-hexane:methylene  dlchlorlde   (97:3  v/v)  and  added  to
the  column.    Fraction  I  was   eluted  with  28 ml  of  n-hexane:methylene
dlchlorlde  (97:3  v/v).   Fraction II  was eluted with  30 ml  of n-hexane:
methylene dlchlorlde  (4:1 v/v).   Fraction  II  was   evaporated  to near  dry-
ness.  An aliquot was then taken for  GC/MS analysis.
    The recoveries of  dlbenzofuran, PCOFs and  PCDDs,  were  reported to  be 95%
(using the method of standard additions).  The  sulfuMc  acid step was  suffi-
cient to  handle  150  mg of trlglycerlde/mi of  acid,  but  only  about  50 mg  of
total liver  Upld/ml of  add.   Emulsions were  routinely  broken  by centrl-
fugatlon.  Fisher A-540  aluminum oxide best  retained I1p1ds  1n  the solvent


1927A                               3-37                              06/23/86

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system  described;  other  aluminum  oxide  types  allowed  partial  elutlon  of
sterol  esters,  waxy  pigments and  various  trlglycerldes.   The final  concen-
trate was suitable for analysis  at the ppt  level  by  GC/MS.
    The  methods for  PCDF  quantltatlon  In  adipose  tissues  recommended  by
Stalling et al.  (1981)  [see also Rappe et al. (1981)]  Involved  Initial  pro-
cedures similar  to those  described by Albro and Corbett  (1977).   Thus,  adi-
pose tissues were blended with 4  times their weight  of  anhydrous sodium sul-
fate and  the  column  extracted  with 100 mft  volumes of methylene  dlchlorlde
for every  10  g  of tissue.   After  removal  of solvent by  rotary  evaporation,
the weight  of  the  oil residue was noted.  This  residue was dissolved 1n 1:1
(v/v) cyclohexane/methylene  dlchlorlde  to  achieve an approximate  concentra-
tion  of 0.2  g/ml.   AHquots (5 ma) were  applied  to a  gel permeation  col-
umn containing  69 g  SX-3  BloBeads resin  (2.5 cm ID  x 48  cm) and eluted  at 5
mi/mln.   The  165-300  ma.  eluent  fraction  of  each  analysis  was  collected,
amalgamated and then  reduced  to  near  dryness   by  rotary evaporation.   The
extract  was  then  passed  through a  column of  potassium  hydroxide-treated
silica  gel  topped with a  small amount  of cesium  hydroxide-treated  gel layer-
ed  on   top  of a  small  band  of  sulfuMc acid-Impregnated  silica  gel.   The
eluent  was  then run  Immediately  through a  column  containing carbon (Amoco
PX-121;  <40 yiti) (Rappe et  al.,   1981) and  dispersed on  glass fibers (Stal-
ling, et  al.  1981).   Planar molecules (such as, toxic  PCDDS  and PCDFS)  were
collected  by  reverse elutlon with  toluene  (30  ml), whereas nonplanar  mole-
cules  could be  eluted  with 1:1   (v/v) benzene/ethyl  acetate  (30 mj.)  In the
usual manner.
    PCOOs  and PCDFs  were then specifically  collected by the  technique  des-
cribed  In  Section  3.3.2.4.2. before  GC/MS.  The  reported recoveries  were
1927A                               3-38                             06/23/86

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>70%.  A slightly revised method was  used  by  Nygren et al., (1986) for human
adipose tissue, mother's  milk,  bovine fat and bovine  milk.   The recovery of
13C,?-labeled surrogates 1s normally found to be >60%.
    Albro et al.  (1985)  evaluated  6 different approaches  1n  an Interlabora-
tory  study  for  3  PCDFs  (2,3,7,8-TCDF;   2,3,4,7,8-PeCDF;  1,2,3,7,8,9-HxCDF)
added  to  human  adipose tissue extracts at  levels  of 5 to  50  ppt.   The adi-
pose  tissue  (600g)  was  combined  with 4.8 kg  of  pesticide  grade anhydrous
sodium sulfate  In a  clean  food-grinder.   After  3 processings, the powder was
packed  Into  two  20 In.  x  4  1n.  diameter pyrex  columns.  The  packing was
eluted  with  3ft.  of  ethyl  acetate  containing  0.001%  butylated  hydroxy-
toluene, and  then 68. of  methylene dlchlorlde.   The  extracts  were combined,
concentrated 1n  vacuo  at  37°C, and the Upld diluted with chloroform to 900
mft.  to  stop  solidification.  The yield was equivalent  to  soxhlet extraction
with chloroform  for 16 hours.   The PCDFs  1n  toluene were  added and the adi-
pose  tissue  solution  (60g  adipose tissue  equivalent)  stirred magnetically.
The  chloroform  was  reduced (water  aspirator) In a  dlsslcator over 24 hours.
Six extraction methods were then evaluated.
     (I)  13C-2,3,7,8-TCDF   and   37Cl-2,3,7,8-TCDF   were  added  as  Internal
standards.   The   sample   was  passed  In   cyclohexane/CHLCl,,  through  two
potassium  silicate/silica  gel  columns  and  then  through carbon  adsorbent
(Stalling et  al.,  1981).   The extracts  were  concentrated at  55°C  1n vacuo
and  then  passed   through  a  H?SO./s1l1ca  gel  column   In  o-xylene.   The
Interference of  chlorinated naphthalenes  can be further  removed  by  a final
alumina  chromatography step.   This  method  1s  derived  from  Smith   et  al.
(1984).
     (II)  13C-2,3,7,8-TCDF  was added  as  Internal  standard  and  the Upld
solution  partitioned  between  hexane/concentrated  FLSO.  for  13-54   hours.


1927A                               3-39                             06/23/86

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The  organic  phase  was  washed  through  silica,  NaOH  on  silica,  silica,
HpSO.  on  silica,  and  silica,  with  5% benzene  1n  hexane.   After  concen-
tration, the residue was dissolved 1n  hexane.  This  solution  was  then passed
through  AgNO»  on silica and  trapped  on basic  alumina.  After washing  with
CCl^/hexane   (4:1),   PCDF/PCDDs   were   eluted   with   CH^/hexane   (3:1),
the  eluate evaporated under nitrogen  and  redlssolved  1n  chloroform.   After
reverse  phase  HPLC,  the appropriate  collected  fractions were  further  purl-
fled  by  normal  phase  HPLC.   This  method  1s  derived  from Lamparskl  and
Nestrlck (1980).
     (Ill)  The 37C1-TCDF,  PCOF,  and  HxCDF  were  added  as  Internal  stan-
dards.   The  samples  were  digested  1n concentrated HC1  for  1  hour,  extracted
twice with hexane and dried over anhydrous sodium  sulfate.   The solution was
washed  through  a   H SO./slUca  gel   column  with  hexane;  the  eluate  was
washed with  water,  dried  and  concentrated.   The concentrate  was  bonded  onto
grade  I  alumina  and  washed  with  5%  CH2Cl2/hexane;  the  PCDFs/PCODs  were
eluted  with  CHpClp/hexane  (1:1),   concentrated  to  1  ma, and  then  loaded
on  Carbopack  C/Cellte treated  as per  Stalling  et al.  (1981).  The extracts
were  concentrated  to 10  yL  with dodecane entralner.  This  was  an original
method.
     (IV)  a7Cl-2,3,7,8-TCOF  was  added  as  Internal  standard.  The  solution
was  then  partitioned  between  hexane/H-SO.  until  the  H0SO.  was  color-
                                         24               24
less.   The hexane  phase  was  washed  with  ^% aqueous  NaOH and water,  dried
over   NapSO./hexane,   and  eluted   with   CHpClp.    The   eluate  was  dried
under  nitrogen,  and the residue redlssolved  In  toluene  or  Isooctane.   This
1s a method derived by Ryan et  al.  (1985a).
     (V)  37Cl-2,3,7,8-TCOF  was  added  as  an  Internal  standard.  The solution
was   diluted  and   partitioned   against  H2S04   and   neutralized  through
1927A                               3-40                             06/23/86

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Ha2C03  and  KOH/s1l1ca.   After  concentration,  the  PCDFs  were  exchanged
Into  hexane  from  cyclohexane,  loaded  onto  acidic  alumina,  washed with  3%
CH2Cl2/hexane,   and   eluted   with   CH2Cl2/hexane   (1:1)   onto   charcoal/
cellte.  This  was  then washed  with  10% benzene/hexane and  back-eluted  with
5054  xylene/hexane  onto  neutral  alumina,  washed  with  3%  CHpCU/hexane,
eluted  with   CH2Cl2/hexane-  (1:1)   and  then  concentrated.   This   1s   an
original method.
    (VI) iaC-2,3,7,8-TCDF  was  added  as  Internal  standard.  After  dilution
with  CH2Cl2/cyclohexane,  the  solution  was  passed  through  slUca/potas-
slum   s1l1cate/Na2SO./potass1um   sH1cate/s1l1ca/carbon   column   combina-
tions.   The   last   column   was  washed   with   cyclohexane   CH2C12   and
CH2Cl2/methanol/benzene   (15:4:1),   and   back-eluted   with  toluene.    The
extracts  were  concentrated  at  35°C,  passed  through  potassium  silicate/
H2$04  on  silica  with  hexane  onto acidic  alumina, washed  with  hexane  and
2%   CH2Cl2/hexane.    PCDFs/PCDDs  were   eluted   with   CHC1 /cyclohexane
(1:1)  and  concentrated.  This  method  was  derived  by  Rappe et al.  (1984).
The  molecular  Ions  of  all   13C/35C1  and  12C/37C1  PCDFs  were  monitored
except  1n  Method IV where  the (M -COC1)* 1on  was monitored by MS/MS.   The
Interferences  from chlorinated  dlphenyl  ethers,  PCBs, chlorinated  methoxy
blphenyls,  p.p'-DDE  and  o,p'-DDE were  accounted  for.   Various  GC  columns
were  used  with  DB-5  and SP-23SO fused  silica capillary  columns were  most
utilized.   Total  analysis/report  writing time varied  between  48  and  140
days, though  each method took between  6 and 26 working days.
    The Isotoplc  Internal  standard  method  was definitely  superior  to  the
external standard method  (Table  3-7);  the absolute quantHatlon 1s  extremely
variable.   Only  methods  II,  III and  VI had  relative  standard deviations  for
unsplked samples of lower  than 25%.   As Table  3-7  shows, method  II was  most
1927A                               3-41                              06/23/86

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                                  TABLE  3-7
                 Error In Estimation of PCDFs by Six Methods3
                     % Relative Error Compared With "Correct" Level In Method
Compound
                     I        II      III     IV         V         VI
2,3,7,8-TCDDD        -50      +10
a,3,7,8-TCDFc        -(1+3)   -(lj
2,3,4,7,8-PeCDFd     +(13+6)  *
l,2,3,7,8,9-HxCDFe   -73      -18
                                      leaked  -90        -73       +70
                                      +(2±3)  (0.5+11)   +(10+8)   +(3.5+2.1)
                                      +(12+7) -(3.5+3.5) +(27+16)  +(24±34)
                                      BO      -100       NM        +9
aSource:  Albro et al. (1985)
b!0 ppt:  (1 sample)
cll ppt:  (average of 2 samples)
d!6 ppt:  (average of 2 samples)
ell ppt:  (1 sample)
BD = Below detection
NM = Not measured
1927A
                                    3-42
06/23/86

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accurate (within 20% of the correct  answer)  for  spiked  PCDF  and 2,3,7,8-TCDD
at  -10-16  ppt.   This  method  took  26  working  days  for sample  processing.
There appeared to be no correlation between recoveries of PCDFs and PCDDs.
    The  results  of  this  blind study  Included certain  commonly  encountered
environmental contaminants that can  Interfere  with  the  quantltatlon of PCDDs
and PCDFs.   Six  laboratories  using 6 different methods  (all  entailing GC-MS
for quantltatlon  of PCDFs)  participated  In  the study.   Comparison  of  the
results  Indicated  the  data  obtained  were  qualitatively reliable;  however
quantltatlon was problematical for some laboratories.
    Another  published  report  (Schecter et al.,  1985a)  describes  the results
of  analyzing blood  and  adipose  tissues  from patients  exposed  to residues
from a  PCB-contalnIng  transformer fire.  The  method  of  analysis  Implemented
In  the latter study  entailed  GC-MS quantltatlon  of  not  only 2,3,7,8-TCDD and
2,3,7,8-TCDF  but  the  sum  of  the  congeners  constituting  each  chlorinated
class   of    PCDDs   and   PCDFs,    Including   the   tetrachlorlnated  through
octachlorlnated  congeners.    The   results  of  this  study  Indicate  that  the
tissue  from  patients  with  no known  exposure  to  PCDDs or  PCDFs had,  In
several  cases,   several  hun- dred  parts-per-trllHon  levels   of  higher
chlorinated   PCDDs   and   PCDFs.    Other   publications  by  Schecter  et  al.
(.1986a,b) and Ryan et al. (1986) have Included the above approach.
    3.3.2.4.9.   Water — There  Is  currently  no   specific  method  for  the
analysis  of  PCDFs  1n water.   The procedure  used  for urine   In  Section
3.3.2.4.8.  but  scaled  up   to accommodate  1 8. of  water   In   the  Initial
extraction stage  should be  sufficient.   A simpler  method would be  to extract
1 I  (or   a   larger  volume)   of  acidified   water   (pH 2)   with  methylene
dlchlorlde and then  concentrate the  extracts.  The  Yusho oil  method (Section
3.3.2.4.2.)  could  then be applied.  Obviously,  further  research  Is required
1n  this area.

1927A                                3-43                             06/23/86

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    3.3.2.4.10.  Sediment — Sediment  samples  (10  g)  have  been  analyzed  by
mixing and blending with  20 g  anhydrous  sodium sulfate, followed by  Soxhlet
extraction for  48 hours  with  100 ml of  toluene  with  subsequent concentra-
tion  of  the   extract,  before  cleanup  and  GC/HS   analysis  (Petty  et  al.,
1983a,b). The  extraction  efficiency 1s >74%.  An article describing analyti-
cal  methodology and  the application  of  this  method  to  the  assessment  of
environmental   contamination by  PCDOs  and  PCDFs  as  a  result of Improper  dis-
posal  of  chemical wastes has   been  published  (Tlernan et  al.,  1985).   The
analytical methodology  employed  entailed  the  use  of GC-MS  to quantHate
parts-per-tr1H1on to parts-per-b1H1on levels  of  PCDFs as well  as PCDDs  In
municipal  refuse-fired   boiler  effluents  and  effluents  from  an  RDF-flred
boiler as well as soot from a PCB-contalnIng transformer fire.
3.4.   GC/HS METHODS FOR PBDFs
    GC  methods  for  the  PBDFs  are  not  as  plentiful  as   those  for  PCDFs.
O'Keefe  (1978b)  has published  a method for separating  PBDFs from PBBs.   The
PBB  (50  mg)  was dissolved  In  2 ml  of benzene and  the  solution was  filtered
through  a sodium  carbonate column  (40 m x 6  mm)  1n  a  disposable  Pasteur
pipette,  followed by  two  5 ml benzene  washings.   The benzene  eluate  was
concentrated  to 1 ml,  10 ml  of  cyclohexane  added,  and  the  solution  evap-
orated  to 1  ml.   This  replacement procedure  with cyclohexane was  repeated
twice.   Methylene  dlchlorlde   (15  ml)  was  then   added,  and  the  solution
loaded  onto a column  of  graphltlzed  charcoal  (Carbopack AHT; Supelco,  Inc;
40 m x 6 mm).
    Nonplanar  aromatlcs  were eluted  with 50 ml benzene/dlethyl ether  (4:6)
followed  by  pyrldlne  (70 ml)   to elute  the planar aromatlcs.  The  pyrldlne
fraction  was  reacted  with  140  ml of  1%  hydrochloric add  and  then  extract-
ed  with hexane  (3x30 ml).  The hexane  fractions  were  combined, washed  with


1927A                               3-44                             06/23/86

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100 ml  water, dried  (sodium  sulfate)  and  then  concentrated.  The  concen-
trate was  placed  onto  an activated  aluminum  oxide  column  (Woelm  Neutral;
40x6  mm)  1n  a  disposable  Pasteur plpet.   The  first eluate,  10 ml  CC14>
contained PBBs,  and the  PBDFs were eluted  with 7 ml  methylene dlchlorlde.
GC/MS was performed  on  this  eluate.  O'Keefe  (1978b)  used  a 6 ft  x 1/8 Inch
Pyrex column,  packed with 3% OV-1 on  100/200 mesh Gas  Chrom Q temperature
programmed  from  260-290°C at  6°C/m1n  to  separate any  PBDFs  before analysis
by MS.   The molecular weight  of  the TBDF  was 479.6996,  and  It  was  the 10054
peak  (M).   Other  peaks were  M-2Br (30%),  M-COBr-2Br (20%),  H-COBr  (6%), M-Br
(654), Mf*  (354)  and (M-2Br)2f  (weak).   PeBDFs  showed peaks  at the  molecu-
lar   1on  561.606.   The  other  major   Ions   were  M-COBr,  M-Br,  M-2Br  and
M-COBr-Br Ions.   This procedure  allowed 5054  recovery of the 2,3,7,8-TBDF and
was applied to analyze pyrolyzed  PBB.
    No  PBDFs  (<0.5 ppm)  were  found In  Flremaster BP-6 by Mass et  al.  (1978)
using a technique  Involving  Florlsll  fractlonatlon  of  a  10 g sample dis-
solved  In  150  ml of  354 methylene  dlchlorlde 1n  hexane eluted  first with
500  ml  of   354  methylene dlchlorlde/hexane  and  then with   500  ml   of  5054
methylene dlchlorlde/hexane.   The latter  fraction contained 0.5 ppm PBDFs on
concentration  and analysis by GC/MS,  using  a  1  m  x 2 mm ID stainless steel
column  packed with  354  OV-101  on  100/120 mesh  Gas  Chrom  Q at  300°C.   No
recoveries  of PBDF standards  were cited and  analytical  conditions  were not
optimal  with  the use of  the  stainless  steel  GC column and the high tempera-
ture.   A methyl-BDF was  subsequently found  1n the polar  fraction  of a Fire-
master  of unspecified type (Moore,  1977).
    Buser  (1986)  used  a  25 m  x 0.31 mm ID  SE-54  glass  capillary  column
(splHless)  1n  conjunction  with temperature  programming.   As expected, the
 1927A                                3-45                              06/23/86

-------
retention times are  longer  and  the elutlon temperatures are  higher  than the
corresponding  PCDF  analogs.  The  electron Impact  mass  spectra  of  TBDF and
PeBDFs agreed with those found by O'Keefe (1978b).
3.5.   OTHER METHODS FOR THE PCDFs
    It  1s  clear  from  Section 3.3.  that  no  one technique  will  suffice  to
separate, quantify  and  confirm the presence  of  the PHDFs.   Sometimes  It  Is
necessary to use all the available methods.
    Hutzlnger et al. (1973) found  that TLC on Merck Silica Gel  F-254 of 0.25
mm  thickness  allowed  2,8-DCDF and OCDF  to be separated 1n  n-hexane solvent
with Rf values of 0.55 and 0.75,  respectively.
    A gel permeation  technique  for the  cleanup  of  PCDDs and PCDFs  was pro-
posed by Stalling et al.  (1975).  The  system used BloBeads  S-X_ with  ethyl
                                                                o
acetate and ethyl acetate/toluene as solvents.   This system  has  been alluded
to  In  Section 3.3.2.4.8.   PCDFs, PCDDs and chloronaphthalenes were  retained
on  a  charcoal column  subsequent  to  gel  permeation chromatography  and were
eluted with ethyl acetate/toluene.
    Perchlor1nat1on techniques have  been  used to  obtain total PCDF  content
(Masuda et al., 1976), but  for reasons outlined  previously are  not  useful  In
Identifying  Individual  toxic  Isomers.   Ballschmlter et al.  (1985)  have used
BMC  reagent  to   achieve  perchlorlnatlon.   Perbrom1nat1on  Is  not  possible
because of steMc hindrance (Rlchtzenhaln and  Schrage,  1978).
    The  Flremaster  BP-6  metabolite,   6-hydroxy-2,2',4,4',5,5'-hexabromob1-
phenyl  decomposes on  OV-101   GC columns  at   230-260°C  to  form  two  PeBDFs
(Gardner et  al.,  1979).   This  demonstrates  that  PBDF  detection alone does
not prove PBDFs were  originally  present  In the  sample.  If  phenolic metabo-
lites are  separated, there  Is  no lack  of specificity.   There  1s  also the
need  for a  good  HPLC  method along  the  lines  of the separation  of  PCDD


1927A                               3-46                              06/24/86

-------
Isomers  (Nestrlck  et  al.,  1979).  The  latter  step should complement  the  GC
step of  GC/MS.  Substantial HPLC  losses  especially  for  lower  PCDFs  have been
reported  (Shushan  et  al.,   1985).   The  losses  vary  from  2- to  5-fold.
Clearly  this  warrants  Investigation.  Mazer  et  al. (1983a,b)  have  success-
fully used  a  reverse phase column  (C,0) with 75%  acetonltrlle/25%  water  at
                                      lo
0.75 mfc/mln with  detection at 235  nm.   They also  utilized  a  normal  phase
Zorbax  NH~  column with hexane as the  eluent at  1.5  mi/mln.   Both  columns
were used  In  cleanup  steps  to produce  pure  Isomers  rather   than to  provide
quantitative  recovery.   Cull   and Dobbs  (1984)  have  also used this  tech-
nique.    The quality  control   and  assurance  required  for HPLC analysis  of
PCOOs and  PCOFs  has been  presented  by  Donnelly  et al.  (1986)  1n  connection
with RCRA Method 8280.
    A  promising  radlolmmunoassay for   2,3,7,8-tetra-PCDF  1n   PCBs  and  1n
environmental  samples has  been recently  developed  (Luster  et  al.,  1980) as a
screening technique.
    Biological monitoring  by  Induction of  arylhydrocarbon  hydroxylase activ-
ity  (Poland et al.,  1979; Bradlaw  and Casterllne,  1979)  1s  considered  1n
Chapter 7.  Hutzlnger  et  al.   (1981)  and Wang et al. (1983)  showed  that  the
toxldty of fly  ash samples  1n  the  cytosol  receptor assay could not  solely
be  explained  In terms  of  2,3,7,8-TCDD  (72  pg 2,3,7,8-TCDD  equivalents  was
the  ED  _).  The  Induction and cytosol  receptor  assay tests  often  disagreed
(Sawyer et al., 1983).  See Chapter 7 for a discussion of these tests.
    Helder et al.  (1982) and  Helder  and  Selnen (1985)  have used a  biological
assay with  rainbow trout  yolk sac fry to  show that the toxldty of  fly  ash
cannot  be  solely  attributed to the 2,3,7,8-TCDD level but to the  cumulative
presence of other  PCDDs and PCDFs.   The  fry  suffered  hemorrhages,  edema,  fin
1927A                               3-47                             06/23/86

-------
necrosis  and  finally  death  at  days 4-12.   2,3,7,8-TCDF  also  caused  this
behavior.  The  raw  fly ash was  as  toxic as the cleaned-up  PCDDs/PCDFs  from
the same fly ash sample reconstituted 1n the same volume.
    A  bloassay  based  on  humoral .antibody  production has  been  utilized  by
Rlzzardlnl et al. (1983).  2,3,7,8-TCDF  at 10 ng/g caused  an  Immunosuppres-
slon  of  25%.    Administration  of both  2,3,7,8-TCDD  and  2,3,7,8-TCDF  caused
much less Immunosuppresslon than the TCDD alone.
1927A                               3-48                             06/23/86

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                        4.  SOURCES TO THE ENVIRONMENT
4.1.   SUMMARY
    PCDFs  occur  as contaminants  of  a  number of  chemical  products  such  as
phenoxy  herbicides,  polychloMnated phenols,  hexachlorobenzene,  polychloM-
nated  blphenyls  and chlorodlphenyl ethers.   PCDFs are also  associated  with
thermal  Insulation  material's.   Thus, both  PCDFs  and PBDFs are  adventitious
copollutants released Into the environment  together  with  economic  poisons  or
Industrial wastes.  There  Is  experimental evidence that PCDFs and  PBDFs may
be  formed 1n  the  environment  by  photolytlc  and  pyrolytlc  reactions  from
chemical  products and combustion  processes.   Many of the products  contain a
larger percentage of PCDDs than PCDFs.   However,  the PCDFs  1n these products
Include  more  of  the  tetra- and  penta- (the  most  acutely  toxic)  compounds
than do  the PCDDs.  The  levels of  PCDFs  containing 4 and  5  halogen atoms are
generally  <20  ppm for  most chlorophenols,  <0.40  ppm 1n most  phenoxy herbi-
cides, <5 ppm 1n PCBs  and <0.5 ppm 1n  the PBB, Flremaster BP-6.   The lower
chlorinated phenols and  PCBs  are  most highly  contaminated with  toxic PCDFs.
The levels of  the 2,3,7,8-TCDF  and 2,3,4,7,8-PeCDF,  the most  toxic Isomers,
are generally <1 ppm In  most  PCBs.
    PHDFs  are  formed by  the  pyrolysls of various  materials.   They have  been
detected  1n  Incinerator  fly  ash   (<1.5  ppm),  1n  pyrolyzed   PCB  (up  to  104
ppm),  1n PCB  that  had  been  used  for 2  years  as  heat exchanger  fluid  (<16
ppm),  In  pyrolyzed  PBB  (up  to  10*  ppm),   In  pyrolyzed  (2-butoxyethanol)
ester  of  2,4,5-T (<20  ppm),  1n some  pyrolyzed commercial chlorophenols  and
1n pyrolyzed chlorinated dlphenyl  ethers.
4.2.   SOURCES OF PCDFs  FROM  CHEMICALS
    The  early  work  on  the detection  of  PCDFs was hampered by  losses during
sample cleanup  and analysis  and  by  the fact that  many  PCDF gas  chromato-
graphlc  peaks  were  frequently  superimposed on those  of chlorinated dlphenyl

1928A                               4-1                               06/23/86

-------
ethers  (Crummett  and  Stehl,  1973).   The  Interfering  chlorinated  dlphenyl
ether usually contained  two chlorine  atoms  more than the PCDF.   In  spite  of
these  difficulties,   OCDF  and  a  HpCDF  were  detected  1n  dipping  wastes
containing pentachlorophenolate used  as  a wood preservative  attributable  to
side-reactions 1n manufacture  (Jensen  and Renberg,  1973).
    PCOFs are  therefore  not commercially  produced but are formed as  trace
unwanted  Impurities  1n the manufacture  of  other  chemicals such as  chlori-
nated  phenols and  their  derivatives,  chlorinated  dlphenyl  ethers,  hexa-
chlorobenzene  and  polychlorlnated  blphenyls,  which  are released  Into  the
environment either as economic  poisons or as Industrial  wastes (Table 4-1).
    An  estimate  of  the  extent  of release  Into  the  Canadian  environment  of
known sources of  PCDFs Is provided 1n  Table  4-2 (Sheffield,  1985a,b).
4.2.1.   Chlorinated  Phenols.   Chlorophenols  are  Industrially  produced  by
two methods,  namely  by the direct chlorlnatlon of phenol  (Hutzlnger  et al.,
1985b)  and  by alkaline  hydrolysis  of  chlorobenzene  1n  different  solvents
(Ahlborg  and  Ihunberg,  1980).   PCDFs appear  as   contaminants  1n both  pro-
cesses with more  formed  In the latter process.  The annual world production
In 1979 was -150,000 tons (Rappe et al.,  1979a).
    Chlorinated phenols  are used  as fungicides, herbicides, s!1m1c1des, wood
preservatives  and  bacterlddes;  they are  also  used  In  the synthesis  of
chlorinated phenoxy herbicides.
    Table  4-3 provides  the  composition  of  two  typical  commercial  PCPs.
Table  4-4 summarizes  some of  the PCDF  and  PCDD levels  found  1n  various
chlorinated phenols.   As expected, the  higher PCDDs and PCDFs  predominated
with  the  PCDDs usually more  abundant.  However, the TCDFs  and PeCDFs 1n all
chlorophenols  were  greater   than  the  content  of  the  corresponding  PCDD
congeners.  Since  the HpCDDs,  HpCDFs, OCDDs  and  OCDFs have  lower  toxlclty
1928A                               4-2                              06/23/86

-------
                                  TABLE 4-1

                  Presence of PCDFs 1n Industrial Chemicals
                     and Their  Entry  Into  the  Environment
Industrial Products
 Containing PCDFs
       Use
                                               PCDFs  (total  concentrations
                                                 1n  Industrial  products)*
                      Concentration
                        1n mg/kg
                       (m1n/max)
                                                                 Reference
Phenoxy alkanolc
compounds
herbicides
Chlorinated phenols    wood preservative
Hexachlorobenzene
Polychlorlnated
blphenyls

Chlorides of Iron,
aluminum and copper
fungicide and
Industrial waste

Industrial use
Industrial use
0.008-0.15
59.8-790


0.35-58.3


0.8-13.6
Rappe et al.,
1978b, 1979a;
AhUng et al.,
1977

Rappe et al.,
1979

Vlllaneuva
et al., 1974

CNRC, 1978b
0.0003-0.060     Helndl and
                 Hutzlnger, 1986
*0nly positive data are considered
1928A
             4-3
                        06/23/86

-------
                                  TABLE 4-2

          Estimated PCDD and PCDF Release to the Canadian Environment
                            from Chemical  Sources*
                                                      Release (q/year)
             Source
                                                  PCDD
                                  PCDF
Chlorophenol production
  Air emission
  Wastewater
               900
                13
   600
    13
Processes using pentachlorophenol

Wood preservation
  Wastewater
  Waste disposal

Leather tanning
  Sludge
              1000
              >500
           negligible
   600
  >300
Chemical products
  2,4-D formulations
  2,4,5-T
  Pentachlorophenol
  PCBs
               100
                 5
           [l.lxlO6]
[0.6x10*]
[750,000]
*Source: Sheffield, 1985a,b
1928A
4-4
 06/23/86

-------
                                   TABLE  4-3

                    Chemical  Analysis  of  a  Typical  Pure  and
                         Technical Pentachlorophenol3
      Source
         Pure
(AldMch, lot 120,717}
                     Technical
                (Monsanto,  lot KA578)
Phenols'5

  Pentachlorophenol
  Tetrachlorophenol

Nonphenollcs (ppm)D
ppm
                                     84.654
                                      3%
D1benzo-p-d1ox1ns
Tetrachloro- <0.1 ppm
Pentachloro- <0.1
Hexachloro- <0.1
Heptachloro- <0.1
Octachloro- <0.1
Dlbenzofurans
Tetrachloro- <0.1
Pentachloro- <0.1
Hexachloro- <0.1
Heptachloro- <0.1
Octachloro- <0.1

<0.1 ppm
<0.1
8
520
1380

<4
40
90
400
260
aSource:  Goldstein et al., 1977a

^Samples were analyzed by GC/MS.  The lower detection limit was 0.1 ppm.
1928A
            4-5
                               06/20/86

-------
TABLE 4-4
CD
3>
Levels of PCDFs and PCDDs In Some Commercial Chlorophenols
Levels of PCDFs and PCDDs (mq/kq)
Chloropheno"
Penta-
Penta-
Penta-
Penta-
er* Penta-
Penta-

Penta-

Penta-

Penta-
Penta-
c Penta-
c Penta-
cc
cr
1 Formulation Tetra- Penta-
Type
CDF CDD CDF CDD
(Monsanto) <4 <0.1 40 <0.1
(Dow) 0.20 <0.02 0.20 <0.02
(Dowlclde 7)
(Dowlclde 7) <0.2 <0.2 <0.2 <0.2
(Dowlclde EC-7) -
(Dowlclde EC-7) 0.45 - 0.03

(Dowlclde EC-7) <0.02 - <0.03

(Dow) 0.20 - 0.20

(Dow) 0.07 - 0.20
(Monsanto) -
(Monsanto) -
(European) 0.9 ? 4 ?
Hexa- Hepta-
CDF CDD CDF CDD
90 8 400 520
13 10 70 130
30 4 80 125
39 9 280 235
<1 1 1.8 6.5
0.30 0.15 0.50 1.1

<0.03 0.03 0.5 1.1

13 10 70 130

9 5.4 60 130
19 11 81 199
90 8 400 520
32 ? 120 ?
Octa-
CDF
260
55
80
230
<1
0.5

0.2

55

65
137
260
130
CDD
1380
210
2500
250
15
5.5

5.5

210

370
1170
1380
?
Total Reference
CDF CDD
794 1908 Goldstein et
al., 1977a
138 350 Rappe et al.,
1979a
190 2629 Firestone.
1977a
549 494 Buser, 1975
3.8 22.5 Firestone,
1977a
1 .8 6.8 Buser and
Bosshardt,
1976
<0.08 6.6 Buser and
Bosshardt,
1976
135 350 Buser and
Bosshardt,
1976
134 3.5 Firestone,
1977a
237 1300 Firestone.
1977a
750 1980 Firestone,
1977a
280 1000 Rappe et al .,
1978a. b

-------
ro
CO
3*













^
1
*"J














O
a*
NJ
to


Chlorophenol


Penta-


Penta-


Penta-

Penta-


Penta-

Penta-

Penta-

Penta-

Tetra-
(2.3,4,6-)
Tetra-
(2.3,4.6-)

Tetra-


Trl-




Formulatlon
Type

(Fluka)


(Fluka)


Na Salt
(Fluka)
Na Salt
(Dow)

Na Salt
(Fluka)
K12

K,

8 samples

(Dowlclde 6)

(Finnish)
Kymnene
Ky-5
Ky-5


(Swedish)


1 nULL f~f I IUM L . J
Levels of PCDFs and PCDDs (raq/kq)
Tetra- Penta- Hexa- Hepta- Octa- Total

CDF CDO CDF CDD CDF CDD CDF CDD CDF CDD CDF CDD
<0.21 - 0.05 ? 15 9.5 95 125 105 160 220 295


0.05 - 0.25 - 36 9.1 320 180 210 280 566 469


<0.02 0.12 0.03 0.03 0.7 <0.03 1.3 0.3 2.1 1.5 4.23 2.0

<0.02 - 0.005 - 11 3.4 50 40 24 115 85 158


<0.02 0.05 0.04 <0.03 11 3.4 47 38 26 110 84 151

ND ND 5.9 92 3.0 1921 29 204 11

ND ND ND ND 98 3.5 39 1.1 1.5 -

4.5 62 35 130 610
e
<0.2 <0.2 <0.2 <0.2 30 6 500 55 135 39 865 100

<0.5 <0.7 10 5.2 70 9.5 70 5.6 10 0.7 160 22


2.0 2.1 2.8 - 21 - 30 0.6 4.0 0.8


1.5 <0.02 18 <0.03 36 <0.03 4.8 <0.1 - <0.1 60 <0.3




Reference


Buser and
Bosshardt,
1976
Buser and
Bosshardt,
1976
Rappe et al . ,
1978a,b
Rappe et al . ,
1978a.b

Buser, 1976a

Paaslverta
et al., 1982
Paaslverta
et al., 1982
Cull and
Oobbs, 1984
Buser, 1975

Rappe et al . ,
1978a.b

Paaslverta
et al., 1982

Rappe et al . ,
1977

CO

-------
(McConnell et al., 1978b;  Poland  and  Glover, 1977), 1t may  seem more  appro-
priate to  concentrate  on  the TCDFs to  HxCDFs.  This can be  misleading,  how-
ever, since  2,3,7,8-TCDD  1s 1000-10,000  times  more toxic than  1,2,3,8-TCDD
{McConnell et al., 1978b; Poland and Glover, 1977).  Nevertheless,  the prob-
ability of encountering a  toxic  compound may be much greater  for  PCDFs  than
for  a PCDD since there are  more  PCOFs  containing  4 or  5 chlorine atoms  1n
the  vicinal   positions,  where  toxldty  1s  conferred.   Firestone  (1977a)
reported  that  the  major  PCDFs In  Dowldde  7 and EC-7  formulations were the
2,3,6,7- and  2,4,6,7-tetra-;  the  2,3,4,6,7-,  1,2,4,7,8-,  2,3,4,7,8-penta-;
and  the  1,2,3,6,7,8-hexa-lsomers.   Rappe  et al.  (1978a,b)  found  the  major
components 1n  an American  PCP to  be  those  given 1n Table 4-5.  The  Isomers
present were  very different  from  those reported  by  Firestone  (1977a).   As
shown  In  Table  4-5,  the   European  trlchlorophenol  formulation  contained
traces of the toxic 2,3,7,8-TCDF  and 2,3,4,7,8-PeCDF.
     In the United  States,  PCP 1s  manufactured by  the chlorlnatlon of  phenol
(Firestone, 1977a).  In Europe, both  this process and the alkaline hydroly-
sis  of   hexachlorobenzene   (135-275°C)  have  been  used.   The  product  from
chlorlnatlon  of  phenol  tends to  have comparatively nontoxlc,  higher  chlori-
nated Isomers.   This process Is  conducted at atmospheric pressure  using two
reactors.   In  the  first,   phenol  1s  chlorinated  at  65-130°C  until  3-4
chlorines  have  been  added  and until the mp  of  the  product  has reached 95°C.
The  temperature  Is  then  adjusted  slowly Into the  195-205°C  range,  a  process
typically  complete  1n  5-15  hours.  Aluminum  chloride  Is  often  added  to
accelerate the  final chlorlnatlon.  Typically,  the  final  product consists of
80-88% PCP and 12-20% 2,3,4,6-tetrachlorophenol  1n addition to hydroxypoly-
chlorlnated  dlphenyl  ethers,  PCDDs,  PCDFs,  chlorodloxlns   (1000-3000 ppm),
1928A                               4-8                              06/23/86

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1928A
4-9
06/20/86

-------
chlorofurans  (200-600  ppm)  and  chlorinated  dlphenyl   ethers  (Firestone,
1977a).  Poor temperature control 1n this final  phase  has  been  postulated to
account for the formation of PCDFs  (and  PCDDs)  from  the  chlorinated dlphenyl
ethers (Firestone et  al.,  1973).   The  length of time  that  chlorlnatlon con-
tinues undoubtedly has some Influence, since  refluxlng of  PCP  In  benzene for
6 hours with chlorine bubbling can produce OCDF  1n  52% yield (Pllmmer,  1973).
    Commercial  sodium 2,4,5-trlchlorophenolate   tends  to contain more  PCDDs
and PCDFs  than  the  chlorophenol  Itself   (Firestone  et  al., 1972).  Most  of
the  PCDFs   possessed  3-6  chlorine  atoms.   While  2,3,4,6-tetrachlorophenol
formulations did contain TCDFs to OCDFs  (see  Table 4-4), no PCDFs or chloro-
ethers were found 1n samples of 2,4- or 2,6-dlchlorophenol.
    Levin  and  Nllsson  (1977)  reported   that  Swedish  sawmill  workers  were
exposed  to  PCDFs   (levels  up  to  6   ppm)  1n  Finnish  2,3,4,6-tetrachloro-
phenolate In the sawdust.
    PCP has  been  detected  1n  urban air  (at concentrations  of  0.25-0.93 and
5.7-7.8  ng/m3),   In   waters   from  various  manufacturing  and   processing
plants,  1n   sewage-plant   effluent  (1-5  vg/it)   In   rain,  snow  and  lake
waters (2284, 14  and 10  ng/9.),  1n  creek water  containing  Industrial  wastes
(at  levels  of  0.1-10  mg/l);  soil  residues  after  application  of 15  and  45
kg/ha  PCP  were  20.4 and  69.1  mg/kg (WHO, 1979).  Trlchlorophenol  (unspeci-
fied  Homers)  has  been   Identified  In  river  water, tap  water  (2.4  mg/i),
landfill leachate  (40 mg/8.),  and  In   effluent  from  sewage  treatment  plants
(WHO,  1979).  Other  contaminants  such  as  PCDDs  and  polychlorlnated  dlphenyl-
ethers have been  Identified  In  technical  grade PCP  (Rappe et  al.,  1978a,
1979a; Nllsson and Renberg, 1974; Buser,  1975).
4.2.2.   PCDFs  In  Polychlorlnated  Blphenyls.   PCBs  are  mixtures  of chlori-
nated  blphenyls widely used 1n a number  of  Industrial  applications,  such as
1928A                               4-10                             06/23/86

-------
heat  exchange,  dielectric fluids, hydraulic and  lubricating  fluids,  plastl-
dzers,  printing  Inks and  flame retardants (WHO,  1976).   Large  amounts  of
PCBs  have been  released  Into  the  environment since  1929.   Because  of  the
stability of  some  Isomers to chemical and  biological  attack,  they are today
ubiquitous and persistent pollutants of ecosystems (Wassermann et al., 1979).
    The  presence  of  PCDFs  In PCBs  has  been  detected  by  several  authors  1n
American, European  and Japanese commercial PCB mixtures  (Vos et  al.,  1970;
Nagayama  et   al.,  1976;   Roach  and Pomerantz,  1974;  Bowes  et  al.,  1975a).
Because  of  production differences  the  PCDF concentrations and  Isomers  vary
with  PCB  type and origin.   Bowes  et  al.  (1975b)  found  levels  of  0.8  and  2
ppm 1n American-made  Aroclor  260  and  1248,  respectively; 8.4  and 13.6 ppm of
PCDF  were  estimated  In   German Clophen   A-60  and  French  Phenoclor  DP-6
(Nlsbet,  1976).  In  the  late 1960s, a significant difference  1n toxlclty  to
chick  embryos was  discovered among  three  supposedly  Identical  PCB formula-
tions  originating  from  three  different  countries  {Vos and  Koeman,  1970).
Large  amounts of  comparatively  more  polar contaminants were  detected 1n  a
German PCB  (Clophen A-60) and  a  French  PCB (Phenoclor  DP-6)  but  not  1n  an
American  PCB  (Aroclor  1260).  Two of  the contaminants  1n the  German PCB were
Identified by GC/MS as a TCDF  and a PeCDF (Vos  et al.,  1970);  these com-
pounds apparently accounted for  the observed acute toxlclty of  the whole  PCB
formulation.   PCDFs  were  found  also  1n American  PCBs  but  not as  much  as  In
the European  formulations  (Bowes  et  al.,  1973).   Kanechlors from  Japan were
also  found  to  contain  PCDFs  (Bowes  et  al.,  1975a;  Roach  and  Pomerantz,
1974).  The  average PCDF  content  1n  Aroclors  1248, 1254  and 1260 from  the
United States was  then put between 1  and  2 ppm.   Less  than ppt  levels were
detected  In   Aroclor  1016 (Bowes  et  al.,  1975a,b).  The 2,3,7,8-TCDF and
2,3,4,7,8-PeCDF  were  detected  1n Aroclors   1248 and  1254,  and In  Kanechlors


1928A                               4-11                             06/23/86

-------
200 and  500 (Bowes et  al.,  1975a,b); Clophen A-60  contained ~8 ppm  PCDFs,
and  Phenoclor   DP-6  contained  -14  ppm.   The  PCBs   with  the  highest  PCDF
contents were toxic to chick  embryos.
    In 1968, some 1200  Japanese people consumed a  rice  oil  (Kaneml)  contami-
nated with  800-1000 ppm of a Japanese PCB formulation,  Kanechlor 400,  which
had leaked  from a heat  exchanger  (Nagayama et al., 1975).   This  caused Yusho
disease.   Several  months  before  this  Incident,  0.50  million  chicks  were
killed  by  a  crude  bran oil  from  the   same  origin  but   the  warning  went
unheeded   (Kohanawa  et  al.,  1969).   The  composition of   Kanechlor  400
resembled  that  of  Aroclor  1248.   Of the  GC peaks  assigned  to PCDFs  six made
up  2  ppm  of  the  PCB.   However,   reports  of  the  total  PCDF  content  varied
greatly  from Investigator to  Investigator.  For example, Roach  and  Pomerantz
(1974)  detected  1  ppm,  Nagayama  et  al.   (1975)  18 ppm and  Kuratsune  et  al.
(1976) reported 33 ppm.  These values were obtained  on  packed GC columns and
so  are  expected  to be maximal figures.    Later capHlary-GC work confirmed a
level  of  2-5  ppm  (Nagayama   et  al., 1977;  Rappe et  al.,  1977), the  major
PCDFs being the  toxic  2,3,7,8-TCDF  (0.45 ppm) and the  2,3,4,7,8-PeCDF  (-0.2
ppm).   It  was  calculated that the contaminating Kanechlor  400  PCB  contained
a  PCDF  level  250 times greater than  the  value found  for an unused  Kanechlor
400 formulation  (Nagayama  et al., 1975).   A 4-fold  Increase  of  PCDFs  (15-20
ppm)  occurred when a  PCB was used for 2  years  1n a heat exchanger 1n a situ-
ation  similar  to the  suspected source  of rice oil  contamination  (Morlta et
al.,  1977a).   More  than 40 Isomers  were  found; of those found,  the  2,3,7,8-
TCDF  was the most abundant  (1.25 ppm).   Later  work  (Mazer et  al.,  1983a,b;
Rappe  et  al.,  1984)  showed  that the 2,3,4,8-TCDF  co-eluted.  The chroma-
tographlc  profile  of  the  TCDF  fraction  was very  similar  to that of  Kaneml
 1928A                               4-12                             06/23/86

-------
oil (Buser  et  al.,  1978d; Rappe et al.,  1977).   A summary of the  levels  of
PCDFs  In various PCB formulations and  1n Kaneml  oil 1s given In Table 4-6.
    Table 4-7  gives  the suspected maximum  levels  of the  toxic  2,3,7,8-TCDF
and  2,3,4,7,8-PeCDF   In  these  formulations  (Morlta  et   al.,  1977a).   The
levels of  the  2,3,7,8-derlvatlves were  Identified  by retention  time  of  the
pure standard  and were  subsequently  confirmed by  Buser et al.  (1978d) using
the GC/MS.   If  the same  order  of  elutlon  Is  followed   on  the GC  columns
utilized  by these workers,  probably  peaks  6-10  and 13-19  of Buser  et  al.
(1978d) correspond  to peaks  2 and 3, respectively,  of  Morlta  et al. (1977a)
(Figure  4-1).   Similarly, peaks  23-33,  37-40,  44-47,  51-52, 53-56,  58-66,
68-70,  71-73,  77-78 and  85  denoted  by  Buser  et  al.  (1978d), correspond  to
peaks 3,  5, 6, 9,  10,  11, 12,  14,  16 and 17 of Morlta et al. (1977a).   The
2,3,7,8-TCDF-der1vat1ve,  therefore,  constitutes >90%  of  peak 6  as observed
by Morlta  et  al.  (1977a), accounting for the  near equivalence of the levels
of the  2,3,7,8-TCDF  found 1n Kaneml  oil by both  sets  of  workers.   Later  It
was found  that the 2,3,4,8-TCDF  co-eluted  (Mazer  et al.,  1983a,b; Rappe et
al., 1984).  The actual  level of  the  2,3,4,7,8-PeCDF Is probably -70% of the
levels  quoted  1n  Table  4-7,  since peak  68 of Buser  et  al. (1978d)  1s 70% of
the  combined  height  of  peaks  68, 69  and  70  corresponding  to peak 12  of
Morlta  et  al.  (1977a).   The  figures   quoted  1n  Table   4-7  are  therefore
unlikely to have an error  >30%  provided that the elutlon  profiles on the two
GC columns  are comparable.  Thus, these two toxic  Isomers  may  have made up
between  5  and 34% of  the total PCOFs  1n the PCBs.  The  low  values for the
Aroclors  T-1242 and  T-1260  are  to  be  noted.  The  low toxldty  of Aroclor
1260  can  thus be  correlated  with  the  low level  of toxic  CDBF   (Vos  and
Koeman, 1970).
1928A                               4-13                             06/24/86

-------
10
CO
3>
             TABLE  4-6


Content  in  Some PCBs and  1n  Kanemi  Oil3
o

\
r\>

•«^
00
PCDF Content (ppm)
Substrate
Yu-Cheng oil5 (3)
Kanpmi oilb (4) (Yusho)
Unused Kanechlor 400
Used Kanechlor 400b (3)
Kanemi oil (Yusho)
Kanemi oil (Yusho)
Used Japanese
PCB (Mltsublshl-
Monsanto T-1248)
Kanemi oil
Kanechlor 300
Kanechlor 300
Kanechlor 400
Kanechlor 400
Kanechlor 400
Kanechlor 500
Kanechlor 500
Kanechlor 600
Kanechlor 600
Phenoclor DP-4
Phenoclor DP-5
Trl- Tetra- Penta- Hexa-

0.15 1.4 2.5 1.6
-
4.2 4.5 5.5 1.4
0.02 0.52 1.3 0.81
6.7 1.6
1.3
0.3 12.2 10.4 0.9
-
1 .
0.2 1.7 1.1 3.1
..
0.2 0.5 0.4
-
1.7 1.6 0.5
4.6 2.7 2.6
Total
0.14-0.18
2-7
33
20-510
5.7
5.0
16
2.7
8.3
1.3
24
18
--
6.1
3.3
1.1
4.0
3.8
9.9
Reference
Mlyata et al., 1985
Mlyata et al.. 1985
Mlyata et al.. 1985
Mlyata et al.. 1985
Buser et al., 1978d
Nagayama et al . , 1976
Buser et al., 1978d
Morlta et al., \977a
Morlta et al., 1977a
Nagayama et al . , 1976
Morita et al., 1977a
Nagayama et al . , 1976
Roach and Pomerantz,
1974
Morlta et al., 1977a
Nagayama et al . , 1976
Morlta et al., 1977a
Nagayama et al . , 1976
Morlta et al., 1977a
Morlta et al., 1977a

-------
VO
ro
CO
3>
                                              TABLE  4-6  (cont.)
o
cr
no
CO
GO
PCDF Content (ppm)
Substrate
Phenoclor DP-6
Phenoclor DP-6
Aroclor
Aroclor
Aroclor
Aroclor
Aroclor
Aroclor
Aroclor
Aroclor
Aroclor
Aroclor
Aroclor
Clophen
Clophen
Clophen
Clophen
aNo data
T-1200
T-1241
T-1242
T-1248
T-1248C
T-1254
T-1254
T-1254
T-1260
T-1260
T-1264
A-30
A-40
A-50
A-60
found for hepta-
Trl- Tetra-
0.2 2
0
0
2
2
0
0.3 5
0
0
0
0
0
4
1.6 2
1.5 5
0.7 8
1

.1
.7
.1
.4
.3
.5
.8
.1
.2
.1
.2
.8
.8
.3
.4
.3
.4

Penta-
2.6
10
0.4
2.7
2.3
2.3
5.6
0.2
0.4
3.6
0.3
0.9
9.4
1.0
6.9
4.1
5.0

Hexa-
5
2
0
0

.6
.9
.5
.8
-
Total
11
14
1
5
4


.0
.9
.5
2.8
0
1
0
1
0
0
2


1
2

.7
.4
.9
.9
.3
.5
.0
•-
--
.8
.2

12
1
1
5
0
2
16
4
14
15
8


.7
.5
.6
.8
.2

.9


.4

Morlta
Bowes
Bowes
Morlta
MorUa
Morlta
MorUa
Bowes
Bowes
MorUa
Bowes
Morlta
Morlta
MorUa
MorUa
MorUa
Bowes

Reference
et al.,
et al..
et al.,
et al.,
et al.
et al.
et al.
et al.,
et al.,
et al.
et al.,
et al.
et al.
et al.
et al.
et al.
et al.,

, 1977a
1975a,b
1975a,b
, 1977a
, 1977a
. 1977a
, 1977a
1975a,b
1975a,b
, 1977a
1975a,b
, 1977a
, 1977a
, 1977a
, 1977a
, 1977a
1975a,b

bYu-Cheng  oil  also  contained  22-113  ppm  PCBs,  9-38  ppm PCQs.   Kaneml  oil  also contained  151-968 ppm
 PCBs, 490-866 ppm PCQs.  Kanechlor 400  also contained 999,800 ppm PCBs, 209 ppm PCQs.  Used Kanechlor 400
 also contained 961,900-999,000 ppm PCBs, 690-31,000 ppm PCQs.

cUsed PCB

-------
                                  TABLE 4-7

  Suspected Maximum Levels of Toxic PCDFs  1n Various PCBs and  In Kaneml 011
          (Kaneml  oil  also contained 900 ppm PCBs  and 800 ppm PCQs;a
     Taiwan rice oil also contained 60-100 ppm PCBs  and  90-180 ppm  PCQs)
Formulation
                     PCDF  Levels  (ppm)
2,3,7,8-b'c    2,3,4,7,8-b'd
   TCOF           PeCDF
Total
Percentages of
  Total PCDFs
 for These Two
  Derivatives
Taiwan rice
oil (2)a
Kaneml oil3
Kaneml o11b
Phenoclor3
DP -4
DP-5
DP-6
Kanechlorb
KC-300
KC -400
KC-500
KC-600
Aroclorb
T-1241
T-1242
T-1248
T-12486
T-1254
T-1260
T-1264
0.001-0.005

0.2
0.28

0.7
2.2
0.9

2.2
1.6
0.7
0.1

1.1
0.2
0.2
1.1
--
-_
2.4
0.02-0.70

0.7
0.42

0.4
0.8
0.6

0.6
0.9
0.7
0.1

0.4
0.1
0.8
1.4
1.6
0.1
2.3
0.08-0.10

2.02
2.68

3.8
9.9
10.5

8.3
23.8
6.1
1.1

5.9
4.5
2.8
12
5.6
2.2
16
20-25

45
26

29
30
14

34
11
23
18

25
7
36
20
29
5
29
1928A
                    4-16
                   06/20/86

-------
                              TABLE 4-7 (cont.)
PCDF Levels (pom)

Formulation

Clophenb
A-30
A -40
A-50

2,3,7,8-b'c
TCDF

1.0
2.1
3.6

2,3,4,7,8-M
PeCDF

0.1
0.7
0.6

Total


4.9
14
15
Percentages of
Total PCDFs
for These Two
Derivatives

22
20
28
aMasuda et al., 1982
Calculated from MorHa et al.,  1977a
cBased on  GC  retention  time,  but  subsequently  confirmed by  Buser  et al.,
 1978d
^Assumed the  order  of  elutlon obtained by  Buser  et  al.,  1978d, Is followed
 on the GC column utilized
eUsed PCB
 -- Below detection limit
1928A
4-17
06/20/86

-------
                                              I 17
                                              V f
                                              \ I1,
    B
                                  FIGURE  4-1
                 Comparison of Specific  Ion Current Profiles
                      after  Chromatography of  Kaneml  011
         Source:   (A)  Morlta et  al.  (1977a);  (B)  Buser et al.  (1978d)
1928A
4-18
06/20/86

-------
    A  similar  Incident  occurred  1n  Taiwan  1n  1978  affecting  nearly  2000
people.  This  has been  dubbed the  "Yu-Cheng" episode  (Chen  et al.,  1981;
Kashlmoto et al.,  1981).  The total  PCDF  content Is provided In Table 4-6,
the congener concentrations  still not  being available.   The  concentrations
of  the  toxic  2,3,7,8-TCDF and  the  2,3,4,7,8-PeCOF  are given  1n Table 4-7.
Masuda et al.  (1982)  also found  0.01-0.02 ppm of  the  2,3,4,6,7-PeCDF,  -0.01
ppm HxCDF  and  0.04-0.05  ppm  of  an unidentified  TCDF.   The PCDF Isomers  1n
the  rice oils  exposing  people   1n  both  Yusho  and Yu-Cheng  episodes  were
Identical but the concentration 1n the  Taiwan  rice oil  was at  most  5X of the
Japanese concentration.  Rappe et al. (1983)  detected  PCDF at  levels  of 1-18
ppm In  Kanechlor  mixtures 300-600.   More  recently,  using a complete  set  of
PCDF standards  and an  Isomer-speclflc analytical method,  Rappe et al.  (1984)
reported on  levels  of  2,3,7,8-substHuted PCDF  congeners  found 1n a  large
number of commercial  PCB products  (Table 4-8).
    Concentrations of  PCDFs  1n   PCBs  are  Indicative  1n  some  cases  of  the
original concentrations  of PCDFs.  However,  Buser  et al.  (1978a) demonstrat-
ed  that  after  2  years  of using M1tsub1sh1-Honsanto  PCB as a heat exchanger,
a  4-fold Increase  1n  PCDF  concentration  occurred,  the  toxic  2,3,7,8-TCDF
being the major component.
4.2.3.   PCDFs  1n  Phenoxy Herbicides.   Phenoxy  herbicides  are  widely  used
for the  control  of wood and herbaceous  weeds by  spraying  from the air  or
from  the ground.   They  reach aquatic  systems   directly when  applied  for
macrophyte  control  1n   lakes, ponds  and  Irrigation  ditches  or  Indirectly
during application near  water, or through  runoff,  reaching concentrations  as
high  as  1-3 mg/l of  water (CNRC,  1978a).  A 50:50 mixture of the  n-butyl
esters  of  2,4-D  and  2,4,5-T  (Agent Orange)  was  used   for military purposes
(defoliation or crop destruction) 1n South Vietnam (NAS,  1974).  The  phenoxy


1928A                               4-19                            06/23/86

-------
CO
                                                                            TABLE 4-8


                                                                PCDFs In Comnerclal PCBs (ng/g)*
PCB-typ
Pyralene
A1254
^ A1260
g A30
A40
A50
A60
T64
Clophen C
Blank
Blank
Trl-
Total
700
63
10
500
1300
7400
770
47
710
ND
ND
Tetra-
2378
53
19
13
35
180
3300
840
23
54
ND
ND
Total
630
1.400
110
573
2.600
20,000
6,900
360
1,200
ND
ND
12348
12378
10
690
48
14
96
760
1100
97
34
ND
ND
Penta-
23478
T
490
56
28
8
1100
990
122
30
ND
ND

Total
35
4000
260
160
1700
8000
8100
840
270
ND
ND

123479
123478
ND
2500
500
50
79
700
1600
520
Nd
ND
ND

123678
ND
2100
120
59
68
360
330
390
T
ND
ND
Hexa-
123789
ND
190
190
ND
ND
18
170
58
ND
ND
ND
Heota-
234678
ND
130
27
ND
T
98
330
41
ND
ND
ND
Total
ND
10.000
1.500
220
310
3.100
6.800
2,600
T
ND
ND
Total
ND
960
1300
T
ND
75
2000
220
ND
ND
ND
Rec 2378-
TCDD-X
79
78
88
79
79
95
95
72
79
90
87
         'Source:  Rappe  et-al.,  1984


         ND =  Not  detected
oo
er

-------
herbicides,  2,4-D,  2,4,5-T,  MCPA,  2-(2,4,5-tr1chlorophenoxy)prop1on1c  add
(Sllvex) and  2-(2,4-d1chlorophenoxy)prop1on1c  acid (Dlclorprop)  are  synthe-
sized by  condensing the appropriate  haloalkanolc  acid with  the  appropriate
chlorophenol, usually under alkaline  conditions during  reflux.  Any  PCDD and
PCDF  Impurities  remain  1n  the product  unless the  latter  Is  purified.   In
addition,  since  PCDOs  and  PCDFs  are  formed  from  chlorophenols under  hot
alkaline conditions,  these  contaminants may also  be  formed  1n the  presence
of excess chlorophenol.
    Most attention has been accorded  to  the  content  of  2,3,7,8-TCDD  1n these
formulations, but PCDFs  have  also  been detected 1n these  products  (Rappe et
al.,  1978c;  Hucklns  et al.,  1978;   Ahllng  et al.,  1977).  The analytical
techniques,  however,  were  not refined  enough to  permit   Identification  of
specific  Isomers.   This  has   now  been  accomplished  (Rappe  et  al.,  1978c;
Cochrane et  al.,  1983).  The  major  PCDDs  present  In 2,4-D are the  compara-
tively nontoxlc 2,7-DCDD-,  1,3,7-TrCDD-, 1,3,4,8-TCDD and 1,3,6,8-TCDD.
    Various  2,4,5-T  formulations  of  European  origin  1n the  1960s  contained
2,3,7,8-TCDD  at  levels  ranging  from  0.1-1  vg/g  as  the  predominant  PCDD
(Table 4-9).  Two samples  showing  the presence of TCDFs did  not  contain the
2,3,7,8-TCDD.  In the  Agent  Orange  samples,  the major  PCDD was the  2,3,7,8-
TCDD  (0.12-5.1  v9/g  levels).   Only  one  sample contained  PCDFs; they  were
one  tr1-,  four  tetra- and  one  penta-CDFs  at  a  total level  of 0.7  yg/g.
The 2,3,7,8-TCDF was not present.  All  samples, however, showed the  presence
of  chlorinated  dlphenyl  ethers,  which are  known  precursors  of  PCDFs  In
pyrolytlc  reactions.   The  chlorinated  dlphenyl ether  content  may range  as
high  as  1%  (Rappe  et al.,  1978c).   The  PCDFs  may  be  formed  from a  metal
Ion-promoted condensation of  two 2,4,6-trlchlorophenolate  Ions, by a  mechan-
ism  similar  to  the  palladium  (II)  acetate  synthetic   method discussed


1928A                               4-21                             06/23/86

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vO
rsj
CD
                                                                                TABLE 4-9


                                                                  PCDFs and PCDDs In Phenoxy Herbicides
                                                                       PCDf/PCOD Amounts (mq/kq)
       Phenoxy
      Herbicide
                           D1-
                 Trl-
                                                      Tetra-
                                                                     Penta-
                                                                                     Hexa-
                                                                                                     Hepta-
                                                                                                 Octa-
                                                                                                                   Total
CDF    CDD    CDF    CDD    CDF      CDD    CDF       CDD     CDF      COD      CDF       CDD       CDF       CDD       CDF
                                                                                                                                               CDD
                                                                                                                                 Reference
      2.4.5-T  Esters


        Butyl


        Isooctyl


        Butoxyethyl


        Butoxyethyl


      Agent  Orange
                     0.01     -     0.95


                            0.15   0.18
         0.96


0.15     0.18


0.11     0.22
        a      a      a     0.13   0.018   0.008   0.007   <0.005   <0.0   <0.005   <0.005   <0.005   <0.005   <0.153   <0.40


       0.15    -     0.02          0.12      -        -         -         -      a        a        a        a         -       0.29


       0.15   0.10   0.50   0.40   1.1     0.20    0.05       -         -      a        a        a        a       0.70     1.80


                     0.02    -5.1--         -         -a        a        a        a         -       5.12
     a = Not analyzed for;  - = Below  detection limit


     1 = Rappe et al., 1978c


     2 = Ahllng et al.. 1977
o
*v
00

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previously.  In  fact,  H Is known  that  the chlorinated dlphenyl  ethers  and
PCDFs  are  formed  at  the  beginning  of  the  reaction  before most  of  the
1,2,4,5-tetrachlorobenzene  reacts,  which  Is  used as  starting material  for
the preparation  of  2,4,5-tMchlorophenol  1n the  European  manufacturing pro-
cess;  PCDDs  tend to be  formed  near the end  of  the process  when  2,4,5-tM-
chlorophenolate  formation  1s favored  (Rappe,  1978;  Adamoll  et al.,  1978).
The  synthesis  of  PCDFs  from  chlorobenzenes  Is  also  discussed   In  Section
2.5.2.2.
    The concentration of the 2,3,7,8-TCDD 1n  technical  2,4,5-T used 1n Agent
Orange  manufactured  between 1958  and 1969  ranged  from  1-32 ppm  (Young  et
al.,  1978).   Levels In  Agent  Purple  (n-butyl  2,4-D:  n-butyl  2,4,5-T:  1so-
butyl  2,4,5-T::  5:3:2)  formulated  1n the mid-1950s  appear  to be  even higher
than  those  In  Agent  Orange.  Levels of 2,3,7,8-TCDD In the technical 2,4,5-T
used  for  Its  formulation have  been  estimated  to  be  as  high as 90  ppm (Young
et al., 1978).   Other herbicides containing  2,4,5-T used In Vietnam, namely,
Agent  Pink (n-butyl  2,4,5-T/1sobutyl  2,4,5-T::  3:2),  Agent  Green (n-butyl
ester  of  2,4,5-T),  Dlnoxol  (1:1 butoxyethanol esters  of  2,4,5-T  and 2,4-D),
and  TMnoxol   (40% butoxyethanol  ester of  2,4,5-T),  have  never been Inten-
sively  studied for  their  PCDD or  PCDF  contents.   However,  only minor amounts
of  PCDF and of  other PCDD  1n  relation to the major  contaminant  TCDD, could
be  found  1n these herbicides.   In  >450 samples  analyzed,  TCDD had the mean
value  of  1.98 vg/g  (Young et  al., 1975,  1983).   As  a   result  of govern-
mental  regulation,  efforts have  been made  to  minimize  the formation  of
2,3,7,8-TCDD and now the products are estimated to contain  <0.1 vg/g.
4.2.4.    PCDFs  In  Chlorodlphenyl   Ether  Herbicides  (PCDPE).  Yamag1sh1  et
al.  (1981) reported  on  the occurrence  of  PCDD  and PCDF  1n the   commercial
dlphenyl  ether  herbicides  CNP, NIP and  X-52.   The  levels  of  the various
Isomers are reported In Table 4-10.

1928A                               4-23                             06/23/86

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                                 TABLE  4-10



      Levels  of  PCDDs  and  PCDFs  1n  Commercial  Dlphenyl  Ether Herbicides*

TrCDDs
TCDDs
PeCDDs
HxCDDs
MCDFs
DCDFs
TrCOFs
TCDFs
PeCDFs
HxCOFs
CNP
ND
14.00
37.00
0.80
ND
0.35
0.41
0.40
1.00
0.20
NIP
0.15
0.38
0.05
ND
0.34
0.12
0.47
0.29
ND
ND
X-52
0.03
0.03
0.01
ND
0.48
0.21
0.45
0.32
0.08
ND
*Source: Yamaglshl et al.,  1981



ND = Not detected
1928A                               4-24                             06/20/86

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4.2.5.   PCDFs In Hexachlorobenzene.  Hexachlorobenzene  Is  a contaminant 1n
the  production  of many  chemicals,  such  as tetrachloroethylene,  trlchloro-
ethylene,  carbon  tetrachlorlde,  chlorine,  vinyl  chloride,  dlmethyltetra-
chloroterephthalate,    Atrazlne®,    S1maz1ne®,   pentachloronltrobenzene   and
Mlrex®.  Hexachlorobenzene  Is  also  used as  an  economic poison for  the  con-
trol  of  wheat bunt and  fungi.   As  an environmental contaminant  1t  has  been
found  In  river  water  samples,  drinking  water,   sewage  treatment  plants,
effluent waters from various chemical plants, urban  rain water  runoff (up to
339  ng/a)  and  surface waters  (2.5  mg/a)  (WHO,  1979).   Vlllaneuva et  al.
(1974),  analyzing  three  commercial  hexachlorobenzene preparations,  Identi-
fied  OCDD, HpCDF and OCDF.   This  last compound  was  present  1n concentrations
ranging  from  0.35-58.3 ppm.  These  data  suggest that PCDFs  may also be found
1n association with hexachlorobenzene.
4.2.6.   PCDFs  1n Hexachlorophene.   The  bacterldde,  hexachlorophene,  1s
prepared commercially  from  2,4,5-tMchlorophenol  (Nllsson et al., 1978).  It
1s purified,  however,  during this process  and  levels of  2,3,7,8-TCDD are <30
vg/kg.    Nevertheless,   hexachlorophene   can  contain   100   ppm   of   the
1,2,4,6,8,9-hexachloroxanthene (Gothe and Wachtmelster, 1972).
4.2.7.   PCDFs  1n PBBs.   The  PBBs  gained  their  greatest  notoriety  as  a
result  of  a   severe contamination of  meat and dairy products  In  Michigan 1n
October,  1973  (Cordle  et  al.,  1978).   The  contaminant,   Flremaster  BP-6
manufactured  by  the  Michigan Chemical  Corporation,  contained 2% tetrabromo-
blphenyls,   10.6%  pentabromoblphenyls,   62.8%  hexabromoblphenyls,   13.8%
heptabromoblphenyls and  11.4% other  bromoblphenyls.   As  a  result  of error,
Flremaster BP-6  was  added  to  cattle feed  Instead  of magnesium  oxide.   The
levels  of  contamination  Included the following:  lot  405,  2.4  ppm;  lot  410,
1928A                               4-25                             06/23/86

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1790 ppm;  and lot 407,  4300 ppm.  Milk  from  affected herds contained  from
2.8-271 ppm  on  a fat basis.   Contaminated  butter (1-2 ppm), cheese  (1.3-15
ppm) and canned milk  (1.2-1.6 ppm) were later  seized  and destroyed.
    PBDFs were  found  In pyrolyzed PBBs  by  O'Keefe (1978b) and Buser  et  al.
(1978a).   PBDFs  were  not  found  1n  one  study on  unheated Flremaster  FF-1
(Hass et al.,  1978).   Hass  et al. (1978) concluded  that  the amount  of BDBFs
must be <0.5  ppm,  and  that  penta- and hexabromonaphthalenes were present  to
the extent of 150 and 70 ppm,  respectively.  A metabolite of  Flremaster BP-6
1n dogs, 6-hydroxy-2,2',4,4',5,5'-hexabromob1phenyl, decomposed at  230-260°C
on an  OV-101  column  1n  a  gas chromatograph to  form two PeBDFs  (Gardner  et
al., 1979).   Thus, PBDFs can be  formed from pyrolysls  on  GC columns  as well
as being originally  present  1n PBB formulations.  Such artifacts need to be
Investigated  before  PBDF  contamination  of  PBB  formulations  Is  considered
confirmed.
4.2.8.   PCDFs  1n  Metal Salts.   Salts of  metals often  used  1n  Industrial
processes may contain  PCDFs and  PCDDs  (Helndl and  Hutzlnger, 1986).   Table
4-11  shows  that  the  chlorides  of Iron,  aluminum and  copper contain between
0.02 and 60 ppb PCDFs and 0.02-0.63 ppt PCDDS,  both mostly as OCDF and HpCDF.
4.3.   PHOTOCHEMICAL  PRODUCTION
    Another  potential   source  of PCDFs  derives  from the  photodegradatlon
reactions  of  a number   of chemicals  present 1n  the  ecosystem  as  pollutants.
Perhaps  the  most Important  potential  source  of  environmental  contamination
Is  the  photochemical   production  of  PCDF  from  PCBs.    Hutzlnger  (1972)
observed 0.2% 2-PCDF production  after  7  days  of ultraviolet Irradiation (310
nm) of  aqueous  solutions of 2,5,2'5'-tetrachloro- and 2,5-d1chloro-b1phenyls
(5  mg/l).   These  products  were  confirmed  by  Crosby and Mollanen  (1973)
(see   Section  2.4.2.   for   more  details  of  laboratory  photochemistry).


1928A                               4-26                             06/23/86

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                                  TABLE  4-11

                   PCDFs and PCDDs In Several Metal Salts*
                                    (ppb)
Salt
FeCl3
A1C13 (A)
A1C13 (B)
CuCl2
CuCl
T1C14
S1C14
OCDF
42
<0.02
34
0.5
0.2
<0.02
<0.02
HpCDF
12
<0.02
0.1
0.1
0.08
<0.02
<0.02
OCDD
<0.02
<0.02
<0.02
0.6
0.03
<0.02
<0.02
HpCDD
<0.02
<0.02
<0.02
0.03
<0.02
<0.02
<0.02
*Source: Helndl and Hutzlnger,  1986
1928A                               4-27                             06/23/86

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However, Hutzlnger (1972) found no PCDFs after  some  aqueous  PCB samples (167
mg/l)  had  been  exposed to  sunlight for  >2 months.   This  discrepancy  may
have  arisen  because  of  the  different  Irradiation  times  and  different
wavelengths  used.    The yield  of  the   products  was  wavelength  dependent.
Irradiation at  254  nm  (mercury arc)  decomposed PCDF photoproducts  but only
slowly  at  310  nm   or   at  the  wavelengths  encountered  at  sea  level  for
sunlight,  or   for  a  solar  simulator.   Triplet  sensltlzers   (for  example,
4,4'-dichlorobenzophenone)   Induced   faster   decomposition   as   observed  In
methanollc solution alone for  the  photodecomposltlon  of  2,8-DCDF  (Crosby and
Mollanen, 1973).  Thus,  the presence of  other compounds  may  be Important.
    After  ultraviolet  Irradiation  of   some chlorophenols,  Crosby  et  al.
(1973)  detected OCDD  but  PCDFs   were  not  sought.   Chlorinated  o-phenoxy-
phenols  (predloxlns), which are  common  Impurities   In  chlorophenols  (1-5%),
also produce  PCDDs after ultraviolet Irradiation (NHsson et al.,  1974) but
again  PCDFs were not sought  specifically.   Another  source of  PCDFs  through
photodecomposltlon Is from  PCDPEs,  which are often present  at  levels  of 100
ppm  In  commercial   chlorophenols.   Irradiation  of  100  ppm  solutlos  In
methanol, ethanol or n-hexane  with  light of  248-579  nm  caused cycllzatlon In
dlphenyl  ethers  containing at  least one ortho-chlorine.  Reductive dehalo-
genatlon was  enhanced  In hexane.   Although  no  yields were explicitly  given,
the  degradation  was  characterized by an  Induction  period and  then  decompo-
sition,  obeying a first-order kinetic   law  (Norstrom  et  al.,  1976a,  1977;
Choudhry  et   al.,  1977a,b).   Photodegradatlon  of polychlorobenzenes   (PCBZ)
can  also  be  a  source of PCDF production.    Laboratory  Irradiation  at  x >285
nm  of  a  solution of   PCBZ  In the  presence of  phenol  yielded  PCDF  (<1%)
containing two  Cl atoms  less  than  the starting  PCBZ.  This  reaction probably
1928A                               4-28                             06/23/86

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proceeds  through  the  Intermedlacy  of PCDPE  (Choudhry et  al.,  1983).   The
relevance  of  these  laboratory  photodecomposHlons  to environmental  sources
of PCDFs Is unknown.
    Another photochemical  process of  potential  environmental Importance  1s
dechlorlnatlon  of  the higher  PCDFs.   This  topic   will  be  considered  1n
Chapter 5.
4.4.   SOURCES OF PCDF FROM BURNING AND OTHER HIGH TEMPERATURE PROCESSES
    In 1978 Dow Chemical  scientists  proposed the  "Trace  chemistries  of fire"
hypothesis.   This  stated  that  many  contaminants  arise  In trace  amounts
during  chemical   reactions  during combustion.   PCDF  and  PCDD are  Included
among  these compounds.   To assess the relative Importance  of these  sources,
Sheffield  (1985a,b)  estimated  the  environmental  release  of PCDF  and  PCDD
from combustion  sources  1n Canada (Table 4-12) using the small  data base at
his disposal.
4.4.1.   Thermal  Degradation of  Technical   Products.  PCDFs  can  arise  from
pyrolysls  of  specific  PCBs, chlorinated  benzenes  and  chlorinated  dlphenyl
ethers,  and  PBDFs from the  analogous  bromlnated  precursors.   The occurrence
of  these compounds must be  taken  Into  consideration since they are released
Into  the environment with  their  co-contaminants  and  may  produce  PCDFs upon
Incineration.
    The  levels  of PCDFs 1n  PCBs  Increase  with the length of time 1n  service
at  high temperatures as heat exchange media (Morlta et  al., 1977b;  Buser et
al., 1978d),  as  originally suggested by Kuratsune et al. (1976).  A contrary
finding  has been  reported by Cull and Dobbs  (1984).   Aroclor 1254 on  pyroly-
sls  also  contained  the  major  toxic  PCDFs,  but the  relative amounts  of the
products differed somewhat  from  those  obtained from  the Mitsubishi-Monsanto
T-1248  (Buser  and  Rappe,  1979).   The  major PCDFs  Identified  In  the used


1928A                                4-29                             06/23/86

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                                 TABLE 4-12

         Estimated  PCOD and  PCDF  Releases  to  the Canadian  Environment
                          from Combustion Sources3
             Sources
                                                   Release  (q/year)
                                                PCDD
                                PCDF
Municipal Incinerator
  Fly ash
  A1r emission

Sewage sludge Incineration
  A1r emission

Coal-fired utility boilers
  Fly ash
  Air emission

Fuelwood combustion
  A1r emission

Residential oil combustion
  A1r emission

Residential gas combustion
 Source: Sheffield, 1985a,b
bPCDD + PCDF release
ND = Not detectable
                                            2900-7100
                                             250-13,700
                                            1400-3300
                                            ND-300
                                            300
                                            1800
                            4900-15,600
                             550-21,700
                            1500-6500
                              30-1300
                             700
                            not estimated


                            not estimated
Air emission
Wigwam burners/Wood waste boilers
Air emission
Railway ties
Air emission
Forest fires
Air emission
Slash burning
Air emission
Cigarette smoke
Air emission
Motor vehicles
A1r emission
900
0-30, 200b
6000°
58,700
3300
2-4
200
not estimated


not estimated
not estimated
not estimated
not estimated
1928A
4-30
                                                                     06/23/86

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MHsublshl-Monsanto  T-1248  were the  2,3,7,8-TCDF  (1.25  ppm),  the 2.3,4,7,8-
PeCDF    (the   pyrolysls   product    of   2,4,5,2',4',5'-hexachloroblphenyl),
1,2,3,7,8-PeCDF,   2,3,4,6,8-PeCDF,   1,2,3,4,8-PeCDF,  1,3,4,7,8-PeCDF  (also
from  pyrolysls  of  2,4,5,2',4',5'-hexachlorob1phenyl)  and  the  2,3,4,6,7,8-
HxCDF.   The 2,3,4,8- and 2,3,7,8-TCDFs  were  later  shown  to co-elute (Mazer
et  al.,  1983a,b;  Rappe et al., 1984).   Whereas  the used MHsublshl-Monsanto
T-1248 was  exposed  for years  to  elevated temperatures  1n  the liquid phase,
the laboratory  pyrolyses  of  Aroclor  1254 and  1260 were  performed In the gas
phase  for  a  few  seconds up to  a  maximum  temperature  of  700°C  (Buser  and
Rappe,  1979).   WHh  Aroclor   1254   (tr1- to  hepta-PCBs),  mostly MCDFs  to
PeCDFs were formed  at  a  level of  -2%.   WHh Aroclor 1260  (penta-  to octa-
PCBs), mostly  TrCDFs to HpCDFs were  produced  at  a similar level.  The toxic
2,3,7,8-TCDF   was   the  most   abundant   TCOF,  most  likely  derived  from
2,4,5,2',4',5'-hexachlorob1phenyl   or  2,4,5,3',4'-pentachlorob1phenyl.   The
acutely  toxic  1,2,3,7,8- and  2,3,4,7,8-PeCDFs  were the  major PeCDFs.   The
former probably  Is  produced from pyrolysls  of  2,3,4,2',4',5'-hexachlorobl-
phenyl ,  and the latter from 2,4,5,2',4',5'-hexa- or 2,3,4,5,2',4',5'-hepta-
chloroblphenyl.   Pyrolyzed  Aroclor   1254 also contained  significant  amounts
of  1,3,4,7,9-PeCDF.    These  results  were  confirmed  by   Paaslvlrta  et  al.
(1985) who  also  found  small amounts  of chlorinated  phenols,  naphthalenes,
and MCDFs and DCDFs  (Table 4-13) produced between 500 and 700°C.
    The  polybromlnated blphenyl,  Flremaster  FF-1, when pyrolyzed  for  20
minutes  at  380-400°C 1n open  glass  tubes,  produced 40  ppm  TBDFs and 4  ppm
PeBDFs based on  PBB  content.  Only  trace amounts  (~1  ppm) were found 1f  the
pyrolysls was  redone  In  a  nitrogen atmosphere   (O'Keefe,  1978b).   It  was
postulated  that  since  2,4,5,2',4',5'-hexabromoblphenyl was  the  major  hexa-
bromoblphenyl present,  nearly  all of the tetrabromo-lsomer  was the  2,3,7,8-
Isomer.    The  larger  yield 1s  expected   from  the  weaker   ring  carbon-bromine

1928A                                4-31                              06/23/86

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rs>
CO
                                                      TABLE 4-13

                 Pyrolysls Products of Aroclor 1254 In a Quartz Tube for Pyrolysls Time of 3 Seconds*
                                    The Carbon Filter Adsorbed any Volatilized PCB
                                                [relative amounts (X)]
INJ
Pyrolysls Temperature
(X)

500
600
700
Filter

cii
0.1
0.3
0.01
52

C12
14
13
5.2
44
PCDF

"3
39
39
29
3.9

C14
40
36
49
ND

C15
7.4
11
15
ND

Cl6
ND
0.8
1.5
ND

"2
17
0.7
4.6
NA
PCDD

"3
10
18
14
NA

C14
73
57
66
NA

Cl5
ND
24
17
NA
     *Source: Paaslverta et al., 1985

     ND = Not detected

     NA = Not analysed
ro
o
CO

-------
bond  relative  to  that of  carbon-chlorine.  The  production  of  PBDFs  from
various PBBs In  sealed ampules  was also studied by  Buser  et  al.  (1978a)  and
has   been   discussed   In   Section  4.2.5.1.   The   10-mlnute   pyrolysls   of
2,4,6-trIbromophenol,   pentabromophenol,   tetrabromoblsphenol   A  and  tetra-
bromophthallc anhydride, all  used as  flame retardants, resulted  In  PBDD  and
PBDF  between 700  and  900°C,  except   for   the  anhydride   that  did  not  form
PBDFs/PBDDs  at   any  of  the  three  temperatures.   In  general,  the  optimum
temperature  to   form   PBDDs  and  PBDFs  was  at  800°C;  2,4,6-trlbromophenol
pyrolysls  produced  8950 ppm  TBDFs, pentabromophenol formed 7042  ppm HpBDFs
with  no detectable  amounts  of the other PBDF congeners.   Small  amounts  were
noted  at  900°C,  although  lower  congeners   did  appear at  700°C.   The tetra-
bromoblsphenol  A still  produced  relatively  high  PBDF concentrations  at 900°C
and PBDFs  predominated over PBDDs unlike  at  other  temperatures  and for  the
other  two  phenols when they were pyrolyzed.   The  absence  of any  PBDDs  or
PBDFs  from  pyrolysls  of the anhydride Indicates that  such compounds will  be
safer  flame retardants.
    Chlorophenolates burned  for  15 minutes on  birch leaves or wood wool  or
heated  at  280°C  for  30 minutes  (Table 4-14)  evolved PCDDs,  but  not  many
PCDFs  (Rappe et  al., 1978b).  Originally,  both  types of formulations studied
(Servarex  Teknlsk  and Kymmene   KY-5,  both  containing  5X 2,4,6-trl-,  50X
2,3,4,6-tetra- and 10% pentachlorophenols  as  the  sodium  salts)  contained  10
ppm each  of tetra-,  penta- and  octa-CDFs   and 70  ppm each of  the hexa- and
hepta-CDFs, with  40-50 Isomers  present  (see  Table 4-4).  The  burnt samples
produced only 10 Isomers and  levels were lower  than the original  levels  (see
Table  4-14).  Nevertheless,  the major TCDF  (unknown)   Increased  100-fold
during  burning   (from  0.04-5  ppm)  and two  others that  were  not  1n  the
original  formulation  were  detected.   The  2,3,7,8-lsomer was  a  very minor


1928A                               4-33                             06/20/86

-------
VD
ro
CD
                                                      TABLE 4-14


                              Levels of Trapped PCDFs and PCDDs on Charcoal from Burning
                                   Chlorophenolate-Impregnated  Leaves  and  Wood  Wool3
uQ PCDF
Commercial
Chlorophenol
£ 2,3,4,6-Tetra-
•*" (Servarex)
(Pure)
2,4,6-Trlchloro-
Pentachloro-
Substrate Tetra-
CDF COD
Birch leaves <10b 35
Wood wool <10b 96
<10b 30
Birch leaves — 2100
Birch leaves — 5
Penta-
CDF
<10b
<10b
<10b
—
—
COD
90
120
84
5
14
or PCDD/q Chlorophenate
Hexa-
CDF
<70b
<70b
<70b
--
—
COD
80
110
82
1
56
Hepta-
CDF
<70b
<70b
<70b
—
—
COD
8
65
8
3
172
Octa-
CDF COD
<10b 0.3
<10b 1.2
<10b 0.4
6
710
     aSource:  Rappe et al., 1978b


     bS1gn1f1es the amount In the original formulation
ro
O
\
CO

-------
component 1n the starting material  (0.1%  of  the total  PCDFs).   When the pure
phenols were  mlcropyrolyzed,  no  PCDFs  could be  detected.   Thus,  the  newly
formed  PCDFs  had  to  arise from  Impurities  1n  the technical  products  (for
example,  PCBs  or  probably PCDPEs)  (Llndahl et  al.,  1980).   K12  formula-
tions  were  particularly contaminated by  PCDF/PCDD contaminants, but KI  and
Ky-5  types  contained  lower  levels  (Paaslverta  et al.,  1982).   Polychlorl-
nated  phenoxyblpheny  dlols   and   polychlorlnated  phenoxyphenols  were  also
detected.   Ky-5  burnt  1n an  open fire  caused enhanced  levels  of  all  PCDDs/
PCDFs  1n  the  residual  ash and  1n smoke  vapor  with disappearance  of  PCDEs
from  the  Ky-5 formulation.   The  PCDDs probably  arose  from  the  polychlorl-
nated  phenoxyphenol and chlorophenol contaminants.
    Samples  of ash  from two  airtight  wood  burning  stoves,  one  open  fire-
place,  and  after  outside  open-air burning  and  from associated  chimney  ash
contained  traces   of PCDDs  and PCDFs  (total PCDD  or  PCDF  never  >15  ng/g).
PeCDFs  to  HpCDFs  dominated.   Unfortunately,  the  recovery of  1,2,3,4-TCDD
varied  between 15  and  80% and of OCDD  between  41 and  92%.   The past history
of the wood was not documented fully (Clement et  al.. 1985b).
    The  production  of  PCDDs and  PCDFs  from  the 2-butoxyethyl   ester  of
2,4,5-T was  studied  by pyrolyzlng the  ester  for  0.6-1  second when  the ester
(1 kg)  was  mixed  with  leaves or  sawmill  wood  chips (Ahllng et  al.,  1977).
The  PCDF  levels usually  exceeded PCDD  levels  (Table 4-15) but  not between
100  and  625°C,  even  though  PCDFs  were  more  concentrated In  the original
formulation  (which also contained  47  mg/g  2,4,5-T,  230 vg/g  of 2,4,5-tr1-
chlorophenol  and  12 wg/g  PCP 1n addition to  the  PCDFs and PCDDs  cited In
Table  4-15).   It was thought that  the  chlorophenols  could  not  be the source
of the PCDDs or PCDFs but  that a  complex mechanism  was Involved.
 1928A                               4-35                             06/23/86

-------
10
INJ
oo
 I
to
                                                                           TABLE  4-15


                                            Production of PCDDs and PCDFs after 0.6  to 1.00 Second  Pyrolysls  In  Air

                                                        of 2-Butoxyethyl-2,4f5-Tr1chlorophenoxyacetate*
PCDF/PCDD Amounts(mg/kq)
Temperature
CO
25
100
500
625
675
800
Tetra-
CDF
0.13
1.0
0.4
0.2
8.0
2.1
CDD
0.018
2.5
2.2
0.4
2.3
0.5
Penta-
CDF
0.008
0.5
1.5
<0.3
7.1
3.0
CDD
0.007
<0.5
<0.5
<0.3
<0.5
<0.3
Hexa-
CDF
<0.005
<0.4
2.0
<0.3
2.8
3.3
CDD
<0.005
<0.5
1.3
<0.3
<0.5
<0.3
Hepta-
CDF
<0.005
2.3
<0.7
<0.3
<0.7
2.4
CDD
<0.005
<0.5
<0.5
<0.3
<0.5
<0.3
Octa-
CDF
<0.005
<0.4
<0.7
<0.3
<0.7
2.3
CDD
<0.005
<0.5
<0.5
<0.3
<0.5
<0.8
Total
CDF
0.36
4.6
5.3
1.4
19.3
13.1
CDD
0.040
4.5
5.0
1.6
4.3
1.9
        'Source:  Adapted  from Ahllng et al..  1977
CO

-------
    Recently direct evidence has  been  obtained of the formation  of  PCOF  and
PCDD from  polyvlnyl  chloride  (PVC)  (Marklund  et  al., 1986a), as  previously
suggested  by  Ahllng  et al.  (1978).   In  laboratory  conditions pyrolysls  of
PVC  results  In  the  formation  mainly  of  TCDF and  HpCDF.   The  pattern  of
Isomers  appeared  similar   to  those  found  1n municipal  and hazardous  waste
Incinerators.  The same Isomerlc  pattern  was also found  1n  emissions  from a
smoke generator  burning hexachloroethane  (Marklund et al.,  1986a),  and from
leaded gasoline containing 1,2-d1chloroethane (Marklund et al., 1986b).
4.4.2.   Incineration of Municipal Waste.
    4.4.2.1.   PRESENCE OF PCDFs  IN  INCINERATOR EMISSIONS — Ol1e  et  al.
(1977) detected  the  presence  of trace  amounts of  PCDDs  and  PCDFs  In fly ash
and  flue  gas  of some   municipal   Incinerators   1n  The  Netherlands.   The
presence of  PCODs and PCDFs  In fly  ash  from  a  municipal and an  Industrial
Incinerator was  later  confirmed by Buser  and Bosshard  (1978)  and by EIceman
et  al.   (1979).   Reports  and   reviews  from  many countries   (Samuelson  and
Llndskog,  1983;  Ch1u et  al.,  1983;  BallschmHer  et al., 1983;  Janssens  et
al.,  1982; Sheffield,  1985a,b)  have  since been  published,  confirming  the
previous results.  The average PCDF  concentration for  total  stack  effluents
1s  -2.8  yg/m3.    However,  the  terms  of  total  levels  Including  those  of
congeners may not be correlated to potential toxldty.
    Buser  and  Bosshardt  (1978) and  Buser  et al.   (19786)  suggested  that the
presence  of  PCDFs  In  the  fly   ash  of  municipal  Incinerators  could  be
explained  by the  pyrolysls of PCBs.   Fly  ash  samples from an  Industrial
heating  facility at  Aarau and a municipal Incinerator 1n Zurich, both  In
Switzerland,  were analyzed.  PCDDs  and  PCDFs were  found In  both  locations
with  levels  of  0.3  and  0.1 ppm  for the  Aarau  and  Zurich  samples,  respec-
tively,  and  were 0.33-0.50 the total PCDDs  present.  The levels of  PCBs were


1928A                               4-37                             06/23/86

-------
the same  as for  PCDFs.   PolychloMnated naphthalenes  were  also present  1n
smaller quantities.  The PCDF congener profile from  fly ash  was  very similar
to  that   from  pyrolyzed  commercial  PCBs,  suggestive  of  a  common  source.
PCDFs were  detected  as follows:  18  tr1-,  21  tetra- (mainly the  2,3.7,8-),
17  penta- (Including  the  acutely toxic  1,2,3,7,8- and  2,3,4,6,8-),  7  hexa-
and  4  hepta-  (1,2,3,4,6,7,8- most  abundant).   Fly  ash  samples  contained
large  amounts   of 2,3,4,6,8- and  1,2,3,4,8-penta- and  other  penta-lsomers
relative to pyrolyzed Aroclor.
    Ol1e  et  al.  (1977)  also detected  large amounts  of chlorobenzenes  and
chlorophenols 1n  the  fly  ash of municipal  Incinerators In  The  Netherlands,
but provided no quantitative data.   The  Dow Chemical  Company has  suggested
that  PCDDs  are  ubiquitous   products  of   the  combustion of  all  chlorinated
material,  Including that found  In municipal  Incinerators (Bumb et  al.,  1980;
Crummett and Townsend, 1984).
    A summary of  the  large amount of work done  since the Initial findings Is
provided 1n Tables 4-16 and  4-17 for  Incinerator fly ash and stack effluent,
respectively.  Lustenhouwer  et  al.  (1980)  postulated  that  polyvlnyl  chloride
pyrolysls  produced chlorobenzenes In  small amounts, and these could further
pyrolyze  to  form  PCDDs and  PCDFs.  Olle  et  al.  (1983)  found that  PCDDs  and
PCDFs  did  not  Increase  when   hexachlorobenzene,  wood  treated  with  penta-
chlorophenol, paper  treated  with hypochlorHe,  old  painted wood or  Hgnln
sulfonate/polyv1nylchlor1de  were   burnt.   However,   Hgnln   sulfonate/HCl
burning caused  a  marked  Increase.  Nevertheless,  L1bert1  and Brocco (1982)
showed that  decreased levels of  PCDDs/PCDFs  occurred  for wastes  pretreated
by  the Dano  process  or 1f paper, plastic  and vegetable matter were removed.
Table  4-18  depicts  the  Influence of  type of waste on PCDD/PCDF  content.
1928A                               4-38                             06/20/86

-------
                                                                 TABLE  4-16
vO
CO









1
to
VO















o
cr
l\3
O
CO
PCDF Composition of Municipal Incinerator Fly Ash Resulting from
Origin of Fly Asha

Arnhem, The Netherlands (1)
Alkmaar, The Netherlands (1)
Unknown, Switzerland (1)
Ontario Canada (1 )
Japan (1)
Japan (1)
The Netherlands (1)
Unknown (25)
One Incinerator over 4 weeks

Milan, Italy (1)
Milan, Italy (1)
Busto. Italy (1)
Deslo, Italy (1)
Unknown (1)
Unknown (2)
Bologne, Italy (1)
Milan, Italy (1)
Alkmaar, The Netherlands
(17 samples over 5 months)
Amsterdam, The Netherlands
(14 samples over 18
months)
Zaanstad, The Netherlands
(24 samples over 20
months)
(8 samples every 20
minutes over 2.5 hours)

West Germany (1)


Recovery Cl3
(X)
NS

NS

NS


100
100

NS
NS
NS
NS
100
100
NM

80b










NS

NM
NM
NM
NM
NM
NM
NM
NM
NM

NM
NM
NM
NM
NM
NM
NM
NM
NM

NM



NM

NM


NM
PCDF
C14

trace
trace
1
3272
789
ND
ND
13-223
50-147

NM
NM
NM
NM
169
223-315
112
51
76-410

12-184



20-471

118-291


0.8-28
(nq/q)
C15

trace
trace
4
5697
3691
3827
ND
42-510
153-239

NM
NM
NM
NM
364
510-560
205
115
165-364

29-122



31-792

222-568


0.3-8

Cl6

trace
trace
30
1415
1069
ND
ND
109-870
282-361

NM
NM
NM
NM
555
840-870
235
177
160-1260

29-287



82-1054

566-1310


0.4-8
Electrostatic Precipitation

C17

trace
trace
40
967
2389
2555
ND
89-407
177-291

NM
NM
NM
NM
287
407-495
345
310
108-300

71-89



47-714

397-699


0.6-10

C18

trace
ND
10
ND
1120
2341
ND
20-26
18-31

166
6-22
0-18
70
32
84-89
425
547
0-126

2-97



4-223

37-145


0.3-14
Reference

Olle et al., 1977

Buser et al., 1978d
Elceman et al., 1979



Lustenhouwer et al., 1980


Cavallaro et al., 1980



Kooke et al., 1981

Llbertl and Brocco, 1982

Olle et al., 1982










Karasek and Vlau. 1983
(rotary
samples)

-------
00
                                                                        TABLE  4-16 (cent.)
Origin of Fly Asha
USA (1)
Florence, Italy (1)
(3 laboratories)
U.S. cyclone ash (1)
U.S. fly ash (1)
Ontario. Canada (1)
U.S. (1) (2 samples)

Vienna, Austria (1)
Ehlme, Japan
8 cities

cinders

Ontario, Canada
USA
PCDF (nq/q)
Recovery
(X)
50-100
NS

75
75
90
NS

NS

50

50

NS
NS
..,
NM
NM

NM
NM
NM
520-580

NM

0.7-32

0.4-14

NM
NN
C14
419
3.2

50
50
294
350-460
(Cl! =
39

0.4-31

0.1-84

965
26-150
C15
107
22

75
100
508
1860
40-42; C12 =
60

ND-180

trace
to 12
1865
52-390
...
263
35

170
400
420
75-91
69-110)
154

trace
to 56
ND-25

1990
120-880
C17
287
9-51

80
300
428
9-11

156

0.1-11

ND-0.8

850
72-380
Reference
25
10-230

5
20
101
0.57-2

168

ND-23

ND-0.9

ND
8-31
Taylor et al.
Brocco et al.

. 1983
, 1984

Czuczwa and Hltes, 1984

Tong et al .,
Halle et al..

Scheldl et al

Waklmoto and
1985


Shushan et al
Clement et al

1984
1985

.. 1985

Tatsukawa,



.. 1985
., 1985a
        aNumber  In parenthesis



        >>1,2.3.4-TCDD



        NS = Not  stated



        NM = Not  measured



        ND = Not  detected
00

-------
CO
                                                                           TABLE  4-17
                                                  PCDF  Composition of Stack Effluent of Municipal  Incinerators
o
CO
Origin of Study
Emission/Number
Unknown, Switzerland
Unknown
Milan, Italy (5 samples)

Milan. Italy (4 samples)

Busto, Italy

Deslo, Italy

Valmadrera, Italy (16
samples over 9 months)
Florence, Italy

Zaanstad, The Netherlands
(14 samples over 6 months)
Unknown, U.S.A.
Ontario, Canada (1)

(2)

Eksjo. Sweden
(? samples)
Florence, Italy
(3 samples)

Recovery
(X)
NS
100a
NSa
c/
NSa
£/
NSa
£/
NSa
£/
85d«e

NSd
£/
80d

81d
NSa
c/
NSa
£/
NSa
£/
NSa
c/

«i,
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM

NM
NM
NM

300
NM
NM
NM
NM
NM
NM
NM
NM
PCDF
C14
trace
460b
NM
NM
NM
NM
NM
NM
NMN
NM
17-2846
309 f
175b
ND
46-556

90
46
8
279
5
25-37
68-525
NM
NM
(nq/ma)
Cl5
trace
960b
NM
NM
NM
NM
NM
NM
NM
NM
17-2261
250f
240b
ND
109-702

NM
153
15
265
5
4.3-10
5.7-87
NM
NM

«u
trace
1600b
NM
NM
NM
NM
NM
NM
NM
NM
22-2928
314f
185b
125
174-1437

62
1712
ND
392
ND
4.3-25
10-80
NM
NM

C17
NM
1130b
NM
NM
NM
NM
NM
NM
NM
NM
17-1414
215f
400b
105
155-504

7.5
47
ND
104
ND
8.3-25
7.3-15
NM
NM

Reference
C18
NM Buser et al., 1978c
140b Lustenhouwer et al., 1980
20-47b Cavallaro et al.. 1980
270-1080
0.9b
90
4-70b
5-10
10b
51
17-749 Glzzl et al., 1982
124^
570b Llbertl and Brocco, 1982
31
0-201 Olle et al., 1982

0.8 Redford et al.. 1983
ND Chlu et al.. 1983
ND
ND
ND
8.3-9 Rappe et al.. 1983a
1.3-5.7
168-498 Brocco et al., 1984
411-546

-------
                                                                      TABLE 4-17 (cont.)
r\>
00
PCOF (nq/m3)
Origin of Study

Emission/Number Recovery Cl3
Germany (1) NSa
c/
a/
c/
a/
c/
a/
c/
a/
c/
a/
£/
£ U.S. (1) (5 days) d/
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
1100-3300

CU
2h
98h
3^
98h
18^
82h
59h
4]h
9h
9]h
2^
98»>
480-2000
S (Cl^ = 300-420; C12 =
Vienna. Austria (1) d/
Quebec, Canada (3) d/
Ontario, Canada (2) d/
NH
NM
NM
100
ND-142
53-4850

C15
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
1300-15,000
400-700)
120
ND-124
64-3960

Cl6
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
170-1800

150
ND-1392
152-2120

C17
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
NM
83-380

110
ND-123
20-880
Reference
"8
7h Ballschmlter et al., 1984,
93h 1985
63h
37h
81^
19h
67h
33^
100h
<1 h
3^
97h
8-24 Halle et al.. 1985

30 Scheldl et al., 1985
ND-3 Sheffield, 1985a,b
10-170
PO
CO
3Part1culate
bng/g
C51gn1f1es "condensate"
^Combined a and c
e2,3,7,8-TCOD
fArithmetic means
91,2,3,4-TCDD
nln % of Homeric class
NS = Not stated; NM = not measured;  ND =  not  detected

-------
00
                 TABLE 4-18



Influence of Type of Waste on PCDF Formation
PCDF (nq/q)
Waste
Untreated

Urban Waste
Agricultural
Waste
Recycled waste3
Unfermented waste
surviving the
Dano process
Coal-fired power
plant, U.S.A.


Coal-fired power
plant, Canada
Low temperature
Incinerator
Pentachlorophenol
Impregnated waste
Plasma Pyrolysls of
Substrate
bottom ash

fly ash
fly ash
sludge
sludge
partlculate
stack emission
sludge
stack emission

fly ash

fly ash

bottom ash

partlculate
condensate
condensate
"3
NM

NM
NM
NM
NM

NM
NM
ND



NM

NM

NM
NM
NM
C14
NM

NM
NM
NM
NM

NM
NM
ND



8

0.3

ND
ND
0.9
"5
NM

NM
NM
NM
NM

NM
NM
ND



32

1.1

ND
ND
4.8
"6
NM

NM
NM
NM
NM

NM
NM
ND



18

0.4

ND
ND
9.1
C17
25

70
ND
ND
ND

ND
ND
ND



15

0.1

ND
ND
18
C18
50

50
ND
ND
ND

ND
ND
ND



ND

0.1

25
ND
18
Reference
Llbertl and
Brocco, 1982







Halle et al.,
1983
Redford
et al., 1983
Chlu et al..
1983





CD
       Aroclor  1254

-------
                                                 TABLE 4-18  (cont.)
ro
CO
 .
rss
CO
Waste

Pentachlorophenol
Contaminated waste
PCB Incinerator
rotary cement
Low sulfur coal

Hazardous waste


Municipal waste


Peat 1
2
Coal (Canada)

In
kiln


1
2
3
1
2
3




Substrate
bottom ash
baghouse ash
partlculate
condensate
fly ash

stack emission
stack emission
stack emission
stack emission
stack emission
stack emission
stack emission
stack emission
fly ash


"3
NM
NM
NH
NH
NH
NH
NH
NH
NH
NH
NH
NM
NM
NM
NM


C14
ND
900
ND
ND
ND
ND
22b
62b
<0.4b
4.5b
4b
21b
<0.0006b
0.15b
ND-0.9

PCDF
"5
ND
1500
ND
ND
ND
ND
NM
NH
NM
NM
NM
NH
NM
NM
ND-
2.8
(nq/q)
cis
ND
150
ND
ND
2
0.1
NM
NM
NH
NH
NH
NH
NH
NH
ND-
0.25

C17
ND
60
ND
ND
4.2
0.2
NH
NH
NH
NM
NM
NH
NH
NH
ND-
0.19

C18
ND
6
ND
ND
0.1
ND
NH
NH
NH
NH
NH
NH
NH
NH
ND-
0.13
Reference
Rappe et al.,
1983a


Czuczwa and Kites,
1984
Oberg and Bergstrom,
1985






Sheffield, 1985a,b

aW1th paper, plastics and  vegetable matter  removed


bng/m3


NH = Not measured


ND -- Not detected

-------
Thus, no PCOFs/PCDDs were  found  1n stack emissions, fly ash  or  coal  at  four
coal-fired power  plants  (Halle  et  al..  1983;  Redford  et al.,  1983).   Some
trace PCDDs/PCDFs were found  In  the stack emissions  when  municipal  waste was
burnt.  The  results are  probably caused by optimum combustion  conditions,
1200°C  for  the coal-fired  plant and  650°C  with a  20-m1nute  residence  time
for  the municipal  waste.   Levels up  to a  few pg/m3  were  reported from  a
large peat Incinerator 1n Sweden (Marklund et al.,  1986a).
    There Is  still  controversy  over whether  the vapor  or partlculate  phase
contains the  most PCDDs/PCDFs 1n  the  stack  emissions  of  municipal  Inciner-
ators  (see  Table 4-17).   The  vapor  generally appears  the preferred  locali-
zation  phase  (Cavallaro  et  al., 1980;  Ballschmlter  et al.,  1984,  1985;
Benfenatl  et  al.,  1986).    A 13C12-labeled  surrogate  added  to the  filter
before  sampling  was  found  preferentially  1n  the  condensate and  adsorbent
(Rappe  et  al.,   1986).   Combustion   In  the  municipal  Incinerators  sampled
occurred  1n  the  temperature range  500-1000°C  with  an  optimum  formation
temperature of ~500°C (Glzzl et  al., 1982).
    Higher  temperatures   (>1400°C)  may  solve  the   PCDF  residue problem as
Indicated by  a study of the PCB,  PCDF  and  PCDD content of  the  residual ash
of  a  cement  kiln.  Residual  PCB  of  -10 mg/kg was  detected for  a  chamber
pyrolysls time of  5 seconds at  700-1000°C   (AhUng  and Llndskog,  1978), but
this  was  drastically lowered  at 1400-1450°C  (AhUng,  1979).  No  PCBs  were
found  In  the flue  gases, and  no PCDDs  or PCDFs found  1n  the kiln residues,
although  peaks corresponding  to the  expected  retention  time for  OCDF  were
noted.   Municipal Incinerators  operating from  320-900°C  favored PCDF forma-
tion  over  PCDD  {Benfenatl  et al., 1983; Taylor  et  al.,  1983).  This  1s so
for  all Isomer classes except for hepta- and  octa-  (Taylor  et  al.,  1983).
 1928A                               4-45                             06/23/86

-------
The highest  emissions  also appeared  to  be related  to  the presence of  HC1,
but not  with participate  matter  (Benfenatl  et  al., 1983).   The degree  of
temperature  control  appears  to be  the dominating  factor  (r=0.839)  and  not
absolute efficiency of combustion/precipitation since the  lowest  temperature
reached Is the most  highly correlated parameter  for PCDF/PCDD  formation  for
a given waste  {Benfenatl  et  al.,  1983).   Ol1e et al. (1982)  recognized  that
the presence of   2,3,7,8-TCDD  could  not  alone explain  the  toxldty of  fly
ash.  They have  calculated an  Index  called  the  "2,3,7,8-TCDD  toxic  equiva-
lents" to describe the  toxldty based on the  presence  of  toxic 2,3,7,8-sub-
stltuted Isomers  (Table  4-19).   Marklund et  al.  (1986a) reported the  toxic
TCDD  equivalents  (Eadon,  1982) based  on the concentrations  of the  toxic
2,3,7,8-substHuted  PCDFs and  PCDDs  found  1n   the stack  emissions  of  a
Swedish municipal Incinerator (Table 4-20).
    4.4.2.2.    ORIGIN  OF  PCDF  IN  INCINERATOR  EMISSIONS  — The  origin   of
PCDF and PCDD In  Incinerator emissions has not been clarified.   The  hypothe-
sis that  the contaminants  are already  present   1n  waste  and  are not  com-
pletely transformed  during combustion Is  generally not accepted.   However,
Ozvaclc et  al.  (1984)  found 1n raw  waste an average  concentration of  2-3
ng/g  PCDF  and  19.8 ng/g  PCDD  to  4 through 8  Cl-subst1tuted.   Although  con-
centrations  of the refuse are  low,  Toslne et  al.  (1985) suggest  that levels
of  PCDD  and  PCDF In feedstock  should not be  Ignored 1n studies  designed to
determine mechanisms  of formation of these substances.
    A  second hypothesis  suggests   PCDF  and  PCDD  formation  from precursors
such  as  PCB,  chlorophenols  and chlorobenzenes  present In  the  raw  refuse.
Laboratory  studies  have  shown  that  pyrolysls of  a variety of  chlorinated
chemicals can lead to  the occurrence  of  PCDF  and  PCDD  (see Section 4.4.1.).
1928A                               4-46                             06/20/86

-------
                                  TABLE  4-19

           Annual Toxic Equivalent of CDBFs Emitted by Netherlands
           Incinerators In Terms of  2,3,7,8-TCDD Toxic Equivalents*
PCDF Isomers
Parameter
Substrate (kg)
Fly ash amount/year
toxic equivalent
Stack effluent amount/year
toxic equivalent
C14
10.4
0.2
2.3
0.048
"5
18.7
0.9
3.8
0.19
"6
27.5
2.1
7.4
0.56
"7
18.8
0.9
4.1
0.21
2,3,7,8-
TCDD

0.2

0.026
'Source:  Ol1e et al., 1982
1928A
4^47
06/20/86

-------
ro
CO
                     TABLE 4-20


Levels of PCDO and PCDF from HSU Incineration, Umea*
                 (ng/Nm3 dg  10% C02)

-^
1
CO









o
cr>
\
o
\
CO
?n
Experiment
Season
Number of
experiments
2,3,7,8-TCDF
Total TCOF
2,3,7,8-TCDO
Total TCDD
1,2,3,7,8-7
1,2,3,4,8-PeCOF
2,3,4,7,8-PeCDF
Total PeCOF
1,2,3,7,8-PeCDO
Total PeCDD
1,2,3,4,7,8-7
1,2,3,4,7,9-HxCDF
1,2,3,6,7,8-HxCDF
Normal
Fall
3

2.5
86
0.5
43

9.0
6.1
97
2.5
53

3.6
3.7
Normal
Chips
Fall
2

2.3
75
0.6
45

8.3
7.3
100
3.6
70

4.6
4.6
Normal
Oil
Fall
2

2.4
68
0.7
52

9.8
7.8
120
3.6
76

5.6
5.5
Low
Temperature
Fall
3

2.6
87
0.4
54

8.3
7.4
110
3.2
80

5.2
5.0
Low
Temperature
Oil
Fall
3

2.1
75
0.3
47

7.1
6.5
87
3.6
70

3.6
3.4
Start
Fall
1

9.5
260
1.3
100

52
40
520
14
280

48
40
Start
Oil
Fall
1

2.3
80
0.7
49

9.0
9.0
120
3.9
90

5.7
5.7
Normal
Spring
3

0.85
19
<0.1
<10

2.5
3.9
43
2.4
49

4.5
4.6

-------
kO
CO
3>








TABLE 4-20 (cont.)
1,2,3,7,8,9-HxCDF
2,3,4,6,7,8-HxCDF
Total HxCDF
1,2,3,4,7,8-HxCDD
1,2,3,7,8,9-HxCDD
1,2,3,7,8,9-HxCDD
£ Total HxCDD
* Total HpCDF
Total NpCDD
OCDF
OCDD
TCDD equivalents
0.8
2.6
33
1.6
3.7
1.3
32
34
18
10
12
9.1
0.8
4.4
46
2.9
5.6
2.4
53
73
29
52
19
10
1.2
4.3
51
3.5
6.5
3.0
72
94
37
50
31
11
1.2
5.1
50
5.1
9.5
3.8
82
67
54
23
14
11
1.4
4.2
37
3.1
6.6
2.6
57
40
36
25
20
10
52
36
380
31
56
20
400
380
380
180
130
53
2.3
5.4
54
4.4
7.9
3.5
70
51
38
41
27
12
3.6
4.3
43
2.3
5.8
2.0
55
49
56
33
52
5.6
     *Source: Marklund et al.,  1986a
IV)
o
00

-------
However, In  experiments  1n which  known precursors  were  either left  out  or
added  to  Incinerator  material,   results  were  contrasting.   Olle  et  al.
(1983), comparing  the  emission  from burned PCP-treated wood  and  60-year-old
painted  untreated  wood,  detected  no   significant  difference  In  PCDF  (0.2
vg/g)  and  In  PCDO formed.   Hexachlorobenzene added  1n  the proportion  of
400 g  to  2 m3 municipal  raw  waste  raised  PCDF  and  PCDD  emission  (Ol1e  et
al.,  1983).    Chlu  et  al.  (1983)  burned  PCB-treated   wooden   boxes  and
discovered PCOD  congeners  In  the  range of  0.4 yg/g  and  only OCDF  at 0.025
yg/g.   On  burning  pine wood with  HC1,  Tlernan et al.  (1983)  detected total
PCDF  (3 yg/g)  that  was  20 times  more abundant  than PCDD,  while no  PCDF
formation  was  found   on  the  combustion  of  untreated  wood.   Conversely,
NestMck and Lamparskl  (1982)  detected PCDF  and PCDD  1n soot  and  ash  of
Incinerated  untreated  wood.  Therefore,  a third  mechanism has been  postu-
lated  1n which  PCDF  and  PCDD are  formed (te novo  from nonchlorlnated organic
compounds  1n  the  presence  of  chlorine  donors   (Choudhry  et  al.,  1982).
Marklund et  al.  (1986b)  have discussed  the  striking  similarities  1n congener
profiles of  PCDFs  and PCDDs found 1n  emissions from  municipal  Incinerators
and  pyrolysls of PVC,  dlchloroethane and hexachloroethane.   They  postulate a
common  mode  of formation.
4.4.3.   Sewage  Sludge  Combustion.   Few data  have  been   published  on  the
production of PCDF from  combustion of  sewage  sludges.   However, sludges have
been  found  to contain much synthetic chlorinated  compounds  so they could be
sources of PCDF  contamination.  Lamparskl et  al.  (1984)  has reported PCDD In
dried  sewage sludge  samples.  Surprisingly  small  differences  have  been found
between samples  collected  In  1981 and  1982  and  dried samples collected In
1933  and  sealed  In glass until analysis.  More recently,  Weeraslnghe et al.
(1985a) analyzed samples  of sewage sludge  from two towns  for PCDD and PCDF.


1928A                                4-50                             06/23/86

-------
They detected  several  congeners  of PCDD  at  both and, except  for  OCDF  (1300
ng/g In one sample), no congeners of PCDF.
4.4.4.    Electrical Equipment  Fires.   PCBs  are  used  as  dielectric  fluid  In
two types of equipment:  transformers containing mixtures  of  PCS  and chloro-
benzenes  (PCBZ)  and  capacitors  containing  only  PCB.    Accidental  fires
Involving  transformers  have been  reported   to  produce PCDF  and   PCOD;  when
capacitors were Involved only PCDF were formed.
    A  summary  of  PCDFs found  after  PCB fires (Rappe, 1983a,b,c,  1985a,b,c;
M1lby  et  al.,  1985;  EMckson et  al., 1985;  Williams  et al.,  1985; Hutzlnger
et  al.,  1985c) Is  provided  In Table  4-21.   The  toxic 2,3,7,8-TCDF  consti-
tutes  -20-25%  of  the TCDF content,  except  for   the Blnghamton  fire  where  H
constituted  50% (Rappe  et  al.,  1983a).   The   Blnghamton  fire concerned  a
dielectric fluid that  contained  65% PCB and  35% chlorinated  benzenes.   This
may explain  why  the Blnghamton data are anomalous.   The  2,3,4,7,8-PeCDF and
1,2,3,7,8/1,2,3,4,8-PeCDF  were 18  and  9% of  the  total   PeCDF,  respectively
(Rappe  et al.,  1983a).   In Blnghamton  soot  the  1,2,3,7,8-  and  2,3,4,7,8-
PeCDF,  and  1,2,3,4,7,8-,  1,2,3,6,7,8- and   2,3,4,6,7,8-HxCDF  were 46,  7.2,
32, 16 and 10%, respectively, of  their Isomerlc  class.
4.4.5.    Incineration  of  Hazardous Waste.   PCDFs  have   been reported  In
emission  of  hazardous  waste  Incinerators (Tlernan  et al.,  1983; Rappe  et
al., 1983a).   A  Swedish waste  Incinerator was monitored  weekly for  PCDF and
PCDD  emissions  that   were  strongly  correlated with the levels  of  total
chlorine  Input  (Oberg  et  al.,  1984).  Table  4-18  contains other  examples  of
PCDFs  produced during the  Incineration of hazardous wastes.
1928A                               4-51                             06/23/86

-------
00
         TABLE 4-21



PCDFs Formed During PCB Fires
PCDF Congener9






_^
i
en
PO













o
c*
CO
00
c*
Site

Stockholm. Sweden.
1978
Stockholm. Sweden.
1981
Blnghamton. NY. 1981



Surahammar. Sweden,
1982



Imatra, Finland, 1982


Hallstahammar.
Sweden. 1982


Railway locomotive.
Sweden. 1982
Klsa. Sweden. 1983




Sample

Liquid on capacitor
PCB after explosion
Floor wipe

Floor soot
Celling soot
Floor soot
Air
Air

Room floor
Wipe 1
Nlpe 2
Mall wipe 1
Mall wipe 2
Soot 1
Soot 2
Soot 3
Metal bar
Mlpe 1
Wipe 2
Floor wipe
Floor wipe 1
Floor wipe 2
Floor wipe 1
Floor wipe 2




"3
3-7b
lib
NN

NN
NN
NN
NN
NN

NN
NN
NN
NN
NN
NN
200
NN
NN
NN
NN
NN
NN
NM




C14
2b
3°
1600

0.028
162
100
4-195b
150°

4000
90
1250
480
1
16
20
1600
5000
50
6900
4900
100.000
500




Cl5
NM
NN
175

0.670
197
120
N0-60b
50b

3300
25
355
210
0.2
1.0
1
360
1800
12
29.000
1500
NM
NM




C16
NN
NN
<0.5

0.965
110
70
2-9b
2-3b

1800
17
150
140
0.04
0.3
NN
600
850
10
14.000
400
NN
NN




C17
NN
NN
<1

0.460
36
20
NN
NN

1500
17
65
60
0.02
0.2
NN
800
550
30
6200
170
NN
NN




C18
NH
NM
<1

0.040
14
4
NM
NM

300
4
13
30
0.01
0.1
NH
1340
440
20
140
40
NM
NM



Reference

Jansson and Sundstrom.
1982
Rappe et al.. 1982,
1983a, 1985b
Rappe et al., 1983a
O'Keefe et al.. 1985a
Schecter and Tlernan,
1985


Rappe et al., 1985b.c



Rappe et al.. 1985b
Elo et al.. 1985

Rappe et al., 1985b,c


Rappe et al.. 1985b.c

Rappe et al.. 1985b





-------
vO
rsj
00
                                                                        TABLE 4-21 (cont.)
PCDF Congener*
Site Sample




^
i
os


Skovde. Sweden. 1982 Floor wipe
Floor wipe
Hall wipe
Bench wipe

London. U.K.. 1983 Overheated
Fresh PCB

1
2



PCB

Turin. Italy Concrete floor wipe
"3
NN
NN
NN
NN

NN
NN
NN
C14
100
600
<1
<1

50-90
ND-70
3852
Cl5
40
100
<1
10

460
150
296
"6
40
60
<1
<1

530-590
130-160
<9.5
C17
a
8
 Not detected
INJ
CO

-------
4.4.6.   Car Exhaust.   BallschmHer  et  al.  (1986)  Identified  a  series  of
PCDFs and  PCDDs  1n  used  motor  oil  from automobiles.   The congener  profile
was similar to that  from  Incinerators burning urban waste.  It  was  suggested
that  chlorinated  additives  In  the  oil were  Involved.   Marklund  et  al.
(1986b) found that the appearance of PCDFs/PCDDs depended  on  the  presence of
l,2-d1chloroethane scavenger.  Contaminants  added  to  the motor oil were  not
responsible.  The average emission from  a car running  on  leaded gasoline was
30-540  pg  2,3,7,8-TCOD equivalents/km,  equivalent  to 10-100 g  2,3.7,8-TCDD
equivalents/year.
4.4.7.   Other Sources.   PCDFs  have also  been  found  1n  the  emissions  from
steel mills and  copper  mills,  baths  using recycled material  contaminated by
PVC and polychlorlnated paraffins  {Marklund  et  al., 1986a).  Bergman  et  al.
(1984)  also  reported on  the formation  of  PCDFs from  chlorinated  paraffins.
PCDFs have  been  mentioned 1n several  patents  for  use In  electrical  Insula-
tion  (British Thompson-Houston Co. Ltd., 1939),  In  capacitors  (Clark,  1940),
flame  retardants  (Dazzl  et al.,  1974;  Boyer, 1971) and  as  bacterlddes
(Shlbata et al., 1952).  Commercial usage of  the products Is not available.
 1928A                               4-54                             06/20/86

-------
              5.  ENVIRONMENTAL FATE, TRANSPORT AND DISTRIBUTION

5.1.   SUMMARY
    PCDFs are  ubiquitous  contaminants.  They  are associated with  the  small
partlculate fraction  and  vapor  of  flue gas and  can thus be  transported  In
the atmosphere  over  very  wide areas.  Weather conditions  can  greatly affect
their transport.  Photodegradatlon  by  sunlight may occur  1n the  presence  of
triplet  sensltlzers   1n  aqueous  solution;  photodecomposltlon  In  the  vapor
phase has not been Investigated.
    In  aquatic  media,  since PCDFs  have  poor   solubility  and  tend to  be
adsorbed, they  are expected  to be persistent  In  sediments or  on partlculate
matter.  Their  presence has  been associated with atmospherically transported
waste  Incineration-derived  PCDF.   In  soil  they  have  been  detected  In  top
soil  layers after  Improper   disposal  of  wastes  or  after  dissemination  of
herbicides, but  quantitative data are  lacking.   As  for translocatlon poten-
tial  from   soil  to  vegetation  1s concerned,  PCDFs  tend  to be  adsorbed  on
external surfaces.  Little data on bloconcentratlon factors exist.
5.2.   INTRODUCTION
    Since  PCDFs are  trace  Impurities  In various  chlorinated  chemicals  (see
Section  4), they will  accompany these  chlorinated  chemicals  when  they  are
released  Into  the environment.   As  concentrations  are  generally  below  ppm
levels,  the quantity released determines  the  extent of  the pollution.   The
content of  toxic  Isomers also determines whether  toxic  effects may occur.
    PCDFs  have  also  been  Identified   1n  effluents  from  various combustion
processes  (Section 4).  Municipal solid wastes and Industrial  waste  Inciner-
ations  have been found to emit  fly ash and flue  gas  containing  PCDF In  the
range  of  yg/m3.  As  PCDF  may   be  associated with  the  small   partlculates


1929A                                5-1                               06/23/86

-------
and wHh  flue  gas,  PCDFs could  be  distributed over large areas.   This  com-
bustion may be responsible for the  ubiquitous  PCDF  pollution  of  the environ-
ment.
    Very  little  data  for the  PCDFs are available,  so  they are  expected  to
act like  PCDDs  1n the environment.   The U.S.  EPA  (1985) gives  an  excellent
summary of  the  environmental  fate,  transport  and  distribution  of  2,3,7,8-
TCDD.
5.3.   ENVIRONMENTAL TRANSPORT
5.3.1.   Air.
    It  1s  very  difficult to assess  the quantity and the  IsomeMc  distribu-
tion of PCDFs  In the  atmosphere as many  variables  Interfere.   Emission  from
Incinerators Is  dependent on the  refuse,  combustion design,  operating condi-
tions,  composition  of  the fuel,  operating  temperatures  and degree  of  emis-
sion control.  The  great heights of  stacks contribute to  disperse  PCDF  over
large  areas  and  reduce concentrations near the  source.  Weather conditions,
height of the stack 1n relation  to  the size and position of natural obstruc-
tions  or  buildings, relative  distribution of PCDFs  1n flue  gas  between  par-
tlculate  fraction  and  particle-free  gas  phase (see 4.4.2.1.),  and particle
size are  all factors that greatly modify the  transport  of  PCDF In the atmos-
phere, as has been suggested for the other pollutants (Somers, 1971).
    PCDFs  may  theoretically  undergo  photodecomposltlon  In  the atmosphere,
but the environmental relevance  of  this  process  Is  not  known.  Photochemical
degradation  has  been  demonstrated under laboratory  conditions  for  the high-
est chlorinated  congeners, but  these  reactions  are  unlikely to occur In sun-
light  (Section 4.3.).  Thus  PCDFs are probably  carried  directly to the soil
or  to  water compartments such as lakes and oceans.
1929A                               5-2                              06/23/86

-------
    A method  to collect  PCDFs  and PCDDs  In  both the partlculate  and  vapor
phase 1s  now  available (Oehme  et  al.,  1986).  This method  Involves  a  fiber
glass filter and a polyurethane  foam  plug  from which the PCDFs were desorbed
by  Soxhlet  extraction with  toluene,   followed  by  liquid  chromatographlc
separation, and  GC/MS  confirmation and quantltatlon.  The  recovery from the
filter     1s     -75-8554     for     13Cno-l,2,3,4-TCDD,     37C1B-OCDD,     and
                                       \c                       o
13C,2-PeCDF;  the recoveries  from  the  foam are  >80%.   Typically,  the  PCDF
congeners  below HxCDF  were  found on  the foam  plug  following  the  filter,
while  the rest  were  found  adsorbed  to particles  on  the  filter.   As  soot
loading  Increased,  more  of  the  lower  congeners were  found  on  the  filter
adsorbed  to soot particles.   Samples  near  an  Industrial  city (Essen, Federal
Republic  of  Germany)  reflected the  congener  patterns  of  nearby municipal
Incinerator stack emission  patterns.   Concentrations decreased with distance
away  from the  source.   Samples  1n  suburbia  and In remote  areas contained
mostly  PCDFs.   Of  the  60 samples  taken, the  highest levels of 5-10 pg PCDDs
fPCDFs/m3  were found  In  a   heavily  Industrialized  area.   In  suburban  areas
the  levels  were 5-10 times  lower.  Thus people living  near Industrial  areas
may  be exposed.  The  highest  2,3,7,8-TCDD  equivalent  level   found  was 0.1
pg/m3   with   2,3,7,8-TCDD  always   below  detection.   Ballschmlter  et  al.
(1986)  have  shown  that PCDFs  can  be emitted from  leaded automobile exhaust
but  not  from  unleaded  exhaust (Chapter  4 also has a discussion of  this  topic
from the  perspective of  accumulation of PCDDs and  PCDFs In leaded gasoline
through  use.   The  1,2,-dlchloroethane additive was  postulated  to be the
chlorine  donor).  Ballschmlter  et  al.  (1986)  showed through pattern recogni-
tion that both automobile  exhaust and  emissions  from municipal  Incinerators
were correlated with lake  sediments  around the world.   The municipal Incin-
erator  component  was  postulated  to  arise   mostly from   pentachlorophenol
 1929A                                5-3                               06/23/86

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Incineration  (Cruczwa  and  Hltes,  1984,  1985,  1986;  Cruczwa  et  al.,  1984,
1985).    The  striking  uniformity  of  the  patterns  of  Isomers  1n  a  given
congener class suggested a more global source of PCDFs/PCDDs  like  automobile
exhaust.  Three basic emission sources were postulated  (Ballschmlter  et  al.,
1985) based on congener profiles.
5.3.2.    Hater.
    PCOFs  are  UpophlUc  and  practically  Insoluble   1n   water   (Section
2.3.3.).  Thus  1n  aquatic media  PCDF  are present  1n  the adsorbed state  to
partlculate matter rich  1n organic  content.   Rappe et al.  (1984)  found  con-
centrations (100 ng/ml)  of  PCDF 1n  a  suspension  of soot/dust In  wash  water
from a  PCB  fire  to  be only  1n  the  adsorbed  state,  since  when the  soot
settled  the  water  did  not  contain  detectable PCDF.   Abiotic  degradation
(photoreactlons,  hydrolysis,   etc.)  and  blodegradatlon  are  not  likely  to
occur In this  compartment.  Thus PCDFs are expected  to be very persistent  1n
aquatic media  where  they show high  affinity  for  sediments.   Czuczwa et al.
(1984), Czuczwa and Hltes (1984) and Czuczwa  et al.  (1985)  found  that fluxes
of PCDF to  lake sediments In  the  United  States  and Switzerland were -0.1-0.3
ng/cnf Vyear"1.
5.3.3.   Soil.
    PCDFs  are rapidly and strongly  adsorbed Into  most soils and  sediments
where  they are  expected to  be  Immobile.   Quantitative data  on  PCDFs are
lacking, but  studies on  2,3,7,8-TCDD Indicate that  these compounds are  prac-
tically  Immobile  (Helling et  al.,  1973), the apparent  half-life  for  TCDD  1n
soil exceeding  10 years  (D1 Domenlco et  al.,  1980a).   PCDF  can be transport-
ed  from soil   to air  or  the  water compartment  through contaminated airborne
dust particles or waterborne eroded soil.
 1929A                               5-4                              06/23/86

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    Volatilization 1s probably not  Important  because of the low  vapor  pres-
sures of  such compounds.   However, D1  Domenlco et  al.,  (1980b)  suggested
that volatilization could be at least partially  responsible  for  the observed
disappearance of  TCOD from  the  topmost soil  layers of the polluted  Seveso
area, 1  year  after   the  accident.   Freeman  and Schroy  (1985)  modeled  the
volatilization of  2,3,7,8-TCOD  adsorbed to Times  Beach soil based  on  moni-
toring the  volatilization  over  a period of  1  year.  Thus H Is  likely that
volatilization will  occur  also  for  the  PCDFs,  and this  should  be  demon-
strated.
    In general,  higher  chlorinated PCDDs  and  PCDFs volatilize  more  slowly
than  lower  chlorinated  dloxlns  since  their  vapor  pressures  decrease  with
Increasing chlorlnatlon (Table 2-5).
5.4.   ENVIRONMENTAL TRANSFORMATION
5.4.1.   Abiotic Transformation.
    PCDFs are  chemically quite stable  and are not  likely to be  degraded by
hydrolytlc reactions under environmental conditions  (Section 2.4.1.).
    Photochemical  degradation was  discussed  In Section  2.4.2.   Photodegrada-
tlon  In  organic  solvents occurs for the higher  PCDFs 1n organic  solvents at
310  nm   (Hutzlnger  et al.,  1972a,b,  1973;  Buser,   1976b; Firestone,  1977b;
Mazer and Hlleman, 1982; Mazer  et  al.,  1983a,b,; Hlleman et al., 1985).  The
degradation 1s much slower In water at 310 nm (Crosby and Mollanen, 1973).
    Direct  evidence  of  PCDF  decomposition  In  the  environment  Is  lacking and
the  Importance  of  sunlight  In   their  environmental   fate  remains  to  be
evaluated.
5.4.2.   B1otransformat1on.
    Currently  virtually  nothing Is known  about  the blodegradatlon of PCDFs.
However  H  1s  conceivable that they are relatively resistant  to blodegrada-


1929A                               5-5                              06/24/86

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tlon, like  the  corresponding  2,3,7,8-TCDD (U.S. EPA,  1985).   Only 5 of  the
100  soil  microblal  strains  tested  have shown  some  ability  to  metabolize
2,3,7,8-TCDD  (Matsumura   and  Benezet,   1973).   Ward  and  Matsumura  (1978)
studied  the blodegradatlon  of   2,3,7,8-TCDD  1n  Wisconsin lake  waters  and
sediments and  found  a half-life  of  550-590  days  In sediments, while  about
70X of 2,3,7,8-TCDD 1n lake water samples alone  remained  unaltered after  590
days.   Moreover,   Matsumura  et  al.   (1983)  estimated   the   half-life   of
2,3,7,8-TCDD 1n an aquatic ecosystem model to be ~1  year.   The occurrence of
a polar metabolite of 2,3,7,8-TCDD with  a probable  hydroxy group  1n position
1 was  found by  PhlUppI  et  al.  (1982)  In  several  microbiological  cultures
after   long   Incubation.    Bumpus   et   al.   (1985)   demonstrated   that
14C-2,3,7,8-TCDD at  a level  of  14  pmol was  blodegraded  to  the  extent  of
~25% by  the white  rot fungus,  Phanerochaete chrysosporlum.  It was  hypothe-
sized that  the  extracellular I1gn1n-degrad1ng enzyme system was  responsible.
14CO_  was   the  metabolic  product  monitored.   PCDFs  are  expected to  cause
the same behavior.
5.5.   BIOACCUMULATION
    High correlations have been  observed between  the octanol/water partition
coefficient  (K   )  of  many  organic  compounds and  bloaccumulatlon  In  fish.
Two  equations  have  been  proposed to  relate  the  two measures.   Lu et  al.
(1978) found that their data  were fitted by  the following equation:

     log [bloaccumulatlon (fish)] = 0.7  log  (partition coefficient) + 0.8
Therefore,  high  K    values  would  Indicate  high  concentration  factors.
K    values  were  reported   1n  Table  2-4.   Using  the  Burkhard  and  Kuehl
1929A                               5-6                              06/23/86

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(1986) recalculated  values,  the values  of  the log  [bloaccumulatlon  (f1sh)J
defined by  Lu et  al.  (1978) would  be 4.51,  4.87  and 6.95  Indicating  high
bloaccumulatlon  for   2,8-DCDF,   2,3,7,8-TCDF   and  OCDF,  respectively.   The
value  for  the 2,3,7,8-TCDF agrees with  that  for 2,3,7,8-TCDD  (Burkhard  and
Kuehl, 1986).  PCDFs  have not been studied 1n model  ecosystem.
1929A                               5-7                              06/23/86

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                     6.   ENVIRONMENTAL  LEVELS  AND  EXPOSURE
6.1.   SUMMARY
    PCDFs have been  found  1n wastewaters and rivers, and also  1n  the fat of
animals, mostly  as  acutely  toxic  2,3,7,8-TCDF and  2,3,4,7,8-PeCDF,  respec-
tively.  Plants  do  not  appear  to  bloaccumulate  PCDFs.   The  similarity  of
lake  sediments  with  respect  to PCDF  and  PCDD  congeneric  patterns  Implies
that  there may be  a common source of  PCDFs and PCDDs with  air  as  the trans-
port medium.  Both  the emissions from  municipal  Incinerators  and from leaded
automobile exhausts  are  correlated to  PCDFs  and  PCDDs.  This  does  not  sup-
port  Dow's  trace  chemistries  of  fire hypothesis.  PCDFs  In milk  and  from
Industrial  accidents are Important routes of exposure also.
6.2.   ENVIRONMENTAL LEVELS
6.2.1.   Introduction.  PCDFs  have  not been monitored  systematically  In  the
environment.  Zltko  (1972) and  Zltko et  al.  (1972) Investigated the presence
of PCDFs In several  wildlife  samples with negative results, but the analyti-
cal methodology  used In  these studies  had  a sensitivity  several  orders  of
magnitude  less  than  that  required for  detection  of  the  probable  environ-
mental  concentrations (ppt)  of PCDFs.   In  a  similar   study,  Bowes  et  al.
(1973)  Investigated  the  presence of PCDFs  1n wildlife  populations  with  high
rates  of  embryonic  death.   Again,  no  PCDFs  were Identified,  either  In
herring  gull  egg  samples  containing  a  total  of  -0.9 g  PCBs or a  sea  lion
sample containing ~1 mg of PCBs.
    The  first positive  report  concerning the presence  of PCDFs  1n  the envi-
ronment  was  by  Jungclaus  et  al.   (1978)  who Investigated the presence  of
anthropogenic organic  chemicals In the wastewater  of a chemical manufactur-
ing plant and using  GC/MS  Identified a TrCDF  among >100 compounds.   The same
compound was  Identified  1n  the water of  a  river  receiving the  industrial
wastewater.

1930A                               6-1                              06/23/86

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    Table 6-1 contains a  summary  of  the levels found  In  environmental  media
to 1986.   PCDFs  have been  found  1n wastewater,  river water, sediments  and
air samples.
6.2.2.   In Soil and Sediments.   PCDFs  deposited  1n soil strongly  adhere to
the  upper   soil  layers.   Thlbodeaux  (1983)   stated   that  PCDFs  and  PCDDs
applied to  the surface of soils having  a high  organic  content generally stay
1n the upper  6-12"  layer,  while 1n more sandy soils they can  migrate  3 feet
or more.  However sediments seem  to  be  the  ultimate  sinks of  PCDFs.  Czuczwa
et al. {1984, 1985) studied the presence of PCDFs  and  PCDDs  In sediments and
sediment cores from the Great Lakes  1n  the  United  States  (Czuczwa and HHes,
1984,  1985,  1986),  and  annually   In  laminated  sediments  from  lakes  In
Switzerland  (Czuczwa,  et  al.  1985).   The  accumulation of  PCDDs  and  PCDFs
paralleled  the rapid growth of  the production  of  chlorinated  chemicals  since
1940.  In  fact  PCDFs  and PCDDs were absent from sediments before  1945,  but
Increased thereafter.   In all cases  OCDD predominated  (>1000  ppt);  HpCDD and
HpCDF  were  the  next  most  abundant  congeners   (1-15 ppt).   The  congener
profiles from Switzerland  and from U.S.  sediments  were  similar.
    The absence  of  PCDFs  from the sediments before 1940  Indicates  that wood
burning,  coal combustion  and  probably leaded automobile  emissions,  which
were  prevalent  before  1940, are  not  Important sources of PCDFs.   The  simi-
larity  1n  the PCDF/PCDD profiles from  the  sediments  In  Switzerland  and the
United Stages suggests  a  common source  Involving  atmospherically-transported
combustlonderlved PCDFs  (Chapter  5).  The  PCDDs  and  PCDFs  In  the  sediments
from  Slsklwlt Lake located  1n  Isle Royale  In Northern Lake  Superior  could
only  have  been   deposited  from  the  atmosphere  (Czuczwa et  al.,  1984).  The
congener  profile of PCDFs  and PCDDs  1n sediments  was  similar  to  that 1n
airborne partlculate  samples  from two  locations remote  from  S1sk1w1t Lake.


1930A                               6-2                              06/23/86

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                                                                           TABLE 6-1

                                                             Levels  of  PCDFs  In  Environmental Media
             Site
           Sample
            TCDF Concentration
                                                                                                                                     Reference
        Water
        Soil/Sediments
CO
Mastewater.  U.S.
Rlverwater,  U.S.

Narragansett Bay,  RI.
  Water and  suspended  particles

Hudson River Sediment,  U.S.
                                Woods Pond Sediment,  MA


                                Saglnaw River/Lake  Huron:

                                  Surface Sediments (6)

                                  Sediment Cores  to 12 cm


                                Buffalo River  Sediment,  IL

                                Sediments:

                                  Albany, Hudson  River,  NY
                                  Tappan Zee Bridge,  Hudson
                                    River. NY

                                Slsklwlt Lake  Sediment,  MI
                                  Cores 0-6 cm

                                        8-9 cm


                                NBS Urban Dust
Surface Sediments from
  lakes In Switzerland

Soil, Amsterdam, The
  Netherlands
Trace of a TrCOF
Trace of a TrCDF

2,4,8-TrCDF found; 0.013-0.25 ng/ml
C14. <3-200; C15. <3-193; C16, <3-377;
Cl7, <3-2436; C18, <3-1010 pg/g

C14. <5; C15, 9; C16, 150; C17, 920;
C18, 270 pg/g
                                       C14,  0.1-3;  C15.  0.01-4;  C16,  0.13-12;
                                       C17,  0.2-30; C18, 0.05-7  ng/g
                                       Cl4,  10-30;  Cls,  100-200; Clfc, 100-200;
                                       C17,  50-400; C18, 5-10 pg/g

                                       2 TCDFs,  OCOF detected
                                       5 ng/g 2.3.7.8-TCDF
                                       29-46 ng/g 2,3,7,8-TCDF
                                       C14, C15, 2-5; C16, 2; C17, 17-20;
                                       C18, 3-4 pg/g
                                       Cl4, <0.4; Cls, <0-*: C16. <0-*:
                                       C17, <0.4-1.6; C18, 1.1 pg/g
C14, 0.03-0.10; Cls, 0.31-1.3; Cl
C17, WO-5.8; C18, ND-1.9 ng/g

C14, 13-170; Cls, <10; C1&, 5-60;
C17, 100-240; C18, 10-510 ng/g
                                                                           ND-1.6;
Jungclaus et al.,  1978
                                                                                                                            Lake  et  al.,  1981
Petty et al., 1983a
C14, 1413-24,000;
C16, ND-115 ng/g
                                                                                            ,  NO-5650;
                                                     Czoczwa and Kites, 1984.
                                                     1986
                                                     Kuehl et al., 1984b
                                                     O'Keefe et al.. 1984
                                                     Czuczwa et al.. 1984. 1985;
                                                     Czuczwa and Kites, 1986
L1 et al., 1985
Czuczwa et al., 1985;
Czuczwa and Kites, 1985

He Ida et al.. 1985

-------
                                                                       TABLE  6-1  (cont.)
            Site
           Sample
            TCOF Concentration
         Reference
       So11/Sediments
       (cont.)
       Air
60 Vapor and partlculate  air
samples. Federal  Republic of
Germany

Surface sediments from:

  Lake Michigan (2)

  Lake Erie (2)

  Lake Ontario
Air Partlculate
  Washington,  DC (NBS)

  St Louis,  MO (NBS)
                               Air Sample, New York

                               U.S. Incinerator Plant Air
5-10 pg/m3 for sum of PCDDs and PCOEs
C14, <10; Cls, <1
C18, 0.5-24 ng/g
C14, <10; C15, <1
C18, 30-60 ng/g
C14. <10; C15, <1
Clg, 3600 ng/g
                                                                                        ;  C16. 8-33; C17. 70-240;

                                                                                        ;  Clb, <10; C17. 40-80;

                                                                                        ;  C16, 200; C17. 1200;
C14, 1.3; C15. 1.2; C16, 0.8; C17, 18;
Clg, 6.2 ppb
C14, 0.2; Cls, 0.2; C16. 0.3; C17. 12;
C18, 0.5 ppb

<0.1-1.9 pg/m» 2,3,7.8-TCDF

Total PCDF was 3 ng/m3
Oehme et al.,
Czuczwa and Hltes, 1986
                                                                                                                           Czuczwa et al., 1984, 1985;
                                                                                                                           Czuczwa and Hltes, 1986
                                                                                            O'Keefe  et  al.,  1985b

                                                                                            Halle  et al..  1985
       NO = Not detected
W
\
00

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They showed that the pattern of  PCDDs/PCDFs  1n  lake  sediments  resembled  that
of the contaminants 1n chlorophenols and could  be  detected  1n  sediments  to  a
depth  of   12  cm.   This  does  not  support  Dow's  trace  chemistry  of  fires
hypothesis.   Reviews  have been  written by  Hutzlnger et  al.  (1985a,b)  and
Weeraslnghe and  Gross  (1985).   A  mathematical  model for  the  transport/fate
of organlcs 1n soils has  been published by  Undstrom and  Plver  (1985).
6.2.3.   In Plants.  Few data  on the concentrations  of  PCDFs  1n plants  and
vegetables exist.  Wild fruits collected from a  Dutch area  seriously  contam-
inated with  organochloMne  waste compounds  showed  no presence of  PCDFs  and
PCDDs  (Table  6-2)  which, however,  were present In  topsoll,  In  fish  and 1n
animals (Helda  and OHe, 1985).   Since there  Is  little bloaccumulatlon of
PCDDs  1n  plants, probably  PCDFs  will not  bloaccumulate  to  any extent  either
(U.S.  EPA,  1985).   Plants'  aerial  parts may be  contaminated through  deposi-
tion of airborne particles or  through  volatilization or  translocatlon  of  the
compounds  present  In  soil.   When 2,3,7,8-TCDD was added  to  soil,  only 0.15%
accumulated  1n  oats  and  soya  beans  (Isensee and Jones,  1971).   Aerial
portions  of  plants  growing   In  contaminated  Seveso areas  contained  less
2,3,7,8-TCDD  than  roots,  which had  lower  levels than the  surrounding soil.
At a  soil  concentration  of  10,000 ppt, fruits were  found  to contain  no  more
than 37 ppt,  with  95% 2,3,7,8-TCDD  being located In  the  peel.  This strongly
suggests  that contamination was due to surface  dust deposition and  not to
plant  uptake  (Wlpf et al.,  1982).   Underground tissues of  some  plants  such
as carrots can take up  UpophlUc  chemicals from the soil  (Cocuccl  et  al.,
1979;  Pocch1ar1 et  al.,  1983).   The  2,3,7,8-TCDD concentration  1n  root
vegetables  ranged  from  3-10%,  and  In  the aerial  parts  from  0.3-1%  of  the
surrounding highly contaminated soil (PocchlaM  et al.,  1983).
1930A                               6-5                              06/23/86

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                                                        TABLE  6-2
uO
CO
o
3>



cr



o
cr>
no
CO
Ranges
Material
Milk fat
Top soil (dry weight)
Worms
Mice/liver
/reference liver
Rabbits/liver
/reference liver
Pheasants/liver
/reference liver
Eel-Inside dump/liver
/muscle and fat
Eel-outs1de dump/liver
/muscle and fat
/reference liver
Pike-Inside dump/liver
/muscle
P1ke-outs1de dump/liver
/muscle
of 2,3,7,8-lCUl) and
1n ppt fresh weight
Number of
Samples Analyzed
6
9
9
4
1
14
5
8
2
2
2
3
1
1
1
3
2
pcui-s in lop sol I am
In a Dutch Hazardous
2,3,7,8-TCDD
<17
<20-1929
<1 5-889
<10-5237
<68
<10-50
<2-<50
<6-33
96-97
104-144
NA
30-42
584
21
<50-103
<30
d Biological s<
Waste Dump3
Total TCDFs
NA
1413-23,920
ND-3020
ND-13809
ND
ND-168
ND
ND
ND
2350-2765
4276-5193
NA
41-47
NA
959
41
ND
ND
ampies
Total
PeCDFs
NA
ND-5650
ND-300
1408-23,097
ND
ND-1121
ND-124
ND
ND
ND-169
182-558
NA
134-147
NA
975
154
ND-1419
263-268

Total
HxCDFs
NA
ND-115
ND-2694
ND-584
ND
ND-1081
ND-132
ND
ND
ND
ND
NA
ND
NA
ND
ND
ND
ND
CO

-------
WO

o
                                                  TABLE  6-2 (cont.)
I
—I
Material
Pike -reference/liver
/muscle
Minnow-inside dump/liver'3
Minnow-outside dump/liver
Blackberries
Elderberries
Pumpkin
Number of
Samples Analyzed
1
2
1
1
8
2
1
2,3,7,8-TCDD
<9
593
<20
ND-<10
<2-<17
<20
Total TCDFs
ND
ND
5808
ND
ND
ND
ND
Total
PeCDFs
ND
ND
ND
ND
ND
ND
ND
Total
HxCDFs
ND
ND
ND
ND
ND
ND
ND
    aSource: Heida and Olie, 1985


    ^Only one specimen analyzed


    ND = Not detectable


0   NA = Not analyzed
ro
CO

00

-------
6.2.4.   In Aquatic Organisms.  Evidence  for  aquatic wildlife contamination
by PCDFs  was  reported by  Stalling et  al.  (1981),  Kuehl  et al.  (1981)  and
Rappe et al. (1981).  Samples of fat  from snapping turtles,  (Chelyda serpen-
tlna). from the Hudson River and Baltic gray  seal,  (Hallchoerus  grupus),  and
from  the  Gulf   of  Bothnia  were  examined  using  a  direct-probe  negative
chemical  lonlzatlon mass  spectrometrlc technique  of sensitivity 0.2  pg  for
2,3,7,8-TCDF.   The  turtle  fat  containing >750 ppm  of  PCBs  was  found  to  be
contaminated by PeCDFs and HxCDFs while the seal  fat,  whose  concentration 1n
PCBs was -100 ppm, contained trace amounts of  PeCDFs (Stalling et  al., 1981;
Rappe et al.,  1981).
    The  same  two samples  were  analyzed  by  Rappe et  al.  (1981)  using high
resolution GC/MS In order to Identify  the single  PCDF  Isomers.   The 1somer1c
PCDF composition of the two  samples  showed a  good correspondence despite the
differences between the  two species and  the  different origins.   The  turtle
fat sample had a total PCDF  concentration of  3 ppb distributed among 18 dif-
ferent  Isomers;  among these the toxic  2,3,7,8-TCDF  and  2,3,4,7,8-PeCDF were
present at a  concentration  of  45 and  620 ppt,  respectively.  HpCDFs,  PeCDFs
and HxCDFs predominated In that order (1000,  820 and 700 ppb, respectively).
    In  the  seal  fat,  the total amount  of PCDF was  40 ppt with  the 2,3,7,8-
TCDF  at 1 ppt  and  the 2,3,4,7,8-PeCDF  at 15  ppt.   The composition  of  the
major  Isomers found  In  these biological  samples  corresponded  fairly well  to
the  pattern  present  1n  commercial  PCBs  while  a  poor correlation  was found
with  the  Isomer composition  of other  PCDF  sources such  as polychlorlnated
phenols  and  Incinerator  fly ash  samples.  This suggested that  the presence
of PCDFs  1n these samples was correlated with PCB pollution.
1930A                               6-8                              06/24/86

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    Yamaglshl et al.  (1981)  also detected the presence of  unspecified  TCDFs
In Japanese fish (Zacco platypus), and Kuehl  (1981)  reported  that  fish  taken
In U.S.  rivers  before  1978  contained a  total  estimated  PCOFs ranging  from
0.5-5 pg/g.  Lake  et  al.  (1981) quantHated a TrCOF  1n Rhode Island  aquatic
life.   In  1978,   the  mussel  (Mytllus  edudls)  contained  643 ppb  and  six
samples in 1979 were found to  have 52-1180  ppb.   Clams  (Hercenarla mercenla)
also contained  26  ppb,  whereas lobster (Homorus  amerlcanus)  hepatocytes  had
1260 ppb.   Kuehl  et al.  (1986)  also detected TrCDFs, TCDFs,  PeCDFs, HxCDFs
and HpCDFs In fish from the Great Lakes.
    These  discoveries  ushered  1n many  Investigations (Table  6-3)  Involving
the major  IsomeMc PCDF classes  1n  tissues  of  fish  living 1n  lakes, rivers
and seas.
    PCDFs  were  Identified  but  not quantHated  In fish  from  18 major water-
sheds  near the Great  Lakes  collected  1n 1979-1981  (Kuehl  et al..  1984a).
They have been Identified  1n   fish  from the  Great  Lakes  (O'Keefe et  al.,
1983; Ryan et al.,  1983; Stalling et  al., 1983).   PCDDs were  not  detected In
fish samples from  Lake  Superior while a series of  PCOFs  could be  Identified
In the  same samples,  Indicating  more widespread  background  levels for  the
PCOFs than  for  PCDDs  (Stalling et al., 1983).  Stalling  et al. (1983)  could
detect   very  little 2,3,7,8-TCDF  In   sediments  but  larger  amounts In  fish;
OCDF  was abundant  1n sediments  but low  1n fish.   Similar  results  (Table 6-4)
were obtained 1n examining sediments  and yellow perch from  Woods  Pond,  which
was  known  to   be  contaminated  by  Aroclor  1260  (Petty  et  al.,   1983a,b).
Stalling  (1982) found carp,  largemouth  bass  and  striped  bass  from the  lower
Hudson   River  contained  2,3,7,8-TCDF at  concentrations   ranging  from  14-18
pg/g.  The presence of  2,3,7,8-TCDF  1n striped bass  was confirmed  by  O'Keefe
(1982).  Since  the upper section of  the Hudson River  was  highly contaminated


1930A                               6-9                              06/23/86

-------
                                                                          TABLE 6-3

                                                                  PCOF Residues In Wildlife
       Wildlife
               Species
                                                                                        PCDF Level (pg/g)
      Reference
       Animals
       Fish
I
__l
o
00
Fat from Snapping Turtle,  U.S.
  (Chelyda serplntlna)

Fat from grey seal, Sweden
  (Hallchoerus grupus)

Seal. Sweden

Yellow Perch, NA


Bloater, Lake Superior

Lake Trout (Salvellnus naraavcush  from:
  Lake Superior (2)

  Lake Ontario (2)

  Lake Michigan (3)

  Lake Huron

Brook Trout, (Salvellnus tontlnalls)
  In Lake Ontario

Walleye (Stlzostedlon v. vltreum):
  Lake Michigan

  Lake Erie

Common carp (Ctenopharynqodon  Idella):
  Lake Erie
  Lake Huron
  Lake Michigan (2)
                          Rainbow Trout (Salmo galrdnerl).
                            Lake Ontario
                                                                          C14, 45; C15, 820; C16, 700; C17, 1000;
                                                                          C1B, 350

                                                                          C14, 1; C15, 15; C16, 8; C17, 10; C18, 3
                                                                          C14. 1; C15. 16; C16, 8; C17. 10; C18, 3

                                                                          C14. 1.1; Clc, 0.64; Clf,, 0.44;
                                                                          C17, <0.005; C18, <0.005

                                                                          C14, 26; C15, 9; C16. 2; C17. 1; C18, 2
                                                                          C14,  10-19;  C15.  5;  C16.  ND-5;  C17, ND-4;
                                                                          C18,  trace-36
                                                                          C14,  34-40;  Cls,  24-48; C1&,  10-29;
                                                                          C17.  ND-6; C18, MD-2
                                                                          C14,  19-35;  C15.  41-61; C16.  8-16; C17,  1-4;
                                                                          C18,  1-6
                                                                          C14.  19;  C15, 9;  C16.  242; C17. <1; C18. <1

                                                                          C14,  19;  C15, 4;  C16,  3;  C17. 3;  C18,  3
                                                                          C14, 4; C15. 4; C16, 0.7;  C17. 0.7; C18, 3

                                                                          C14. 18; C15, 9; C16, 6; C17, 5; C18,  2
                                                                          C14.  5;  C15,  5;  C16.  2;  C17.  4;  C18.  2
                                                                          C14,  27; C15, 44;  C16.  34;  C17,  44;  C18.  4
                                                                          C14,  5-37;  C15,  12-73;  C16,  5-145;  C17,  6-31;
                                                                          C18,  1-4

                                                                          C14,  39; C15, 10;  C16,  2;  C17,  ND;
                                                                          C18,  NO
Rappe et al., 1981;
Stalling et al., 1982
Buser et al., 1985

Petty et al., 1983a,b
                                                                                                                                Petty et al., 1983b;
                                                                                                                                Stalling et al., 1983
Stalling et al., 1983



Stalling et al., 1983




Stalling et al., 1983




Stalling et al., 1983

-------
                                                                       TABLE 6-3 (cont.)
10
co
o
        Wildlife
        Bird


        Ecosystem
 ro
 CO

 CD
               Species
              PCDF Level (pg/g)
Herring, Sweden


Guillemot. Sweden


Herring, Sweden

Herring, Sweden

Guillemot, Sweden

Herring gull (Larus  arqentatus).
  Lake Huron

Contaminated animals and  fruits  1n  a
Netherlands Dump:
  Worms (9)
  Mouse liver (4)
  Rabbit liver (14)
  Pheasant liver  (8)
  Eel liver (2)
  Eel muscle/fat  (2)
  Reference eel muscle/fat  (3)
  Pike liver
  Pike muscle
  Pike liver 2 (3)
  P1ke muscle 2 (2)
  Minnow liver 1
  Minnow liver 2
  Blackberries (8)
  Elderberries (2)
  Pumpkin (1)
C14, 50; C15, 430; C16, 420; C17, 1400;
C18, 100

C14, 10; C15, 800; C16, 1000; C17, 2500;
C18. 250

C14. 5; C15. 8; C16, 2

C14, 4; C15, 8; C16, 2

C14, 2; C15. 184; C16, 41

C14, 15-16; C15, 28-50; C16. 40-57;
C17, 7-17; C18. 3-5
C14, ND-3020; C15, ND-300; C16, ND-2694
C14, NO-13,800; C15, 1408-23,097; C16, ND-584
C14, ND-168; 015, ND-1121; C16, ND-1081
C14. C15. C16, NO
C14, 2350-2765; C15, ND-169; Clfc, ND
C14, 4276-5193; C15, 182-558; C16, ND
C14, 41-47; C15, 134-147; C16. ND
C14, 959; C15, 975; C16. ND
C14, 41; C15, 154; C16, ND
Cl5, ND-1419; C14, Clfe, ND
C15. 263-268; C14, C16. ND
C14, 5808; Cls, C1&. ND
C14, C15, C16, ND
C14, Cls, Cle, ND
C14. C15, C16. ND
C14. C15, C16, ND
                                                                                                                                        Reference
Fish (cont.) Lake Ontario Fish:
Smelt (4)
Catfish
White Perch
Lake Trout (2)
Rainbow Trout
Ontario Salmon

3-112 C14
99 Cl4
15 C14
8.5-24 C14
200 C14
153 C14

Ryan et al., 1983





                                                                                                                                  Buser  et  al.,  1985
                                                                                                                                • Rappe et al.,  1985d
Stalling et al.,  1983
                                                                                                                                  Helda and 011e,  1985
        ND = Not detected

-------
                                  TABLE 6-4

                   PCDF Distribution In a Pond Known to be
                        Contaminated by Aroclor 1260*

TCDF
PeCDF
HxCDF
HpCDF
OCDF
Total PCOF
PCB (vg/g)
PCDF/PCB
Ratio

Sediment
0.005
0.009
0.15
0.92
0.27
1.35
60

22.5xlO~6
PCDF Concentration (pq/q)
Yellow perch
1.06
0.64
0.44
0.005
0.005
2.14
170

12.6xlO~6

Aroclor 1260
290
1330
1810
780
29
4240
neat

4.24x10"*
*Source:  Petty et al.,  1983a,b
1930A
6-12
06/23/86

-------
by  PCBs  from  Industrial  discharges  (Horn  et  al..  1979),  O'Keefe  et  al.
(1984) compared  the  PCOD and PCDF  concentrations  1n striped bass from  this
basin and  from  two  other locations  along the Atlantic  coast.   They  found
2,3,7,8-TCOF 1n  the  fish  from all  three locations with concentrations  vary-
ing  from  6 ppt  1n  Atlantic  coast  to 78  ppt  In  Hudson River.  Analysis  of
sediments and of nonmlgratory fishes confirmed the source  of  contamination.
    Among  fishes  living  Inside  and 1n  the near  surroundings of a dump  con-
taminated  with  waste organochloMne compounds, eels accumulated the  highest
levels of  PCDFs (see Tables  6-2  and  6-3).   These  amounted  to 5,000 ppt  1n
the  whole   body  and  2500 ppt  In   the  liver.  The  levels  1n  topsoll   were
1500-2400 ppt (Helda and Ol1e, 1985) (see Table 6-2).
    A search for  toxic  2,3,7,8-conta1n1ng  Isomers 1n wildlife has also  been
conducted  by many Investigators (Table  6-5).  As  expected,  the more highly
chlorinated members  bloaccumulated more than  the TCDFs.   The levels quoted
are  lower  than  the actual  levels because recoveries  varied widely  between 50
and  100% (Smith  et al.,  1984).  Stalling et  al.  (1985a,b)  have also  utilized
principal  components  analysis to  ascertain the sources of PCDFs 1n  environ-
mental  media.    The   toxic  2,3,7,8-substHuted  Isomers predominate  In  all
wildlife with  residues,   these  also being the predominant Isomers found  In
Yusho  victims.   Norstrom et  al.,   91986)   reported  that  crustaceans  can
contain Isomers other than the 2,3,7,8-substHuted.
    ZHko  and  Choi  (1973) and  ZHko  et al.   (1973)  provided the only avail-
able  Information concerning  accumulation  and metabolism  of PCDFs In  fish.
ZHko and  Choi  (1973)  fed  a  group  of 35 juvenile Atlantic  salmon  (Salmo
salar) several  times dally  for 140  days  with  dry  fish  food  spiked with  a
mixture  of 2.1, 4.4,  2.2 and  9.7  yg/g food, respectively.   An analysis  of
the  muscle  and  gut  of fish that died between the 81st and  135th day and  of
fish  that  survived for 140 days Indicated  that only OCDF  could be  detected.

1930A                               6-13                             06/23/86

-------
                  TABLE  6-5



Levels of Toxic PCDF Isomers In Wild Animals







cr>
i
*














o
\
w
00
CT>

Wildlife Sampling Site/Spec les
Animal Hudson River, U.S./
Snapping turtle fat
(Chelyda serpentlna)
Gulf of Bothnia, Sweden/
Seal fat (HaHchocrus
grupus)
Seal fat

Fish Lake Ontario, Canada
Smelt (4)
Catfish
White perch
Lake trout (2)
Rainbow trout
Ontario salmon
Pacific salmon
Eel (2)
Hudson River. Water ford. NY
Carp (5), 1981
Goldfish (5). 1981

Hudson River, Albany, NY
Goldfish (3), 1981
Hudson River, Tappan Zee Bridge
Striped bass (9). 1981
Striped bass (4). 1983
Hudson River, Poughkeepsle
Striped bass (2), 1983
PCDF (pq/q)
«v
- 1
1 1 1 ooeo
, , coco co co f"- —
«o _ r»___ r~.r"j; ' — >*— •**>*

45 620

1 15

1 1 15 4


3.2-34
54
15
9-24
12
79
<10
NO

5
<9


<5

54
56

74-78

ci ,1
r- a
*7: *•£ Reference

Rappe et al.,
1981

Rappe et al.,
1981
5 5 Buser et al.,
1985

Ryan et al..
1983






O'Keefe
et al., 1984
O'Keefe
et al.. 1984
O'Keefe
et al.. 1984
O'Keefe
et al.. 1984

O'Keefe
et al.. 1984

-------
TABLE 6-5 (cont.)
vO
CO
o
3»










I
















0
^
ro
Jj*
CD

Wildlife Sampling Site/Species
Fish Bayonne Bridge. Newark Bay
(cont.) Striped bass. 1983
Chesapeake Bay, MD
Striped bass (4). 1983
Long Island, NY
Striped bass (4), 1983
Rhode Island Coast (4), 1983
Striped bass (5), 1982
Common carp 1
2
Grass carp

Sweden
Herring
Guillemot
Herring
Herring
Guillemot
Bird Hudson River, Catsklll. NY
Black duck (6), 1980
Mallard duck, (12), 1980
Wood duck. 1980
Green Bay and Lake Michigan, WI
Night heron (Nyctlcorax
nyctlcorax)
1978
1982
Cormorant (Phalacrocorax aurlth)
1983

Herring Gull 1
2
PCOF (Da/a)
X.
COCO CO 0
00 r*> p- r» — » r* — » r- •*—
• — • •.— • • » irt « \ft U"»
ntj oo CM co *— • CM -— n-—
CM CM i— (— r- CM

26

8.5

16
25
14
11 2 2 5 11
11 3 314
1.5 211


50 100 80 250
10 50 750
41 116
31 116
2 trace 4 180

79
44
13



<2-8
4

2

4 <2 <2 16
2 <2 <2 20

> ,
oo oo r- oc
**" r""£ * 71 * ^ Reference
r> co — «*> ^ r> «

-------
The  detection  limit was  -0.02 yg/g  wet  weight  for  PCOF,  TrCDF  and  TCDF.
The  concentration  of OCDF  1n muscle  was  0.03  yg/g  1n  dead  fish and  0.01
yg/g  In  surviving  fish.   The  concentrations  in gut   were  0.21  yg/g  In
dead  fish  and  0.02  yg/g  In  living  fish.   The  percent  Hpid  In  muscle  and
gut  of  dead  and  surviving fish was also measured  and found to be higher  in
gut.  Concentrations  of  OCDF  1n  I1p1d were calculated  to  be  3.53 yg/g  and
1.30  yg/g  In muscle  of   dead  and alive  fish,  respectively,  and  17.36  and
0.99  yg/g,  respectively,  in  gut  of  dead and  live  fish.   Although  the
concentration of OCDF was higher  In dying  fish than  1n  surviving  fish,  it  1s
unknown whether OCDF  caused  the  toxic effects.  The  data indicate,  however,
that  the  concentration  of  OCDF  in fish was considerably lower  than 1n  the
spiked food.
    Zitko  et  al.   (1973)  also showed  that only a small  portion  of  orally
administered 2,8-DCDF was accumulated  1n  the   tissues of  brook trout  (Salve-
linus  fontinalis).   Several  fish were  fed a cumulative  dose  (In  gelatin
capsules)  of  107-361  yg DCDF/g  wet  fish weight   over  variable  exposure
periods.   The   tissue    residues  ranged   between  0.052  and  0.340   yg/g
(0.01-0.13%  of  administered  dose)  1n muscle and  between 0.146 and  1.04
yg/g  (0.08-0.4% of administered  dose)  1n  liver.  Mass  spectral analysis  of
the  organic compounds Isolated from  the water  containing  excreta  from one of
the  fish indicated the presence of a DCDF  and  of a hydroxy-DCDF metabolite.
    The  results  of Zitko et  al.   (1973) and ZHko and Choi  (1973)  indicate
that  PCDFs are poorly absorbed  1n the gut of fish.   The  limited metabolic
information  provided  by  Zitko  et  al.   (1973)  suggests  that   DCDFs  are
hydroxylated by aquatic organisms.
6.2.5.   In Birds.   Tables  6-3 and 6-5 summarize  the present  data.   O'Keefe
et  al.  (1984)  determined   the   presence   of   PCDF   in   three  duck  species


1930A                               6-16                             06/23/86

-------
collected near the Hudson River.   Concentrations  of  2,3,7,8-TCDF  ranged  from
13-79 ppt  1n  fat tissues.  PCDFs  and  PCDDs  were also detected In  birds  and
bird  eggs  In  Wisconsin  (Stalling  et  al.,  1985a).   2,3,7,8-Chlorlnated
congeners were the major constituents.  The  pattern  of PCDF  and PCDD contam-
ination  was  compared  In  birds and  fishes  living  In the  same  Great  Lakes
area.  The ratio  of  PCDFs  to PCDDs  1n  bird  eggs were lower than  In  fish of
the Great  Lakes,  Indicating  that  1n birds the  rate  of metabolism of  PCDF 1s
probably higher than that of PCDDs.
6.2.6.   In Terrestrial  Animals.   These  data are summarized  1n Tables  6-3
and  6-5.   TCDFs were  determined  In tissues  of a horse  grazing close  to a
wire  reclamation  Incinerator;  TCDF (unspecified Isomers)  concentrations  were
165 pg/g  In the  fat  and  57  pg/g In the liver with unspecified TCDD levels of
45 and <6  pg/g  1n  the  fat  and liver, respectively (Hryhorczuk et al., 1981).
Recently  Rappe  et al.  (1985) found 2,3,7,8-chlorlnated  PCDFs and  PCDDs 1n
milk  from cows  that  had  grazed  near  an  Incinerator 1n  Switzerland.   The
levels were found  to be  related to the distance between the grazing area and
Incinerator.
    Helda  and  OHe  (1985)  analyzed soil  and  biological  samples  collected
from  a  household waste dump  near  Amsterdam, which  appeared  to be seriously
contaminated  with  organochlorlne  compounds (2,4,5-T, dlchlorobenll, Undane,
tetrachlorodlfon).   Fish,  game animals,  worms  and mice  contained measurable
amounts  of the  most toxic PCDDs  and  PCDFs  (see  Tables  6-2  and 6-3).   The
highest  levels  were detected  In  fish,  especially eel  (see  Table 6-2).   The
worms  tended  to  have  the same congeneric  pattern  as soil  (see  Table 6-3),
while  1n mice the toxic Isomers prevailed  probably  as a result of differen-
tial  blodegradatlon  and excretion  rates.
 1930A                               6-17                             06/23/86

-------
    Recently, Ryan  et  al.  (1985a)  found PCDDs and  PCDFs  1n 40  chicken  and
pork tissue  samples also  positive  for  pentachlorophenol.   HxCDDs,  HpCDDs  and
OCDDs were present  In 50, 62 and 46% of  the samples  at mean levels of 27, 52
and 90  ppt,  respectively.  Similar  levels  of  HxCDF  and HpCOF were  found In
some of  these samples.   TCOFs,  PeCOFs and OCOF were  not  detected.  Compari-
son of  the  congeneric  patterns of  the chicken samples with  those of penta-
chlorophenol -treated wood Indicated  that pentachlorophenol was  probably  the
main  source  of  contamination.   Residues  1n   humans   are   considered   1n
Chapter 7.
6.3.   EXPOSURE
6.3.1.    Food.   Food may  be an  Important  route of exposure since  PCOFs have
high bloaccumulatlon  coefficients   (Section  5.5.).   Since their  concentra-
tions 1n PCBs 1s of most  concern,  It 1s  Instructive  to calculate the maximum
PCDF exposure levels associated with PCS exposure.
    The  present  dietary  Intake  1n the  United States of  PCBs  from  fish Is
-175 yg/day  (Cordle et  al.,  1978).   If  the  amount  of  2,3,7,8-TCDF  Is  the
same as  In a used Kanechlor 400  formulation  (similar  to  Aroclor  1248), I.e.,
1.25 ppm, the amount of  this Isomer  stored  1f  there  1s no excretion would be
-0.2 ng/day.
    Workplace air  levels of Aroclor 1242 can range as  high as  2.22 mg/m3
(Ouw et  al., 1976).   If 1t  1s present  as airborne  partlculate,  It  would
contain  ~3  ng/m3  of the  2,3,7,8-TCDF.   If  the same assumptions are used to
estimate the levels of  this Isomer 1n fish, the  levels of  PCBs  reported  for
various  environmental   compartments  are  as  follows:   ambient  air  (<100
ng/m3),  surface  waters   (10-50  ng/i),  foundry  effluent   (12-335  ppb),
paper mill  effluents  (0.01-25  ppb),  snow (0.17-0.24 ppb), wastewater (<520
ng/a)  and  sewage  sludge  (16  mg/kg)  (Chapter 4).   PCB   residues   1n  human


1930A                               6-18                             06/23/86

-------
adipose  tissues   1n  the  United States  are  near  detection  limits:   below
detection limit (34.2%), <1 ppm  (33.3%),  1-2  ppm  (27.3%)  and  >5.2 ppm (5.2%)
(Yobs, 1972).  Human milk  can contain up to  100 ppb of PCBs  (Savage et al.,
1973).  HxCDFs, HpCDFs and OCDFs have  been  detected  In  cow's  milk, blood and
tissue  fat,   after  pentachlorophenol  was  Ingested  1n  the  feed  by  a  cow
(Firestone et  al.,  1979).  Thus cow's  milk may be  a  source  of  exposure  to
animals exposed to  PCDFs/PCDOs.  Nygren et al. (1986) also reported low ppt
levels of  PCDFs  and  PCDDs In  samples of  bovine fat, bovine  milk, and  1n
commercial cream  from  Sweden  and Scotland.  Rappe et al.  (1985e) also  docu-
mented the PCDFs  and PCDDs  In bovine  milk from Switzerland, with the highest
levels being  found  In  samples collected  1n proximity to  municipal and  other
Incinerators.  Human milk 1s also another  possible source  (Chapter 7).
    Concern  has   been  expressed  over  the  formation  of  PCDDs  during  the
cooking of food.  Liver,  steak  and  hamburger  from  female  Holstelns have been
examined, but  only  raw liver  contained significant amounts of  PCDDs;  levels
decreased when the liver  was cooked.  Variation  from  sample  to  sample was
high  so  that  no  firm  conclusions  could be reached (Zablk and  Zablk,  1980).
The situation  1s  rather different  for  the PCDFs, especially If  the tissues
contain PCBs.  The  PCDFs  might possibly  be formed from PCBs  during cooking,
by  the mechanisms  cited  1n  Section  2.5.2.1., and  verification of  this  Is
Important.  Cooking appears to decrease PCB  levels 1n foods  such as poultry
and milk as well  as PBB  levels  1n  poultry (Zablk  et  al.,  1978).  The decline
appears to be  related  to the  amount of fat rendered  In the cooking process,
although  a  complete  mass balance  should  be made  using GC/MS.   Firestone
(1977b) found  0.4 ppb  of HpCDFs and 0.4  ppb  of OCDFs  In  2 of  15 commercial
U.S. gelatins.  PeCDFs, HxCDFs and  HpCDFs  were found  1n  one Mexican sample.
1930A                               6-19                             06/23/86

-------
    It was thought that the PCDOs/PCDFs  In  fly  ash  would not be bloavallable
on Ingestlon  (Hutzlnger  et al.. 1985b),  but  rats,  guinea pigs  and hamsters
fed fly  ash  admixed with  their food  showed  2,3,7,8-substltuted  Isomers  1n
their   livers   (Berg  et  al.,   1985a).   These  results  Imply  that  fly  ash-
contaminated   food,  or  particles  1n  the air  whose  size  1s  greater  than
resplrable (15  vm)  and  which  are  cleared  eventually  to  the  stomach,  will
be partially  absorbed  by animals and probably  humans.
6.3.2.   A1r.    The  Inhalation  of  fly  ash  particles  containing  PCDDs  and
PCDFs  1s  likely around  municipal Incinerators  1n  addition  to  PCDFs  emitted
In automobile exhaust (Ballschmlter  et  al.,  1986).   PCDFs and  PCDDs  In both
vapor  and partlculate  form have  been detected  1n Germany  (Oehme et  al.,
1986).  The vapor and resplrable particles will be  absorbed  through the lung
alveoli,   and   the  nonresplrable   partlculate  fraction  may   be  partially
Ingested.
    Another source  of PCDF  exposure Is  during and  after  electrical  fires
where  PCBs were originally present  (Chapter  4).   Risk  of exposure to PCDFs
Is high  for  fireman  fighting  electrical  fires and the extent  of  exposures
should be Investigated  as should  workplaces  Involving PCBs   Including  the
following:  chemical  plant handling or manufacturing  halogenated aromatlcs;
factories  making or  repairing  transformers   or  capacitors,  using  casting
waxes  or  having heat-exchange systems;  In offices  utilizing carbonless copy
paper  containing PCBs; and during Incineration of  halogenated aromatlcs.
6.3.3.   Other  Exposure  Routes.  Analysis  of  latex  nipples  (Gorskl,  1981)
revealed   PCDDs  and  PCDFs  to  be present.  TCDFs and  PeCDFs  were  not  found,
but HxCDFs (0.02-0.8  ppb), HpCDFs  (0.1-3.1  ppb) and OCDFs (0.3-28 ppb) were
confirmed.  These were  not extractable by water, unlike pentachlorophenol.
1930A                               6-20                             06/24/86

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Gamma-Irradiation of the nipples  for  sterilization  purposes  was suggested as
a  possible way  that  toxic   Isomers  could  be  produced.    Exposure  through
drinking water 1s unlikely.
1930A                               6-21                              06/23/86

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           7.   TOXICOLOGICAL  EFFECTS  IN  HAN  AND  EXPERIMENTAL  ANIMALS
7.1.   SUMMARY OF EFFECTS OF  POLYCHLORINATED DIBENZOFURANS
7.1.1.   Tox1cok1net1cs.   PCDFs  are  easily  absorbed by  passive  diffusion
across cell membranes.   For  the highest  chlorinated  congeners  I1poph1l1dty
can  result  1n  such  Insolubility that  absorption may  be strongly  Impeded.
The  congeners  with  2,3,7,8 chlorine-substitution are retained  In  tissues  of
animals and humans.  The presence of  two  adjacent unsubstltuted carbon atoms
predispose towards metabolism and hence excretion;  therefore these congeners
have  not   been  detected  1n  the  tissues  of animals and humans  even  when
exposed  to high  levels.   Broad  species  variations  have been observed  1n
metabolism and  excretion;  the  position  that humans  occupy  regarding meta-
bolic  fate  and excretion  relative  to  other  species  1s  still  undetermined.
Physiological  pharmacoklnetlc models developed  1n  some animal  species  do not
permit  extrapolation  to man since  little  metabolic Information  about  the
pattern of  the different  Isomers within  species Is  available.  Some  of the
most relevant  features are  summarized here.
    Studies  on   the  absorption,  metabolism  and   elimination of   labeled
2,3,7,7-TCDF  and  of  a  mixture  of   PCDFs  consisting  of  tetra-,  penta- and
hexa-CDFs In laboratory animals (rats,  guinea pigs, monkeys,  mice)  show that
CDFs  preferentially  accumulate In  the  liver and fat.   The  2,3,4,7,8-PeCOF
accumulated more  than other  Isomers  In  the  livers of monkeys and  rats dosed
repeatedly with the mixture.   Accumulation  of the same Isomer  several years
after  accidental  contamination  was  also  observed   In  the   liver  of  human
patients with  Yusho  or  Yu-Cheng disease.   Accumulation  of  PCDFs across  the
placenta 1n the  rat  fetus  Is limited,  but  transfer  to suckling offspring  Is
much  greater.   In the  rat,  the whole-body  half-life of  2,3,7,8-TCDF  1s  <2
days  after  a  single  1.v.  dose of  30.6 yg/kg  bw.   In  contrast, the  guinea


1931A                               7-1                               06/30/86

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pig has  a  minimum whole-body half-life of  20  days  after a single  1.v.  dose
of 6  vg/kg.  A  maximum whole-body half-life  of  40 days  was calculated  In
guinea pigs manifesting no toxic effects.   Intermediate  behavior  1s apparent
1n the monkey with a whole-body half-life of 8  days  after  a  single  1.v.  dose
of 30.6  vg/kg.   In all  3 species, excretion  of  unmetabollzed  2,3,7,8-TCDF
1s negligible and  Us  metab6Hsm  appears  to represent a detoxification  pro-
cess.   Excretion 1s predominantly  by feces.
    Highly chlorinated Homers accumulate In the liver and adipose  tissue  of
humans and  persist for  many years.   2,3,4,7,8-PeCDF  and 1,2,3,4,7,8-HxCDF
are retained by the liver at  higher concentrations than  other  Isomers.   They
have been detected 1n  the Hver and the adipose tissue  of  Yusho  and Yu-Cheng
patients  many years  after Intoxication.   PCDFs and  PCDDs  have been  assayed
In tissues  of patients 2 years  or more after exposure  In  a  building contam-
inated with these compounds;  levels of PCOFs were elevated,  especially  those
Isomers found In the building.  Many of these were  similar to those found  1n
Yusho and  Yu-Cheng  patients.  Surprisingly, high levels of  2,3,7,8-chlorlne
substituted congeners  have  been  found In adipose  tissue and  1n  breast  milk
of the  general   population   from  highly  Industrialized  countries  of  Europe
and North   America.   Lower   levels  have  been  detected  In populations  from
North Vietnam  that was  considered  not contaminated by  phenoxy   add  herbi-
cides  and   that  had  a  low   level  of  Industrial  contamination.   Therefore
levels of  PCOFs  In  fat biopsies  should be  considered as a useful biological
Indicator of levels of exposure  for ep1dem1olog1cal  studies.
    Studies  establishing the human metabolism and  the  kinetics  of  these
compounds are still  needed.   The kinetics  of  the more  persistent  hexa- and
hepta-1somers warrant  Intensive Investigations.  When  the  general population
Is exposed  to unknown  contamination through the food chain and air, subjects


1931A                               7-2                              06/30/86

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with a  high body  burden  can transmit  toxic  PCDFs  to their  progeny  through
placenta and milk, Indicating that such babies are a population at high risk.
7.1.2.    Tox1c1ty.   Some   PCDFs   have  high  acute  toxlclty.   -.The 2,3,7,8-
TCDF, and 1,2,3,7,8- and 2,3,4,7,8-PeCDFs are  some  of  the  most acutely toxic
Isomers.   The  acute  oral  LD5Q  of  2,3,7,8-TCDF  1s  5-10 vg/kg In  guinea
pigs  (2-4  times  higher than  2,3,7,8-TCDD),  >6000  yg/kg  In  the mouse  and
the  rat  (20 times  higher  than 2,3,7,8-TCDD),  and  1000  yg/kg  In  the  rhesus
monkey.   The  symptoms  of  toxlclty  were very  similar  to  those  reported  for
2,3,7,8-TCDD; for example, thymlc atrophy  1n  all  species;  liver pathology 1n
rabbits,  rats  and mice; hydroperlcardlum  1n  chicks;  alteration  of skin  and
adnexa,  liver  bile duct  and  gastrointestinal  tract  1n  addition to  hyper-
plastic  and metaplastlc changes  In the melbomlan  glands  of  the  eyelid  and
the cerumlnous glands of the ear  canal  1n  the rhesus  monkey.   The eyelid and
ear canal are  the most  sensitive Indicators of PCDF  toxlclty 1n the  monkey.
There  Is  a  lag of several  days between  administration and the appearance of
clinical  toxic  responses.  Two of three monkeys died  on a diet containing 5
vg/kg  (food)  administered  over  6  months.   The  acute  LD™  values,   In
yg/kg,   for  Hartley  strain  guinea  pigs   over  30  days   are  as  follows:
2,3,7,8-TCDF    (7);   2,3,4,7,8-PeCDF    (<10);    2,3,7,8-TBDF   (<15);   and
2,3,4,6,7,8-HxCDF (120).
    It   Is  highly  probable  that  continuous  exposure  at  low  levels  causes
cumulative  toxic effects,  especially  In  view of  the  lesions  observed  1n
monkeys at an acute dose,  which was  <4% of  the LD,0.
    Few studies  relate to  the  subacute  toxlclty of  PCDFs.   The most  complete
data concern  the effect of  2,3,7,8-TCDF on  mice,  chicken, guinea pigs  and
rhesus  monkeys.   Common  signs  for  various  species  seem to be  a  decrease In
body weight and  Involution of  the thymus.   In  some  species (rodents and mon-
1931A                               7-3                              06/22/86

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keys)  "hver  morphological lesions  were observed  such as  changes of  endo-
plasmlc  retlculum,   cytoplasmlc   I1p1d  droplets  and  mltochondrlal  altera-
tions.  These  ultrastructural  effects  should  be considered with  particular
attention and  carefully  controlled  1n planned studies using single Isomers,
as  such  alterations have been recently  observed 1n  the  Hver of  patients
known  to  be exposed to  PCDFs.  Ultrastructural  alterations  of Hver  mito-
chondria In Hver biopsies, together  with  the  monitoring of  the contaminants
1n  fat biopsies,  are  useful  biological   markers  for exposure  to PCDF  and
related chemicals.
    It appears likely that PCDFs contribute  substantially  to the toxlclty of
commercial  PCBs  and polychlorophenols  and are responsible for  the symptom-
atology of Yusho and Yu-Cheng diseases.
    Dermal  toxlclty  Is  a common effect In animal species  Including  humans.
However,  the  different   species  develop   different   types  of   skin  lesions.
After  treatment  with  various  mixtures  of  PCBs,  rabbits  and  rats  develop
lesions resembling the chloracne observed  1n Yusho and Yu-Cheng patients.
    Information  on  PCOF  effects  on the  Immune  system  1s   stm  limited,
although reduction  1n thymus weight  and humoral  antibody  production has been
observed  1n  all  the  animal   species  tested.   The   results with   pure  PCDF
Isomers  show  that the pattern  of  1mmunotox1c1ty for  PCDF-active  Isomers 1s
similar to  that  of  the  corresponding PCDD  Isomers,  provided that higher dos-
ages  are  given  to  laboratory  animals.   Data  obtained with 2,3,7,8-TCDD In
mouse  strains  eliciting  different sensitivities  to  Induction  of aryl hydro-
carbon-hydroxylase  (AHH), suggest  that  the Individual genetic  background may
play a role 1n the degree of PCDF-1nduced  Immunotoxlclty.
 1931A                               7-4                              06/22/86

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    A number  of PCOF  Isomers  show the capacity  to cause a  relatively  high
degree of Induction of some  liver  mixed function  oxygenases,  such as AHH and
ethoxyresoruf1n-o-deethylase (EROO)  both  In yjvo  and  ±n vitro.   AHH  Induc-
tion  activity  has  two  structural requirements:   first,  halogen  atoms  must
occupy at least  3  of the 4  lateral  ring  positions (2, 3, 7  and  8);  second,
at least 1 vicinal  carbon  position must be unsubstHuted.  Structureactlvlty
studies conducted in  vitro  demonstrated  the existence of a  broad difference
In potency of  PCDF Induction.  The  lack  of kinetic studies  In  rodents  does
not  allow precise  comparisons  to  be  made  between  In  vitro  and in  vivo
results.  However,  recently good  correlations were  obtained  by  plotting the
Inducing  capacity  of  AHH   of  a  single  PCDF  congener versus  the  rat  body
weight  loss  or  thymlc  atrophy.   This  approach  seems   to   be  particularly
useful for testing mixtures of PCDFs  with  an unknown exact composition.
    Biochemical  studies  have   shown  that  for  the manifestation of  their
Inducing effect  PCDFs must  bind  to  a  cytosollc  protein binding  site.   The
occupancy of  the receptor   seems  to  be crucial.  This event  not  only  causes
AHH and  EROD  Induction  but (more  Important) represents  the  first step  trig-
gering the toxic effects displayed by  these compounds.  Recent  results  on on
the  Interaction  of  TCDD with  EGF  receptor or with  receptor  protein present
In the  thymlc  epithelial cells reinforce  this point  of  view.   So far  there
are  no  Indications  that  AHH Induction could  be a cause  of  toxldty  per se,
but this fact could be an  Indication of  the potential  susceptibility of  this
organism to more profound toxic signs.
7.1.3.   Epidemiology.   Information  on  the toxic  effects   of  PCDF  In  man
comes mostly  from  Japan and  Taiwan where 1n  1968 and  1979,  respectively,
many  people ate  rice  oil that was later  found  to  be contaminated with  PCBs,
PCDFs and PCQ.   More  than  4000 people  1n  the  two episodes were Intoxicated.


1931A                               7-5                              06/22/86

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Some general symptoms Included:  retarded growth, abnormal  I1p1d  metabolism,
liver  disturbances,   acneform  eruption,   skin   pigmentation   and  cutaneous
lesions.  The  clinical  profile of  this  syndrome has  been well  defined  but
long-term toxldty, carcinogenic risk  and  mortality rate consequent  to  PCDF
exposure have not yet  been assessed.
7.2.   INTRODUCTION
    The toxlclty of PCDFs  1n  laboratory  animals has received  attention  as  a
consequence  of  their  Identification  In  widely  used  Industrial  chemicals,
such as the  PCBs and  polychlorophenols.   Evidence 1s accumulating  that  many
of  the  toxic  effects  of  various  commercial  chemicals  may actually  result
from traces  of  PCDFs.   The  critical observation leading  to  the hypothesis
that a  trace contaminant might  be  the  major  toxic factor was  made by Vos and
Koeman  (1970)  who found  significant differences In  toxlclty  between  three
commercial  PCB  preparations.   Later,  Vos  et  al.  (1970)  showed  that  most
acutely toxic  preparation  contained  TCDFs and  PeCDFs.   Out of  135 possible
Isomers of  PCDFs only  10-12  are expected  to have  significant  acute toxlc-
lty.  The  most acutely toxic  Isomers  appear  to be 2,3,7,8-TCDF, 1,2,3,7,8-
PeCDF and 2,3,4,7,8-PeCDF  (McKlnney  et al., 1976; Poland et al.,  1976;  Moore
et  al.,  1979).  Dlbenzofuran  (DF)  and OCDF  have low acute  toxlclty (Gold-
stein et al.,  1978b).   Toxlcologlcal studies  of PCDFs  reveal  marked similar-
ities to  the effects  of PCDDs  (Moore  et al., 1979; WHO, 1978b).   The estim-
ated  difference  1n  toxlclty  between  2,3,7,8-TCDO  and  2,3,7,8-TCDF Is  at
least 10-fold  (Klmbrough,  1974; Klmbrough et  al., 1978;  Moore et al., 1979),
but  It  1s  consistently  dependent on  the  animal  species  considered and on the
specific  parameter  Investigated.    The  earlier  studies  were  essentially
devoted  to  Identifying  the  acute toxic  effects.  The  series  of  Incidents
Involving  a  large number  of  people  from  the general  population  or  from


1931A                                7-6                              06/22/86

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exposed workers  In  which  PCDFs  have been Implicated  as  the major class  of
compounds  responsible  for  the  toxic  effects  have  prompted researchers  to
design more extensive  studies on  the kinetics, subchronlc toxlclty and  bio-
chemical mechanisms.  Therefore, studies on  long-term  effects of  these  chem-
icals are warranted.
7.3.   TOXICOKINETICS
7.3.1.   Introduction.   The  disposition  of the PCDFs  In  animals  depends  on
the  physlcochemlcal  properties  of  the single  Isomers.  Their relative  lipld
solubility,  which  Increases  with  Increasing  halogenatlon,  promotes  their
passive absorption  from  the gastrointestinal tract but Impedes  their  excre-
tion directly 1n  the urine  and  the  bile.   In addition, since PCDFs are  Upo-
phlUc, animals  with high adipose  weight/body weight  ratios tend  to  retain
them.  Thus, metabolism  1s  the  rate-limiting factor 1n the  fate  of PCDFs  In
animals.  A particular aspect  that  must be  considered  In  assessing the  b1o-
avallablHty Is  the Influence  of  environmental  matrices,  route  of adminis-
tration and  vehicles when  PCDFs  come from  environmental  pollution or  from
contamination of chemicals (Kamlnsky et al.,  1985).
    Metabolism  Is  also  dependent   on  molecular   characteristics,  since  the
less highly  halogenated  Isomers and those with unsubstHuted vicinal  carbon
atoms  are  more  readily  metabolized.   In all  animal  species  studied,  the
metabolites, and  to some  extent the parent  compound,  are  excreted preferen-
tially 1n the feces, through the bile and to  a  lesser extent  1n  the urine.
    Data  on  distribution,  metabolism  and  excretion  of  2,3,7,8-TCDF  are
available  for  several  different animal  species.   Recently, a  physiological
pharmacoklnetlc model was developed for 2,3,7,8-TCDF (King  et al., 1983).
7.3.2.   Absorption.   PCDFs  are  I1p1d  soluble  compounds  and  are absorbed
                                                                       a
from the gastrointestinal  tract by  passive diffusion  across  cell  membranes.


1931A                               7-7                             06/22/86

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In rats  (Blrnbaum et al.,  1980,  Decad et  al.,  1982), mice  {Decad et al.,
1981a;  1982)  and  guinea  pigs  (Decad et  al.,  1981b;  1982)   2,3,7,8-TCDF
appears to be absorbed to a very high  degree.  In  guinea  pigs, absorption  of
TCDF  was estimated at >95% 1n  the gut  after  an oral  exposure.
    As for other halogenated compounds (Damstra et al., 1982) the  absorption
tends  to  decrease  with  Increasing  halogenatlon above  a certain  point.  For
the  1,2,4,6,8,9-HxCDF the degree of  absorption  seems  to  be  lower than for
TCDF   (Blrnbaum,  1985).   That  highly halogenated PCDFs  could  be  less  easily
absorbed  has  been  suggested  but  not Investigated  because  of  the lack  of
appreciable amounts of the various  congeners needed  for  these  studies.
    Absorption  can also  be  strongly  Influenced  by  the  vehicle.   In the
guinea  pig acute  toxlclty  of  2,3,7,8-TCDD (LD™)  1s  approximately one-
eighth  of Its  LD    In  corn  oil  (Sllkworth et  al.,  1982)  and  3-5  times
higher levels of TCDD are needed to cause toxic effects when  they  are  admin-
istered mixed  with dirt  (McConnell  et al.,  1984).   It  has  been  suggested
that   similar  differences  may also  apply  to PCDF  (SUkworth  et  al.,  1982).
However,  direct  evidence Is  lacking   for PCDF.   Berg  (1985b,  1986)  report
that   the  bloavallablUty of PCDF absorbed on fly ash  of a  municipal Inciner-
ator   and  administered with  the  diet  was  very scant  In  different animal spe-
cies.
7.3.3.   Distribution,  Metabolism   and  Excretion.   Disposition  has  been
studied 1n various animal species.   However, a critical comparative analysis
of the  results  Is  difficult as PCDF mixtures of variable  (and In  some cases
unknown)  composition  have been  used  and  the experimental  conditions,  doses,
routes  of administration, duration and schedules  of data recording  differ.
Only  a few  trials used  single purified PCDF  Isomers.   However, from all
   o
these  data, which  are summarized  1n  the  following  sections,  1L  appears that
1931A                               7-8                              06/22/86

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liver and adipose tissue are the preferential  tissues  for  localization,  that
elimination 1s by metabolism, and that metabolites,  once  formed,  are excret-
ed without delay.
    7.3.3.1.   RAT — Kurokl  et  al.  (1980)   used   a  PCDF  mixture   (14%
1,2,7,8-TCDF;  35% 2.3.7.8-TCOF;  1%  1,2,4,7,8-PeCDF;  49%  1,2,3,7,8-PeCDF;  1%
2,3,4,7,8-PeCDF; and 1% unspecified HeCDF)  to  Investigate  the  persistence  of
PCDF In  the liver of rats and monkeys.  Four  male Wlstar  rats  (-100 g  and 4
weeks of  age) were  given  a single 1.p.  dose  of PCDF 10 mg/kg bw.   The  rats
were killed after  5 days  and  their  livers were  removed  for GC/MS  assay  of
PCDF.   The   data   are   presented   In  Table   7-1.    The   1,2,7,8-TCDF   and
1,2,4,7,8-PeCDF   were not   detected,  and  the  2,3,7,8-TCDF  was  present  at
0.6-2/5%  of  the total   dose.   The  amounts  of  2,3,4,7,8-PeCDF  and  HeCDFs
retained  1n the  liver were 76-82% and 100% of the  total  dose,  respectively.
Thus, 2,3,7,8-TCDF  was  eliminated  from the liver 1n  these  rats  with a  resi-
dence half-time of ~1 day.
    Blrnbaum  et  al.  (1980) and Decad  et al.,  1982  Investigated  the absorp-
tion, distribution  and  excretion of  radlolabeled 2,3,7,8-TCDF  In  200-500 g
male Fisher 344 rats.   The  compound  was administered at oral doses  of  30.6
(0.1  ymol/kg)  and  306  ymol/kg (1.0  yg/kg  bw), and  at  an   1.v.  dose  of
30.6  yg/kg bw.   About  90% of  both  oral doses was  absorbed.   Table  7-2
shows  that the  adrenals,   liver,  lungs  and   kidneys  contained, the  highest
level  of  radioactivity  15 minutes  after   the 1.v.  Injection   (0.1  pmol/kg
bw).  Subsequent redistribution to  adipose  tissue  followed,  the  concentra-
tion was  maximum there  7  hours  after  administration.   The pattern of distri-
bution  of radlolabel 1n  liver  fat  muscle, skin  and blood, and  the amounts
excreted  In urine  and  feces 3  days  after  administration  were  essentially
Independent of  the  dose  and  route of administration (Table 7-3).   No  evl-


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                                                       TABLE 7-1

          Percentages of the Total Intake of Original PCDF Isomers Found In the Livers of Monkeys and Ratsa.b
      Mixture  Administered
                                  1,2,7,8-
                                   (14%)
2,3,7,8-
  (35%)
                                                                       CDF
1,2,4,7,8-
   (IX)
1,2,3,7,8-
  (49%)
                                                                                          2,3,4,7,8-
                                                                                             (1%)
               Hexa-
               (1%)
      Male  Hlstar  Rat
      (100  g)
                  1
                  2
                  3
      Mean  *  S.D.
                                     ND
                                     ND
                                     ND
                                     ND

                                     ND
1
1.5
2.5
0.6

1.4*0.8
 ND
 ND
 ND
 ND

 ND
   18
   17
   21
   11

   18*3
81
80
82
                                                                                           80*3
109
104
108
107

107*2
i
o
      Rhesus  Monkey

                  1
                  2
                  3

      Mean  *  S.D.
                                    ND
                                    ND
                                    ND

                                    ND
0.02
0.09
0.04*0.05
 0.4
 0.3
 0.2*0.2
   0.2
   0.2
   0.2

   0.2
5.2
1.7
0.8

2.6*2.3
0.8
0.1
ND

0.3*0.4
o
V.
ro

CO
     aSource: Kurokl et al., 1980

     bThree  monkeys  were  fed  Kanechlor  400 (0.25; 0.5  mg/kg  bw) and PCDF  (1.25;  2.5 vg/kg  bw)  for up  to  32
      days.   Rats were  Injected  l.p.  with 10  mg PCDF/kg  bw and  killed after  5 days.   The total  Ingested
      Kanechlor  400  was  86, 88  and  30 mg  In  monkeys  designated  1,  2 and 3, respectively; the total  Ingested
      PCDF  was  430,  440  and 151  wg,  respectively.   Levels  of Kanechlor  1n  the liver were  1.7,  0.8 and  0.04
      ppm,  and  of PCDF 5.4, 4.2 and 1.1 ppb, respectively.   Levels of  Kanechlor  In  fat were 8.6,  25 and  1.2
      ppm, and of PCDF 0.9, 26 and 0.2 ppb,  respectively.

     ND = Not detectable

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                                  TABLE 7-2
    Concentration of "C-2.3.7.8-TCOF 1n Tissues of Male Fisher 344 Ratsa»b
Tissue
Blood
Liver
Fat
Muscle
Skin
Kidneys
Adrenals
Thyrus
Spleen
Testes
Brain
Lungs
Heart

15 Minutes
0.12±0.04
4.4 ±0.2
0.20±0.03
0.25±0.01
0.17±0.02
0.67±0.04
7.4 ±6.9
0.52±0.12
0.37±0.07
0.09±0.01
0.25±0.01
1.08^0.08
0.66i0.03
% Total Label (q/tlssue basis)
180 Minutes
0.04±0.01
5.1 ±0.4
0.44±0.07
0.06±0.00
0.20i0.01
0.17±0.03
4.7 tl.3
0.54±0.13
0.08±0.02
0.09±0.01
0.15±0.03
0.24±0.02
0.1HO.OO

1 Day
0.03*0.01
2.2 ±0.4
0.64±0.11
0.30±0.02
0.07±0.01
0.08±0.01
0.34±0.14
0.07±0.03
0.02±0.00
0.06±0.02
0.02±0.00
0.07±0.02
0.02±0.02
aSource: Blrnbaum et al.,  1980
bDosed with 0.1  ymol/kg bw 1.v.
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dence  of  enterohepatlc   circulation  was  found      Examination  of  tissue
extracts showed that nearly all radlolabel 1n  blood  and  tissues,  at least up
to 1  day postadmlnlstratlon, was  present  as unchanged  2,3,7,8-TCDF.   Thus,
the  half-time  of  radlolabel  loss  from selected  tissues showing a  blphaslc
rate  (Table  7-4)  represent  half-times  of  loss  of  2,3,7,8-TCDF.  The  loss
from skin was blphaslc, the early  component  having a half-time comparable to
other  tissues  (see  Table  7-4), followed  by  the slow component with  a half-
time of -11 days,  which accounted  for  <1% of  the total dose.
    In  contrast with  blood and tissues,  >99% of the radlolabel  excreted 1n
the  feces  and  urine  was  associated with metabolites  of  2,3,7,8-TCDF.   Since
the  metabolites  appeared   to  be excreted as  soon as  they  were  formed,  the
half-times of radlolabel  1n the urine  (1.3 days)  and feces  (1.8 days) repre-
sent  the half-time of  elimination (by  metabolism)  of  2,3,7,8-TCDF.   These
values  agree  with the half-times  1n  blood  and  liver (see Table 7-4).   The
feces  was  the primary route  of excretion,  accounting for -85% of  the total
dose,  while  <6%  was  excreted  In  the urine.   The  ratio  of  kidney  to  bile
clearance was 0.03.
    Yoshlmura et  al.  (1984) studied the tissue  and  subcellular  distribution
of 2,3,4,7,8-PeCDF  given  orally to the  rat.   More than  60% of the  dose was
accumulated  In the  Hver  after  5 days  and  persisted  over   a  period  of  3
weeks.   The  small percentage  of radioactivity distributed In  all other  tis-
sues  was eliminated  quickly.   The subcellular  liver distribution  of PeCDF
was  parallel  to  that  of  cytochrome P450.   Excretion of the  unchanged  com-
pound  1n the feces  amounted  to -32%  of the  dose during the  first  24 hours
with  progressively  smaller  amounts during the following 3 weeks.   No excre-
tion  was recorded In urine up  to  day  21.   The fecal excretion of  PeCDF can
be  Increased  by treatment with activated  charcoal  beads (Yoshlmura  et  al.,


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                                   TABLE  7-3

         Distribution of Radioactivity 3 Days After Administration of
                               to  200-250 g Male  Fisher  344  Rats*
Percentage Total Dose
Tissue
Liver
Fat
Skin
Total excreted
In feces
In urine
Oral
1.0 pfflol/kg
3.9±2.2
9.8+3.6
1.H0.6
68 ±6
1.5+0.3

0.1 timol/kg
5.0+0.4
4.6+0.8
1.H0.2
70 ±4
1.76+0.01
l.v.
0.1 ymol/kg
5.9±0.3
12 t2
1.2±0.3
63 ilO
2.0±0.4
*Source: Blrnbaum et a!., 1980
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                                   TABLE  7-4

                 Components  for  the Elimination of  Radioactivity
                        from Tissues  of Fisher 344 Rats3
Tissue
Blood
Liver
Fat
Muscle
Skin
Component
1
2
1
2
1
1
2
1
2
Pool Size
(X total dose)
1.3+0.4
0.9+0.2
29 +6
31 ±3
18 +1
25 +2
6.7il.5
6.8*0.5
1.2+0.4
Decay Rate
(day-*)
32 +22
0.6 ±0.3
7.0 +2.7
0.55+0.08
0.19+0.04
29 +6
0.96^0.50
1.6 +0.3
0.06+0.41
Mean Half-Time
(days)
0.02
1.1
0.10
1.3
3.8
0.024
0.7
0.45
nb
 aSource:  Blrnbaum et al., 1980

 DComplex  redistribution occurs making the calculation of an S.D. tenuous.
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1986).  Such treatment  in  rats  for 3 weeks  stimulated  excretion  -3-fold and
significantly  suppressed  PeCDF  toxlclty  (thymus  atrophy  and  liver  hyper-
trophy).  PeCDF  levels  In  blood,  adipose tissue and, to  a  lesser extent,  In
liver, tended to decline.
    Recently,  Brewster  and  Blrnbaum (1986)  found  that  the disposition  of
2,3,4,7,8-PeCDF  1n  the  rat  was  similar in  animals  given either an  oral  or
1.v. dose; they  confirmed the greater accumulation  of  the administered chem-
ical 1n liver.   Fat, skin and muscles were found to be minor depots.  Excre-
tion by feces was <1% of  the administered  dose per day and <0.5 in the urine
within 3 days.  No PCDF  was detected 1n  expired air.
    Data  from  Blrnbaum  (1985)  Indicate  that 1,2,3,6,7,9-HxCOF  Is  not easily
metabolized  by  rats,  compared with  the TCDFs  and PeCDFs and Is  excreted  in
feces  less  than TCOF  (ratio feces/urlne  13 for HxCOF  and 31.4  for  TCOF).
The half-life for elimination has  been  calculated  at 13 days.   These results
confirm the data obtained by Kurokl  et  al.  (1980)  who showed that rats elim-
inate 2,3,7,8-TCDF and retain PeCDFs and HxCDFs.
    The  few  data available  Indicate that  in  the  rat  PCDFs concentrate  In
liver more than  in  fat  with a tendency for  higher  levels of halogenatlon  to
result  in  higher liver  concentrations  (liver/adipose % total dose  1.30 for
2,3,7,8-TCDF, 1.8 for 1,3,4,5,7,9-HxCDF) (Blrnbaum, 1985).
    7.3.3.2.    MOUSE — Morita and Olshl (1977)  gave male ICR mice  a  single
i.p. dose  of a  mixture  of  0.5 g  PCDF  1n  corn oil.  The  mixture  contained
unspecified 2-TCDFs, 4-PeCDFs and  4-HxCDFs.  The less  chlorinated PCDFs were
eliminated from  tissues faster  than the highly  chlorinated  ones.   The half-
times 1n tissues were a week or  less.
    Decad et  al. (1982) studied the  distribution  and excretion  of  2,3,7,8-
TCDF  in  two  strains  of  mice  given  30.6 yg 1.v.  radlolabeled  2,3,7,8-


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TCDF/kg bw.  Higher concentrations  of  radlolabel  were observed  1n  the  liver
than  In  any of the other  12 tissues  sampled  up  to 10 days  postadmlnlstra-
tlon.  DBA/2J mice  had  -1.6 times as much adipose  tissues  as  C57B1/6J  mice,
and  the  nature of  adipose  tissue radlolabel kinetics differed  considerably
In  the  two strains, with the  concentration  of radlolabel  peaking  later  and
at  a  higher  level  1n  the adipose tissue of  DBA mice.  Nearly  all  the tissue
radlolabel  was unmetabollzed  2,3,7,8-TCDF,  while  essentially  all  of  the
radlolabel  In  urine and  -80% of the  radlolabel  In  feces, after  the  first
postadmlnlstratlon  day,  represented metabolites.   The whole-body  residence
half-time, calculated from  the rates of  excretion of  radlolabel  In the urine
and  feces,  was  ~2 days   1n  C57B1/6J  mice  and  ~4 days 1n  DBA/2J  mice
(Table 7-5).
    Nagayama et al.  (1980)  studied  the transfer of  PCDFs  to  the fetuses  and
offspring  of  ddN  mice  (25 g bw)  fed a diet  containing 0.6 ppm  of  a mixture
of  PCDF  (48% TCDFs, 49% PeCDFs and  3% HxCOFs)  for  18 days after  mating  and
14  days  after  delivery.    Accumulation  of  PCDF  1n  the  fetuses across  the
placenta was only 0.003% of  the  total  amount Ingested by  the  dam.   There was
much  greater  transfer  of  PCDF   to  suckling  offspring  (1.2% of   the  total
amount  Ingested by  the dam).   PCDF  accumulated  more 1n  the  dams'  livers
(5.1% of  the total  amount Ingested) than  1n other  tissues.  Data  from Weber
and  Blrnbaum (1985) confirmed that  <0.1%  of the total dose appeared In  the
fetuses 1 day after acute exposure on day 11  of gestation.
    7.3.3.3.   MONKEY — The  PCDF mixture  reported  In Section  7.3.3.1.  was
given orally,  In  combination with a commercial PCB  mixture,  to  1  female and
2 male monkeys  dally for  26-32 days, after which  the monkeys  were killed and
adipose  tissue  and  liver  analyzed for  their  content  of  PCDF  Isomers (Kurokl
1931A                               7-16                             06/22/86

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                                  TABLE 7-5



        Excretion  of  2,3,7,8-TCDF-Derlved  Radioactivity by Three Mice*
Mouse
Strain
C57B1/6J


DBA/20


Elimination
Route
Urine
Feces
Urine +• feces
Urine
Feces
Urine * feces
Mean +_ S.D. Cumulative
Excretion of
Dose by Day 10 (%)
12. 6+ 0.1
81.9±13.0
97. 0± 9.2
19.9+ 4.6
55.8+ 4.8
75.7 + 5.8
Mean
Half-Time
(days)
2.8
1.8
2.0
4.9
5.4
4.0
*Source:  Decad et al.,  1982
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et al.,  1980).   As  In  the rat,  PeCDFs  and HxCDFs  were retained at  higher
concentrations than TCDFs (see Table 7-1).
    In the only kinetic  study using a  single  Isomer  (Blrnbaum et al.,  1981),
three male  rhesus  monkeys were given  30.6  yg 2,3,7,8-TCDF/kg bw  l.v.   Loss
of radlolabel from blood was monitored only for  18 minutes  In order  to avoid
an extended  period of  sedation  (Ketaset  50 mg 1.m.) and  to  minimize stress.
The monkeys  were  killed 21 days  after  treatment,  and the pattern of  radio-
label distribution In the tissues was determined (Table  7-6).  Less  than 10%
of the  Injected  dose remained  In  the  body at this  time.  As with  the rat,
all radlolabel extractable from liver, fat, skin and muscle  was  unmetabollz-
ed  2,3,7,8-TDCF,  but  about  one-third  of  the  small  amount of  extractable
radlolabel  In  blood  did  not  co-chromatograph with  the  parent  compound  and
may  have  been associated  with metabolites.   Only  metabolized  2,3,7,8-TCOF
was extracted  from the urine,  and  nearly  all radlolabel extracted  from the
feces represented  metabolites.  Thus,  the  half-times of  radlolabel  1n urine
(6.2  days)  and 1n feces (10.3 days)  represent  estimates of  the  whole-body
half-time.   Eight  percent  of  the dose was  excreted  1n the  urine and  4354 1n
the feces.
    King  et  al.   (1983),  using the  data for  the  monkey  (Blrnbaum  et  al.,
1981), rats  (Blrnbaum et al., 1980), and mice  (Decad et  al., 1982),  compared
the tissue to blood distribution ratios (Section  7.3.3.5.).
    7.3.3.4.   GUINEA  PIG --  The  extremely high toxlclty  of the  PCDFs  In
guinea  pigs  (Moore  et  al.,  1979)  makes   1t  difficult  to  obtain  reliable
Information  concerning  their  disposition.    Decad  et al.   (1981b)  reported
that  the  distribution  of 2,3,7,8-TCOF radlolabel  In guinea pigs  during the
first  24  hours  after  either  oral  or  l.v.  administration of  6  yg/kg  bw
(near  the LD  )  was  similar  to  that  1n  other species,  with   liver,  fat,


1931A                               7-18                             06/22/86

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                                  TABLE 7-6
          Distribution of  2,3,7,8-TCDF-Der1ved Radioactivity  In Three
                    Rhesus Monkeys  21  Days After Treatment3
Tissue
Blood
Liver
Skin
Fat
Percentage Total Doseb
0.37±0.02
1.0 ±0.8
2.4 ±1.6
3.7 ±2.8
pmol TCDF/g T1ssuec
4.8± 0.3
47 ±30
12 ± 6
47 ± 0.2
aSource: Blrnbaum et al., 1981

b1.v., 0.1 vmol/kg bw

cMean + standard deviation
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muscle and skin containing much of the  radlolabel, but  the  ratio  of  liver  to
adipose  tissue  was lower  than  1n the  rat  (Table 7-7).   During  the  second
24-hour  period,  however,  redistribution to  the liver  began.   Subsequently,
the amount of radlolabel 1n the liver rose  to  over 50% of  the  total  adminis-
tered amount  by the ninth  day  postadmlnlstratlon.   This redistribution and
accumulation was  at least  partly the  consequence  of  mobilization  of  body
fat, a  toxic  effect of 2,3,7,8-TCDF.   In  this study a minimum half-life  of
20  days  has  been  Indicated,  but  1n  view  of  this fat  loss with release  of
radlolabel, no  reliable half-life  can  be  calculated  from  these data.   In
fact In a more  recent  study by  loannou  et al.  (1983)  the half-life calculat-
ed  on  data from  animals  showing little  or no  significant  effects  of  TCDF
Intoxication was  -40  days.   In a multiple  oral treatment   the  concentration
In adipose tissue  was  proportional  to the dose.  With  Increasing time after
dosage, the distribution starts  to shift from adipose tissue to  liver.
    The  amounts of  radlolabel  excreted  In  the urine  and feces  of  these
guinea pigs were  comparable,  only -6.6% being excreted by  each route  by the
ninth day after  1.v.  Injection.   While  radlolabel  was  excreted In the urine
as metabolites, >90% of  the radlolabel  excreted In the feces was unmetabol-
1zed  2,3,7,8-TCDF.   Thus,   although  urinary excretion  by  these  guinea  pigs
appeared  comparable with  that  In  other  species  at  exposures  that do not
cause toxldty,  fecal  excretion was markedly  lower  compared with the  other
species and was restricted  largely to parent 2,3,7,8-TCDF.
    Attention has  been paid 1n recent  years  to the  b1oava1labH1ty of  PCDF
from different  matrices.  Berg  et al.  (1985b) studied  Us  availability  from
fly ash  of a  municipal Incinerator  1n the  rat,  hamster and  guinea pig.  Fly
ash was  mixed with the standard laboratory diet and  animals were allowed  to
eat ad  libitum  for 3  months.   Contamination  of  the  PCDF  Isomers was  1n the
1931A                               7-20                             06/22/86

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                                   TABLE  7-7

           Distribution of 2,3,7,8-TCDF-Derlved  Radioactivity  During
          the First  24 hours  In Liver,  Fat  and Skin  of  Guinea  P1gsa»b
Time After
1.v. Injection
(hours)
1
3
7
24
Percentaqe
Liver
43
23
17
15
.1*1.
.6*3.
.8*0.
.4*3.
4
8
8
7
27.
31.
68.
55.
of Total Dosec
Fat
4* 7
4* 0
5*11
2*19

.6
.7
.3
.8
Skin
14.6*0
22.5*0
20.9*1
19.4*3

.9
.1
.8
.3
aSource: Decad et al., 1981b

bHartley  guinea  pigs received  a  single  1.v.   dose  of  (1*C)-2,3,7,8-TCDF
 0.02  ymol/kg.    Three  animals  were  killed  at   each  time  1,  3,  7  and  24
 hours, respectively.

cMean * S.D.
1931A                               7-21                              06/22/86

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range of  0.5-3.6  yg/g food.  Rats  and  hamsters retained mainly  the  Isomers
with 2,3,7,8-substltutlon  patterns  whereas  guinea  pigs retained  also  a  num-
ber of other substituted Isomers probably because  of  less  effective metabol-
ism.  Usually recovery 1n  the liver was  below  10%  for all  three species.  In
a subsequent paper Berg et  al.  (1986) gave  rats and hamsters oral treatments
with fly ash at higher concentrations (15%  1n  food compared with the earlier
concentrations of  2.9%); they  found higher  liver  retention,  from 20-60% for
penta and  hexa congeners.   In  rats,  retention was  highest for  1,2,3,7,8-
PeCDF (41%) and very low for 2,3,7,8-TCDF  (1.1-2.8%);  1n  hamsters the high-
est retention was  for 2,3,4,7,8-PeCDF  (71%) and -38% for  2,3,7,8-TCDF.   The
authors suggested  that the hamster  probably metabolizes TCDF less efficient-
ly  than the  rat.   As a whole,  these results  Indicate that the bloavallabll-
Hy for PCDF, when absorbed on fly ash,  1s very low.
    7.3.3.5.   PHYSIOLOGICAL  DISPOSITION MODEL — When  uptake,  accumulation
and  disposition  parameters are  known,  pharmacoklnetlc models  can be useful
to  predict  the  overall  distribution and to  describe  the time course of tis-
sue concentrations and excretion of metabolites.   These models  can provide a
means  of  estimating  the  metabolic  and  excretory  clearance, difficult  1n a
complex In vivo system.
    The disposition  data  for 2,3,7,8-TCDF  1n  the  mouse (two strains) (Decad
et  al.,   1982),  rat   (Blrnbaum  et   al.,  1980)   and  monkey   (Blrnbaum  et  al.,
1981) were  compared  by  King et  al.  (1983) with simulated data generated by a
physiological  pharmacoklnetlc  model.    In  developing the model,  King et  al.
 (1983)  used  t1ssue-to-blood concentration ratios from  the  studies  previously
discussed  1n  Section 7.3.3.3.  to estimate partition  coefficients.  Metabolic
clearances were calculated from the data sets as cumulative  total  radlolabel
excreted  (urine and  feces) divided  by  the total area under  the  curve  of con-


 1931A                               7-22                             06/22/86

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centratlon In hepatic venous blood.  Values  of  these  parameters  are given In
Table 7-8.
    Concentrations  predicted  by the  physiological  model  generally compared
well with measured  concentrations  In all  three  species.   Metabolic clearance
displayed the dependence  on  body weight to  the  power  of  0.7  that 1s charac-
teristic  of  many  physiological  functions.   Extrapolation  to  man on  this
basis yields a  whole-body half-life estimate of  5-12  days for 2,3,7,8-TCDF.
This Indication  that  TCDF would not be expected to persist  for  long periods
1n  man  does  not disagree with  the values determined  1n  tissues  of patients
exposed  to  PCDF.  In fact  2,3,7,8-TCDF  was  less persistent  than the higher
chlorinated  hexa and  hepta congeners.   However,  the whole  body half-life
seems to be  greatly underestimated.  In general  the  possibility of extrapo-
lating  these pharmacoklnetlc  data Is  limited   by  the fact  that metabolism
varies  between  species and  particularly  as  far as PCDF  metabolism 1s con-
cerned,  the  differences and  similarities  1n  the metabolic fate 1n humans and
laboratory animal species are not  yet satisfactorily distinguished.
    7.3.3.6.   MAN  — Pharmacok1net1cs  of PCDFs 1n  man   (Including  absorp-
tion,  metabolism,  excretion and  half-lives)  are  unknown.    However,  PCDFs
have been detected  1n  tissues  of subjects exposed  1n  different ways to these
compounds.   Measurements  of tissue levels  of the  various  Isomers over time
provide  a gross  estimate  of  the extent of exposure and can help  to elucidate
the structural  rules  governing  the  metabolism  and  elimination  of  these
classes  of  compounds.  As methods are now  available  to  detect  dlbenzofuran
Isomers  In  human tissues  In the ppt  range (Albro  et  al., 1985),  measurement
of  PCDFs 1n  fat biopsies can  be considered  a biological marker  of exposure.
PCDFs have  been detected In man after  different types of exposure to recog-
nized sources  of contamination  and, very  recently,  also  1n the general popu-


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                                  TABLE 7-8
       2,3,7,8-TCDF  Pharmacoklnetlc  Parameters  for  Physiological  Model3
House
C57 DBA
Distribution ratio5
Liver 100 100
Fat 25 40
Skin 8 12
Muscle 2 4
Clearances
Metabolism5 0.07 0.06
km(mi/m1n)
Metabolites excretion ratio 0.14 0.27
kk/ke
Rat Monkey
100 30
35 30
4 7
2 2

1.0 2.25
0.03 0.19
aSource: King et al., 1983
bFor parent TCDF
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latlon  that  1s  evidently  exposed to  unknown contaminations.   Depending  on
the higher detection  limit  of the method used In  the  first  reports,  1n many
cases not Indicated,  the concentrations  1n  these  studies  are not comparable,
particularly  the levels 1n  control  subjects,  but  the  earlier results  are
reported  here  when  they  are  significant  1n the  context of  the  scientific
merit of recent observations.
    PCDFs have been  found  1n tissues of Yusho and  Yu-Cheng  patients  Intoxi-
cated In  Southwest  Japan (1968)  and  1n Taiwan (1979), respectively  by con-
sumption  of  a  commercial rice  oil  contaminated  with  high concentrations  of
PCBs, PCDFs  and  PCQs.  Although  the  PCDF  concentrations  In  the Taiwan rice
oil were  lower  than  In the  Japanese  oil,  (Table  7-9)  It   has  been  roughly
estimated that the  average  Intake during  the whole Intoxication  period  was
similar:  973, 3.8  and 586  mg  In Taiwan (Chen et  al.,  1985a)  and 633,  3.3
and 596 mg In  Japanese  patients  (Hayabuchl  et al.,  1979)  for PCBs, PCDFs  and
PCQs, respectively.   An example  of the  tissue   PCDF  distribution with  the
relative  concentrations of  the  various  Isomers detected was  obtained  by  the
analysis  of  samples  from  a Taiwanese  patient  who  died  ~2  years after  the
onset of  poisoning  (Chen and H1tes,  1983).   The PCDF congeners retained  1n
all the tissues  were  essentially  the same,  with higher levels*1n liver.  The
relative  amounts of  the Individual  PCDF   congeners differed  1n  liver  and
other tissues  (Table 7-10).   The major congeners   detected  were  1,2,4,7,8-
and 2,3,4,7,8-PeCDFs; 1,2,3,4,7,8-HxCDF.   Minor  amounts  of  2,3,7,8-TCDF  and
1,2,3,4,6,7,8-HpCDF   were  found.   All   the  PCDFs  retained  have at  least  3
chlorine atoms at 2,3,7,8 positions and  no  vicinal  hydrogens in the dibenzo-
furan ring.   As   stated  in  Section  7.4.,  these  bioaccumulative  PCDFs  also
strongly  Induce   benzo(a)pyrene  hydroxylase  and  DT-dlaphorase  and  cause
severe  atrophy  of  the  thymus and  significant hypertrophy  of  the liver  in


1931A                               7-25                            06/22/86

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                                  TABLE 7-9
         Concentrations  of PCBs,  PCDFs  and  PCQs  In  the  R1ce  011s  from
                              Japan and Taiwan3
Concentration (ppm)

PCBs
PCDFs
Unknown tetra-
2,3,7,8-tetra-
2,3,4,7,8-penta-
2,3,4,6,7-penta-
hexa-
TOTAL
PCQs
Japan R1ce Oil
900
0.65
0.20
0.70
0.35
0.12
2.02
800b
Taiwan
A
60
0.04
trace
0.02
0.01
0.01
0.08
90b
R1ce Oil
6
100
0.05
trace
0.02
0.02
0.01
0.10
180b
aSource: Masuda et al., 1982
^Approximate concentration
A and B = two different oil samples
Trace = 0.001-0.005 ppm
1931A
7-26
06/22/86

-------
rats (Yoshlhara et al.,  1981;  Nagayama et al., 1983); and  these  Isomers  can
be considered the most toxic compounds, at least 1n animals.
    No congeners with adjacent unsubstltuted carbon atoms have  been  detected
1n  tissues  of  the Yu-Cheng  patient  (see  Table  7-10).  By contrast  these
unhalogenated  v1c1nal-C-atom congeners  were  present  In the  rice-bran  oil
that the  patient  had  Ingested  (Table 7-11).   A  similar pattern  of  Isomers
had been  detected  by Rappe  et  al.  (1979b)  In  a  Japanese Yusho  patient  who
died 18 months after  the exposure.   Thus,  It has  been  suggested that congen-
ers with  at  least two  vicinal   hydrogens   In  the ring  are metabolized  or
excreted  during  the  Interval.   Some  other  autopsy  results  (Kurokl  and
Hasuda, 1978)  are  provided  In  Table 7-12.   Preferential accumulation  In  the
liver, followed by adipose  tissue sequestration for the  Isomers  with Cl sub-
stitution 1n  the  2,3,7,8-posltlons,  was  also observed (Rappe et  al.,  1983b)
1n tissues of a Taiwan Yusho baby (Table 7-13).
    A  correlation  between  the severity  of clinical symptomatology  In  Yusho
patients and  the.estimated  contaminated  oil Ingestlon (PCBs +  PCDFs  + PCQs)
was reported promptly  (Kuratsune  et  al.,  1972;  Nagayama  et  al.,  1976)  (Table
7-14).  However there  1s much  evidence  to  support  the  hypothesis that PCDFs
and not  PCBs  are  responsible  for the disease.   Analysis of the concentra-
tions  of PCDF  and  PCB In the liver and  adipose tissue of Yusho patients  and
of control subjects killed  In traffic  accidents revealed  comparable  PCB con-
centrations  In tissues of  the  two groups,  but PCDF   (1n  the  range of ppb)
only In the  organs of Yusho patients  (Masuda  and  Kurokl, 1982).   Other evi-
dence  of  the  Importance of PCDF and  PCB  In determining Yusho  and  Yu-Cheng
syndrome has  been  obtained  more  recently.  Kashlmoto et al. (1985)  compared
the  blood  levels of Yusho  (11  years  after the  outbreak)  and  Yu-Cheng
patients with that of  occupationally PCB  exposed workers  (19  years  after


1931A                               7-27                             06/22/86

-------
                                  TABLE  7-10

       Concentrations of PCDF Congeners 1n the Tissues of the Deceased
                       Patient with  Yu-Cheng  1n Taiwan*
Tissue
Liver
Intestinal fat
Bronchus
Large Intestine
Heart
Stomach
Small Intestine
Kidney
Lung
Brain
Spleen

1,2,4,7,8-
3.4
0.9
0.4
0.3
0.2
0.05
0.05
0.04
0.01
0.01
0.01
Level of PCDF Conqener
2,3,4,7,8-
6.3
4.0
1.8
1.2
0.8
0.23
0.21
0.18
0.06
0.06
0.08
(ppb)
1,2,3,4,7,8-
25.4
7.8
3.2
2.3
1.4
0.40
0.34
0.32
0.12
0.15
0.10
*Source:  Chen and Hltes,  1983
1931A
7-28
06/22/86

-------
                                  TABLE 7-11

            Structural Assignments of  PCDF Congeners  1n  the Toxic
           Rice-Bran 011  Ingested by  the Deceased Yu-Cheng Patient*
                                  Structure
                           2,3,6,8-TCDF

                           2,3,4,8-TCDF (major)

                           2,3,7,8-TCDF (minor)

                           1,2,4,7,8-PeCDF

                           1.2,3,4,8-PeCDF

                           1,2,6,7,8-PeCDF

                           2,3,4,7,8-PeCDF

                           2,3,4,6,7-PeCDF

                           1,2,3,4,7,8-HxCDF

                           1,2,3,4,6,7-HxCDF

                           1,2,3,4,6,7.8-HpCDF
*Source:  Chen and Hltes, 1983
1931A                               7-29                             06/22/86

-------
10
CO
                                    TABLE 7-12


PCB and PCDF Concentrations In Liver and Adipose Tissue of Deceased Yusho Patients3
                          (Exposure was In May-June 1968)


1
co
o




06/22/8
Case
1
2
3

4
5

aSource
bA = 2,
B = 2,
C = 1,
D = 2,
E = 1,
Time of
Death
July 1969
July 1969
May 1972

April 1975
March 1977

Tissue
liver
liver
adipose
liver
adipose
adipose
liver
adipose
PCB
Concentration
(ppm)
0.14
0.20
2.8
0.03
4.3
0.2
0.006
1.2
PCDF Concentration (ppb)b
A B C D E Total
0.7 0.3 7.1 6.9 2.6 18.0
0.08 0.02 0.4 1.2 0.3 2.0
0.6 0.3 1.0 5.7 1.7 9.3
0.03 0.005-0.01 0.09 0.3 0.03 0.45
0.08 <0.005 0.2 0.8 0.2 1.3
0.4 <0.005 0.8 0.1 0.5 1.8
<0.005 <0.005 0.02 0.1 0.04 0.16
<0.005 <0.005 0.2 0.5 <0.005 0.7
: Kurokl and Masuda, 1978
3,6,8-TCDF
3,7,8-TCDF
2,4,7,8-PeCDF
3,4,7,8-PeCDF
2,3,4,7,8-HxCDF
+ 1,2,3,6
,7,8-HxCDF


-------
                                  TABLE  7-13

       Levels  of  PCDF  (pg/g)  and  PCB  (ng/g)  1n  Tissue  Samples  of a  Baby
            from  a  Woman  from Taiwan  Suffering  from Yusho  Disease*

2,3,7
1.2,4
1,2,3
2,3,4
1,2,3
PCDF
PCB
Isomer
,8-TCDF
,7,8-PeCDF
,7,8-PeCDF
,7,8-PeCDF
,4,7,8-HxCDF


Adipose
Tissue
17
14
44
68
88
231
316
Liver
60
42
194
91
193
580
27
Muscle
ND
ND
ND
ND
ND
ND
38
Omen turn
ND
ND
ND
ND
ND
ND
64
Diaphragm
ND
ND
ND
ND
ND
ND
46
*Source: Rappe et al.,  1983b

ND = Not detected
1931A
7-31
06/22/86

-------
CO

»
—J
I
CO
ro
                                                      TABLE  7-14


                          Relationship Between the Amount of Rice 011 Used by Yusho  Patients,
                              Amounts of PCBs  and PCDFs  Ingested,  and Clinical  Severity3
Consumed**
Rice 011
Consumed
(no*)
<720
720-1440
>1440
PCBs
(g)
<0.7
0.7-1.4
>1.4
PCDFs
(mg)
<3.6
3.6-7.2
>7.9
Unaffected
10 (12.0)
0
0
Number of People0
Light Cases
39 (49.0)
14 (31.0)
3 (14.0)
Severe Cases
31 (39.0)
31 (69.0)
18 (86.0)
Total
80
45
21
     aSource:  Kuratsune et al., 1972;  Nagayama  et  al.,  1976


     Calculated on  the  basis of the  concentrations  of PCBs  (1000  ppm),  PCDFs  (5  ppm)  found  In  the contami-
      nated rice oil  by Nagayama et  al. (1976)


     Percentage of cases Is given 1n  parentheses.
o
a*
>x
no
00
a*

-------
termination) and unexposed  people.   In spite  of  high levels of PCBs  1n  all
the  samples,   detectable  amounts  of  PCDFs  were  only  found  1n  blood  of
Yu-Cheng patients.   In  113  Yu-Cheng patients  there was  a  clear  correlation
between  the blood  PCDF  concentration and  the  severity  of  dermatologlcal
symptoms.  PCQs were present  In  blood  of all  the  Yu-Cheng  patients  6  months
after exposure and  In  54  of the 56 living Yusho  patients 11  years  after  the
outbreak.  So  the presence  of  PCQs  In blood can  be considered  a  good  marker
of past 1ngest1on of contaminated oil.
    In  the  blood  of Yu-Cheng patients  there was a  distinctive  PCB  pattern,
very different from the original pattern  (Masuda  et al.,  1985)  and  richer 1n
the more  chlorinated Isomers (for  example,  2,3,4,5,3,4-hexa-CBs a  PCB  with
high  bloaccumulatlve properties).   This  distinctive chromatogram  has  now
been adopted as  one of  the  criteria for  Identification  of  Yu-Cheng disease.
An example  of  the  levels of  three  halogenated congeners 1n  tissues of  dif-
ferent categories subjects 1s given  1n  Table 7-15.
    Preliminary data  In the three  Taiwan Yusho  patients  Indicated that  1n
the  first  year after  exposure  blood  concentrations of penta- and  hexa-CDF
dropped 20 and 15%,  respectively.  Thus,  the half-time of  highly-chlorinated
PCDF  In  man appears to exceed  1  year  (Rappe  et  al., 1983c).  Rappe  et  al.
(1979b) actually detected reliable levels of  PCOF  In blood  of Yusho patients
10 years after the  Intoxication.  Of particular  Interest  1s the detection of
high  concentrations (100-500 ppt)  of  2,3,4,7,8-PeCDF and  1,2,3,4,7,8-HxCDF
In the  placenta  of  Yusho  women  5 years after  exposure.  The Implications of
these  results  In  relation to  the   Increased  mlcrosomal  enzyme  activity
detected  1n  the  placenta  of  these  patients  Is   discussed  under  Section
7.4.5.5.2. (Wong et al., 1985).
1931A                               7-33                             06/22/86

-------
                                                    TABLE  7-15
GO
3>


ton
Case

centrations or v
and
Age Sex

IBS, Kturs ana HH/S in ine (issues or TUSPO
1n the Milk Fat of a Worker Occupatlonally
Time After Tissue
Exposure (or fluid)
(years)
caiienis,
Exposed to


PCBs
unexposeu inai
PCBs3
Concentration

PCDFs
IV lUUd 15
(ppb)

PCQs
Yusho patients




-j
CO
4*







o
^
1

2

3

4

5

Unexposed
Avg.
PCB worker


25 H

46 F

72 M

59 M

59 N

Individuals
53 M,F

37 F

1 Adipose tissue
Liver
4 Adipose tissue
Liver
7 Intestine
Liver
9 Intestine
Liver
9 Intestine
Liver

Adipose tissue
Liver

11 Milk fat

5090
226
6091
68
3472
114
3630
64
1273
18

803b
33b

6241

5.3
70.1
9.6
15.5
2.5
6.2
2.2
6.1
0.2
0.02

0.019b
0.006b

0.02

2400
218
1444
144
1770
51.7
416
6.3
24.5
0.97

1.53b
0.41b

0.2

ro
ro

CO
aSource: Hlyata et al.. 1985

bAverage concentration from 14 persons

-------
    Rappe and  Buser  (1981)  reported measurable  levels  of PCOF  In  the  blood
of workers  exposed to  2,3,4,6-tetra-chlorophenol  and  in workers exposed  to
pentachlorophenol  or  pentachlorophenol  laurate.    Tables   7-16  and  7-17,
respectively, report the  levels  of  chlorophenols found  1n urine samples  and
of PCDF and  PCDD In whole blood.  The pattern of  PCDD and PCDF  1n  the  blood
differed  In workers  exposed  to 2,3,4,6-tetrachlorophenol  or  pentachloro-
phenol.  This parallels the difference  In  the  concentrations of  contaminants
In the  two products:   more  PCDFs  were present  in 2,3,4,6-tetrachlorophenol
than 1n pentachlorophenol.
    Recently,  Rappe et  al.   (1983b)  analyzed samples  of  liver and  kidney
tissue of  a worker who had been employed  1n the  production  of  phenoxy acid
herbicides.  He  died  of  a  pancreatic tumor  3-4  years  after  the  exposure
ceased.  The  findings   confirm  the  prolonged storage of  the hlghly-halogen-
ated PCDF  Isomers  and  their  preferential  accumulation  In  the  liver  (Table
7-18).    In  a subject  hospitalized  for granulocytopenla, probably  caused  by
long-term  exposure to  PCP,  levels  of  highly chlorinated  CDF and  CDD were
detected In adipose  tissue (Gorskl  et  al.,  1984).   The  Interest  of this case
consists 1n  the  two adipose  tissue biopsies made at  a  2-year  Interval.   A
rough estimate of  the  half-lives of  these congeners has thus been suggest-
ed.  Data  reported In  Table  7-19 confirm, although  only preliminarily, that
the half-lives  of PCDF  1n humans exceed 1  year.
    Schecter et  al.  (1985a,b) reported  a high  level  of  PCDF  residues In adi-
pose tissue  of a patient  who had been  Involved  In the  Incident  of  the  elec-
trical  transformer  In   the Blnghampton State Office  Building (BSOB) 1n  NY.
This transformer contained  65%  PCB and  35% chlorinated  benzenes.   The soot
samples  contained  a  mixture  of PCDFs and  PCDDs  1n  which  the most  toxic
2,3,7,8 substituted congeners were  present.   From  Table  7-20 H  appears that


1931A                               7-35                             06/22/86

-------
10
co
                                                      TABLE  7-16


                    Levels of PCDD and PCDF  1n Blood Samples from Workers In the Saw Mill Industry

                                   After Exposure to  2,3,4,6-Tetrachlorophenolatea
Number Profession
Blank A
Blank B
1 Loader0
1 Loader6
2 Cleanerd
g 2 Cleaner6
3 Loaderd
3 Loader6
5 Packerd
5 Packer6
7 Control
aSource: Rappe and Buser
bMajor Isomer 1,2,3,4,6,
o cMajor Isomer 1,2,3,4,6,
v! dSamp!1ng 6 months after
K 6Sampl1ng after 1 month
CD
Chlorophenols
In Urine
(vg/mi)
—
—
0.04
5.2
<0.02
0.23
0.03
0.83
<0.05
0.11
<0.01
, 1981
7,8-HpCDD
7,8-HpCDF
latest exposure
exposure

PCDD (pq/q blood)
octa heptab hexa penta
7 <2 <3
<2 <1 <1 <1
5 <2 <3
7 <1 <1 <1
5 2 <3 —
22 8 <1 <1
18 10 3
3 <1 <1 <1
<3 <2 <3
4 <1 <1 2
3 <1 <1 <1



octa
<3
<2
<3
<2
<3
<2
<3
<2
<3
<2
<2


PCDF (pq/q blood)
heptac hexa
2 <3
<1 <1
40 <3
22 <1
30 <3
17 <1
18 <3
17 <1
7 <3
12 <1
3 <1



penta
__
<1
—
<1
--
5
__
1
—

-------
                                                     TABLE 7-17

              Levels of PCDD and PCOF  In  Blood  Samples  from Workers  In  the  Textile and  Leather  Industry
                            After Exposure  to Pentachlorophenol  (PCP) or  PCP  Derivatives3
vO
3»
Number
3
4
5 M
6
7
53 10
15
16
17
Profession
Textile

Textile
Textile
Textile
Tannery0"
Tannery''
Tanneryd
Tanneryd
Chlorophenols
1n Urine
(vg/ml)
3.12
—
<0.01
0.42
0.16
0.55*
0.04e
0.03e
—
PCDD (pq/q blood)
octa
304
3
10
105
30
20
80
12
7
heptab hexa penta
59 <1 <1
<1 <1 <1
1 <1 <1
15 <1 <1
6 <1 <1
7 <3
30 3
4 <3
2 <2
PCDF (oq/q blood)
octa heptac
10 33
<2 <1
<2 <1
<2 <1
<2 <1
<3 7
7 18
<3 3
<3 3
hexa penta
<1 <1
<1 <1
<1 10
<1 <1
<1 1
<3
3
<3
<3
    aSource: Rappe and Buser, 1981

    bMajor  Isomer 1,2,3,4,6,7,8-HpCDD

    cMajor  Isomer 1,2,3,4,6,7,8-HpCDF

o   dBlood  sampling 8 months after last exposure
\
£   eUr1ne  sampling 6 months after last exposure
CD

-------
                                  TABLE  7-18

           Levels of PCDF 1n Tissue Samples of a Worker Exposed to
                             Phenoxy Herbicides3
              Isomer
                                                    Concentration
                                               Liver
                                            (pg/g  organ)
                                Kidney
                             (pg/g organ)
2,3,7,8-TCDF

2,3,4,7,8-PeCDF

1,2,3,4,7,8- + 1,2,3,6,7,8-HxCDF

1,2,3,4,6,7,8-HpCDF

OCDF
           10 (2)

           55 (2)

          100 (4)

           <3
 7 (2)

 8 (2)

 6 (4)

<3
aSource: Rappe et al., 1983b

''The detection limits are In brackets
1931A
7-38
 06/22/86

-------
the Isomers  that  were  high  1n the  patient's  sample were  also high  In  the
soots  to which  the  patient  was exposed.  Hence,  In  comparison  to  the levels
of unexposed subjects,  It would  appear that these high  levels  arose through
exposure to  the soot.   In this  case the persistence of  the  2,3,7,8 substi-
tuted  Isomers 1s  noteworthy.   On  the other hand,  the pattern of  high levels
of hexa- to  octa- chlorinated  dloxlns  1n adipose tissue of both  exposed  and
unexposed subjects  Is consistent with  a  more general environmental contamin-
ation.
    Recent  findings  document   the  presence  of  PCDF  and  PCDD In  the general
population.   Ryan et al. (1985a) reported  the  presence  of 2,3,4,7,8-PeCDF  In
adipose tissues of  Canadian patients at  a  level  of 17 pg/g, confirming earl-
ier data  of Mlyata  et  al.  (1977a) who  found  the same  Isomer  1n  tissues  of
controls In  a  study on Yusho  rice oil poisoning.  More recently  Ryan  et  al
(1985b) found 8-10  PCDDs  and  PCDFs, all with  2,3,7,8 chlorine  substitution,
In 46 adipose  tissue  samples  from accident victims  (1n  Canada).   Major con-
stituents were  OCOO 800 pg/g), PeCDF,  PeCDD,  HxCDD and HxCDF.  No  TCDF  and
OCDF were detected.   Levels  ranged  between  17 and 39 ppt, 2-3 orders  lower
than those  associated  with  adverse  effects  1n Yusho and  Yu-Cheng patients.
Similar patterns of congeners  were  found by  Rappe et al.  (1984) from samples
of  human  Swedish control  tissues.  2,3,7,8 Cl-subst1tuted PCDFs have  been
detected In  the general population  from New  York  State  by Schecter  et  al.
(1985a,b) who compared  tissues of  subjects unexposed and  exposed  to  chemical
contamination (see Table 7-20).  Schecter et al.  (1986a)  also  found  PCDD and
PCDF at detectable  levels In the general population  of  South  and  North Viet-
nam, areas  of  respectively  high  and low potential dloxln  exposure.   In both
populations   PCDFs  were  present,   the  North Vietnam samples  showing  levels
1931A                               7-39                             06/22/86

-------
                                  TABLE  7-19
                     Half-lives  and  Contents  of  PCDDs  and
                        PCDFs  1n Human Adipose Tissue3

1,2,3
1,2,3
OCDD
1,2,3
OCDF
Compound
,6,7,8-HpCDD
,4,6,7,8-HpCDD

,4,6,7,8-HpCDF

Content In
(ppb, on
April 1981b
0.8
4.4
5.2
0.8
1.5
Adipose Tissue
a fat basis)
November 1983C
0.5
2.6
4.0
ND
0.4
Half-Life
(years)
3.5
3.2
3.7
<1.7
1.8
aSource: Gorskl et a!.,  1984
bOeterm1ned by HR 6LC-EC
Determined by GLC-EC
ND = Not detected (<0.2  ppb)
1931A
7-40
06/22/86

-------
                                                                   TABLE  7-20


                   PCDD and PCDF Levels In Blnghamton,  New York Adipose Tissue Levels (ppt) In Exposed and Unexposed Subjects
                                              Soot Sample Levels  (ppm) from  the Transformer F1rea
PCDDsb
2.3.7.8-TCDO
Other (4)

1,2,3,7,8-PeCDO
Others (7)

,2.3.4.7,8-HxCDD
,2,3.6.7,8-HxCDO
,2,3,7,8,9-HxCOD
,2,3,4,6,8/1,2,4,6,7.9/1,2,4,6,8,9-HxCOO
,2,3.6,8.9/1.2,3,6,7.9-HxCDD
,2,3,4,6,7-HxCDO

,2.3,4.6,7,9-HpCDO
,2.3,4,6.7.8-HpCDD

OCDD

TOTAL









Soot
0.6
0.6

2.5
2.5

0.7
0.6
0.4
1.2
1.3
0.5

4.0
3.0

2.0

19.9









Exposed Unexposed PCDFsb
(n=l) (n=4)
11.6 7.7 2.3,7,9-TCOF
1,3,7,9-TCDF
Others
15 10
1,2,3,7,8-PeCOF
2.3,4.7,8-PeCOF
1,2,4,7.8-PeCOF
72.6 55.4 1,2.4,7.9-PeCDF
7.3 7.3 1,3,4,7,8-PeCDF
2,3.4,8,9-PeCDF
1,2,3,6,7-PeCDF
2.3,4,6.7-PeCDF
Others (12)
9.6 2
209 86 1.2.3.4.7.8-HxCOF
1.2,3,6,7.8-HxCDF
690 602 2.3,4.6,7,8-HxCDF
1,2,3,4,6,8-HxCDF
1.2,3,6,8,9-HxCDF
1,2.4,6,7,8-HxCOF
1,3,4,6,7,8-HxCOF
Others (8)
1,2,3.4,6.7.8-HpCDF
1,2,3,4,6,7.9-HpCDF
1.2,3,4,6.8,9-HpCDF
1.2.3,4,7,8,9-HpCDF
OCDF
TOTAL
Soot Exposed
(n=l)
12.0 ND
1.0
15.0

310.0
48.0 74.7
25.0
22.0
65.0
25.0
60.0
12.0
110.0

310.0 149
150.0 112
10.0
30.0
38.0
50.0
125.0
250.0
230.0 39.3
120.0
55.0
55.0 25.9
40.0 1.6
2168
Unexposed
(n=4)
ND




14.2








14.2
8.9






13.6


10
0.7

•SJ
^
CO
aSource: Buser, 1985; Schecter et al..  1985a,b

bNumber In parentheses refer to the number of Isomers

ND = Not detected

-------
lower  than  In  other  more  Industrialized  countries.   Comparative  data  are
reported 1n Table 7-21.
    Further Investigations prompted Ryan et  al.  (1985b) to  seek  Information
on the  distribution  and  levels  of  PCDF 1n  different  tissues  from the  same
subjects.  From  samples  of two  deceased  elderly patients,  they found  that
PCDF  levels decreased from adipose tissue to liver,  muscle and  kidney  1n wet
tissues, but  the values  were  closer  when  calculated  on  the basis of  I1p1d
content.  In a  more  complete  study  Ryan et al.  (1986)  showed that  between  8
and 10  PCDDs and PCDFs  with  2,3,7,8 chlorine substitution occur  In all  tis-
sues  tested, the relative amounts and  specific Isomers  being the same  (Table
7-22).  Fat shows the highest  levels and 1s  probably a storage  tissue  but on
a  Upld  basis,  liver and other  tissues have the highest levels,  suggesting
these may be target organs (Table 7-23).
    Recently PCDDs  and  PCDFs  have  been detected  1n breast  milk from  human
populations of  different countries.   Particularly   high  levels of  2,3,7,8-
TCDD  In milk of a South Vietnamese  population  were  found  In  1973  samples
(Table  7-24) but 1n  five 1983 breast milk samples  the  values were  below the
detection  limits (Schecter et al.,  1986a).   However, milk of the  general
population also  appears  to contain highly  chlorinated PCDDs and PCDFs  (see
Table 7-24).
7.3.4.   Metabolic Fate.  No  satisfactory  metabolic pathway  for halogenated
DF has  yet been reported although  the metabolism has been  regarded  as  a
route  of  detoxification  for  PCDF  (Matthews and  Blrnbaum,  1983).  The  more
readily metabolized  PCDF  have adjacent unsubstHuted  carbon atoms.   Data Is
scant  on  the  Identification  of  metabolites of  PCDF  Isomers;  quantitative
studies are lacking.   One of  the few  published  Investigations  on  the  metab-
olism  of  PCDF  reports that  In salmon, an unidentified  hydroxylated  metabo-


1931A                               7-42                             06/22/86

-------
                                                                           TABLE 7-21
10
CO
3>



2.3.7.8-TCDO
1.2,3,7,8-PeCDO
1.2.3,4,7,8-HxCDO
1,2,3,6,7,8-HxCDD
1.2,3.7,8.9-HxCOD
T1 1.2.3.4.6,7,8-HpCDD
" OCOO
2,3,7.8-TCDF
2,3,4,7,8-PeCDF
1.2.3,4.7,8-HxCDF
1,2.3,6.7.8-HxCDF
2.3,4.6.7,8-HxCDF
1,2,3.4.6,7.8-HpCOF
OCDF
Levels (pg/g) of PCDDs and PCDFs In Human Samples from Sweden. U.S.A. and
Adipose Tissueb
Sweden [31] Canada [10] U.S.A. [6]
C A B C
3 (0-9) 10 10/10 6.4 (3.7-8.3)
10 (3-24) 13.2 10/10 9.7 (7.5-13.8)
ND
15 (3-55) 90 10/10 57.8 (46.2-64.2)
4 (3-5)
97 (12-380) 116 10/10 95.2 (30.4-119)
414 (90-763) 611 10/10 585 (428-695)
4 (0.3-11)
54 (9-84) 18.4 9/9 14.7 (10.9-17)
6 (1-15) 17.3 8/9
5 (1-13) 28.7 (15.1-52.8)
2 (1-7)
11 (1-49) 39.4 7/9 16.4 (12.5-23.8)
4
Vietnam Subjects3

South [15] North [9]
A B A B
27.9 12/15 ND
15.4 15/15 3.8 1/9
99.8 15/15 11.4 6/9

178 15/15 28.8 6/9
1326 15/15 104 8/9

21 15/15 14.7 6/9

58.3 15/15 13.3 7/9
28.8 15/15 7 3/9

CO
aSource: Nygren et al., 1986; Ryan et al.,  1985b;  Schecter et al.,  1986a

bNumbers In brackets refer to number of samples

A = Hean of positives
B = Number of positives
C = Ranges

-------
lO

>
                                                                          TABLE 7-22

                                           2,3,7.8-ChloMne-SubstHuted PCODs and PCDFs In Human Unexposed Subject*
                                                            (Values In pg/g on a wet tissue basis)
Fat
Compound
2,3,7,8-TCDO
2.3,4,7,8-PeCDF
1.2.3.7.8-PeCOD
1.2,3.4,7.8-/
1.2,3.6,7,8-PeCDF
1,2,3,6,7,8-HxCDD
1.2.3,4.6.7.8-HpCOF
1.2,3,4,6.7,8-HpCDD
1,2,3,4,6.7,8,9-OCDD
X L1p1d
Abdominal
5.7
17
7.8
52

64
15
110
680
75
Subcutaneous
6.0
17
8.2
22

60
12
120
700
75
Adrenal
3.8
4.9
3.1
8.5

35
3.5
55
600
28
Bone
Narrow
ND
4.4
12
9.4

30
2.7
48
540
28
Liver
ND
ND
ND
4.2

6.5
2.1
22
220
6.0
Muscle
ND
1.1
1.2
2.1

7.9
ND
14
170
9.0
Spleen
ND
ND
11
ND

1.9
ND
13
46
1.8
Kidney
ND
ND
ND
2.1

2.5
ND
5.2
31
3.0
Lung
ND
ND
ND
ND

1.4
ND
2.9
21
2.2
        *Source:  Ryan et al.,  1986

        ND = Not  detected
IV
IV
CO

-------
                                  TABLE  7-23

             Total PCDD and PCOF Levels (pg/g) In Tissue Samples
                          from an  Unexposed Subject*
Tissue
Fat, abdominal
Fat, subcutaneous
Adrenal
Bone marrow
Liver
Muscle
Spleen
Kidney
Lung
%
Llpld
75
75
28
26
6.0
9.0
1.8
3.0
2.2
Total
Wet
Basis
870
890
690
630
250
190
72
39
25
PCDDs
Llpld
Basis
1160
1180
2440
2440
4220
2160
3980
1290
1150
Total
Wet
Basis
84
51
17
17
6.3
3.2
3.2
2.1
--
PCDFs
Llpld
Basis
110
68
60
63
110
36
180
70
.._
*Source: Ryan et al.,  1986
1931A
7-45
06/22/86

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                                                      TABLE  7-24
to
> 	 	 	

2,3,7,8-TCDD
1,2,3,7,8-PeCDO
Total HxCDOs
1,2,3,4,6,7,8-HpCDD
^ OCDD
2,3,7,8-TCDF
1,2,3,7,8-PeCDF
2,3,4,7,8-PeCOF
Total HxCOFs
1,2,3,4,6,7,8-HpCDF
OCDF
Levels of

Germany8
n=53
NDd
11.0 (<1-40)
46.3 (9-168)
48.8 (11-174)
142.8 (13-664)
4.2 (
aSource: WHO, 1986
bSource: Nygren et al., 1986
cSource: Schecter et al., 1986a
dfielow detection level (5 ppt)
eBelow detection level (2 ppt)
fflelow detection level (0.5 ppt)
QBelow detection level (10 ppt)

-------
lite Is  formed  from 2,8-DCDF  (Z1tko  et al., 1973).  Veerkamp  et  al.  (1981)
reported Investigations  on  the metabolism  of  various  PCDFs 1n  the  rat.   No
metabolites  were  detected  In urine,  feces and  tissues  of  rats  receiving
OCDF.   Conversely,  2-MCDF,  2,8-DCDF  and  2,3,8-TrCDF  1n rats  form mono- and
dl-hydroxylated metabolites.   Moreover, metabolites containing  sulfur  (sul-
fone,  thloether)  could  originate  from 2-MCDF  and 2,8-DCDF.   Hydroxylatlon
can  take place  at  various positions  1n the rings.   Five monohydroxy deriva-
tives  have  been  found  from  2,8-DBCF,  the  most  Important  probably  being
2-chloro-8-hydroxy-DF,  that  can  originate  from the 1,2  or  2,3 corresponding
epoxlde.
     A  molecular model  developed  by  Veerkamp  et  al.  (1983)  predicted  PCDF
metabolites.   In  contrast to  the  corresponding PCDD  1n  which hydroxylatlon
takes  place only  In  the 2  and  3  positions   PCDFs  can  give  rise  to  many
products  depending  on  the  chlorine  substitution pattern.   Recently  the
metabolism  of  2,3,7,8-TCDF  was studied by  Polger et al.  (1984)  In  the rat,
unfortunately  using  a  compound  containing  considerable  amounts  of  other
PCDFs.   B1le was collected  for 48  hours;  no TCDF or other PCDFs were detect-
ed   1n  the  extract.   From  the  13  chlorinated  metabolites  present,  which
accounted  for 8.6%  of  the total  dose, four  methoxylated compounds that prob-
ably originated from the corresponding hydroxylated species were present 1n
the  major  amounts.   They  were  Identified  as  tr1chloromethoxy-DF,  tetra-
chloromethoxy-DF  and  two tr1chlorod1methoxy-DF  Isomers.   The  remaining  9
compounds  wee  detected In traces and  their origin  (from the parent compound
or  Impurities)  remains  unclear.
7.4.    ACUTE, SUBACUTE  AND CHRONIC TOXICITY
7.4.1.   Acute  ToxIcHy.   PCDFs are  all  toxic  and some are  acutely toxic.
The  toxlclty depends  on the  number  of Cl  substltuents  and on  their  posl-


1931A                               7-47                             06/22/86

-------
Hon.  The  tetra-,  pentaand hexaderlvatlves  are the most  toxic.  The  most
acutely toxic PCOFs are  the PCOF  congeners substituted  In  the  lateral  2,  3,
7 and 8 positions.
    There Is a long latent  period between  administration  and  the  first  signs
of  toxlclty;  the  LD,.-  must  be established  30 days  after  treatment.   The
                     DU
main  signs  1n monkeys and  guinea  pigs were  severe  weight  loss,  atrophy  of
the  thymus  and  spleen,  debilitation of  the lymphatic system,  hemorrhage  of
the  adrenals  and  urinary  bladder,  and  single-cell   necrosis  1n   the  liver.
Hlstologlcal examination of tissues revealed loss of lymphold cells  1n the
thymlc  cortex and  hyperplasla  of  epithelial  cells  In the renal  pelvis,
ureter and  urinary gladder.   These lesions,  together with a lack of  liver
pathology,  hypocellularlty  of  bone marrow,  seminiferous  tubules,  lymphold
elements  1n  spleen  and  Peyer's patches,  were similar to  those  described for
guinea pigs  given   large doses of   PCDD  (McConnell  et a!., 1978b;  McConnell
and Moore, 1979).
    The toxic effects of  PCDFs are markedly  species-dependent, as  are  those
of PCODs.  The guinea pig  Is  the most  sensitive species  followed  by the mon-
key,  rabbit,  rat and mouse.   In the  guinea pig, the ID™  for  2,3,7,8- TCOF
1s  between   5  and   10  yg/kg  bw (McKlnney  and   McConnell,  1981).  The  same
authors  showed   that  there  was no  significant   different  In  acute  toxlclty
(LDcn)  between  2,3,7,8-TCDF,   2,3,4,7,8-PeCDF   (<   10  v9/kg)  and  2,3,7,8-
   Du
TBDF,  while  the  LD50  of  2,3,4,7,8-HxCDF  was  120 vg/kg  (Moore  et  al.,
1979;  McKlnney   and  McConnell, 1981).   The  rat Is   quite  resistant  to the
acute  toxic  effects  of  2,3,7,8-TCDF.   The  monkey manifests  Intermediate sen-
sitivity.
1931A                               7-48                             06/22/86

-------
    These  differences  depend  on  the  species'   ability   to  metabolize  and
excrete  the  parent  compound.  Since  2,3,7,8-TCDF  has a whole-body  halftlme
of <2  days  1n the rat,  this species Is  quite  resistant  to  the  acute toxic
effect.   The guinea  pig,  on  the  other hand,  1s  extremely sensitive  (an
LD__ between  5 and  10 yg/kg)  because   the  compound has  a  wholebody  half-
time of  at  least  20 days.   The  monkey   has  Intermediate sensitivity because
the  whole body half-time  Is  ~8 days.   The pathological  effects  of  acute
treatment with  2,3,7,8-TCDF 1n  the  rhesus  monkey  are  summarized  1n  Table
7-25.   Table 7-26  sets  out the  LD™   for  2,3,7,8-TCDF   1n  several  animal
species.
    Mixtures  of  PCDFs  were often  used  1n  toxlclty  studies.   Mixtures  of
TrCDFs and TCDFs  given  orally  to rabbits at doses of 0.4  and 1  mg/kg (Bauer
et al., 1961) caused severe liver necrosis and often proved fatal.
7.4.2.   Subacute  Toxlclty.  The most complete  data relate to  2,3,7,8-TCDF.
Mice given 22  oral  doses  over  30 days  of  30,  200, 300 yg/kg bw  of  2,3,7,8-
TCDF  did  not  develop  clinical   signs   of  toxlclty  (Moore  et  al.,  1979).
Autopsy showed "liver weights and the  liver we1ght/bw ratio elevated, and the
thymus weight/bw ratio was low.
    When  2,3,7,8-TCDF  was  fed  to chicks  for  21  days  at  doses  of  1 and  5
vg/kg  bw/day,  mortality  was 16  and 100%,  respectively  (McKlnney  et  al.,
1976).   2,3,7,8-TCDF  at  5  yg/kg bw/day affected the  liver  moderately  and
caused thymlc Involution and edema.
    2,3,7,8-TCDF   caused  sickness and  some  deaths  In  two groups  of  three
rhesus macaques,  fed  for  6  and  2  months with  5 and 50 yg/kg  diet  (corres-
ponding to 5 and  50 ppb)  (McNulty et  al.,  1981).  The principal  pathological
changes were  trophy or  squamous  metaplasia of the sebaceous  glands, Involu-
tion of  the  thymus  and hypoplasla of the bone marrow.  In animals  that  did
1931A                               7-49                             06/22/86

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                                 TABLE  7-25

       Summary of  Pathologic  Effects of  2,3,7,8-TCOF  1n Rhesus Monkeys*
    Tissue
      Gross Effects
  Microscopic Effects
Skin and adnexa
Fat

Lymphold
Liver

B1le duct
Intestine
Clinical
pathology
Facial edema,  dry skin,
loss of eyelashes, loss
of finger and  toe nails,
streaks on ocular surface
of eyelids, and occlusion
of external ear canal

Moderate to severe loss

None
No effect

Markedly thickened
Hyperemla, petechlal
hemorrhage, focal ulcera
tlon and mucosal cysts
Hyperkeratosls; squamous
metaplasia, cystic
dilation of glands
None

Thymlc atrophy from
lymphold cell loss;
moderate atrophy of
lymphold cells In spleen
and lymph nodes

No lesions observed

Hypertrophy of biliary
duct and gall bladder
epithelium. Increased
mucous secretion

Loss of parietal cells,
Increased mucous cells,
mlcrocystlc dilatation
of crypts

Anemia, low serum
cholesterol, mild
lymphopenla, neutro-
phH1a, low serum
protein and albumin,
elevated SGOT, BUN
*Source: Moore et al., 1979
1931A
               7-50
                06/22/86

-------
                                  TABLE  7-26

           Acute Tox1c1ty of 2,3,7,8-TCDF  1n  Several  Animal  Species
  Animal
   LD50
Ug/kg bw)
Interval  Between
 Administration
   and Death
     (days)
  Reference
Chicken
Guinea pig
ND = No data
      <5
  >5
     21
      9-20
McKlnney
et al., 1976

Moore et al.,
1979
Rat
Monkey
Mouse
6000
1000
>6000
ND
14-31
ND
Moore, 1975
Moore et al.,
1979
Moore, 1975
1931A
                 7-51
                               06/22/86

-------
not die  during  the feeding, recovery was  complete  after  3 months of a  diet
free of  2,3,7,8-TCOF.   It was suspected  that  the toxic effects  of  2,3,7,8-
TCDF might  accumulate above  a certain  critical  dose  and  might be  similar
whether  the  substance was  administered acutely  or  Ingested gradually  over
weeks or months.
    Male  guinea  pigs given  2,3,7,8-TCDF  1n six  or more weekly doses   of  1
yg/kg  bw  showed  Irreversible toxldty  when  a  body  burden  of   -5.6-6.6
yg/kg  bw  was   attained,  resulting  In  progressive weight  loss  and  death
(Decad  et  al.,   1981b).   A  later  paper from  loannou  et al.  (1983)  reported
that a single  dose  of  4 yg/kg or  multiple doses  of 1  yg/kg  for  4  weeks
did not  produce  any  observable toxldty by day 36; when animals were killed
the authors  estimated the body burden  of these  animals to be  2.1  and  2.8,
respectively. A  body  burden  two or  three  times  higher  resulted 1n the deaths
of  three of  the four animals treated.  These data  Indicate that,  despite
differences  1n   Individual  sensitivity,  PCDF toxlclty  appears  only  after  a
critical body burden  1s  reached.  Similar  results were  obtained  by  Luster et
al. (1979) In female guinea pigs.
    Inbred  C57B1/6N  mice, treated  1.p.  with 2,3,4,7,8-PeCDF (30 yg/kg  once
a  week for  6-12 weeks) developed hlstopathologlcal signs  1n  the liver,  thy-
mus  and spleen.   In  an   "unresponsive" strain,  the changes  1n  these organs
were generally mild (Nagayama  et al., 1985a).
    Administration to  rats  of an  unspecified mixture of PCDF  (TCDFs, PeCDFs
and  HxCDFs)  at   a  concentration of  10  ppm In the diet  (corresponding to 0.5
mg/kg  bw)  for  4 weeks Induced chloracne-Uke  lesions  on  the ears,  loss of
body weight, low  hematocrlt  and  hemoglobin values, Increased  serum choles-
terol  and  liver llplds,  and  low  serum trlglycerldes.   At  1  ppm In  the diet
these  effects were less marked (01sh1 et al., 1978).


1931A                               7-52                             06/22/86

-------
    A  summary  of  the subacute  toxic  effects of PCDF  1n  various  animal  spe-
cies 1s provided 1n Table 7-27.
7.4.3.   Chronic  Toxlclty.    Planned  studies  of  toxic   effects  of  chronic
treatment  with PCDFs  are  lacking.  McNulty  et  al.  (1981)  reported  that
2,3,7,8-TCDF administered to  three  male rhesus macaques  In  the  diet (5  ppb)
for 6  months caused  sickness  and  two  deaths.  The major pathological changes
were  atrophy  or squamous metaplasia  of  the sebaceous glands, mucous  meta-
plasia of  the  gastric mucosa,  Involution  of  the thymus and hypoplasla of the
bone  marrow.   Animals  that  did  not  die during  TCDF dosing  recovered  com-
pletely after  3 months  of TCDF-free  diet (see  Section  7.4.2.).   Because of
the small  number  of  animals  employed,  these findings  are preliminary.   How-
ever,  It  1s apparent that some cumulative  action does occur, and  H  may be
reversible  to   some  extent.    Death  1n  the  monkeys  was  preceded  by  weight
loss,  anorexia  and  depression, but no  specific chemical  lesion  was Identi-
fied.
    A  study was made using monkeys  fed a 20-week  diet  containing  a mixture
of PCBs,  PCQs  and  PCOFs with congeners  similar  to those  found In Yusho  oil,
or a  mixture  of PCBs or  PCQs,  or commercial PCB  (Kanechlor 400).   Only the
first  group developed  hair  loss, edema of   the  eyelids,  acneform eruptions,
dermal hyperkeratosis  and pigmentation (Kunlta et  al.,  1985).  These  data
confirm PCDFs  Involvement 1n the Yusho disease.
7.4.4.   Contribution of  PCDF  to the  Toxldty  of  Industrial Products  and
Environmental   Contaminants.   PCDFs  are  released  In the  environment  as  con-
taminants of Industrial products  and must be considered  as adventitious  pol-
lutants.    Several studies have compared the toxlclty  of  Industrial products
contaminated with PCDFs with  that of  pure active  Ingredients.   Vos and  Koe-
man (1970)  found  significant  differences in the toxlcltles  of three commer-


1931A                               7-53                             06/22/86

-------
                   TABLE  7-27



Subacute Toxlclty of PCDFs In Laboratory Animals


-. J
1



o
N:
CO
cr
Compounds
2,3.7.8-TCDF
2-1somers-TCDF
4-1somers-PeCDF
4-1somers-HxCDF
2.3.7,8-TBDF
2,3.4.7.8-PCDF
2,3.7,8-TCDF
PCDFs
2.3,7,8-TCDF
2.3,7,8-TCDF
2,3,7,8-TCOF


Species/
chick
Sprague-
Dawley
rat
C57B1
mouse
mouse
adult
rhesus
macaque
(3)
mature male
guinea
pig («)
Immature
female
guinea pig


Dose
(pg/kg/day)
1 (21 days)
5 (21 days)
50 (28 days)
500 (28 days)
30-300
(30 days)
50
(10 weeks)
90
(6 months)
300
(2 months)
1 pg/kg bw week
(6-7 weeks)
1 pg/kg bw week
(6 weeks)


Mortality
W
16
100
none
none
none
none
67
33
50
30


Route
gavage
1 ppm
10 ppm
diet
gavage
0.6 ppm
diet
5 ppb
50 ppb
diet
oral
oral
Intubation


Clinical Pathology
Edema; thymlc Involution; slight
or no liver damage; no porphyrla;
no ALA Induction
Thymlc Involution; dermal lesions;
hypercholesterolemla; hyper 11 pi d-
emla; hemolytlc anemia; thrombopenla
Thymlc Involution; hepatomegaly
Dermal lesions; hyper keratosls;
dilated hair follicles with kera-
tlnous material; damaged hepatocytes
Atrophy or squamous metaplasia
sebaceous glands, mucous metaplasia
and hyperplasla of the gastric
mucosa; Induction of the thymus;
hypoplasla of the bone marrow
Bald patches, dehydration, swelling
around eyes, no hepatomegaly
Hepatomegaly and thymlc atrophy


Reference
HcKlnney
et al., 1976
Olshl et al.,
1978
Hoore et al.,
1979
Nagayama
et al., 1979
McNulty
et al., 1981
Decad et al.,
1981
Luster
et al., 1979



-------
clal PCBs with Clophen A-60 and Phenoclor  DP-6  causing  the  highest,  and Aro-
clor 1260  the lowest mortality  1n chicks fed  for  60 days diets  containing
400 ppm of each product.  Subcutaneous and abdominal  edema  and  centrllobular
liver  necrosis  were  recorded  only  In   chicks  fed  Clophen  or  Phenoclor.
Hydroperlcardlum was recorded  In  nearly  all  chicks fed Clophen  or  Phenoclor
but only occasionally In chicks fed Aroclor.  Chemical  porphyrla was attrib-
uted to a direct effect of  the  PCB.   Chemical analyses  revealed the presence
of  polar  compounds  In  the  25%  dlethyl  ether fraction of Clophen  and  Pheno-
clor.  The  polar  fraction  of  Clophen was toxic  1n the chick  embryo  assay,
and the differences In toxldty of  the three PCB  preparations  were confirmed
by  this  assay.   Mass  spectrometry  analyses   Indicated   the  presence  of
tetra- and penta-CDF 1n the polar fraction of  Clophen  and  Phenoclor (Vos  et
al., 1970).
    Later, Vos  and  Notenboom-Ram (1972)   compared  the toxic effects  In rab-
bits of  Aroclor 1260  (which was  shown   to  contain  1  yg   PCDF/g)  and  of  a
pure PCB  Isomer,  2,4,5,2',4',5'-hexachloroblphenyl.  The rabbits  were given
120 mg of  Aroclor  and  the hexachloroblphenyl dermally  5 times  a week  for  28
days.  The  animals  receiving Aroclor 1260  showed more severe  skin  lesions,
hyperplasla  and  hyperkeratosls of  the  folUcular  and epidermal  epithelium
than those  receiving the  pure  hexachloroblphenyl.   Liver damage (subcapsular
and zonal  necrosis,  hydropic degeneration,  peripheral  and  perlnuclear shift
of  cell organelles, focal cytoplasmlc  hyaline degeneration, proliferation  of
smooth endoplasmlc retlculum) and  Increased  fecal  coproporphyrln levels were
similar 1n  both  groups.   From  these  studies,  the  probable contributions  of
PCOF  and   pure  PCB  to  the toxldty  of  crude  preparations  were  assessed
(Table 7-28).
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    Goldstein  et  al.   (1978a)  showed  that  porphyrla,  cutaneous  lesions,
changes 1n liver enzymes and morphological changes  1n  the  liver  were Identi-
cal 1n female CD rats  (Charles River) fed  pure  hexachlorobenzene contaminat-
ed with  4 ppm  OCDF  and  decachloroblphenyls  for  4 months,  Indicating  that
these changes were produced by hexachlorobenzene rather than by  the  contami-
nants.
    Klmbrough and  Under  (1978)  compared the toxic effects  of  purified  and
technical  grade  pentachlorophenol  (PCP) In Sherman rats  given  dietary  con-
centrations  of  up  to  500  ppm of  each  compound for 8 months.   At  500  ppm,
technical  PCP had  severe  effects  on  the livers of  female  rats,  mainly  caus-
ing degeneration of  liver  cells  and  bile  duct  proliferation.    In male  rats
the alterations  were  less  marked.  At  100  ppm, similar but less  pronounced
effects were  observed;  only mild alterations were noted  at  20  ppm.  At  500
ppm,  purified PCP  1n  the  diet caused slight enlargement of  liver  cells  with
occasional eosinophlUc cytoplasmlc  Inclusions; no alterations were  observed
1n the  livers of rats fed  100 and 20 ppm.   These  results suggest that  most
of the  toxicity  associated  with  feeding technical   PCP  to  rats at  these  con-
centrations   stems  from  toxic  contaminants  rather than  from  PCP  itself.
Technical  PCP has  been shown  to  be   contaminated  with PCDD  and PCDF  (Gold-
stein  et  al., 1978b)  but  the contributions  of the various  Isomers to  the
toxic effects of PCPs have yet to  be  established.
    The toxicity of  a  soot  that  contaminated  an office building in  Bingham-
ton  (NY)  after  a  fire  Involving an electric  service  transformer  and  its
dielectric fluids  that was composed  of Aroclor 1254  (65%)  and  chlorinated
benzenes (35%) with some trace additives, was studied;  the soot  was  found to
contain PCDO  (2.8  ppm) and 2,3,7,8-TCDF  (124-273  ppm) (Smith et  al.,  1981)
and a  tentative estimate of  the  total   amount  of  PCDF was  In  the  range  of


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                                  TABLE 7-28

            Probable  Contributions  of  PCDF  1n  Aroclor  1260  and  Pure
         2,4,5,2',4',5'-Hexachlorob1phenyl  to the Tox1c1ty In Rabbits
                       of  PCBs  Applied at 120  mg/50  cm2*
       Dose                Chloracne       Edema       Liver         Hepatic
                                                       Damage       Porphyrla
Aroclor (with PCDF)           n-            t+           tt

PCB (PCDF-free)               +             -            +•             n-


*Source: Vos and Notenboom-Ram, 1972
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0.5%.   In  guinea pigs  the  oral LD5Q  of  the  soot  (0.75% aqueous  solution)
was  410  mg/kg with an  equivalent  of  0.5  and 20  vg/kg of 2,3,7,8-TCDD  and
TCDF, respectively.   On  the basis  of  the  reported respective LD5Q  (Huff  et
al., 1980) the  toxlclty  could  not  arise only  from  these  halogenated congen-
ers  but probably  came  from other  pollutants as  well  (SUkworth  et  al.,
1982).   After acute  treatment  with the soot  serum, trlglycerldes were  ele-
vated;   alkaline  phosphatases   decreased;  body,  thymus  and  kidney  weight
decreased;  and  hyperplasla   of  the pancreatic duct developed.   Guinea  pigs
fed  soot developed  liver steatosls and smooth endoplasmlc retlculum prolif-
eration and  mltochondrlal ultrastructural alterations  (Turner  and  Collins,
1983, 1985).  Dermal  application  to the  rabbit  at a dose equivalent  to  500
mg/kg for 24  hours  caused no overt toxlclty,  although  hepatic  centrllobular
hypertrophy was  observed.  For subchronlc studies  soot was administered  to
guinea  pigs for 90 days,  mixed  Into food  at  five  dose  levels  between 0.2 and
231.5 ppm.   Mortality reached  35% at  231.5  ppm  and  30% at  46.3  ppm.   No
effect  attributable to  soot  exposure  was  noted In  animals receiving 0.2  ppm
soot.   Toxic  effects  were  similar but  rose  at  slightly lower total  doses
than with acute exposure (DeCaprlo  et  al.,  1983).
    The l.p.  toxlclty In Immature  Wlstar  rats (lOOg)  of a PCDF  composition
the  same as  that found  1n  Yusho  oil  was  compared  (Bandlera  et al.,  1984a)
with that  of  the corresponding PCB  composition;  20% weight  loss  and  50%
reduction In thymus weights  relative to controls  was caused by  398 mg PCB/kg
bw.  The PCDF  mixture was as follows:  2,3,7,8-TCDF,  7.4%;  1,2,4,7,8-PeCDF,
6.1%;  1,2,3,7,8-PeCDF,   19%;  2,3,4,7,8-PeCDF, 29.4% and  1,2,3,4,7,8-HxCDF,
39.1%.
    The PCQ  contaminants In Yusho oil were  as   toxic  as PCBs  In  eliciting
Yusho symptoms  (Hor1  et  al., 1978, 1982).  Thus,  PCDFs  are  the  most  probable


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causal agents of Yusho.  This was also  shown  (Kunlta  et  al.,  1985)  explldty
by experiments on rats and monkeys.
7.4.5.   Some Particular Aspects of  the  Toxic  Reactions.
    7.4.5.1.   DERHAL TOXICITY — Chloracne can  be  produced by a  number  of
chlorinated aromatlcs  and has  been  observed  among workers  In contact with
these  compounds.   Chlorinated  naphthalenes,  PCB,   PCDD and  PCDF  can  all
Induce chloracne  In man.  Chloracne  Is  described  as  the formation  of  come-
dones with  or  without  cysts  and pustules.  In chloracne  the  folUcular ori-
fices become  clogged with  sebaceous  and keratlnous  material.   Hyperkeratosls
of the  epidermis,  cystic dilatation  of  the  hair follicles, and an  Increase
In melanin  pigment  are fairly common findings.  Chloracne can be  Induced by
external contact with these chemicals or by systemic absorption.
    Investigations  In  animals have shown  that  different  species develop dif-
ferent types  of  skin  lesions on exposure  to  chloracnegenlc compounds.  Rab-
bit  ear  skin  provides  a good  test  for  the  development of acneform  derma-
titis.  Application of  a  mixture of  IrCDF  and TCOF  to the rabbit  ear result-
ed  In hyperplasla  and  hyperkeratosls (Bauer  et al., 1961).   Yos and  Beems
(1971) reported  that  application to rabbit   skin of  a  25%  d1ethylether-ex-
tracted polar  fraction  of  Phenoclor  and  Clophen  (Identified as consisting of
TCDFs  and  PeCOFs)  caused hyperplasla  and hyperkeratosls of the  folUcular
epithelium.   The fraction  from Phenoclor  was  more  active  than  that from
Clophen.
    Vos and  Notenboom-Ram (1972)  compared the skin toxldty of Aroclor 1260
with  2,4,5,2',4',5'-hexa-CB.   Dermal  application   of 120  mg PCB/50  cm2  5
times a  week for 4 weeks  to the shaved  backs  of  rabbits resulted  1n  early
macroscopic  skin lesions  In  the  Aroclor group, but  not In the group  given
the pure PCB  (see Table 7-28).


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    TCDFs and PeCDF  Induced  hyperkeratosls  of  the skin when  applied  to rab-
bit  pinna  for  3  days.   When  dally  doses of  4  yg of  2,3,7,8-TCDF  were
applied  to the  rabbit ear for  5  days, the animals  developed hyperkeratosls
of the  treated  ear (Klmbrough et  al.,  1978).   Hyperkeratosls was  also pro-
duced 1n hairless mice fed rice oil  contaminated  with Kanechlor  400 (Inagaml
and  Koga,  1969).   Ear lesions  resembling chloracne  were  reported within  3
weeks In Sprague-Dawley  rats  fed  a mixture of two  tetra-  ,  four  PeCDFs,  and
four HxCOFs (Olshl et al., 1978) at  a  dose  of  10  ppm PCDF  1n the diet and 1n
mice fed 0.6  ppm  PCDF  (Nagayama  et al.,  1979).   No acnelgenlc  response In
the  rabbit ear  bloassay  was  reported  with  2,8-DCDF  and 2,4,8-TrCDF  (Kodba
and Cabey, 1985).
    The  dermatologlcal severity  In  Yu-Cheng patients 0.5  years  after  expo-
sure was  related  (Kashlmoto  et al., 1985)  to  the presence of PCDF,  PCQ  and
PCB  In  blood,  but workers  exposed to similar amounts  of  fresh  PCBs  showed
only mild  clinical  signs.   Investigations  on 10 female  Cynomolgus  monkeys
(Kunlta  et al., 1985) Indicated that dermal symptoms  characteristic of  Yusho
could be Induced after 16-20  weeks  by  oral  administration  of PCDF from Kane-
chlor  400  (20  vg/day),  or  PCB (5  mg/day) plus  PCDF  (20  yg/day) but  not
by PCB alone (5 mg/day),  or by PCQs (5  mg/day).
    7.4.5.2.    ULTRASTRUCTURAL LIVER ALTERATIONS — A number of  character-
istic ultrastructural alterations  1n  hepatic  cells  have  been  seen  1n rats
and monkeys In response  to dloxlns  and PCBs and  In  guinea  pigs  fed with BSOB
soot (Klmbrough  et al.,   1972;  Burse et  al.,  1974;  Sllkworth et  al.,  1982;
Turner  and Collins,  1985).   They  consisted  of  I1p1d  droplet  formation,
Increased  smooth  and rough  endoplasmlc  retlculum and mitochondria!  altera-
tions.    Mitochondria! lesions In  animals seem to be reversible  and  tend to
return to their usual structure with the passage  of  time.


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    In humans similar mltochondrlal structural alterations have  been  report-
ed after exposure  to  chlordecone  (Guzellan  et al., 1980), to PCDFs +  PCB  1n
the Yusho  Incident  (Yamamoto  et al.,  1971;  Hlrayama  et al., 1969),  to  PCB,
PCDD,  PCDF, naphthalenes and blphenylenes 1n  the BSOB  electrical  transformer
fire (Schecter et al., 1984).
    From these  studies mltochondrlal  alterations  (mltochondrlal  pleomorph-
1sm, giant  mitochondria,  arrangement  of  the mltochondrlal  crlstae parallel
rather than perpendicular  to  the  mitochondria!  axis)  seem the most specific
ultrastructural  lesions for humans  exposed  to PCB and  furans, while  changes
In endoplasmlc  retlculum  and  Intracytoplasmlc llpld droplets are  frequently
seen  after toxic  damage  following  exposure to  nonchloMnated  hepatotoxlc
chemicals  (Schecter  et  al., 1984).   Therefore,  ultrastructural analysis  of
livers,  together  with  the  analysis of  fat  biopsies  for their  chlorinated
chemical levels, may  provide  a  useful  biological  marker  1n  evaluating human
exposure to dloxln and  related  compounds  (Schecter et  al., 1985b).  The role
of PCDF  1n  these  ultrastructural  morphological  lesions remains to be  clari-
fied.
    7.4.5.3.   PORPHYRIA ~ In  birds  and mammals,  exposure  to  PCB  and  PCP
causes changes  1n  hepatic porphyrln synthesis, producing a  form  of  hepatic
porphyMa similar  to  human  prophyMa  cutanea tarda (Goldstein et  al.,  1973,
1975,  1977a,  1978a).   Disturbances  of  porphyrln biosynthesis have been  con-
nected with  an  Increase  In the activity  of the  rate limiting enzyme,  ALA
synthetase  (Goldstein  et al.,  1976).    PCDFs  have been  shown  not to  cause
hepatic  porphyMa  and  to  Induce  only  slight  ALA  synthetase  activity  In
laboratory animals.  Goldstein et al.  (1976)  found that 2,3,7,8-TCDF  did not
Induce ALA  synthetase  In  chicks after 21 dally doses  of 1 yg/kg bw  and did
not produce  porphyrla  even at  the lethal  dose of 5  pg/kg  bw/day,  whereas
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specific PCB produced  both  effects.   In rats, a mixture of  PCDF  (2  TCDFs,  4
PeCDFs and 4 HxCDFs) at dietary concentrations of  10  and  100 ppm for 4 weeks
only  slightly  Induced ALA  synthetase activity  and  slightly  Increased  uro-
porphyMns (Olshl  and Hlraga, 1978).   2,3,7,8-TCDF  did not  cause  porphyrln
accumulation In livers of mice up  to  28  days  after a  dose as high as 4 mg/kg
bw (Goldstein et al.. 1974).
    The  lack  of effect of  PCDF  on porphyrln  accumulation 1n the  liver  had
already  been  emphasized  by  Yos et  al.  (1970), who observed  that  three com-
mercial  60%  chlorinated  PCB  mixtures  (Phenoclor  DP-6,  Chlophen 1-60,  and
Aroclor  1260)  Induced a  similar  degree and  type  of  porphyrla  although  the
degree of contamination by  PCDF varied  for  these formulations.   Chlophen  and
Phenoclor contained  TCDFs and  PeCDFs  1n amounts responsible  for  other toxic
effects.  These  findings  suggest  that  PCDFs, at  least In  the  experimental
conditions  tested,  do not  play  an   Important  role   1n  the  porphyrogenlc
effects of the Industrial  chemicals they contaminate.
    Based on  some common mechanism of  action  of  PCDF with PCDD and other
porphyrogenlc  chlorinated  compounds,   the  hypothesis  that  PCDF  can  also
elicit porphyrla cannot be  ruled out, although this has not  yet  been experi-
mentally established.
    7.4.5.4.    IMMUNOSUPPRESSION -- Few  studies  have   aimed  at   finding
alterations  of  the  Immune  system  by  PCDFs  1n laboratory   animals.   Toxic
doses  of 2,3,7,8-TCDF and  2,3,4,7,8-PeCDF  and 2,3,7,8-TBDF   have  been shown
to cause severe thymlc atrophy  1n  the guinea pig and  mouse  (Moore  et al.,
1979).   Lymphopenla, atrophy of the thymlc  cortex, and  reduction In the num-
ber  of germinal  centers  In  the  spleen appeared  In  chicks  dosed  with  1-5
ug/kg  bw  for   21  days  (McKlnney  et al.,  1976).   Studies  1n the  female
guinea pig (Luster  et  al.,  1979) showed that  the  effects  of 2,3,7,8-TCDF on


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the  Immune  system resemble  those  of  2,3,7,8-TCDD. Depression  of  cell-medi-
ated  responses  was  found  only at  higher  dosages  tested  (0.5-1  yg/kg  bw
weekly  for  6  weeks).    In  this  animal  species  the  LD5Q  Is  5-10  vg/g.
Humoral Immunity was only  slightly  depressed.   These  results  were  Interpret-
ed  by the  authors  as   Indicating  possible  marked  effects of  PCDFs  on  the
Immune  system.    As  for  2,3,7,8-TCDD,  consequences  would   be  severe  If
2,3,7,8-TCDF were administered  during the developmental phase  of  the Immune
response.
    Single  doses  of 2,3,7,8-TCDF  have  been tested  1n  mice.   Reduction  In
thymus weight and splenocyte numbers  were  observed  with  relatively  low  doses
of  2,3,7,8-TCDF  given   either  orally  or   1.p.  (100  vg/kg  bw)  to  C57B1/6
mice,  where the  LD5Q   for  2,3,7,8-TCDF  Is  reported  to be  >6000 vg/kg  bw
(Moore  et   al.,  1979).    Humoral  antibody  production  was  significantly
Inhibited with  a  dose-response  curve similar  to  that of  2,3,7,8-TCDD,  but
2,3,7,8-TCOF was  -30  times less active  than 2,3,7,8-TCDD, the  latter  being
as  suppresslve  after  6  weeks   as  after  1   week,  while  recovery  from  the
effects of 2,3,7,8-TCDF  was complete by 6 weeks (Vecchl et al.,  1983a).
    The effects of  a mixture  of TCDD and  TCOF on Immune  responses  (thymus
weight and  humoral  antibody production)  were Investigated using  the toxins
at  different  ratios  (TCDD:TCDF  =  1:1;  1:10;  1:100 pg/kg) to  cover  differ-
ent  "natural"  conditions  of  exposures  (Vecchl  et al.,  1985).  TCDF  given
alone at  each of  the  three doses used had no  effect  on  thymus  weight;  added
to  the  TCDD, 1t  did  not modify  Us  effect  on  thymus weight.   Work now  In
progress shows that an additive  depressive effect  appears  at  the 1:100  ratio
1n antibody production.
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    Increased susceptibility to endotoxln has been described  In  mice  treated
orally with  a 1CDF  (12%)  and PeCOF  (88%)  mixture once  a  week  for  4  weeks
(Oishi and Hiraga, 1980).
    2,3,7,8-TCDF-1nduced  thymlc   atrophy  and  Immunosuppresslon  were   more
marked  1n  mouse  strains   sensitive  to  Induction  of  AHH  by  3-MC  or  by
2,3,7,8-TCDO  than In  strains genetically  more resistant  to Induction,  as
described  for  1CDD  (Vecchl  et  al., 1983b),  suggesting that  the  Individual
genetic background may play a role  In  the degree of  PCDO- and  PCDF-1nduced
1mmunotox1c1ty.
    Recent  data  have  shown  a  positive  correlation   between AHH  Inducing
ability  (see  Section 7.4.6.) of  different  PCDFs given  as  single  doses, and
thymlc  Involution (Yoshlhara et  al., 1981).   Studying jn  vivo  and  in  vitro
structure-activity relationships,  Mason  et  al. (1985)  found a good linear
correlation  (v  = 0.88) for  15 PCDF  between thymlc atrophy  and  ]n vitro AHH
Induction.   Thus, toxlclty of DFs  to  the Immune system could be  related 1n
some way  to their  Inducing potential.
    Interestingly, there are  also  reports (Kunlta  et  al., 1985;  Hor1 et al.,
1981)  that,  In  female monkeys,  commercial PCB  preparations  (Kanechlor 400)
specifically  treated to eliminate  contaminant  PCDF,  given In the diet for 20
weeks,  were more  Immunosuppresslve  on  humoral  antibody production  than the
commercial  PCB with  PCDF  Impurities or  normal  commercial  PCB preparations.
An  antagonistic  effect  regarding Immunosuppresslon and enzyme  1nduc1b1l1ty
In  mice was reported  by Rlzzardlnl  et  al.  (1983)  who administered to C57B16
mice  an artificial mixture of 2,3,7,8-TCDD and  2,3,7,8-TCDF at  the  ratio of
about  1:8 and  found that  the mixture  elicited  a  significantly  lower effect
on  antibody  production (50%  Inhibition)  than  TCDD alone  (80% Inhibition).
These data seem to be preliminary and need further Investigation.  Converse-


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ly, other  reports  suggest  that  the simultaneous presence of PCDF and PCDD In
BSOB  soot  with  the approximate composition of  1.2  ppm TCDD,  48 ppm TCDF and
0.5%  PCB may  have synerglstlc  effects  with  regards  to  toxldty  In guinea
pigs  (Sllkworth et al., 1982).
    Male Sprague-Dawley rats  (Nakan1sh1  et  al., 1985a) given  1.14 mg PCDF/kg
bw  by gastric  Intubation  3 times/week or 6 t1mes/2 weeks showed necrosis of
the Clara  cells  in  the Itmg bronchioles and  marked  atrophy  of  the thymus,
whereas  similar treatment  with 11.4  mg Kanechlor  400/kg bw  had  only  mild
effects.   Male  Sprague-Dawley rats and  female  Cynomolgus  monkeys (Kunlta et
al..  1985)  given  67  vg  PCDF  from  Kanechlor  400/kg  bw and  8 vg PCDF/kg
bw/day,  respectively,  over  22-day  and 20-week  study periods presented Immun-
osuppresslon and thymlc atrophy.   The PCBs  from Kanechlor 400 were much less
potent than the PCDFs.
    Recently Kochman  et al.  (1985) found,  In  human  subjects  exposed to PCDF
as a  consequence of a  PCB  transformer fire  and of the dispersion of the soot
1n  the environment, an Increase In a  specific  subpopulatlon  of T suppressor
cells, although the total  suppressor  as well  as  the total helper cells  were
similar 1n control and 1n  exposed subjects.
    7.4.5.5.   ENZYME  INDUCTION —
    7.4.5.5.1.    Introduction —The  mechanism  of  toxlcity   of  PCDFs   has
been  extensively  studied  but has  not yet been elucidated.   These  compounds
are potent Inducers of one  of  the  hepatic mixed function oxldases,  AHH,  that
metabolized  precarclnogens   such   as   benzopyrene.   Investigations  both  jji
vitro  and  jjn  vivo to  clarify  the  biochemical  basis of  the Inductive effect
of TCDD and related polyhalogenated congeners  have  led to the Identification
of a  macromolecular  species 1n hepatic  cytosol of  rodents that  binds  these
compounds specifically with  high affinity (Poland et  al.,  1976).   The  cyto-


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sollc protein 1s known  to  act  as a receptor for AHH  Inductive  activity.   No
evidence 1s  currently  available of  direct  Involvement  of  the Induction  of
AHH with any sign of toxlclty  Induced by  these  compound.s;  however,  the bind-
ing  to  the  Ah  receptor as  a  mediator  of toxlclty  1s now accepted  from  the
data  available   on  structure/activity  studies  and   genetic  segregation  of
toxlclty with the Ah locus  (Roberts et  al.,  1985).
    7.4.5.5.2.    AHH Induction — PCDFs are  potent Inducers  of the  hepatic
mlcrosomal   n-monooxygenase  system  (Goldstein et al., 1978b;  Poland  et  al.,
1976; Kawano  and Hlraga,  1978).   This  enzyme  complex  (also called  hepatic
mlcrosomal   drug-metabolizing  enzymes)   metabolizes  drugs  and  other  foreign
compounds.    It  consists of NADPH-cytochrome  P-450 reductase and  cytochrome
P-450,  the  terminal component  that  contains the  active site  of  the enzyme
and  determines  substrate specificity.   There are several  distinct  Isoenzymes
of cytochrome P-450 1n  liver mlcrosomes that have  different  substrate speci-
ficity and are Induced differently  by a number  of compounds.
     Compounds that  Induce  hepatic  mlcrosomal monooxygenase activities can be
divided  Into two  major  classes:   one   1s  typified  by  phenobarbltal  that
Induces  several  subspecies of cytochrome P-450  and associated  monooxygenase
activities  directed toward  a wide  variety of  substrates;  the  other 1s repre-
sented  by   3-methylcholanthrene  (3-MC)  that Induces  distinct  Isoenzymes  of
cytochrome  P-450 termed respectively  1n the rat cytochrome P-450C  or P-450d
(Thomas  et  al.,  1983)  and  In  the  mouse  P,- and  P -P450  (Nebert  and
                                                 I        O
Neglshl, 1982).   These Isoenzymes  are associated with  enzyme activities for
a  more  limited  group  of  substrates and  AHH activity  Is  one  of  them.   The
PCDFs belong to  the same class of Inducers as 3-MC.
 1931A                               7-66                             06/22/86

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    In the rat  (female  CD  strain,  Charles  River),  2,3,7,8-TCDF  (89% pure and
2%  unspecified  PeCDF)  given  for  3  days  at  doses  of  0.1-2.5 vg/kg  bw/day
was a potent  Inducer  of  hepatic  drug-metabolizing  enzymes  (Goldstein et al.,
1978b).   The  approximate  ED5Q  for AHH  Induction  In the  rat (0.5  yg/kg  bw
x  3 days)  Is roughly  double  that  reported  for  2,3,7,8-TCDD  (as  a  single
Injection); which  1s  30,000 times  more potent  that  3-MC  (Poland  and Glover,
1974) 2,3,7,8-TCDF  reduced  N-demethylase activity  at all  doses  (Goldstein  et
al.,  1978b)  and Increased  P-448 [Previous terminology for  cytochrome  P-450
Isoenzymes  Induced  by 3-MC was  "cytochrome  P-448."   This term will  be used
In  this  paragraph  to denote all  forms of cytochromes  Induced by  3-MC  class
of  Inducers as  simplified  expression.]   Kawano  and Hlraga  (1978)  Investigat-
ed  the  effect  of   a  mixture of  tetra- (12%)  and  penta-CDF  (88%)  In  male
Wlstar JCL  rats (105-165 g bw)  at doses of  10,  100, 1000  yg/kg  bw/day for
3 days.   They found effects similar to  those elicited  by  3-MC  (20 mg/kg bw)
on  mlcrosomal drug-metabolizing enzymes.   Both drugs  Increased  p-n1troan1-
sole  demethylase  activity, moderately  Increased aniline  hydroxylase  activ-
ity,  and  produced   Uttle  change 1n  amlnopyrlne demethylase  activity.   Fur-
thermore, both drugs Increased cytochrome P-448.
    The AHH  Inducing  potencies  of PCDF,  TCDD and PCB were  compared  In  rats
by  Nagayama  et al.  (1983).   A  mixture  of  PCDF   (13%  1,2,7,8-TCDF;  35%
2,3,7,8-TCOF; 1%  1,2,4,7,8-PeCDF ;  49%  1,2,3,7,8-PeCDF ; 1%  2,3,4,7,8-PeCDF;
1%  unspecified  hexa-CDF)  and  TCDD  at  the  dose  of 5  yg/kg bw  and a  PCB
mixture (Kanechlor-500)  at  the dose of  50  mg/kg bw were given 1.p.  TCDD only
enhanced   AHH  activity 1n  the  prostate, thymus  and  spleen.   In the  kidney,
lung and  liver  the order  of AHH InduclbllHy was TCDD  >  PCDF »  PCB.  PCDF
caused the  greatest  Induction  In  the  lung.   Thus, the lung  and kidney  seem
more sensitive than the  liver  to the  Inductive properties  of  these  compounds.


1931A                               7-67                             06/22/86

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    Recently, Bandlera et al. (1984a) treated rats with a  reconstituted  mix-
ture of PCDF and PCB  that reproduced the  approximate  composition  of  the  PCDF
and  PCB  persisting 1n  the   liver  of Yusho  patients  according  to the  most
recent data  (Rappe et al.,  1983a;  Masuda and Kurokl, 1982; Nagayama  et  al.,
1983).   The  mixture  of   PCDF,   Including   2,3,7,8-TCDF;   1,2,4,7,8-PeCDF;
1,2,3,7,8-PeCDF; 2,3,4,7,8-PeCDF and 1,2,3,4,7,8-HxCDF  (7.4, 6.1,  19.0,  24.9
and  38.1%,  respectively), was  Injected  1.p.  at various doses.  The  dose-re-
sponse pattern  on AHH  Induction  showed  that the  mixture elicited,  4- and
40-fold Increases, respectively, In  the liver enzymatic activity  of  rats,  at
doses  of  22 and 63 yg/kg bw.   All the  PCB mixtures  were  significantly  less
active as  AHH  Inducers than PCDF.   From an  analysis of the PCBrPCDF ratios
1n  the contaminated  rice oils  In  Taiwan  (100:0.32)  and In  Japan (100:0.16)
and  of  the ratios   of  the  respective  EC5Q  for  AHH  Induction  (at  least
1:700), the  authors suggest  that PCDF must be considered  the major etlologlc
agent  In  the contaminated  rice oils and  In  Yusho  poisoning  of victims still
suffering from this syndrome (Bandlera et al., 1984a; Sawyer  and Safe, 1985).
     Induction of  AHH  activity by  3-MC  Is expressed  almost  exclusively  as a
single autosomal  dominant   trait regulated  by the  Ah locus  (Nebert  et  al.,
1975).  In  Inbred  strains  of mice AHH  1nduc1b1l1ty  Is  genetically separate.
Eight  PCDF   were  given 30  vg/kg  1.p.  to four Inbred  strains of mice  with
different  phenotypes  of Ah  locus  (Nagayama  et  al., 1985b).   In responsive
mice (C57)  with  the  exception of  1,2,3,6,7-PeCDF  and  1,2,3,4,6,7-HxCDF all
the  PCDFs were active;  In   unresponsive  strains  (DBA and ODD)  no Induction
was  elicited by the  8  PCDFs tested.   Results Indicate  that  AHH responsive-
ness 1n mice segregates  with the AHH Inductive activity by PCDF and may also
segregate  with  the toxic potency  of the Isomers as  In fact  has  been demon-
strated for  the 1mmunotox1c1ty  (Vecchl  et al., 1983b).


1931A                               7-68                              06/22/86

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    Human tissue appear  to  have  Ah receptor molecules with  properties  simi-
lar to  those  observed In animals  (Nebert  and Jensen, 1979; Roberts  et  al.,
1985;  Gaslewlcz  and  Rued,  1984).   Recently Wong  et al. (1985,  1986)  con-
ducted a study on pregnant  Chinese women  1n  Taiwan  exposed 4-5 years  earlier
to contaminated rice oils containing PCOFs,  PCBs  and  PCQs.   Placental  mlcro-
somal  fractions  from exposed subjects  presented  significantly high  AHH  and
ethoxyresoruf1n-o-deethylase  (EROD)  activities.   In  the  same  subjects  pla-
centa! mlcromes were  found  to contain  a protein  that  cross-reacted with  the
antibodies against  cytochrome P-450,  Isoenzyme 6.   This   Isoenzyme 1s  known
to be Induced by polychlorlnated  hydrocarbons.
    The effect  of  PCDF  was  studied  1n human lymphoblastold cell  lines  with
different AHH  1nduc1b1l1ty  for  3-MC  (Nagayama  et  al.,  1985b).   Degrees  of
the enzyme  1nduc1b1lH1es  of PCDFs  Increased proportionally with those  for
3-MC,  Indicating that 1n humans  also,  AHH  1nduc1b1l1ty for PCDF reflects  the
genetic  susceptibility  of   the  cells.    Induction   with  2,3,4,7,8-PeCDF;
1,2,3,4,6,7-HxCDF and 1,2,3,4,7,8-HxCDF was  comparable to  that  with TCDD  and
higher  than  with TCDF,  Indicating a  species difference  compared with  the
laboratory animals.
    7.4.5.5.3.   Structure-Activity    Relationship    for     Induction  —  The
structure/activity relationship  of PCDFs  to  AHH  activity was  studied  using
the chick  embryo by  Poland et  al.  (1976) who found that  2,3,7,8-TCDF  and
2,3,4,7,8-PeCDF, as well  as  the  corresponding CDD derivatives,  were the  most
active Isomers.  These studies showed  that both the  number  and the position
of the  chlorine  atoms are  Important.   The Isomers  that  Induce  AHH activity
have two common properties:  halogen atoms should occupy  at  least  three,  and
for maximal potency,  four  of the  lateral  ring  positions   (positions  2, 3,  7
1931A                               7-69                             06/22/86

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and 8);  at least one  ring perl-position  (positions  1,  4,  6,  9) should  be
unsubstUuted.
    Nagayama  et  al.  (1983)  demonstrated  In  rat  lung and liver  mlcrosomal
preparations  that chlorlnatlon  at position  1  reduced AHH  InduclblHty.   In
fact 2,3,7,8-TCDF and 2,3,4,7,8-PeCDF are more active on  liver  AHH Induction
than 1,2,3,7,8-PeCDF and 1,2,3,4,7,8-HxCDF.  A similar reduction  was  observ-
ed for Induction In the lung by  2,3,6,7-TCDF and  2,3,4,6,7-PeCDF  In  relation
to  1,2,3,6,7-PeCDF  and  1,2,3,4,6,7-HxCDF.   Moreover,  an  additional  Cl  sub-
stitution  at  the C-4 (or   C-6)  position  Increases the AHH  Induction  potency
In relation to the corresponding C-l  or  C-9 substitutes.
    Several data suggest   that  species  differences  may change  the order  of
PCDF  Isomers  for AHH-1nduc1ng activity.   In mice 2,3,7,8-TCDF elicited  the
highest  AHH  Induction  (Nagayama et  al.,  1985b,d),  In rats  2,3,7,8-TCDF  for
some  authors  (Yoshlhara et  al.,  1981;  Nayayama  et  al.,  1983)  In  liver  and
lung  mlcrosomes  but  2,3,4,7,8-PeCDF  for others  (Bandlera  et al.,  1984b;
Mason et al., 1985)  1n liver.
    The  small number of in vivo  kinetic  data available on this  class of com-
pounds make  1t  difficult  to compare in  vivo and  in  vitro results.  The role
of  tissue  distribution, blotransformatlon  and  elimination  of  PCDFs should be
carefully  considered for  each  compound  under study.  Only  2,3,7,8-  TCDF  has
been  studied  1n  some detail 1n this regard  (Decad  et al., 1981a,b;  Blrnbaum
et al.,  1980, 1981;  Blrnbaum, 1985).
    The  most  extensive structure/activity  relationship   studies  have  been
made  using  the  highly  (AHH)   Induclble  rat  hepatoma H-4-11-E   cell  lines
(Bradlaw and  Casterllne, 1979; Bandlera et al., 1984a,b;  Mason et al., 1985).
    Mason  et al.  (1985)   correlated the  in vitro  AHH-1nduc1ng  potency  of
PCDFs with the  thymlc atrophy  or  body  weight loss caused  by each congener 1n


1931A                                7-70                             06/22/86

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rodents.   Although  this 1s  an  obvious oversimplification  of  the problem  It
may  be accepted  as  a  good  model  when a  rapid  Indication  of the potential
tox1c1ty  of  new  congeners  1s  needed.   This point  will  be discussed In more
detail  In  other Sections.
     Bradlaw  and  Casterllne  (1979),  working with rat hepatoma  cell  culture
[as  a  rapid  screen  test for detecting minute (pg) amounts of  certain classes
of  compounds,  e.g.   PCDFs,  PCDDs and PCBs],  found  that  AHH  activity was
Induced by PCDF containing  at  least  3 or  4 lateral  ring positions substitut-
ed by  chlorine  atoms  In the ring positions at  2,3,7,8; congeners with two  to
fewer  chlorine  atoms  In the lateral positions  showed  no Inductive effect  up
to a dose  of 5 or 10 mg/kg bw.
    Table  7-29   summarizes  the  quantitative  jji   vitro  data  reported   by
Bandlera  et  al.  (1984b) and Mason et  al.  (1985)  concerning the relationship
between the  different  TCDFs  In  their  AHHand EROD-1nduc1ng potency.  Bandlera
et  al. (1984b)  showed  that the  AHH  Inductive  ratios  of  the  2,3,4/1,3,8,
2,6,7/1,3,8,   and  2,3,4,6/1,2,4,8 pairs of PCDF  Isomers  were 128, 7  and  9,
respectively.
    Figure 7-1  reports  a   plot  of the  -log EC5Q   values  for In vitro AHH
Inducing  potencies  versus  the  -log  ED5Q  values  for body  weight loss and
thymlc atrophy  for  a  series of PCDF congeners, a  PCDF mixture with  a compo-
sition similar  to that found 1n the liver  of Yusho patients  and TCDD.   Sta-
tistical analysis of  both plots  showed an  excellent correlation, corroborat-
ed by  the  fact  that the compounds  tested  differed widely In both jm  vivo and
In vitro  biological  and toxic potencies.   2,3,7,8-TCDF  was the  most  active
AHH Inducer in vitro and the most powerful  and  toxic congener in vivo.
1931A                               7-71                              06/22/86

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                                 TABLE  7-29

    Effects  of  Different PCDF Congeners on Rat Hepatic Cytosollc Receptor
  Binding  Avidities, AHH and EROD Induction In Rat Hepatoma H-4-II E Cells3
PCDF
Congeners
Dlbenzofuran
2-
3-
4-
2,3-
2,6-
2,8-
1,3,6-
1,3,8-
2,3,4-
2,3,8-
2,6,7-
1,2,3,7-
1,2,3,6-
2,3,4,7-
2,3,4,6-
2,3,4,8-
2,3,6,8-
2,3,7,8-
1,2,4,8-
1,2,4,6,7-
1,2,4,7,9-
1,2,3,4,8-
1,2,3,7,8-
1,2,4,7,8-
1,2,3,7,9-
Receptor Binding Avidities
(ED50) M
<10
2.8x10'*
4.2±0.6xlO~5
<10"3
4.72xlO"6
2.46xlO"4
2.57xlO"6
4.40xlO~6
8.50xlO~5
1.9xlO"5
1.0±0.1xlO~6
4.5xlO"7
1.12xlO"7
3.54xlO~7
2.51xlO~e
3.5xlO"7
2.0xlO"7
2.2xlO~7
4.H0.6xlO~8
>10"5
6.77xlO'5
2.0xlO~5
1.2xlO~7
7.45±2.04xlO~ed
1.3xlO"6
3.98xlO~7
Enzyme Induction
(EC50)
AHH (M)C
ND
ND
ND
l.OxlO"5
2.19xlO"6
6.17xlO~s
3.95xlO~5
2.53xlO"6
1.94xlO"5
1.51xlO"7
2.49xlO~6
2.80xlO~6
2.70xlO~5
>10"*
1.79xlO"8
1.32x10"*
4.14xlO~8
1.04xlO~6
3.91xlO~9
1.20xlO~5
3.25xlO~7
3.77x10"°
2.09xlO"7
2.54xlO~9
1.06X10"7
8.60x10'°
Potencies
EROD (M)C
ND
ND
ND
1.71xlO~5
4.84x10"*
6.31xlO~5
4.0xlO"5
3.37x10'*
3.02X10"5
2.48xlO"7
1.56x10"*
3.13x10'*
6.30xlO~5
>10~4
1.48x10"°
1.13x10"*
3.76x10'°
7.79X10"7
2.02xlO"9
9.26xlO~5
3.48xlO"7
3.84x10"°
1.63xlO"7
3.06xlO~9
1.48X10"7
8.60x10'°
1931A
7-72
                                                                     06/22/86

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                             TABLE 7-29  (cont.)
PCDF
Congeners
1,2,4,6,8-
1,3,4,7,8-
2,3,4,7,8-
2,3,4,7,9-
1,2,3,4,7,8-
1,2,3,6,7,8-
1,2,4,6,7,8-
2,3,4,6,7,8-
2,3,7,8-TCDD
Receptor Binding Avidities
(ED50) M
3.09xlO~6
2.00xlO~7
1.50±0.1xlO"8<1
2.00xlO~7
2.3xlO~7
8.3xlO"6
4.7i0.4xl08d
l.OxlO"8
Enzyme Induction
(EC50)
AHH (M)c
l.OOxlO'5
1.60xlO~9
2.56xlO"10
7.90xlO~»
3.56xlO~10
1.47xlO"9
4.24X10"8
6.87xlO~10
7.23X10'11
Potencies
EROD (M)c
1.20xlO~5
1.40x10"'
3.79xlO"10
1.24xlO~9
3.79xlO~10
1.24x10"'
2.93X10"8
5.75xlO"10
1.85xlO"10
aSource:  Bandlera et  al.,  1984b;  Mason  et al.,  1985

bAHH = Aryl hydrocarbon  hydroxylase

CEROD = Ethoxyresorufln  o-deethylase
     dose-response competition  experiments were carried out  In triplicate and
 Illustrate the reproduclbUHy of  the  assay with  the PCDF.

ND = Not detected
1931A
7-73
06/22/86

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               10
            I  6

                                           .,
                                          \
                                   fCOf m,.
                                   l.J.1 •'.»--


                                       •
      .  [ •— 2 3 76-TCOO |


       • —J 34 ;.»-


      -J.J.4.«.7«-
                          34567

                             Thymic Atrophy
             10
                                                —J.i.7« rcoo
                                        r • — PCOf


                                        -12 3.6 r e
                                    2.3 4 7»

                                    1 J47»-
                      1.2 3 7 « —.
                        34567

                           Body Wf Lota  (-tog CO JO'
                                    FIGURE  7-1

    A  plot  of  the   -log  £659  values  for  AHH  Induction   In  rat  hepatoma
H-4-IIE  cells  vs.  the ^n  vivo  -log  ED5Q  values  for  thymlc  atrophy  (top)
and  body weight  loss  (bottom) for  several  PCDFs,  2,3,7,8-TCOD and a  recon-
stituted  PCDF  mixture

Source:  Mason  et al.,  1985
1931A
7-74
06/22/86

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    In human lymphoblastold cells Nagayama  et  al.  (1985c)  showed that chlor-
Inatlon  1n  position  1 has  an  activating effect.  In these  cells  the HxCDFs
and PeCDFs  (1,2,3,4,7,8-,  1,2,3,4,6,7-  and  2,3,4,7,8-)  were  more potent than
TCDF and  a  sex effect appeared, with females  consistently  presenting higher
1nduc1b1l1ty.   As  far as  species  differences  1n  AHH  Inducing  activity  are
concerned,  In  rats and  mice PCDFs were  always  less  active  than  TCDDs but In
human  cells the most  active   Isomers were  as  potent  as  TCDDs  (Nagayama  et
al., 1985c).   This must  be taken Into  account  In  relation  to their reported
high persistence 1n tissue  of  humans  (Rappe et al.,  1983a)  and undomestlcat-
ed animals  In evaluating their toxic potency.
    A  structure-activity  relationship  similar  to  that  on AHH  Induction  was
reported  by Nagata  et al.  (1981) for  the effect of  PCDFs on the  mlcrosomal
metabolism  of  progesterone.   Both  2,3,7,8-TCDF and  2,3,4,7,8-PeCDFs  selec-
tively  Increased  7a-hydroxylat1on,  but  strongly  suppressed  2a,  60  and
16a  hydroxylatlon  and  5a  reduction  of  progesterone.   This  change In  the
progesterone  metabolic   pattern  results  In  a  marked  depression  of  total
metabolism  of   the   steroids.    2,8-DCDF;   1,3,6,7-TCDF;   1,3,6,8-TCDF  and
1,2,4,6,8-PeCDF do not affect  progesterone metabolism.
    7.4.5.5.4.   AHH Induction  and  Cytosol  Receptor  Binding  —  The  signifi-
cance of  the Induction of  drug-metabolizing  enzymes  by  PCDFs  and chlorinated
aromatic  hydrocarbons 1n  general  In the Interpretation of their  toxldty  Is
still an  open  question  (Poland et al.,   1979;  Yoshlmura et al.,  1979;  Poland
and Kende,  1976).  An  Important  observation was the  correlation between  AHH
Induction and binding affinities for the  hepatic cytosol  receptor  protein  of
a certain number of  PCDF  congeners (Nagayama  et  al.,  1983;  Poland  et al.,
1979; Yoshlhara  et  al.,  1981; Bradlaw  and  Casterllne,  1979).   Recently  the
effect of structure on  rat hepatic  cytosol  receptor  affinity  and  AHH 1nduc-


1931A                               7-75                             06/22/86

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tlon potency  was studied  for  26 pure  PCDFs  (Bandlera  et  al., 1984b)  (see
Table  7-29)  that were  synthesized  according to  a  new reported  procedure
(Safe  and  Safe, 1984).   As for  AHH Induction,  the most  active  PCDFs  for
receptor binding were  substituted  In all four lateral  positions.   Moreover,
compounds with  additional  Cl groups  at  C-4 or C-6  bind  with  higher  affinity
to  the receptor  than  Isomers  with  substHuents  at C-l  or  C-9.   However,
there  1s no linear correlation between  the  receptor  binding affinity and AHH
Induction potencies  for  the 26  Isomers.  This  suggests that  after  Initial
binding of  PCDF Ugands  with the receptor  some  molecular features  (such  as
conformation of the llgand-receptor  complex, differential  Ugand/receptor-
nuclear  Interactions)  distinct  from  those required  for attachment,  affect
events In the complex enzyme Induction  process.
    Structure/activity relationship  (SAR)  studies  have  been  recently  con-
ducted  (Mason  et al., 1985)  with a number  of pure  PCDFs  and a  mixture  of
PCDFs  resembling  the  compositions   of  the   mixture  persisting   1n  Yusho
patients  (Bandlera   et  al.,  1984a)  1n  an attempt  to  correlate  their  AHH
Inductive  properties and  toxic  effects  (thymlc atrophy  and  weight  loss).
Results  Indicated an excellent  linear  correlation between jji  vitro  and  In
vivo activity  for  the congeners  that  are  substituted  1n both phenyl  rings
and do not  contain vicinal  unsubstltuted  carbon  atoms.   The  effect of chlor-
ine  substitution  at  the  four  different  positions  of the dlbenzofuran  ring
can  be summarized as follows:  3,7  >  2,8 >  44,6  > 1,9.  This differs  from
PCDDs, 1n which all  the lateral positions are equivalent because  of the sym-
metry  of  the  d1benzo-p-d1ox1n  ring  system.  Inspection  of these  results and
of  the suggested hypothetical structural  features  Indicate  that  a  molecule
can  be hypothesized  with  high  affinity for the  receptor but  scant Inductive
1931A                               7-76                             06/22/86

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power, thus  eliciting  no toxic  effects.   Such  a molecule might  be  an  anti-
dote for the most toxic PCDF.
    Keys  et  al.   (1986)  have  recently  reported   that  two  TCOF  congeners
2,4,6,8-TCDF and 1,3,6,8-TCDF possess the  peculiarity  of being  poor  In  vitro
Inducers of  AHH  and  EROD activities but have relatively high  binding avidi-
ties  to  the cytosollc  receptor protein.   These  compounds  competitively dis-
placed TCDD  from  the  receptor  and their coadm1n1strat1on  with  TCDO  was sig-
nificantly  was  reduced  In  the  expected additive  Induction  of AHH  and EROD
activities.   On  the   other  hand,  2,3,7,8-TCDF  administered  together  with
2,3,7,8-TCDD gave additive enzyme Induction responses.
    Cheney  (1982) and  Cheney and Tolly  (1979) developed a  theoretical  model
suggesting  that  four  structural  factors,   Including the fused  trlcycHc aro-
matic  system,  were  Important  for   the  attachment  and  stimulation  of  AHH
Induction, while the electronegative substHuent of the lateral  ring did not
Influence  Induction  and  binding  In the  same manner.  More precisely,  the
latter appears  to Increase  Induction  to  an  extent that  Is  greatly out  of
proportion  to  Us  effect on binding.   The  lateral  ring   substitution  seems
particularly Important  to switch  the receptor-complex  to  an active  state  to
promote AHH Induction.
    In conclusion, the  toxldty  of  PCDFs  seems   to  correlate well  with  their
potential capacity to  Induce AHH; however,  toxldty  Is not bound  directly  to
AHH activity, but  both AHH  Induction and  toxic  effects are  to  be considered
secondary to the Initial binding to  the  cytosollc protein  receptor.
    In the  last  2 years a   link  has been  found between  TCDD,  which 1s  the
most powerful and  the  most  widely  studied of the  polychlorlnated hydrocar-
bons, and  the  regulation of epidermal  growth factor   (EGF) binding  1n  human
keratlnocyte lines was  demonstrated (Hudson  et  al.,  1985, 1986;  Osborn  and


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Greenlee, 1985;  Greenlee et  al.,  1985a).   These  authors demonstrated  that
TCDD can  modulate the proliferation  and  differentiation of  epidermal  kera-
tlnocytes both j_n  vivo and  in vitro.  This  was  explained  by  the competition
of TCDD with EGF  1n binding  to the  Ah receptor present In basal cells.
    Another  Important example  of the relationship  between the  binding  to a
specific receptor and manifestation of a  toxic  effect was  reported by Green-
Ice et  al.  (1985b)  who  showed that TCDD-lnduced thymlc  atrophy was mediated
by a receptor  protein  In thymlc epithelial  cells.   The  major consequence of
this fact  appears to be altered thymus-dependent maturation  of T-lymphocyte
precursors,  mediated through  direct  cell-cell  contact between thymocytes and
thymlc  epithelial cells.
7.5.    REPRODUCTIVE/DEVELOPMENTAL TOXICITY
7.5.1.   Introduction.   The literature base on the potential  reproductive
and  developmental toxldty  of  the PCDFs  1s limited, and prior assessments
have relied  largely  on the  similarity of  these agents with the dloxlns  (U.S.
EPA,  1983,   1984a).  Recently,  however,  several laboratories have conducted
studies that focus on the  dlbenzofurans.   This chapter will pay particular
attention  to  these  studies,  as well as  summarize those studies  that have
been  reviewed 1n previous   U.S. EPA  documents.   In  general,  the greatest
focus  has been  on  prenatal  development,  with  little  Information  on   other
aspects of  the  reproductive  process.  Most  laboratory  studies have concen-
trated  on 2,3,7,8-TCDF,  since  the  TCDD  homolog 1s  known  to  be highly  toxic
and  teratogenlc.
7.5.2.    Development.  The  studies by Nagayama  et   al.  (1980) Indicate that
polychlorlnated  dlbenzofurans  (PCDFs)  are  capable  of  being transferred  to
the  developing mouse, both prenatally through  the placenta  and  postnatally
through the breast milk.   Exposure of  the  dams   to  a mixture  of tetra-,


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penta- and hexachlorodlbenzofurans  was  through the diet during  the first 18
days of pregnancy  or  during the first  2 weeks  of  postnatal  (PN) life.  Low,
but measurable,  levels  of  PCDFs were found both  1n  fetuses  at gestation day
18 and  In neonates at 1 and  2  weeks of PN life.  Whole  body concentrations
were highest In  the neonates, with  the  percentage  of total Intake at PN week
2 double  those  at  PN  week 1, suggesting an accumulation  of  the PCDFs during
the early postnatal  period.   Weber and  Blrnbaum (1985)  also  examined  the
transplacental   transfer  of radioactive  2,3,7,8-TCDF  1n the  C57B1/6N mouse.
Exposure  was by  gavage  on gestation day 11 at  a  dose known  to  cause a high
level   of   cleft  palate.   Low  levels   of  radioactivity  were  found  1n  the
embryos at gestation  day  12,  but  radioactivity  1n  the  embryos  was  below
detectable limits  by  gestation  days 13 and 14.  Together,  these two studies
Indicate  that  the  PCDFs  are transferred  at   low  levels   to  the embryo  and
fetus  transplacentally, and  at  higher  levels  to the  nursing  neonatal animal
during early PN life.
    Weber  et al. (1984) studied  the  effect on  prenatal  development  of single
and multiple exposures  to  2,3,7,8-TCDF  1n  C57B1/6N  mice.  The  2,3,7,8-TCDF
was 98% pure  (primary  contaminant  was  PeCDF).   Administration  was  by  oral
gavage 1n corn  oil (10 mil/kg/treatment).  Single  exposure was  on  gestation
day 10  (plug  day  = gestation day 0) at  0 (vehicle  control),  250,  500  and
1000  jig   2,3,7,8-TCDF/kg   bw.   Multiple  exposures  were   on  gestation  days
10-13, with  dally  exposure  levels  at  0,  10, 30,  50 and  100 v9  2,3,7,8-
TCDF/kg bw.  The maternal  animals were  monitored  for  body  weight changes  and
signs  of  toxlclty  during  gestation, and  the  uterine contents were  examined
on gestation day 18 before  parturition.  The fetuses  were  examined  for gross
and visceral malformations,  but  were   not examined  for skeletal anomalies.
There  were no signs of maternal  toxlclty, except  for  changes  1n  absolute  and


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relative liver weight at the highest dose under both  exposure  regimens.   The
authors Indicate that this  Is  probably a metabolic response of  the  liver to
2,3,7,8-TCDF exposure, although  they  note that a  toxic effect  on the  liver
cannot be ruled out.
    In terms of developmental toxldty,  the most significant effects  were on
the kidney  and  palate.   Following  single exposure, there was  a  significant,
dose-related Increase In Utters with  hydronephrosls  at all doses  (250,  500
and  1000  yg/kg) and  litters with  cleft palate  at  the  highest dose  (1000
yg/kg).   Following  multiple exposure  a similar  pattern  was  observed,  with
an  Increase In Utters  with hydronephrosls  starting  at 30 yg/kg/day and an
Increase  1n  litters with  cleft   palate  starting  at  50  yg/kg/day.   The
authors also reported an Increase  1n  fetal mortality  above  control  levels at
all  doses  following single exposure  (0% In  control;  12.6% at 250;  14.7% at
500;  21.IX at  1000  yg/kg).   However,  even  though  this  was  statistically
significant,  the finding must  be viewed with caution,  since  a total absence
of  fetal  mortality  1n  mice,  even  1n  the  control population,  Is  uncommon.
For  example,   the  control   group  for  the  multiple exposure  design  In   this
study  (Weber  et al., 1984), as well  as a control group  In  another  study by
this   laboratory  (Weber et al.,   1985),  exhibited  11.7%  and  10.5%  fetal
mortality,  respectively,  at a  level   comparable  to  the 2,3,7,8-TCDF-exposed
groups.   There were  no  other  gross  or visceral   malformations  observed and
there  was  no  effect  on  fetal  weight.   The  authors  do not  Indicate why the
ICDFs  would  not be  expected  to   produce  skeletal  changes.    However,  the
exclusion  of  this   major class  of   anomalies, which  1s  often quite  sensitive
to  Insult,  may have limited the effects  that were  seen.
     These  results  demonstrate that 2,3,7,8-TCDF  Is  a developmental  toxicant
 1n  the mouse  at exposure levels that  are not maternally toxic.  Based on the


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Utter, which 1s generally  considered  the experimental unit  1n  this  type of
study  design,  the  LOAEL  was at  250 yg/kg/day  following a  single  exposure
and 30  yg/kg/day  following  the 4-day  exposure.   A NOEL  was  not established
for a  single exposure;  for multiple  exposures  the  NOEL was 10  yg/kg/day.
Several  additional   points   should   be  recognized  In  analyzing  the  data.
First,   the  number  of  animals/dose  group  was  low.   The  current  U.S.  EPA
recommendation Is 20  Utters/dose  group (U.S.  EPA, 1984b); however,  1n this
study,  the number of  Utters ranged  between 6 and  11.  This  does  not reduce
the Importance  of  the  observations,  but  had  the  number  been Increased  the
power  of  the study  to  detect  change may  have been  Increased,  with  effects
being  seen  at  lower  doses.   Second,  while  the  Utter   1s  considered  the
experimental  unit In this study design, the  Individual  fetal  data  should  not
be discounted.  Kidney changes as a  mean  percentage of  fetuses were signifi-
cantly  Increased  following multiple  exposure  at the  10  yg/kg/day  dose.
Since  these  changes  were consistent  with the dose-related  response  of  the
other endpolnts on both  a Utter  and Individual fetus  basis,  1t Is  possible
that 10  yg/kg/day  would  be the LOAEL  following multiple exposure.   Third,
hydronephrosls  can   be   a  reversible   alteration   1n  development;  and  the
authors note  that  preliminary  studies  suggest  this may be the  case  for  the
kidney changes observed  following TCDF.   However,  without Information on  the
level and duration  of exposure and  the postnatal  age at observation,  1t 1s
not possible to determine the significance of  these findings  relative to  the
developmental  toxldty   of  the agent.   Moore  et  al.  (1973)  examined  the
effect of pre- and postnatal exposure  combinations to TCDD on the  postnatal
observation  of  kidney  lesions  and  concluded  that the  Incidence  of  hydro-
nephrosls Is probably a  function  of  dose and  length  of exposure.   Moreover,
the developmental  significance  of transient  changes  Is  not  well-understood


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but should  not  be arbitrarily discounted.   Thus,  these three points  should
be kept  1n  mind In the overall assessment  of  the  toxlclty of the  PCDFs,  as
they may Influence the final  determination of the effect levels.
    Recently, Blrnbaum et  al.  (1986) have  reported,  1n abstract form,  pre-
liminary data  from their  studies on  the  relative  teratogenlcHy  of  three
PCDFs.   C57B1/6N  pregnant  mice were  exposed to 2,3,4,7,8-PeCDF;  1,2,3,7,8-
PeCDF; or 1,2,3,4,7,8-HxCDF on gestation  days 10-13 and  examined  for  terato-
genlc  effects  on  gestation  day  18.   All  three PCDFs  were teratogenlc,  as
evidenced by  the occurrence of  cleft palate at doses  that did  not  produce
maternal toxlclty.   The  ED5Qs  were  40,  100  and  400  pg/kg for  2,3,4,7,8-
PeCDF,  1,2,3,7,8-PeCDF  and  1,2,3,4,7,8-HxCDF,  respectively.   The  NOEL  for
2,3,4,7,8-penta-CDF  was  1  vg/kg,   apparently  lower   than   that   for  the
2,3,7,8-TCDF.  Hydronephrosls occurred at even  lower  doses.   Further  analys-
is of  this  study  will be done  as  the Information becomes available  since the
apparent Increased  toxlclty of  2,3,4,7,8-PeCDF may  have an  effect  on  the
reported NOEL.
    Weber et al.  (1985) reported  on  the teratogenlc  potency of  TCDF and TCDD
when  exposure  to  these  two agents  1s combined.   Individually,  each  agent
showed  a steep  dose-response curve  for the Induction of  cleft  palate, with
TCDD  -30 times  more potent  than  TCDF.   In combination, the two  agents were
additive 1n  their  contribution  to cleft palate  Induction,  with  no Indication
of a  synerglstlc or antagonistic effect of combined exposure.
    Hassoun  et  al.  (1984)  also  examined  the  developmental   effects  of
2,3,7,8-TCDF  1n  mice  of the C57B1  strain,  using an  1.p.  route  of  exposure.
Purity  of  the  agent was  90%; 8%  was  hexachloroterphenyls,  which  the  authors
Indicate "are probably  less  toxic and teratogenlc" than  TCDF.   Exposure was
by  a   single  Injection  on gestation  days  10,  11,  12  or  13 to  the  dloxane


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vehicle or  TCDF  at concentrations  ranging  from 0.1-0.8 mg/kg  bw.   The ani-
mals  were  examined  on  gestation  days  16  or  17  for  Implantation  sites,
resorptlons,  and  live and  dead  fetuses.   Fetuses  were  examined  for  cleft
palate and  hydronephrosls.   The  number of treated  dams  In each  dose  group
ranged from  5-14  (average  = 8.8), which  1s less  than optimal.   Furthermore,
the use of  the l.p. route  Is  generally not  recommended since a mechanical or
acute  chemical  Insult  can  occur  1n  the  vicinity of  the  uterus.   Neverthe-
less,  this  study  supports  the findings of Weber  et  al.  (1984)  and Indicates
that  the  most sensitive  exposure period  during gestation  for  the Induction
of cleft palate and hydronephrosls Is gestation days 11-12.
    In relation  to human exposure  to the PCDFs,  Kuratsune  (1976,  1980)  has
reviewed  epidemlologic   studies  on  Yusho  (oil  sickness),  the Incident  1n
Japan  1n  which  humans  were exposed  to rice oil contaminated with  PCBs con-
taining a  high  level  of PCDFs  and  other  organochlorlne  compounds.   Of  13
women  who were  exposed  during pregnancy  (11  showing signs of  Yusho; 2 with
husbands showing  signs),  9  offspring had unusual  grayish/dark  brown pigmen-
tation of the skin, glnglvae  and  nails, and most  showed  a  discharge from the
eyes.  Since  similar  signs were  almost  never  seen  elsewhere  In  Japan,  the
findings suggest  an  association  between  prenatal  exposure and  adverse out-
come  at  birth.    However,  Kuratsune  (1976,  1980) pointed  out  that  the  low
number of cases  does  not allow for a  clear cause  and effect  relationship to
be drawn.   Kuratsune  (1976, 1980) also noted  that 12 of the 13  babies were
small  by  national standards,  but  this difference  disappeared  with  age  and
the children  had no apparent  physical or  mental  handicap.  In  relation  to
postnatal  exposure,  Kuratsune (1976,  1980) summarized  a   report  suggesting
that boys of  school age  exposed to  the contaminated  oil  showed  a significant
decrease  In  both  height and  weight  relative  to  unexposed  boys.   Exposed


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girls did not  show  any  such decrease relative to  unexposed  girls.   Finally,
from  one  case  report,  a  child exposed  only by  nursing  from the  exposed
mother began showing signs of Yusho,  Indicating  transfer  of  the toxic agents
through the breast milk.
7.5.3.   Reproductive Function/Fertility.   Studies designed  to monitor  the
effect of  the  dlbenzofurans  on male  and female  reproductive function  and
fertility,  apart  from  the  developmental  toxldty  studies  noted above,  are
minimal.   Olshl et  al.  (1978)  compared  the  toxldty of a mixture  of TCDFs,
PeCDFs and  HeCDFS with  that  of a  commercial  polychlorlnated  blphenyl  mix-
ture.  Male rats  (100-130 g) were exposed through  the  diet  to 0,  1  or 10 ppm
PCDF  for  4  weeks.  In  relation to  the reproductive system,  they  found  that
the  relative  testes weight was Increased at  both the 1  and  10 ppm doses.
There  were  other  signs   of  general  toxlclty  at  these  doses,  Including
decreased body  weight and  food  consumption,  and  1t 1s  likely that the effect
on  relative testes weight  was   associated  with  these  changes.  At  10  ppm,
there  were  reductions  In  the  absolute and  relative weights  of  the seminal
vesicles  and  ventral  prostates, as  well  as  a decrease 1n  the concentration
of  testlcular  testosterone.   However,  because of  the other  general  and  sys-
temic  toxlclty seen at this dose level,  1t  Is not possible  to determine 1f
PCDFs  had a direct  effect  on  the male reproductive system.   In reviewing the
Yusho  Incident, Kuratsune  (1980)  noted  a  report  Indicating  that  Irregular
menstrual  cycles  and  abnormal  patterns of  basal  body  temperature  were
observed  In  60 and 85% of  the  exposed women patients,  respectively.  Unfor-
tunately, other reproductive effects  of  the  PCDFs  must  be assumed from stud-
ies  on similar agents  such as  dloxln.  A recent  Health  Assessment Document
for  Polychlorlnated D1benzo-£-D1ox1n  (U.S.  EPA,  1985)  has  summarized  this
literature  and 1t  will  not be  repeated  here.   However,  1n  the  few studies


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that have  examined  reproductive endpolnts not  associated  with  developmental
toxldty,  there  has been  no clear  Indication  of an  adverse effect  of  the
dloxlns on reproduction.
7.5.4.    Summary.   The  data  clearly  support the  developmental  toxldty  of
2,8,7,8-tetrachlorodlbenzofuran  1n  the  C57B1/6N  mouse  at  relatively  low
levels   of  exposure.  The  -study of  Weber et  al.  (1984)  provides  the  most
direct  support of this  toxlclty, demonstrating  an  adverse  effect  following a
single   exposure  to  250  yg/kg on gestation  day 10 and following  a  multiple
exposure  to  30  yg/kg/day   on  gestation  days   10-14.   A  NOEL  could  not  be
determined from  the results  following  a single  exposure.   Following  multiple
exposure,  no  effect was observed  at 10  yg/kg/day when the  data  were anal-
yzed on  a Utter basis.   Considering  the  additional  points that are noted
above on study design and  data  Interpretation,  It  Is possible that biologic-
ally significant changes would occur at even lower  levels  of exposure.
    The  potential  human developmental  toxldty of  the PCDFs  has  not  been
systematically  studied.    However,  the  findings  associated  with the  Yusho
Incident are  suggestive  that the PCDFs  can  have  an  effect on  the fetus  and
on the  developing child.
    Studies on  other  reproductive effects  associated  with PCDF  exposure  do
not provide sufficient  data to  be  more than suggestive.   Effects have  been
reported on specific aspects  of both the male  and female  systems.   However,
additional study would  be  required  to clearly  delineate any  possible  direct
effect  of the  PCDFs  on  reproductive function and fertility.
    As   noted  1n  Section  7.5.1.,  the  literature base on   the  chlorinated
dlbenzofurans  In the area  of  reproductive and developmental  toxlclty Is  very
limited.  Many laboratories have focused on  the dloxlns, with a considerable
extension of that data base,  at  the  expense  of  the dlbenzofurans. Since  the
data base  on  the dloxlns  1s  more  extensive,  1t would be useful  to  continue

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and  expand  reviews  that  address  the  similarities  and  differences  In  the
action  of  these  two classes  of agents.   More  directly,  however,  studies
should be designed  to more  adequately assess the low end of  the  PCOF  effect
range  relative  to   developmental  toxlclty,  and studies  on  fertility  and
reproductive function should  be  Initiated.   In addition, a  clearer  picture
should  be  developed  regarding  the  effect  of  chemical  species  (since  the
majority  of studies have  examined  2,8,7,8-TCDF)   and animal  species  and
strain  (since  most  studies  have used the  C57B1/6N mouse).  Finally,  a  better
understanding  of  the pharmacoklnetlcs and metabolism of  these  agents,  espe-
cially  as  related  to  transplacental transfer,  transfer  through the  breast
milk, and  localization/duration of  exposure In  the  embryo/fetus  and neonate
would help  In  establishing  appropriate  experimental  models  and  extrapolating
data from animal to  the  human condition.
7.6.   MUTAGENICITY
    Schoeny   (1982)  tested    four   chlorinated  dlbenzofurans   (2,8-DCDF,
3,6-DCDF,  2,3,7,8-TCDF,  and   OCDF)   In  the  Salmonella hlstldlne  reversion
assay.   Four doses   (0.1-10 yg/plate) of  2,8-DCDF were assayed  In  Salmonel-
la.  strains  TA1535,  TA100,  TA1975, TA92,  TA2322,  TA1537,  TS24,  TA2637,
TA1538,  TA98 and  TA1978.  3,6-DCDF  was  tested  Identically except  that strain
TA1538  was  not  used.  Five  doses  (0.1-20 yg/plate)  of 2,3,7,8-TCDF  were
assayed  1n  strains TA1535,  TA100,  TA1537, TA98  and TA1978;  three  doses
(0.1-5  yg/plate)  of octachlorodlbenzofuran  were tested  1n strains  TA100,
TA1975,  TA92,  TA2322, TS24, TA1537  TA2637,  TA98  and TA1978.   All four PCDFs
were  tested  In  the absence  or  presence  of  Aroclor-lnduced  rat  S9  mix.
2,3,7,8-Tetrachlorodlbenzofuran  was also  tested In  the  presence of  S9 mix
from  rats  induced with  3-methylcholanthrene, phenobarbltal  and 2,3,7,8-TCDF;
OCDF  was  also  tested  1n  the  presence  of S9  mix   from  rats  Induced  with
2,3,7,8-TCDF.

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    The results were negative  (mutagenldty was  reported  as  none).   Toxlclty
was  not  observed except  for  2,3,7,8-TCDF at  1  vg/plate  1n the absence  of
S9 mix.   Schoeny (1982)  commented that  the  Salmonella  hlstldlne  reversion
assay  Is relatively  Insensitive  to  chlorinated hydrocarbons, perhaps because
the  S9 preparations  cannot  effect dechlorlnatlon  or  some other  reaction
necessary to produce active metabolites.
    2,3,7,8-TCDF  was  also studied  (along  with  several  chlorophenols  and
chlorophenol  Impurities)   In  Saccharomyces cerevlslae  strain  MP-1  and  was
negative for  forward mutation, mltotlc crossing  over  and mltotlc  gene  con-
version at  concentrations up  to 1.0 mg/ml  (FahMg et al,  1978).   Survival
was  91X at  1.0  mg/ma.   Stationary  phase cells  were  tested In  the absence
of exogenous  activation.   The control  values  varied widely among  the  tests
of the Individual chemicals.
     In  summary,  two studies  (both  negative) on  the mutagenlc  potential  of
chlorinated  dlbenzofurans  have  been reported.  Additional studies are needed
before  any  conclusion can  be reached  concerning  the  mutagenldty  of  these
compounds.
7.7.   CARCINOGENICITY
7.7.1.   Animal.  Close structural  similarity  of PCDFs to  PCDDs,  especially
2,3,7,8-TCDD, which  Is a  proven animal carcinogen,  raises  concern  as to the
potential carclnogenlcHy of  2,3,7,8-TCDF.  However, no animal  cardnogenlc-
Ity  bloassay data on PCDFs are currently available 1n the literature.
     However,  as  PCDFs  are contaminants   of  commercial   PCB  and might  have
contributed  to  the  toxic  effect 1n animals and  man  (Olshl  et  al.,  1978; Vos
et al.,  1970;  Cordle et  al.,  1978), It can  be hypothesized  that they play a
role   (e.g.,   promotion,   cocarclnogenesls,   Initiation)   In  the  suspected
carcinogenic effect  of PCB.


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    PCB mixtures  (Aroclor  1254 and 1260,  Kanechlor  400 and  500)  reportedly
produce  hepatic  tumors  In  mice  and  rats   (WHO,  1978b;  Klmbrough,  1974;
Klmbrough  et  al.,   1972).    Recently   the  hepatocarclnogenlc  potential  of
Aroclor 1260  was  confirmed In Sprague-Dawley  rats  (dose of 100 yg/g  In the
diet  for  16 months),  a  strain with a  low Incidence of  spontaneous  hepato-
cellular  neoplasms  (Norback  and  Weltman,  1985).   After 18  months,   In  the
PCB-exposed  group  hepatocellular neoplasms  were present  1n 95%  of   the  47
females and  1n  15% of  the  46  males  with a  significant sex difference.   In 81
controls  only  one   hepatocellular  neoplasm  occurred.   The  appearance  of
tumors  In  the liver  and stomach  that  do not occur spontaneously  In  control
rats was  also  reported after  treatment with Aroclor  1254  (25-100  ppm  1n the
diet) suggesting that  PCBs  Initiate lesions  de novo  rather  than  promote the
development of naturally-occurring lesions  (Ward,  1985).
7.7.2.   Human.  Amano et  al.  (1984)   recently  completed  a  16-year  cohort
mortality study of 1086 Yusho  victims  1n Japan.   In  1968,  these victims suf-
fered  an   acute toxicosis  from  consuming  rice  oil  contaminated  with  an
Industrial  oil  consisting  of  a  mixture of  PCBs, PCDFs  and  PCQs.  The  581
males and  505  females  sustained  a  total  of  70  deaths  (42 males  vs.  45.81
expected  and  28  females  vs. 31.3  expected).    These  data  are  based  upon
Japanese national death rates  over  age  40  through October  31,  1983.  In this
population,  for  persons  over  40  years of age  overall  cancer  mortality  was
greater than expected  1n  men  but  no  different  In  women.   In  male  Yusho
victims 19  cancer deaths  occurred  vs.  11.50 expected  and 1n female  Yusho
victims 7 cancer deaths occurred  vs. 7.20  expected.   However,  by  organ site,
the risk  of liver  cancer was  consistently found to be  higher  than expected
In  both men and women during the  entire  16-year observation  period.   Even
after  a 9-16  year   latent  period,  the  risk of  liver  cancer  1n   males  was


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significantly higher (observed, 5;  expected,  0.75;  p<.01).   This 1s a  short
latency period  when compared with  most known  carcinogens.   In females  the
results were 2 observed vs.  0.45 expected.
    As a result of  an  1n-depth  review  of this  study and  consideration  of  the
overall PCDF  toxldty  relationships,  1t has  been  hypothesized  by CA6  that
the PCDFs  component of the 'PCBs  could have been a factor  In the  statisti-
cally  significant  liver  cancers  seen  1n  these victims.   Particular  Isomers
of the  Ingested PCDFs  were  found  1n liver  tissue 1n  nearly the  same  propor-
tions as PCBs several years  later  (Kuratsune  et al., 1975).
7.8.   EPIDEMIOLOGY -- SYSTEMIC TOXIC EFFECTS
    Two mass  food  poisonings,  the  first 1n Japan  1n 1968 and the  second  In
Taiwan  1n  1979, were found  to  be caused by the Ingestlon of  rice  oil  highly
contaminated with  PCB,  PCDF and  PCQ,  but  not with PCDD.  The  Japanese  epi-
sode  Involved 1788  people at the  end  of 1982  and the Taiwan  episode  totaled
2062  patients at  the beginning of  1983 (Masuda et  al.,  1985).  It has  been
roughly estimated that the  average  Intake  during the  whole  Intoxication  per-
iod was 973,  3.8  and 586 mg In Taiwan  (Chen et al.,  1985a) and  633,  3.3  and
596 mg  In  Japanese  patients (Hayabuchl et  al., 1979) for PCB,  PCDF and  PCQ,
respectively.  The  syndrome  known as Yusho 1n  Japan  and  Yu-Cheng  1n  Taiwan,
has been  attributed mainly  to PCDF,  although  the  presence  of  PCB and  PCQ
should  not  be  overlooked (Chen et  al., 1981; Kashlmoto  et al., 1981).   The
animal  data  (Kashlmoto et al.,  1985; Kunlte et al.,  1985)  Indicate that  PCB
and PCQ components alone cannot cause Yusho symptoms.
    Speculations on  the  levels of  the three  contaminant congeners detected
1n blood and tissues of Yusho  and Yu-Cheng  patients also support  the  hypo-
thesis  that  PCDFs are  the main  agents  responsible for the poisonings  (Masuda
et al., 1985; Mlyata et al., 1977b, 1985; Chen et  al., 1985a).
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7.8.1.   The  Japanese  Incident  (Yusho  disease).   Yusho  disease  has  been
described  In  several  papers  and  comprehensive  reviews  (Kuratsune,  1972,
1975, 1980; Klmbrough, 1974; Hsu et al.,  1985;  Urabe  and  Asahl,  1985;  Yoshl-
mura and Hayabuchl,  1985).   Therefore,  only an overview of  clinical  effects
will be given here.
    The early symptoms presented by 89 males and  100  females 1n  the Japanese
Yusho  Incident  are listed In Table 7-30.   The available  Information  allows
only a qualitative description of the  clinical  effects; case control  studies
were aimed  only  at Identifying  the  etlologlcal role  of rice oil.   The asso-
ciated estimates of  the amount of oil  consumed  (Ingested  quantity of  PCB and
PCDF) and severity of clinical acute-subacute  findings could be  described 1n
a few  cases  (see Table  7-14) (Kuratsune, 1972, 1975; Nagayama et al., 1976;
Strlk, 1979).  Other available Information will be briefly discussed.
    7.8.1.2.   VARIOUS  CLINICAL  AND   BIOCHEMICAL  FINDINGS — Besides  those
reported for  the acute  and  subacute  phase  after  exposure  (see  Table 7-30),
other  abnormal  nonsystematlc findings  are discussed  In  the following  sec-
tions.
    7.8.1.2.1.   Liver — Slight rises  In  serum  transamlnases   and  alkaline
phosphatase,  occasionally  low   blllrubln  levels;  marked  proliferation  of
smooth  endoplasmlc  retlculum  In a  liver  biopsy  sample  from  one  exposed
Individual.   Unspecified   liver  enlargement   and   disturbances  were  also
reported.
    7.8.1.2.2.   L1p1d  Metabolism —  Serum  trlglycerldes  Increased  to  four
times  the  normal  value,  but plasma  cholesterol and  phosphollpld levels  were
always  normal.    This  hypertrlglycerldemla  persisted  for  several   years.
Follow-up of  24 patients showed lowered levels 5-7 years  after the accident.
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                                  TABLE  7-30



            Signs  and  Symptoms  of  Yusho  Disease  1n  Adult  Japanese*

SIGNS
Blackening of nails
Black spots In all pores
Excessive sweating In palms
Acnellke skin eruption
Red spots on limbs
Change 1n skin color
Swelling of hands and feet
Hardening of backs of hands
Pigmentation of mucous membranes
Sebum (gum secretion In eyes)
Hyperemla of mucous membrane of eyes
Temporary falling of eyesight
Jaundice
Swelling of upper eyelids
Fever
Vomiting
Diarrhea
SYMPTOMS
Itching
Sense of weakness
Numbness of hands and feet
Hearing difficulty
Spasms of hands and feet
Headaches
Males (n=89)
1%)

83.1
64.0
50.6
87.6
20.2
75.3
20.2
24.7
56.2
88.8
70.8
56.2
11.2
71.9
16.9
23.6
19.1

42.7
58.4
32.6
18.0
7.9
30.3
Females (n=100)
(X)

75.0
56.0
55.0
82.0
16.0
72.0
41.0
29.0
47.0
83.0
71.0
55.0
11.0
74.0
19.0
28.0
17.0

52.0
52.0
39.0
19.0
8.0
39.0
*Source:  Kuratsune,  1972
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    7.8.1.2.3.   Dermal Signs — The dermal lesions  described  1n Table 7-30
were the most notable manifestations of Yusho.  All  skin  symptoms  diminished
gradually but persisted  with a tendency  to  cyst  formation  1n  severe  cases.
This was the  Initial  criterion used to designate Yusho patients.   The acne-
form eruptions decreased  markedly  after  3-4  years leaving a  small  number  of
cysts.  Black comedones  disappeared  between  5 and 6  years:   folUcular  dots
disappeared within  4  years;  pigmentation disappeared  after 10 years,  last
from the nails.   Ingrown nails are still apparent  1n 1985  (Urabe  and  Asahl,
1985).
    Some  women   who  consumed  contaminated rice  oil  gave   birth   to  "coco"
(heavily black plgmented) babies (Klkuchl et  al..  1969, 1977).
    7.8.1.2.4.   Porphyrln  Metabolism — Strlk  (1979)  found  no  alteration
of  this factor   1n  Yusho patients  and  no other manifestations  of porphyMa
cutanea  tarda such  as  light sensitivity  or hyperkeratosls.   Increased excre-
tion  of  a-ketosterold  was an  occasional  finding  and  lower  than  normal
1mmunoglobul1n  levels  were reported 1n  38 patients  2  years after the acci-
dent.
    7.8.1.2.5.   Ocular  Signs — Although some signs  subsided,  84%  of  75
patients  examined  still  showed abnormal  changes  of  the  melbomlan glands 10
years after the  accident; 64%  of the patients  complained  of  eye  discharge.
    7.8.1.2.6.   Neurological   Signs —  Reduced  sensory  nerve   conduction
velocity  (9  of  23  cases)   was  observed more frequently than  reduction of
motor  nerve conduction (2 cases only).   No follow-up studies have  been made.
 Dullness,   headache,   heavy-headedness,  indefinite  stomach   ache,  numbness,
 pains  In the extremities,  and swelling and  pain  of joints  were still being
 reported in 1985 (Urabe and Asahi,  1985).
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    7.8.1.2.7.   Respiratory ~ Chronic  bronchitis  with  mucus  production
was present  1n  40X of  the  cases.   There was a  very slow Improvement  1n  79
patients that were followed for 5 years.  Coughing  and  bronchHIs-Uke  symp-
toms were still being reported  1n 1985  (Urabe and  Asahl,  1985).   An  Investi-
gation of 401 Yusho  patients  showed that one-half  of the  subjects were com-
plaining of  respiratory distress.   Follow-up  showed a gradual  Improvement
over the 10  years  following onset of the disease;  however,  from  10-15  years
after  onset  Uttle  or  no  further   Improvement  was observed  In  most  cases
(Nakan1sh1  et al., 1985a,b) and some pulmonary function test  Impairment per-
sisted long after the Initial  Yusho  Incident.
    In conclusion, although the clinical profile  of Yusho disease  has  been
described In several papers, there  Is  Uttle precise and  quantitative  Infor-
mation on clinical manifestations, Including the  most severe.
7.8.2.   The Taiwan  Incident  ("Yu-Cheng"  Disease).   On  May,  1979, the  first
report of a  Yusho-I1ke  disease 1n Talchung County,  Taiwan was  recorded with
1843 cases  over a wide area   up  to November 1980  (Hsu et al.,  1985).   The
Initial diagnosis for 1670  victims  was based on dermal phenomena set out  In
Table  7-23.   By  February  1983 there  were  2062 recognized  cases.   In  nine
particularly  afflicted  townships,  the morbidity  rates were  0.095, 0.338,
0.392, 1.35, 0.248, 0.688,  0.056, 0.421 and 0.131X.  The  Kanechlor 400/Kane-
chlor  500  contamination In rice  oil  varied from  31-300  ppm,  the period  of
exposure from 3-9 months   and  the  estimated  total Intake  per  person  from
0.77-1.84 g.  The  average   latent period  to the onset  of visible signs  was
3-4 months  (range  1.5 to >6  months).   In the first year, blood PCB In  613
patients ranged from  3-1156  ppb with  82.5X  being 11-150  ppb;  27.6X  had
levels >100  ppb.  Hyperplgmentatlon  and  growth retardation  In  newborn  of
pregnant mothers  exposed to  PCBs was  noted  along  with  enhanced mortality


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(weakness and  lung problems).   In  adults,  24  deaths were  reported  mostly
from hepatoma,  liver  cirrhosis  or  liver  diseases with  hepatomegaly.
    PCB-exposed patients  In  the  first year  suffered  from Infections  at  the
following sites:  respiratory tract, skin, and Immunosuppresslon  (Lu  and  Wu,
1985).  Ocular  symptoms  Included  Increased discharge  from eyes,  swelling of
eyelids, weakness of eyesight, soreness, easy Irritation  and easy fatigue of
eyes  (Lu and  Wu,  1985).   Other  major   complaints  were  hyperplgmentatlon
(especially   In nails)  (Wong  et  al.,  1985), headache,  dizziness,  general
malaise, reduced appetite, soreness and  weakness  of limbs, swelling  or  pain
of the  joints  and  feet,  Ingrown  nails (especially  the big  toe)  and numbness
of the  limbs (Lu and Wu,  1985).   Both  sensory (In  43.6%  of  the patients)  and
motor (1n 21.8%  of  the  patients)  nerve conduction  velocity  (NCV) were lower
than control (Chen et al., 1985b).  The major dermatologlcal  signs, as noted
above,  were  acne-comedones,  nail pigmentation  and prurltls.   Abnormal  men-
struation and   hyperhydrosls  of  the   palms   and  soles  were   noted  1n  some
females  -10%).   Placental  tissues obtained  from women who had  been  exposed
3-4  years before conception,  showed large  Increases 1n monoxygenase enzymes,
particularly AHH  (Wong  et al.,  1985).  Males did  not  complain of Impotence.
Because  of   Immunosuppresslon  (humoral  and  cellular),   secondary  mlcroblal
Infection often arose.   Initially,  total T,  active T  and helper T cells were
decreased but  not  B  or  suppressor  T  cells.   Three  years  later, only  the
helper  1  cells were  still  low giving  an  Immuno-regulatlng Index  of 63% of
unexposed controls.   Studies  3   years  later showed  Improvement  of  general
conditions,   of  subjective  symptoms  and  of  cutaneous changes  (Lu  and  Wu,
1985).
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    No association could  be  established between severity of  the  disease  and
PCB level In blood.  However,  the  Individual  variations  In  the levels are so
wide that no conclusion could  be drawn  from the reported results  (Lu and  Wu,
1985).   Correlations   between  Yusho  and  Yu-Cheng  symptomatology  and  PCOF
levels In tissues have been discussed 1n previous sections.
7.8.3.   The  Blnghamton,   N.Y.  Transformer  Accident.   An   Incident  with
explosion and  fire In  a  tr1- and  tetrachlorlnated  benzene-containing  elec-
trical transformer took place  In  Blnghamton, New York,  on  February  5,  1981.
The consequent  overheating led to the release  of  -750 8, of  fluid  contain-
ing 65%  PCBs  and 35% trl- and tetrachlorlnated  benzenes.   Pyrolytlc  conver-
sion of  these  compounds  led  to the formation of several  PCOFs and  traces of
PCDDs (Schecter  et al.,  1984).  A  total of  -500 persons  were believed  to be
exposed,  but  data  are available only  on  50 patients  who voluntarily sought
medical   surveillance.   Among  them, one case of  chloracne,  several  transient
skin rashes,  three cases  of skin  cancer,  three subjects with liver  altera-
tions with  no   other  known  cause  were   observed.   Psychological  symptoms
(nervousness,  Irritability, fatigue,  etc.)  were recorded.
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           8.   EFFECTS  OF  MAJOR  CONCERN  AND  HEALTH  HAZARD  ASSESSMENT
8.1.   EXISTING GUIDELINES AND STANDARDS
    No guidelines, standards or  recommendations are available for PCDFs.
8.2.   SOURCES OF EXPOSURE
    PCDFs  enter  the environment as  unwanted trace  Impurities  1n  commercial
mixtures  of  polychlorlnated  blphenyls  (PCBs), products  derived  from  poly-
chlorinated  phenols   (PCPs),  chlorinated   naphthalenes,   2,4,5-trlchloro-
phenoxyacetlc  add   (2,4,5-T)  formulations   and  through  pyrolysls of  PCBs,
2,4,5-T  and   polychlorlnated   dlphenyl   ethers.    Incinerators  (municipal,
Industrial and others),  combusting  organic  materials  and  chlorinated  com-
pounds appear  to a  major  source  of  PCDFs 1n  the  environment.   The  presence
of PCDFs  In  the  emissions from Incinerators  can be  explained  by the  pyroly-
sls of  chlorinated  aromatic  compounds.   The chlorinated benzenes, PCBs  and
PCPs,   which  are  present  1n high  concentrations  In  emissions  from  waste
Incinerators,  have  also  been  suspected  to  act,   either  Individually  or  1n
combination,   as   precursors  or  Intermediates  for   PCDF  formation.    PCDFs
emitted  from  Incinerators  Include  tetra-,   penta-,  hexa-,   hepta- and  octa-
chlorodlbenzofurans.
    PCDFs are very widespread,  appear to  be  highly stable 1n the environment
like  PCDDs,  and  can  bloaccumulate   1n  aquatic and terrestrial  organisms.
PCDFs  have been  detected  1n fish,  turtles,   seals, and  fish-eating birds,  In
animal and human  adipose  tissue,  and 1n animal and  human milk.   Exposure  to
the human  population  can  occur by  Ingesting fish  from contaminated  water
bodies. Human  adipose  tissue and  breast milk from selected  populations  have
been found to bloaccumulate  PCDFs.  Considerable concern  has arisen over  the
public health  Impact of  the emission of PCDFs  from waste  Incinerators  and
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presence of  PCOFs  1n human  adipose tissue  and  breast milk.  Public  health
Implications of  nursing  Infants  by mothers  whose  milk contains  residues  of
PCOFs are many.
    Accidental   fires  1n electrical  equipment,  especially PCB-fllled  trans-
formers and  capacitors  have been a  source  of  exposure to PCDFs  for a  great
number of people.
    Wood  preserved  by  chlorophenols  Is  another   source of  PCDFs  1n  the
environment.  High levels of PCDFs  have  been detected  In  dust  from sawmills,
sludge from wood dipping tanks, and other sources.
8.3.   HIGH RISK POPULATIONS
    Populations  with  high  risk of  exposure  to PCDFs  Include  the following:
workers  In  the  wood or  tanning  Industry  who produce  or  use  chlorophenol
preserved  products;  firefighters  working  on electric  or  transformer  fires;
workers  at  the Incinerators;  factory  workers  making  or  repairing  trans-
formers or  capacitors,  using casting waxes  or heat  exchange systems;  office
workers using  carbonless copy  papers  containing  PCBs;  auto mechanics working
on  cars  that  use  leaded  gasolines; people  who  have  a  high  Intake of fish
from  PCDF  contaminated  water  bodies;  and  Infants  who are nursed by mothers
whose milk contains PCDF residues.
    PCDFs  are   extremely  toxic  to  animals  and  humans   as  demonstrated  by
short-term  exposures.   Long-term  exposure  and  health experiences are notably
lacking.   Signs  and  symptoms  of  toxlclty are very  similar to those caused by
2,3,7,8-TCDD.   Of  the total 135 possible  Isomer congeners so  far determined
for  PCDFs,  2,3,7,8-TCDF, 1,2,3,7,8-PeCDF and 2,3,4,7,8-PeCDF seem to be most
toxic.   However, the relative tox1cH1es  of all the  congeners  have not yet
been  fully  studied.
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    Information on adverse health effects  In  humans  was  gathered 1n 1968 and
1979  from  observations In selected  Japanese  and Taiwanese  populations,  who
accidentally  consumed  PCB-/PCDF-contaminated  rice  oil.   Severe  acute  toxic
effects were  observed  1n  the  affected  population.   Retarded  growth, abnormal
I1p1d  metabolism,  liver  dysfunction,  acneform eruptions, skin  pigmentation
and cutaneomucosal lesions were some of  the general  symptoms observed 1n the
affected Individuals.  Nine babies born  of mothers  from  these affected  popu-
lations had  grayish/dark  pigmentation  of the skin  ("coco" babies), glnglval
and nails,  and the  majority  of these babies  had  an  unusual  discharge  from
the eye.
    Liver  and  adipose tissue  from  affected  populations   examined  several
years  after  exposure  showed  retention  of  PCDFs at  ppb levels;  2,3,4,7,8-
PeCDF  was  found to  be retained by the  liver at higher  concentrations  than
other  Isomers.
8.4.   BASIS AND DETERMINATION OF  RISK
    There  Is  no  experimental  evidence   from human,  animal or  mutagenesls
assays  that  pure  PCDFs are carcinogenic  or  mutagenlc 1n mammals.   PCDFs  do
not give a  mutagenlc  response  In mlcroblal  assay systems.   Furthermore,  no
long-term chronic  human epidemlologic or  animal  bloassay toxlclty  data  are
available that  can be  used  for determining  human  health risk  from chronic
exposure to pure PCDFs.
    The  only  animal  data  available  for  hazard   assessment  result   from
short-term exposure.   Blrnbaum et  al.  (1986)  and  Blrnbaum (1986)  found  3
yg/kg/day to  be the  lowest observed  effect  level  (LOEL) for  hydronephrosls
In  the mouse fetus  because  of in  utero exposure to  2,3,4,7,8-PeCDF  during
days  10-13  of  the  gestation  period,  while  for   cleft  palate   H  was  5
yg/kg/day.    The  LOAEL for   hydronephrosls   for  2,3,7,8-TCDF,  1n  a  mouse
teratogenlclty study  by Weber  et al.  (1984) was  found to  be 10 yg/kg/day.

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    Because of  the short  duration (4  days)  for  the j_n  utero exposure  to
PCDFs resulting  1n  hydronephrosls  and cleft  palate  1n the mouse  fetus,  the
available  teratogenlclty  data  are not  adequate to  determine  human  health
risk  from  chronic  exposure.   Consequently,  the   lowest-observed-adverse-
effect level  (LOAEL)  1s determined  using the  TCDO-equ1valent  extrapolation
approach
8.4.1.   Estimation  of  LOAELs.   Structurally   and   tox1colog1cally,   PCDFs
resemble  their  PCOO congeners.  Their  structural-activity relationships  to
AHH activity have been  studied  1n  a rat  hepatoma cell line (Bandlera et al.,
1984b; Mason  et al.,  1985).   Like 2,3,7,8-TCDD, PCDFs  need  to bind  to  the
cytosollc Ah receptor site for  manifestation  of their AHH  Inducing activity.
The  chlorine   atoms  have  to  occupy   at  least  three  of   the  four  lateral
positions  (2,  3,  7 and 8) and  at  least  one vicinal   carbon position must be
unsubstHuted.  A  linear relationship  for a series of  PCDFs, a PCDF mixture
typical  of  exposure to Yusho  patients  and  2,3,7,8-TCDD  was  obtained  when
-log  EC     values  for  AHH  Induction  responses  were  plotted  against  -log
EDrri  values for  body  weight loss or  thymlc atrophy (Mason  et al.,  1985).
  bU
In all cases  2,3,7,8-TCDD  was  found to  be the most  active substitute for AHH
Induction in vitro and  for Iji vivo short-term toxic  effects.
    Taking  Into  consideration  the  AHH  activity  and  other   acute  toxic
effects,  1t has  been   estimated  that  2,3,4,7,8-PeCDF  and 2,3,7,8-TCDF  are
3- and 20-fold,  respectively,  less toxic than 2,3,7,8-TCDD (Bandlera et al.,
1984b; Mason et al., 1985) (see Table 7-29 and Figure 7-1).
    Reevaluatlon  of  the Murray et al.  (1979)  primary  data from a 3-genera-
tlon  Sprague-Dawley  rat  reproductive  effect   study  with  2,3,7,8-TCDD  by
Nlsbet and  Paxton (1982)  and  subsequently by  U.S. EPA (1985)  revealed that
the LOAEL for 2,3,7,8-TCDD was  0.001 vg/kg/day.
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    Toth et  al.  (1978,  1979) exposed  male Swiss  mice  to 0.007  yg/kg/week
of  2,3,7,8-TCDD for 1  year, which  resulted In  amyloldosis  of the  kidney,
spleen and liver, and dermatitis at  the  time of  death.   The duration of this
study was  649  days.   In  this  study 0.001  yg/yg/day was  also found  to  be
the LOAEL.
    The LOAELs  for 2,3,4,7,8-PeCDF and 2,3,7,8-TCDF  are  estlmted  to be 0.003
jig/kg/day  and  0.02  yg/kg/day,  respectively,  from  the  above  animal  long-
term chronic studies using the TCOD equivalent approach.
    For comparative  purposes,  an attempt will  now be made  (In consultation
with Dr. J.J.  Ryan)  to  determine the LOAEL  for  2,3,4,7,8-PeCDF In the Yusho
poisoning Incident.
    The minimum quantity of  rice oil  that  led  to an observed effect (grade 3
Yusho response) 1n a 42-year-old person  after a  latent  period of 30 days was
121 ma,.   The mean  latent  period  1n  the Yusho  episode  was  estimated  to  be
71 days (range:   20-190  days)  (Hayabuchl et al.,  1979).   The average amount
of  total PCDFs  1n the  rice oil has  been estimated (Ryan,  1986) from several
sources  (Buser  et al.,  1978; Mlyata  et al.,  1978 and  Maguda,  1982)  (see
Chapter 4) to be 3.85 yg/g (ppm).
    Using  the  peak  heights  on  the chromatogram  In  the  Buser  et  al.  (1978)
study,  from  peak  68  It  has been estimated  that  2.3.4.7.8-PeCDF was -8.4% of
the total  PCDFs of  the  Yusho oil  (Ryan, 1986).   The content  of 2,3,7,8-TCDF
1n  the  oil  1s assumed  to  be  negligible  since both Masuda et al.  (1982) and
Chen and Kites  (1983)  have found that the  peak  elutlng  near  2,3,7,8-TCDF  Is
1n  fact   2,3,4,8-TCDF.    Moreover,   the  contribution   of  1,2,3,4,7,8- and
1,2,3,6,7,8-HxCDF 1s not considered  to be  significant  since:   a) HxCDFs were
present  1n  lower concentrations than  PeCDFs In  the oil,  b) HxCDFs  accumu-
lated  less   In  tissues   of  Yusho  patients  than  PeCDFs  (Kurokl and  Masuda,
1978), and c) the HxCDFss are less  toxic  than PeCDFs 1n animals.

1932A                               8-5                              06/30/86

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    Using the estimations on the total oil consumed,  the  average  quantity of
total PCDFs  1n  the oil, and  the  percentage  of 2,3,4,7,8-PeCDF In  the  total
PCDFs In the oil,  the LOAEL 1n a  70  kg man  for 2,3,4,7,8-PeCOF  1s determined
to be:
                           121  mft  x  3.85  ug  x 0.084
                               71 days x 70  kg
                              = 0.007 yg/kg/day
    For   2,3,4,7,8-PeCDF,  this  estimated  LOAEL of 0.007  yg/kg/day from  the
Yusho Incident  Is  supportive of  the LOAEL  of 0.003 yg/kg/day derived  from
animal studies using the TCDO  equivalent  approach.
8.4.2.   Derivation of  Reference  Dose (RfD).   In  the  absence  of  long-term
chronic   animal   bloassay  data  on  2,3,4,7,8-PeCDF   It  seems  reasonable  to
determine a  Reference Dose  (RfD)  based  on the LOAEL  estimated  following  the
TCDD equivalent approach.  A composite uncertainty factor of  1000 1s  used to
estimate  the RfD.   This  uncertainty  factor  represents  10 because  adverse
effects   observed  In animals are  extrapolated to humans,  and another  10 Is
used  to account  for  the  expected   Interhuman  variability  In  the  toxldty
response  to  this  chemical, an  additional  uncertainty  factor  of  10  1s  used
because   the  RfD  Is  based on  a  LOAEL and   not  a  NOAEL;  thus,   this  latter
factor  adjusts  the LOAEL  Into  the  range of  the  expected NOAEL.    An  uncer-
tainty  factor  of 10 to account  for  the  short duration  of  the study  Is  not
used  because the  critical  toxic  effect, teratogenldty,  1s encompassed 1n
the   duration   of   the   study.    Consequently,  an   uncertainty   factor   of
100x10=1000  Is used.
    8.4.2.1.   THE  RfD  FOR  2,3,4,7,8-PeCDF  — The  RfD  for  2,3,4,7,8-PeCDF
1s estimated to be as follows:
                                     , 3 x ,0-« M,/kg/day
1932A                               8-6                              07/01/86

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    The following 1s a series of calculations  that  estimate  the  criteria  for

2,3,4,7,8-PeCDF 1n various media.

    1.  For a  70  kg man  Inhaling  2,3,4,7,8-PeCDF  In  20 m3 of  air/day
        the criteria would be:


                      - 3 x 10"* yg/kg/day x 70 kg
                                20  mVday

                      = 1.1 x 10~5  yg/m3


    2.  For a 50 kg woman Inhaling  2,3,4,7,8-PeCDF 1n 20 m3 of  air/day


                        3 x 10~6 yg/kg/day x 50 kg

                               20 mVday

                      - 7.5 x 10"6  yg/m3

        [The  above calculations  assume  that  exposure  occurs  only  by
        Inhalation.]


    3.  Since  2,3,4,7,8-PeCDF  residues  have  been detected  1n  mother's
        milk  samples  from Isolated populations,  a  virtually safe level
        for Ingestlon  of  2,3,4,7,8-PCDF  1n  mothers'  milk Is  also estim-
        ated.  In  this calculation,  the total body  weight of  an Infant
        1s considered  to  be  10 kg  (ICRP, 1975).  The  total  quantity of
        fat  1n  100 ml of  mother's  milk 1s 4.5 g and  the  average dally
        Intake of nursing mother's milk  by  the baby 1s considered to be
        850  mt  (ICRP,  1975).   Therefore,   850  mil  of  mother's  milk
        will contain 38.25 g of fat.

        Therefore,  for virtual  safety for  an  Infant,  the  concentration
        of 2,3,4,7,8-PeCDF In  fat  from  the  nursing  mother's  milk should
        not exceed the following:

                  3 x  10~6 yg/kg/day  x 10 kg
                         38.25  g/day

                =  7.8  x 10~7  vg 2,3,4,7,8-PeCDF/g  of fat.


    4.  Since fish  has been  found  to  bloaccumulate  PCDFs easily, a cri-
        terion for  a  70   kg  man from Ingestlon of  contaminated  fish 1s
        also  determined.   The  average dally consumption of  fish 1n the
        United  States 1s considered to  be  6.5 g (Federal  Register,
        1980).
1932A                               8-7                              06/23/86

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        Therefore, the criterion 1s as follows:
                           3 x 10"* mg/kg/day x  70 kg
                                   6.5 g/day
                   = 3.2 x 10~5 mg 2,3,4,7,8-PeCDF/g of fish.
        This  calculation  Is   based   on  fish  as  the  sole  source  of
        2,3,4,7,8-PeCDF.

    8.4.2.2.   THE   RfD   FOR   2,3,7,8-TCDF — Following   TCOD   equivalent
approach  from  animal data,  the  LOAEL  for  2,3,7,8-TCDF  has  been  estimated
(Section  8.4.1.)  to  be  0.02 vg/kg/day.   Based  on  this  LOAEL,  In  the
absence of any chronic  animal  bloassay data  on  2,3,7,8-TCDF  H  seems reason-
able to determine a RfD for this compound.
    A  composite  uncertainty  factor  of  1000 1s  used to  estimate  the  RfD.
This uncertainty  factor  represents  10 because adverse  effects observed  In
animals  are extrapolated  to  humans,  and  10  to  account  for  the  expected
Interhuman variability  1n the toxlclty response  to  this chemical,  an  addi-
tional  uncertainty  factor  of  10 because  the RfD Is based on a  LOAEL and not
a  NOAEL;  thus,  this  latter   factor  adjusts  the  LOAEL  Into  the  range  of
expected NOAEL.  An  uncertainty  factor  of  10 to account  for  the  short  dura-
tion of  the study  Is not  used  because  the  critical  toxic effect,  terato-
genlclty, 1s  encompassed  In  the  duration  of  the  study.  Consequently,  an
uncertainty factor of 100x10=1000 1s used.
    The RfD 1s estimated to be:
                   0.02  ug/kg/day    _   ,.__    ..  ..
                   - —**—a	J-  = 2  x 10  5  yg/kg/day
                        1000

    The  following  Is a  series of  calculations that  estimate  criteria
for 2,3,7,8-TCDF  1n various media.
1932A                               8-8                              07/01/86

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    1.  For a 70  kg  man Inhaling  2,3,7,8-TCDF  1n 20 m3  of  air/day the
        criteria would be

                       2 x  10"5  yg/kg/day  x  70 kg
                              zu m3/day

                     =  1  x  10~*  mg/m3
    2.  For a 50 kg woman Inhaling 2,3,7,8-TCDF 1n 20 m3 of air/day

                   _  2  x  10~5  mg/kg/day  x  50  kg
                               ;>u  m3/day

                   =  1  x  10~4  iig/m3  air.
        [The previous  calculations  assume that exposure  occurs  only by
        Inhalation.]
    3.  Since 2,3,7,8-TCDF residues have  been  detected  1n mother's milk
        samples from  specific populations,  a  virtually  safe  level  for
        Ingestlon of  2,3,7,8-TCDF  1n  mothers'  milk  1s  also  estimated.
        In this calculation,  the total  body  weight  of an Infant Is con-
        sidered to be 10  kg  (ICRP, 1975).  The total  quantity of fat In
        100 ma  of  mother's milk 1s  4.5 g and  the  average  dally Intake
        of nursing  mother's  milk  by  the baby  Is  considered  to  be  850
        ml  (ICRP,   1975).   Therefore,  850  ml  of  mother's  milk  will
        contain 38.25 g of fat.

        Therefore,  for  virtual  safety for an  Infant, the concentration
        of 2,3,7,8-TCDF 1n  fat  of  the nursing  mother's  milk  should  not
        exceed

          2 x 10~5  yg/kg/day x 10 kg
            »fl ,,-  /Ha	=  5.2  x  10-* yg 2,3,7,8-TCDF/g of  fat.
            oo.£i> g/oay

    4.  Since  fish  has been  found  to bloconcentrate  PCDFs  easily,  a
        criterion for a 70 kg man  from Ingestlon  of  contaminated fish
        1s also  determined.   The average  dally consumption of  fish  In
        the United States  Is  considered to be  6.5  g  (Federal  Register,
        1980).

        Therefore,  the criterion 1s as follows:

          2 x 10~s  yg/kg/day x 70 kg
             6.5 g/day
                                     = 2 x 1Q-* Mg 2,3,7,8-TCDF/g of fish.
1932A                               8-9                              06/23/86

-------
    These estimations  provide general  guidance only.   To  determine a  more
accurate  criteria   1t  will  be  necessary  to   do  a  comprehensive  exposure
assessment  taking  Into consideration  the  exposure through  various  compart-
ments of  the  environment  and valid chronic bloassay  data on 2,3,4,7,8-PeCDF
and 2,3,7,8-TCOF.
 1932A                               8-10                              06/24/86

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Vos, 3.G., J.H. Koeman, H.L. van der Maas, M.C.  ten  Noever  de  Brauw and  R.H.
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ZHko, V.   1972.  Absence  of chlorinated  dlbenzodloxlns and  dlbenzofurans
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