AMBIENT WATER QUALITY CRITERIA FOR

                  ACROLEIN
                Prepared By
    U.S. ENVIRONMENTAL PROTECTION AGENCY

 Office of Water  Regulations  and  Standards
      Criteria and Standards Division
             Washington, O.C.

     Office of Research and Development
Environmental Criteria and Assessment Office
              Cincinnati, Ohio

        Carcinogen Assessment Group
             Washington, D.C.

     Environmental  Research Laboratories
             Corvalis, Oregon
             Duluth, Minnesota
            Gulf Breeze, Florida
         Narragansett, Rhode Island

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                              DISCLAIMER
     This  report  has been reviewed by  the  Environmental  Criteria  and
Assessment Office,  U.S.  Environmental  Protection  Agency,  and approved
for publication.  Mention of trade names or commercial products does not
constitute endorsement or recommendation for use.
                          AVAILABILITY NOTICE
      This  document is available  to the public  through  the National
Technical Information Service, (NTIS), Springfield, Virginia  22161.
                                     ii

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                               FOREWORD

    Section  304  (a)(l)  of the Clean Water  Act of 1977 (P.L. 95-217),
requires  the Administrator of the Environmental  Protection  Agency to
publish  criteria for water  quality accurately  reflecting  the latest
scientific knowledge on the kind and  extent  of  all  identifiable effects
on  health and  welfare  which may be  expected  from the presence of
pollutants in any body of water, including ground water.  Proposed water
quality  criteria  for  the 65  toxic pollutants listed under section 307
(a)(l) of the Clean  Water Act were developed  and a notice  of their
availability was  published for public comment on March 15, 1979 (44 FR
15926), July 25, 1979 (44 FR 43660),  and  October  1, 1979 (44 FR 56628).
This  document  is a revision  of those proposed  criteria  based upon a
consideration of  comments  received from  other  Federal  Agencies, State
agencies,  special interest  groups,  and  individual  scientists.   The
criteria contained in  this document replace any previously published EPA
criteria  for the 65 pollutants.    This criterion  document  is  also
published in satisifaction of paragraph  11 of the  Settlement Agreement
in  Natural  Resources  Defense  Council, et.  al.  vs.  Train,  8 ERC 2120
(D.D.C.  1976), modified, 12 ERC 1833 (D.D.C. 1979).~

    The  term "water  quality criteria" is used  in two  sections of the
Clean Water Act, section 304 (a)(l) and section 303  (c)(2).  The  term has
a different  program impact in each  section.  In section 304, the term
represents a non-regulatory,  scientific assessment  of  ecological  ef-
fects. The criteria presented in  this  publication are such scientific
assessments.   Such water quality criteria associated with specific
stream uses when adopted as State  water quality standards under section
303 become  enforceable  maximum  acceptable  levels  of  a  pollutant in
ambient waters.   The water quality criteria adopted in the State water
quality standards could have the same numerical  limits as the criteria
developed under section  304.  However, in  many situations States may want
to adjust water quality criteria developed under  section 304 to reflect
local  environmental   conditions   and  human  exposure patterns  before
incorporation  into  water  quality standards.    It is not until  their
adoption as  part of the  State water quality  standards that the criteria
become regulatory.

    Guidelines  to assist  the  States in the modification of criteria
presented  in  this  document,  in  the  development  of  water  quality
standards, and in other water-related programs of this Agency, are being
developed by EPA.
                                    STEVEN SCHATZOW
                                    Deputy Assistant Administrator
                                    Office of Water Regulations and Standards

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                                  ACKNOWLEDGEMENTS
   Aquatic Life Toxicology:

       William A. Brungs, ERL-Narragansett
       U.S. Environmental Protection Agency
David J. Hansen, ERL-Gulf Breeze
U.S. Environmental Protection Agency
   Mammalian Toxicology and Human Health Effects:
       Patrick Durkin (author)
       Syracuse Research Corporation

       Terence M. Grady (doc. mgr.)
       ECAO-Cin
       U.S. Environmental Protection Agency

       Mary F. Argus
       Tulane Research Laboratory

       John L. Egle
       Medical College of Virginia

       Betty LaRue Herndon
       Midwest Research Institute

       Steven D. Lutkenhoff, ECAO-Cin
       U.S. Environmental Protection Agency

       Donna Sivulka, ECAO-RTP
       U.S. Environmental Protection Agency

       Woodhall Stopford
       Duke University Medical Center
Jonathan Ward.  •
University of Texas Medical  Branch

Robert M. Bruce,  ECAO-RTP
U.S. Environmental Protection Agency
Jan Connery
Energy Resources Company, Inc.

Rolf Hartung
University.of Michigan

George J. Jakab
Johns Hopkins School of Hygiene

Alan B. Rubin, CSD
U.S. Environmental Protection Agency

Anne Trontell
Energy Resources Company, Inc.
Technical Support Services Staff:  D.J. Reisman, M.A. Garlough, B.L. Zwayer,
P. A. Daunt, K.S. Edwards, T.A. Scandura, A.T. Pressley, C.A. Cooper,
M.M. Denessen.
Clerical Staff:  C.A. Haynes, S.J. Faehr, L.A. Wade, D. Jones, B.J. Bordicks,
B.J. Quesnell,  T.  Highland, R.  Rubinstein.

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                          TABLE OF CONTENTS
Criteria Summary

Introduction

Aquatic Life Toxicology
     Introduction
     Effects
          Acute Toxicity
          Chronic Toxicity
          Plant Effects
          Residues
          Miscellaneous
          Summary  .
     Criteria
     References

Mammalian Toxicology and Human Health Effects
     Introduction
     Exposure
          Ingestion from Water
          Ingestion from Food
          Inhalation
          Dermal
     Pharmacokinetics
          Absorption
          Distribution
          Metabolism
          Excretion
     Effects
          Acute, Subacute and Chronic Toxicity
               Subacute Toxicity to Experimental Mammals
               Chronic Toxicity to Experimental Mammals
               Effects on Humans
          Synergism and/or Antagonism
          Teratogenicity
          Mutagenicity
          Carcinogenicity
     Criterion Formulation
          Existing Guidelines and Standards
          Current Levels of Exposure
          Special Groups at Risk
          Basis and Derivation of Criteria
     References
                                                                Paae
A-l

B-l
B-1
B-l
B-l
8-2
B-3
B-3
B-3
B-4
B-5
B-l 2

C-l
C-l
C-4
C-4
C-8
C-13
C-20
C-20
C-20
C-22
C-22
C-24
C-24
C-24
C-33
C-38
C-39
C-43
C-43
C-44
C-45
C-50
C-50*
C-50
C-51
C-51
C-54

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                               CRITERIA DXUMENT
                                   ACROLEIN
CRITERIA
                                 Aquatic Life
    The available  data  for  acrolein indicate that acute and chronic toxicity
to  freshwater  aquatic  life  occur at concentrations as low as 68 and 21 ug/1,
respectively,  and  would occur  at lower concentrations among species that are
more sensitive than those tested.
    The  available  data  for  acrolein  indicate  that  acute toxicity  to salt-
water aquatic  life occurs  at concentrations as low as 55  ug/1  and would oc-
cur at lower concentrations  among  species  that are more sensitive than those
tested.   No data  are available  concerning the chronic  toxicity of acrolein
to sensitive saltwater  aquatic life.

                                 Human Health
    For the protection  of human  health from the toxic properties of acrolein
ingested  through contaminated  aquatic  organisms,  the  ambient water criterion
is determined to be 320 ug/1.
    For the protection  of human  health from the toxic properties of acrolein
ingested  through  contaminated  aquatic  organisms  alone,  the  ambient  water
criterion is determined to be 780 ug/l«
                                      VI

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                                  INTRODUCTION
                 -•• .                 -.                  •                .
     Acroleln has a  wide-variety of applications.  It  is  used directly as  a
 biocide for  aquatic weed  control;  for algae,  weed,.and mollusk control  in
 recirculating process water  systems;  for slime  control  in the  paper  indus-
 try; and  to  protect liquid fuels  against microorganisms.  Acrolein is also
 used directly for  crosslinking protein collagen  in  leather tanning and  for
 tissue fixation in histological samples.  It is widely used as  an  intermedi-
 ate in the  chemical industry.  Its dimer,  which is prepared  by a  thermal,
 uncatalyzed reaction, has several applications, including use as an  interme-
 diate 'for crosslinking agents, humectants, plasticizers,  polyurethane  inter-
 mediates,  copolymers and homopolymers, and Greaseproofing cotton.  The mono-
 mer is  utilized  in  synthesis  via the Oiels-Alder reaction as a dienophile or
 a  diene.   Acrolein  is widely  used  in  copolymerization, but its  homopolymers
 do not appear commercially important.   The copolymers of acrolein are used
 in photography,  for  textile treatment,  in the paper industry, as builders in
 laundry and dishwasher  detergents,  and as  coatings  for  aluminum  and steel
 panels,  as well as  other  applications.  Hess,  et  al.  (1978)  described mar-
 keting  aspects of acrolein.  In 1975,  worldwide production was about 59 kil-
 otons.   Its  largest  market was for methionine manufacture.  Worldwide capac-
 ity was estimated at 102 kilotons/year,  of which U.S.  capacity was 47.6 kil-
 otons/year.
    Acrolein  (2-propenal)   is  a liquid  with a  structural formula of CH_ «
 CHCHO and  a molecular weight  of 56.07.   It melts at -86.95"C,  boils  at*52.5
 to  53.5*C, and  has  a density of 0.8410  at  20* C (Weast,  1975).  The vapor
 pressure at 20*C is  215 mm Hg,  and its water solubility  is 20.8 percent  by
weight at 20"C (Standen, 1967).
                                     A-l

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     A flammable liquid with a pungent odor, acrolein is an unstable compound
 that  undergoes  polymerization  to  the  plastic  solid  disacryl,  especially
 under light  or  fn the .presence of alkali or  strong acid (Windholz, 1976).
 It is the simplest member of the class of unsaturated aldehydes, and the ex-
             t
 treme reactivity  of  acrolein  is  due  to  the  presence  .of  a  vinyl  group
 (HgC-H-)  and  an aldehyde  group on  such  a small  molecule  (Standen, 1967).
 Additions to  the carbon-carbon double bond  of  acrolein are  catalyzed  by
 acids and bases.  The addition of halogens to this carbon-carbon double bond
 proceeds  readily (Standen,  1967).
      i
     Acrolein  can enter the aquatic environment by its use as an aquatic her-
 bicide,  from  industrial  discharge, and from the chlorination of organic com-
 pounds in wastewater  and drinking water treatment.  It  is  often present in
 trace amounts in foods  and is  a  component  of smog, fuel  combustion,  wood,
 and  possibly other  fire, and cigarette  smoke.  An  evaluation  of available
 data  indicates that,  while  industrial  exposure to manufactured  acrolein  is
 unlikely,  acrolein from  nonmanufactured sources  is pervasive.   Acrolein ex-
 posure will  occur through  food  ingestion  and  inhalation.   Exposure through
 the  water or  dermal  route  is  less likely.  However,  analysis  of municipal
 effluents  of  Dayton,  Ohio  showed  the presence of  acrolein  in  6 of  11  sam-
 ples,  with concentrations ranging  from 20 to 200 ug/1 (U.S. EPA, 1977).
    Bowmer, et al. (1974)  described the loss  of  acrolein by volatilization
 and degradation  in sealed bottles  and tanks  of water.   The amounts of acro-
 lein  dissipated  after eight days  were 34  percent from the tank  and  16  per-
 cent  from the bottles.   The rate  of disappearance of acrolein  in  the  tank
was 0.83  day"* at a pH of  7.2.   The lack of turbulence  in  the  tank reduced
 acrolein  loss  by volatilization to  1/20 of  what  would be expected  if vola-
 tilization were  controlled  only by  resistance  in  the gas  phase  and any dis-
                                      A-2

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 crete surface layers.  The authors agree  with  Geyer (1962), who states that
                                                                .•.-
 the  primary degradation reaction  is  reversible  hydrolysis  to 8-hydroxypro-
 pionaldehyde, which  is  1-ess volatile  thari  acrolein.
     The  fate of acrolein in water was observed in buffered solutions and  in
 natural  channel waters  (Bowmer and  Higgins, 1976).   An equilibrium between
 dissipating  acrolein and  degradation products was  reached in  the buffered
 solution  following dissipation  of  92  percent of the acrolein, but  in natural
 waters there was  no  indication  of  an  equilibrium, with the dissipating reac-
 tion  apparently being continued to completion.   In natural waters, the accu-
mulation  of  a reaction  (degradation) product was greater  at  higher initial
 acrolein  concentration, and  decay was  rapid  when  acrolein  concentrations
fell  below  2 to  3 mg/1.  The  initial period of slow  decline preceding the
rapid dissipation period is thought to be the result of microbiological pro-
cesses.  Unlike  earlier  works  (Bowmer,  et  al. 1974),  there was  an 8-  to
10-fold increase  in  the  observed dissipation rate as compared to the expect-
ed rate  in  two of four flowing water channels,  suggesting major  losses  in
volatilization and absorption.
                                     A-3

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                                   REFERENCES

 Bowmer, K.H. and M.L. -Wiggins,.   1976.  Some  aspects  of the persistence  and
 fate of acroleln herbicide 1n water.   Arch. Environ.  Contain.   5:  87.

 Bowmer, K.H., et al.   1974.   Loss of  acroleln  from water by  volatilization
 and degradation. Weed Res.   14:  -325.

 Geyer,  B.P.  1962.   Reaction with Water.   In: C.W.  Smith (ed.), Acroleln.
 John Wiley and  Sons,  Inc.,  New York.

 Hess,  L.B., et al.   1978.  Acroleln  and Derivatives.   In_; A.  Standen  (ed.),
 Klrk-Othmer Encyclopedia of Chemical  Technology.  3rd ed.  Intersclence Pub-
 Ushers, New York.

 Standen, A.  (ed.)  1967.  Kirk-Othmer  Encyclopedia  of Chemical  Technology.
 Intersclence  Publishers,  New  York.

 U.S.  EPA.   1977.  Survey of  two municipal wastewater  treatment plants  for
 toxic substances.   Wastewater Res. D1v. Municipal Environ.  Res. Lab., Cin-
 cinnati, Ohio.

Weast,  R.C.  (ed.)   1975.  Handbook of  Chemistry and Physics.  56th ed.   CRC
 Press,  Cleveland, Ohio.                                                *

Wlndholz,  M.  (ed.)    1976.  The  Merck  Index.  9th  ed.   Merck and Co., Inc.,
Rahway, New Jersey.
                                      A-4

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 Aquatic  Life  Toxicology*
                                  INTRODUCTION
     Much  of  the  data concerning  the  effects of  acrolein  on freshwater
 aauatic  organisms  has been  determined  using  static  test  conditions  with
 unmeasured  concentrations.   Conseauently,  these data  may underestimate the
 toxicity  of this  volatile,  unstable chemical.   The study  of Bond,  et al.
 (1960)  showed  acrolein to have  a  substantially  greater acute  toxicity to
 fish than the  14  other herbicides tested.  This relationship is also seen in
 a toxicity bibliography of five herbicides  (Folmer, 1977).
     Acrolein  has  been applied  directly to the saltwater environment to con-
 trol  fouling  organisms in cooling  water  systems  of  coastal  power plants.
 The data  base for  toxicity  of acrolein  is limited to the  results  of acute
 exposures of one  fish  and three  invertebrate  species,  performed with unmea-
 sured test concentrations.
                                    EFFECTS
 Acute Toxicity
     The  data base  for freshwater  invertebrate species  is limited  to  two
values for   Daphnia  magna.  The  reported  48-hour  values from  static tests
with unmeasured concentrations are 57 and 80 ug/1 (Table 1).
     Three  96-hour LCgg  values   are  reported  for  two  freshwater fish  spe-
cies,  bluegill  and  largemouth bass,  both in the family Centrarchidae.  These
results were also  obtained from static tests with unmeasured concentrations.
*The reader  is  referred to the Guidelines  for Deriving Water Quality Crite-
ria for  the  Protection of Aauatic  Life  and Its Uses 1n order  to better un-
derstand the  following discussion  and recommendation.   The following tables
contain  the  appropriate data that were  found  in the literature,  and at the
bottom of  each  table are calculations for  deriving various measures of tox-
icity as described in the Guidelines.
                                      B-l

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 Ninety-six-hour  values  of 90  and  100  ug/1  for  bluegill and  160 wg/1  for
 largemouth bass have been reported (Table 1).
      Based on  only two_ifish  species, no  conclusion can be  drawn regarding
 the relative species  sensitivity  to acrolein.  Also because  of  a  paucity of
 data, no  comparison .of relative  sensitivity between freshwater invertebrate
 and fish species can be made.
      Among the  tested saltwater  species,  the eastern oyster  was most  sensi-
 tive with a  96-hour  ECgg,  based  on decreased  shell  growth,  of 55  ug/1,
 (Table 1).  Tests with other species  (Table 5) were conducted for less  than
 the standard  testing times for  those species or life stages.
 Chronic Toxicity
      The chronic toxicity data base  consists  of  one value for fish and  one
                                 c
 for invertebrate species.
      Macek, et al. (1976) conducted the only freshwater  invertebrate chronic
 test.   Based  on  the  cumulatively reduced  survival  of Daphnia magna through
 three  generations, a  chronic  value of  24 ug/1 is  obtained   (Table 2).   The
 acute  value  for  this  species  by  the  same  investigator is 57 ug/1 and  this
 results  in an  acute-chronic ratio  of 2.4.   These  data  show that there  is
 little difference in  concentrations between the acute and chronic  effects  of
 acrolein on Daphnia magna.
     A  life cycle test with the  fathead  minnow, also conducted by Macek,  et
 al.  (1976), resulted in a  chronic value  of 21  wg/1  (Table  2).  Survival  of
 newly-hatched  second  generation fathead minnow fry was significantly reduced
 at 41  wg/1 but was not  significantly  different from  control  survival  at  11
 ug/1.   A  dilutor malfunction  killed  or  severely stressed  the fish  at  an
 intermediate concentration, 21  ug/1,  so no  second generation fish were pro-
duced.   Although no  96-hour LC5Q for  this species  is   available, a  6-day
                                      B-2

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 incipient  LCgQ  for fathead  minnows  of  84  ug/1  was  reported by the  same
 authors  using a flow-through test  with  unmeasured concentrations  (Table  5).
 Also,  Louder and McCoy  (1962)  reported a 48-hour  LC?Q of 115 ug/l for  fat-
 head minnows.
     No  saltwater species  have  been tested to evaluate  chronic effects.
     Species  mean acute  and chronic values are summarized  in  Table  3.
 Plant  Effects
     Although  published  literature  does exist describing the  use of acrolein
 to  control  aauatic macrophytes  and algae, no  appropriate  plant effect  data
 are available.   In  some  cases,  test methods were insufficiently described  to
 evaluate  reported  results.   In  others,  because  of  the  methods  used,  no
 actual exposure concentration under  field conditions could be calculated  or
 results were  reported  as control of  the weeds with no quantitative measure-
 ments made.
     The  effects of  acrolein on  saltwater  and  freshwater  plants have  not
 been studied.   Because acrolein is  a herbicide,  phytoxicity to aauatic  spe-
 cies might be expected.
 Residues
     Bluegills  exposed  for  28  days  to 13  wg/1  of  14C-acrolein  bioconcen-
 trated acrolein  344 times (Table 4).  The half-life was  greater  than seven
 days.  Thin-layer chromatography was  used to  verify concentrations.
 Miscellaneous
     Ninety-eight percent  of adult  snails  and 100 percent  of snail -embryos
 died after a 24-hour exposure to 10,000 ug/1  (Ferguson, et al. 1961).
     Nine short-term  exposures  with  seven fish species yielded acute toxic-
 . ;y values in  the range  of 46 to 115  ug/1 (Table  5).  Static tests with  un-
measured concentrations  were run  by  Bond,  et al. (1960),  Louder  and McCoy
                                      B-3

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 (1962),  and Bridie,  et al.  (1979).   The studies of  Burdick,  et al.  (1964)
 and  Macek, et  al.  (1976)  were performed  under flow-through conditions with
 unmeasured concentration^.  That of  Bartley and Hattrup (1975)  reporting  32
 percent mortality of  rainbow trout  in 48 hours at 48  ug/1 was  the only flow-
 through  study  with measured acrolein concentrations.  Because  of differences
 in test  methods and the valatility  of  acrolein, no meaningful comparison  of
 relative  sensitivity  among the fish  species  is possible.
     The  avoidance  response of rainbow  trout at 100  ug/1  is above  reported
 acute  levels  (Folmar,  1976).  Folmar  (1980) reported  flavor impairment  of
 rainbow trout  flesh up  to  four days  after  a  four-hour  exposure to 90  ug/1.
     Various  species of  aauatic weeds  were  damaged  or destroyed following
 treatment  with  500 to 25,000 ug/1 of  acrolein (Table 5).
     The  48-hour ICgg  values for three  saltwater species  are in  the  range
from 100 to 2,100 ug/1  with  the brown shrimp being the most  sensitive.
Summary
     Appropriate  acute  freshwater toxicity  data for  acrolein are limited  to
LCgg  values from five  tests with  one invertebrate  and two  fish   species.
The species  mean acute values are  68  ug/1   for Daphnia magna,  95  ug/1 for
bluegill,  and  160 ug/1  for  largemouth  bass.  Because  these results were all
obtained from  static  tests with unmeasured  concentrations,  these data  prob-
ably underestimate the  toxicity of this volatile, unstable chemical.
     The chronic  values for acrolein, 24  ug/1 for Daphnia  magna and 21 ug/1
for the  fathead  minnow,  reveal  similar  sensitivity  between these  species.
                                                                      »
No 96-hour IC-.  is  available for  the fathead minnow  but  two nonstandard
tests showed acute effects at 84 and 115  ug/1.   Thus, it appears that  there
is little  difference between  acute and chronic toxicity for  acrolein.
                                      B-4

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                                   CRITERIA
     The  available  data  for  acroleln  indicate  that  acute  and  chronic
toxicity to freshwater  aquatic  life  occur at concentrations as low as 68 and
21 ug/1, respectively,  and would  occur at lower concentrations among species
that are more sensitive than those tested.
     The available  data for acrolein  indicate that acute  toxicity  to salt-
water aquatic  life  occurs  at concentrations as  low as  55 ug/l and would oc-
cur at lower concentrations among species  that are  more sensitive than those
tested.  No data are available concerning  the chronic  toxicity  of acrolein
to sensitive saltwater aquatic life.
                                     B-5

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                                                            Tab la I.  Acuta valuaa for acrolala
00
Spacla*
Cladocaran,
Daphnla aagna
Cladocaran,
Daphnla aaflna
Bluaglll,
Lapoals Mcrochlrus
Blueglll,
Lapo*ls Mcrochlrus
Largaaouth bass,
Mlcroptarus salaoldas

Eastern oystar
Crassottraa vlrglnlca
Saaclac Meaa
LCM/ECM Acute Valwa
Mathod* Ipgyi) 
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   Tabla 2,  Chronic wluac for acrolala (Macafc. at al.  19761

                                                   Spaclaa Maan
                                        Llailts     Chronic Valua
Spacla»                      Mathod"    lug/I)        luo/l)

                        FRESHWATER SPECIES

Cladocaran,                   LC        17-34           24
Daphnla a»gna

Fatttaad •Innow,               LC        11-42           21
Plaaphala* proa* Iat
• LC - Ufa eye la or partial Ilia eye la
                       Acuta-Chronlc Ratio

                            Chronic     Acuta
                             Valua      Valua
    Spacla«                  tiifl/O     lug/I)     Ratio

    Cladocaran,                24         97        2.4
    Daphnla aaona

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    Table 3.  Species Man acute Md chronic wlues for ecroleln



Rank*      Specie*
oo
                                                                                   Species Mean
                                                                                   Acute Valua
                                                                      FRESHWATER SPECIES
                                                       Large«outh bass,
                                                       Mlcroptarut sal«old«s

                                                       Bluaglll,
                                                       LapoaiU iBCfochlrus

                                                       Cladocaran,
                                                       Daphnla aagna
160
 66
                                                                      SALTWATER SPECIES
                                                       Eastarn oystar,
                                                       Crassostraa virginlea
            Acuta-Chronlc
                Ratio
                                                              2.4
                                            * Rankod fro* least sensitive to w>st sansltlva basad on speclas moon
                                              acut* value.

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                                                      Table 4. Raclducs for Bcrolcl* (U.S.  EPA,  1978}

                                                                                     BloconcMtratlon     Duration
                                           Sp«cU«                       TUiua           Factor          
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                                  Tabla  9.  Otbar data  for acrolaln
    Spaclas
    Aquatic Macrophytas,
    Majas sp.,  CaratophylluM
    sp.,  and Jooawa sp.

    Pondvaad,
    PotoMoqaton crlspus

    Aquatic Macrophyta,
    Elodaa dansa

    Snail (adult).
    Australorbls glabratus

    Snail (aatryos)
    Australorbls glnbratut
   Chinook
    (finger I Ing),
   Oncorhynchus t«hatiyt«cha

   ftalnboo trout
    (flngarllng),
    Salao aalrdnarl
   Rainbow trout  (fry),
   Salap aalrdnarl

   Ralnbo« trout,
   Salao galrdnarl

   RalnboM trout,
   So IBO aalrdnarl
    Brown trout
    (finger I Ing),
    Salao trutta

*   Goldfish.
    Carasslus  auratus
Duration          Effact

         FRESHWATER SPECIES
                     RMUlt
                     (no/»
  9 hrs


 24 hri
Oastroyad or badly   29.000
Korchad ona Maak
aftar application

Oacayad In 6 days    20,000


Call 
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Tabla 5.  (Cofltlnuad)
tpaclas
Fathaad Minnow,
PlMaphalat pronalat
Fathaad Minnow,
PlMaphalat proaalat
Bluaglll (flngarllng),
LapoMlt Macrochlrut
Moaqultoflth,
GaMbutla afflnlt
Barnaclas (adult)
Balanut aburnaut
Barnaclat (adult)
Balanut aburnaut
Brown thrlap (adult)
Panaaut aitacut
Longnota kllllflth
(juvanlla)
Fundulut tlMlllt

Duratloa
6 dayt
48 hrt
24 hrt
48 hrt
48 hrt
48 hrt
48 hrt
48 hrt
Effact
Inclplant LC50
LC50
Maan tlMa to daath
LC90
SALTWATER SPECIES
LC90
LC50
EC50
LC50
fteault
(MQ/I)
84
115
79
61
2,100
1,600
100*
240
Rafaranca

Macak, at al. 1976
Loudar i McCoy. 1962
Burdlck, at al.
Loudar i McCoy,
Oahlbarg. 1971
Dahlbarg, 1971
Butlar, 1965
Butlar, 1965
1964
1962


•  EC50 basad on lose of aqull Ibrliuu

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                                   REFERENCES

 Bartley, T.R.  and  A.R.  Hattrup.   1975.   Acrolein  residues  1n  Irrigation
 water and effects on rainbow trout.   Bur. Reelam.  Rep.  REC-ERC-75-8.

 Bond,  C.E.,  et  al.   1960.   Toxldty  to  various  herblcldal  materials  to
 fishes.  B1ol.  Problems  1n Water Pollut.,  Trans. 1959  Seminar,  U.S. Dept.
 Health, Edu.,  and Welfare,  PHS Tech.  Rep. W60-3; 96*101.

 Bridle, A.L.,  et  al.   1979.  The acute  toxlclty  of some petro-chemlcals to
 goldfish.   Water Res.   13:  623.

 Burdlck,  6.E.,  et al.  1964.   Toxlclty  of agualln to flngerllng brown trout
 and bluegllls.   N.Y. Fish Game Jour.  11:  106.

 Butler,  P.A.   1965.   Commercial fisheries Investigations.  Effects of pesti-
 cides  on fish  and wildlife,  1964 research  findings  F1sh W1ldl.  Ser.  U.S.
 F1sh WUdl. Ser.  C1rc.

 Dahlberg, M.D.   1971.  Toxlclty of acroleln to barnacles, Sal anus eburneus.
 Chesapeake Sc1.   12: 282.

Ferguson, F.F.,   et al.  1961.   Control of Australorb1s  glabratus  by acro-
 leln 1n Puerto R1co.  Public Health Rep.   76: 461.

Ferguson, F.F.,  et al.  1965.   Preliminary field trials  of  acroleln 1n  the
Sudan.  WHO Bull.  32:243.
                                     B-12

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 Folmar,  L.C.   1976.  Overt  avoidance reaction of rainbow  trout fry to nine
 herbicides.   Bull.  Environ.  Contain. Toxicol.   15: 509.

 Folmar,  L.C.   1977.  Acroleln,  dalapon,  dlchlobenll,  diquat, and endothall:
 Bibliography  of  toxicity to aquatic organisms.  U.S. Fish W1ldl. Ser., Tech.
 Paper 88.

 Folmar,  L.C.   1980.   Effects of  short-term field  applications  of acrolein
 and  2,4-0 (DMA)  on flavor  of  the flesh  of rainbow trout.   Bull.  Environ.
 Contam. Toxicol.  24: 217.

 Louder,  O.E.  and E.G. McCoy.   1962.   Preliminary investigations of the use
 of aqualin for collecting fishes.  Proc.  16th Annu. Conf.  S.E.  Assoc. Game
 Fish Comm.  p. 240.

Macek, K.J.,  et  al.  1976.   Toxicity of four pesticides  to water  fleas and
fathead minnows:  Acute  and chronic  toxicity  of  acrolein,  heptachlor, endo-
sulfan,  and  trifluralin  to  the water  flea  (Daphnia magna)  and  the fathead
minnow (Pimephales promelas).  U.S. Environ. Prot. Agency, EPA 600/3-76-099.

Unrau, G.O.,  et  al.  1965.   Field trials in  Egypt  with acrolein herbicide-
molluscicide.  WHO Bull.  32: 249.
U.S.  EPA.   1978.   In-depth  studies on  health  and environmental  impacts  of
selected water  pollutants.   U.S. Environ. Prot. Agency,  Contract  No. 68-01-
4646.

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Van Ov.rb.ck.-O., et .1.   1959.    cr,«n    r     contro,  of
disease-carrying water snails.  Science.  129: 335.
                                 B-14

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Mammalian Toxicology and Human Health Effects
                           INTRODUCTION
     Acrolein, a colorless volatile liquid, is the simplest of the
unsaturated aldehydes:
                           CH2 » CHCHO
Table 1 describes  its  salient physical properties.   Since it is a
highly  reactive  organic chemical and  capable  of self-polymeriza-
tion,  the marketed  product  contains  an  inhibitor  (0.1  percent
hydroquinone) to prevent its  degradation.   It is extremely reactive
at high pH (Hess, et al. 1978; Smith, 1962).  Methods for acrolein
analysis are summarized in Table 2.
     The present technology for acrolein preparation employs cata-
lytic oxidation of propene in the vapor phase.  A typical reaction
process consists of feeding propylene and air  at  300°C to 400°C and
30 to 45 psi over the catalyst (usually of bismuth, molybdenum, or
antimony)  (Hess, et al. 1978).
     An evaluation of  available  data indicates that, while indus-
trial exposure to manufactured acrolein is unlikely, acrolein from
nonmanufactured  sources is  ubiquitous.   Acrolein  exposure  will
occur  through  food  ingestion and  through inhalation.   Exposure
through the water  or  dermal  route is unlikely.  Acrolein is often
present in trace amounts in foods and  is a component of smog, fuel
combustion, wood and possibly other fires, and cigarette smoke.
                               C-l

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                           TABLE 1
              Physical Properties of Acrolein*
  Empirical Formula
  Molecular Weight
  Melting Point, °C
  Boiling Point, °C
  Vapor  Pressure at 20°C,  KPa (mmHg)
  Refractive Index  no  (20°C)
 Viscosity at 20°C, cS
 Solubility in Water  (weight %)
 Critical Properties:
     Temperature,  °R
     Pressure,atm.
     Volume, cc/g-mole
*Source: Smith, 1962; Hess, et al. 1978
   C3H4o
   56.06
  -86.95
   52.69
   29.3  (220)
   1.4017
   0.393
  20.6
510
 51.58
189
                      C-2

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                           Table 2

              Methods for Acrolein Measurement*
    Analytical Method
Detection Limit
Interferences
NMR (Aldehydic proton)          100 mg/1
Colorimetry
  2,4-D
  4-Hexylresorcinol

Fluorimetry
  Direct
  J-Acid
  m-Aminophenol derivative
Differential pulse               30 ug/1
  Polarography

Gas chromatography
  Flame-ionization              500 ug/1
  Mass spectral                  50 ug/1
                       few
so ug/i
700 ug/1
20 mg/1
20 ug/i
10 ug/i
many
many
very few
very few
very few
                       few
                     very few
                     very few
*Source: Brady, et al. 1977; Kissel, et al. 1978; Bellar and
 Sigsby, 1970
                            C-3

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                             EXPOSURE
 Inqeation from Water
      There is no evidence  that acrolein  is a contaminant of potable
 water or  water  supplies.   Available  monitoring studies  have  not
 noted its  presence/  and  acrolein  is not  listed in compendia  on
 water monitoring  (Junk  and  Stanley/  1975; Shackelford and  Keith/
 1978; AbramSr  et al. 1975).  Investigations on the fate of acrolein
 in  water  suggest that it dissipates  with a half-life of 4 to  5
 hours.     Based   on  these  studies  and  its  half-life  in  water
 (Table 3), it  can be assumed that acrolein is present in water sup-
 plies in negligible  amounts.
      Acrolein  is applied to canals  as  a  biocide  for  the control  of
 harmful  organisms and aquatic weeds  (Van Overbeek/  et al.  1959).
 This  application has prompted studies to delineate the  amount  of
 acrolein required to maintain effective pest control  (Bowmer and
 Sainty,  1977;  Hopkins and Hattrup/ 1974).  These studies have exam-
 ined  dilution problems  and  pathways  for loss.    Degradation and
 evaporation  appear  to  be the  major  pathways  for  loss/  while  a
 smaller  amount is lost  through  absorption and  uptake  by aquatic
 organisms  and  sediments.  In a  review of the Russian  literature/
Helnikov (1971)  indicates that  acrolein is used as  a  biocide  in
water reservoirs.
     Kissel/ et  al.  (1978) have demonstrated the analytical  prob-
                                                            •>
 lems  in  a  study  of the effect of pH on the rate of degradation of
aqueous  acrolein.  Their study compared  acrolein measurement  by  10
analytical  techniques  in six pH buffer  systems (pH 5, 7, and 9).
                               C-4

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                        TABLE 3

   First Order  Rate  Constants of Acrolein  Degradation
               in  Laboratory Experiments*
Watera

Supply
Supply
Drainage
Supply
Supply
Supply
Distilled
£1

7.3
7.3
7.8
7.2
7.2
7.2

Initial
Acrolein
ppm

8.0
6.8
6.4
6.1
17.5
50.5
6.4
103k
hr'1

23.7
15.9
45.1
13.3
14.2
11.4
2.7
SE

2.4
2.0
7.5
1.9
2.5
1.0
0.3
*Source: Bowmer and Biggins, 1976
^ater from canal supply, canal drainage, or distilled
 water
                        C-5

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The analytical methods were:
      (a)  bioassay with an ATPase enzyme  system,
      (b)  bioassay by a plate count method,
                   _i
      (c)  bioassay by fish kill  (bluegill sunfish),
      (d)  chemical titration with bromide-bromate  solution-iodide-
          thiosulfate,
      (e)  colorimetric by the 2,4-dinitrophenylhydrazone  (DNP),
      (f)  fluorometric analysis  (m-aminophenol) with excitation at
          372 run and emission at 506 run,
      (g)  gas-liquid chromatography (on 6' Poropak Q with  injection
          temperature of 250 C and column at  200 C) ,
      (h)  nuclear magnetic resonance using aldehyde proton  at  9.44
          ppm vs. tetramethylsilane,
      (i)  polarographic analysis,
      (j)  direct fluorometric analysis of acrolein with excitation
          at 276 nra and emission at 370 nm.
Kissel,  et  al.  (1978)  separated  the analytical  techniques  into
three groups:   bioassay,  derivatization,  and direct measurement.
Differences between bioassay  methods were less than for  any other
group.   They  considered  bioassay a good  measure  of true acrolein
concentration.   Some  titrimetric  methods were  satisfactory,  but
others were poor.  Among  the  direct methods, they considered  that
GLC and  direct  fluorimetry  were poor,  but  that  NMR and  polaro-
graphic  analyses were  better  methods.  Kissel,  et al.  (1978)  did
not identify reasons for the large discrepancies.  Also,  they noted
that acrolein rapidly degraded at pH  9.
     Bowiner  and coworkers  (Bowiner  and Higgins,  1976;  Bowmer and
Sainty,  1977;  Bowmer,  et  al.  1974; O'Loughlin  and Bowmer, 1975)
have measured  acrolein degradation rates in laboratory  and field
studies.  They  evaluated  the  possible degradation pathway  in  buf-
                                C-6

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fared, distilled water.  At pH 5, the acrolein reacted by .a revers-
ible  hydrolysis  and yielded  an  equilibrium  mixture  containing
/o-hydroxypropionaldehyde:acrolein  in  a  92:8  ratio.
                    -«    .
                H2O + CH2 » CHCHO	^HOCH2CH2CHO
In alkali the primary reaction was  consistent with a  polycondensa-
tion.   In natural waters they observed no evidence for  an  equili-
brium.   They considered the  initial  product to be  from  chemical
degradation and suggested, but did not  demonstrate,  that  it  further
degraded  to  a carboxylic acid via  a microbial pathway.   Acrolein
was analyzed  by colorimetry using  the 2,4-DNP  method and by bio-
assay.  Results were conflicting, and  they concluded  that  the ana-
lytic complication (as  described by Kissel,  et al. 1978)  resulted
from  the  ability of the hydroxypropionaldehyde to form a  2,4-DNP
derivative.   They  resolved  the  analysis problem by  flushing  the
volatile acrolein from a sample by means of an air  stream, which
left the nonvolatile hydroxypropipnaldehyde  in  solution.  Acrolein
concentration was measured as  the  difference  between  the sum of
absorbances for acrolein and  2,4-DNP  in  samples before  and after
air flushing  (Bowmer, et al. 1974).  Their laboratory, studies uti-
lized samples sealed in  bottles  and maintained  at 20.6°C.   Table 3
summarizes their results.  The authors also examined  acrolein loss
in field studies,  using actual  irrigation channels.   The  apparent
dissipation rate,  k, was estimated  at  0.16 hr  ,  which is  about an
order of magnitude  faster than measured  in laboratory experiments.
They suggested that the  difference  could  result in part  from*vola-
tization and absorption.
     Hopkins  and  Hattrup  (1974)  examined acrolein  loss in field
studies in canals of the Columbia  River  basin.  Their  analytical
                               C-7

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 technique was  fluorometric  analysis of the m-aminophenol  deriva-
 tive.  The work of Kissel, et al. (1978), which is discussed above,
 suggested that this, analytical  method  could yield higher acrolein
 concentrations than were actually present.  Table 4  describes  the
 acrolein concentration  in  a flow-plug  measured during  a  48-hour
 study  period in two canals.  Hopkins and Hattrup  (1974)  suggested
 that  dissipation resulted  from acrolein degradation,  volatiliza-
 tion,  and absorption  by weed tissue.
     Potable water is  normally treated with  a chemical  oxidant,
 usually  chlorine  or less often  ozone.   These  oxidants will  react
 with olefins and are very likely to react with  the olefinic portion
 of acrolein.   It is likely  that ozone will  initially  yield  a  raalo-
 nozonide.   Aqueous chlorine  (which  exists as HOC1)  will probably
 degrade  acrolein as  follows (Hess,  et al.  1978):   2(CH2"CH-CHO)  +
 2(HOC1)—>HOCH2CHC1CHO + C1CH2CH(OH)CHO.  The relative amounts  of
 the two  possible reaction  products  and their  degradation products
are not  known  (Morris,  1975).
 Ingestion from Food
     Acrolein,  at  yg/g  concentrations, is a  common component  of
food.  It is commonly generated  during  cooking or  other processing
and is sometimes produced as an  unwanted by-product in  the  fermen-
tation of alcoholic  beverages.   The  information  on acrolein  in
foods has been generated primarily to identify  organoleptic  proper-
ties, so  its relevance  to exposure levels  is limited.       '
     Acrolein   can  be  produced  by  cooking  potatoes  in  water.
El'Ode,  et  al. (1966)  investigated  acrolein  production in potato
extract  (Katahdin  variety)  and synthetic mixtures  of the extract.
                               C-8

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                                              TABLE 4

                         Acrolein Dissipation in Two Canals of the Columbia
                                     River Basin Over 48 Hours*
o
Canal
Potholes


-




East Low






Intended
Application
ppm
0.14


Booster application at
12.6 miles




0.11






Sampling Point
Miles Below Initial
Appl. Point
1.0
10. 0
12.5
13.5
15.0
20.0*
30.0
35.0
1.0
5.0
10.0
20.0
30.0
40.0
64.5
Acrolein
ppm
t>-
0.14
O.lfr
0.09
0.20
0.18
0.15
0.08
0.05
0.09
0.10
0.10
0.08
0.06
0.02
0.03
        *Source:  Hopkins  and Hattrup,  1974

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The  synthetic  mixture contained  amino  acids  (glycj.ne,  glutamic
acid,  lysine,  methionine, and  phenylalanine)  and sugar  (glucose,
fructose,  maltose,  and sucrose).   Acrolein was  identified  by  gas
chromatography  (GO  as a  product of heating some but not  all mix-
tures  of amino  acid and sugar.  They did not identify acrolein as a
product of  heating  the actual potato  extract  (30  minutes at  180°C)
or of  heating the synthetic  potato  mixture  (60  minutes  at  100°C),
     As reviewed by  Izard  and Libermann (1978), acrolein is  gener-
ated when  animal  or vegetable fats are subjected to  high  tempera-
                    *
tures.  In these cases, acrolein is formed primarily from the dehy-
dration of  glycerol.
     Kishi, et  al.  (1975)  identified acrolein production from cook-
ing potatoes or onions in edible oil.   They detected  acrolein  at
concentrations  ranging from  2.5  to  30 rag/m   in  the  air  15  on above
the surface of  the  heated oil.   Cooking about 20 g of  potatoes  or
onions in  the oil yielded 200 to 400 yg of acrolein.   The authors
did not determine whether  the acrolein came from the oil, the pota-
toes, the onions, or from  all three sources.
     Hrdlicka and  Kuca (1965.)  examined aldehydes  and  ketones  in
turkey before cooking  and in volatiles produced  by either boiling
(3 kg in 6  1 of distilled water for 3 hours) or  roasting  (3 kg  at
170°C to 190°C  for 3 hours).  Raw turkey  was extracted  at  2°C with
75 percent  ethanol  for 72 hours, and  volatiles were collected  by
vacuum distillation.   Derivatives were formed from carbonyl frac-
tion with  2,4-DNP,  and these were  identified  by paper  chromatog-
raphy.  Acrolein was identified in raw turkey and  in the  volatile
products from both cooking methods.
                               C-10

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     Love  and  Bratzler (1966) identified  acrolein in wood  smoke.
                                                    *•
Samples  (whole  smoke  and  vapor phase)  were collected from commer-
cial  smokehouses (operated at 48°C to  49.5°C)  and from hardwood
sawdust  (mainly maple) burned on a hot plate (490°C to 500°C).   The
carbonyl compounds were trapped in 2,4-DNP solution, and the  deriv-
atives were identified by GC.   Acrolein was identified in all smoke
samples but was  not quantified.
     Levaggi and Feldstein  (1970) examined  acrolein concentrations
in  the  emissions from a commercial coffee  roaster.  Acrolein  was
trapped  in Greenberg-Smith impingers  containing 1 percent  sodium
bisulfite solution and was quantified  by the 4-hexylresorcinol col-
orimetric  method.   At the  emission outlet  (afterburner  abatement
device)  they measured 0.60 mg/nr acrolein,  while no acrolein  was
detected in the  inlet air.
     Boyd, et al. (1965)  measured the unsaturated aldehyde fraction
in raw cocoa beans and chocolate liquor. The 2-enols  were measured
by absorbance (at 373 nm) of  its 2,4-DNP derivative.  Samples were
                                           /i?\
extracted with  hexane and  cleaned  on  Celite^ prior to preparation
of derivatives.  The 2,4-DNP  derivatives were  separated  into frac-
tions prior to measurement.  They measured  2-enol concentrations of
0.6  to  2.0  umol/100 g  fat  in  raw cocoa  beans  and 1.3  to  5.3
umol/100 g in the chocolate liquor.
     Alcoholic  beverages  often contain trace amounts of acrolein
(Rosenthaler and Vegezzi,  1955).   It  is sometimes a problem ^since
it causes an organoleptic condition called  "pepper" by the alcohol
fermentation industry.  According  to  Serjak, et al.  (1954), acro-
lein is detectable in low-proof whiskey at concentrations as  low as
                               Oil

-------
    10 mg/1.  This value probably represents the upper limit for acrolein,
    since industry has adapted corrective procedures to reduce "pepper"
    by reducing acrolein concentrations.
         The chief point of entry of  acrolein into the  alcoholic bev-
    erages   has  been  reported   to  be  the  mash  fermentation  process
                                                    .'
    (Serjak,  et al.  1954;  Sobolov  and Smiley,  1960;  Hirano,  et  al.
   1962) , where if glucose levels in  the mash  are  low, some bacterial
   strains convert glycerol to  acrolein.
        Avent (1961)   investigated the  contamination of  a wine, which
   was initially acrolein-free, with  14 ug/g of  acrolein.   In  this
   case,  the possible source  was a  glycerol-impregnated  oak cask.
       Hrdlicka,  et  al. (1968)  identified  acrolein in  the  volatile
  fraction  of a hops  sample.  No quantitative data were  available.
       Alarcon  (1976a)  has  demonstrated  the  formation  of acrolein
  from methionine,  homoserine,  homocysteine, cystathionine,  sper-
  mine,  and  spermidine under  conditions similar to  those  used in food
  processing (neutral pH, 100°C).
      The  information reviewed herein  is insufficient  to develop  a
 conclusive  measure  of  acrolein exposure  in food,  but it indicates
 that acrolein is a component of many  foods and  that processing can
 increase the acrolein content.  Volatile fractions collected during
 cooking suggest that some acrolein would remain in the  food.
      A bioconcentration factor  (BCF)  relates  the concentration of a
 chemical in aquatic  animals  to the concentration  in the water  in
 which they  live.   The  steady-state  BCPs  for  a  lipid-soluble  com-
pound in the  tissues  of various aquatic animals  seem  to  be propor-
tional to the  percent lipid in the  tissue.   Thus, the  per capita
                              C-12

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 ingestion of a lipid-soluble chemical can be estimated from the per
.capita consumption of fish and shellfish, the weighted average per-
cent lipids of consumed  fish  and  shellfish,  and  a .steady-state BCF
for the chemical.
     Data from a recent survey on fish and shellfish consumption  in
the United  States were  analyzed  by  SRI International  (U.S. EPA,
1980).  These  data  were  used  to estimate that the  per  capita con-
sumption  of  freshwater  and estuarine  fish  and shellfish in the
United States  is 6.5 g/day (Stephan, 1980).   in   addition,  these
data were used with  data  on the fat content of the edible portion  of
the  same  species  to estimate  that  the  weighted   average  percent
lipids for consumed  freshwater and  estuarine fish and shellfish  is
3.0 percent.
     A measured  steady-state  bioconcentration  factor  of 344 was
obtained for acrolein  using bluegills  (U.S.  EPA,  1978).   Similar
bluegills contained an  average  of  4.8  percent lipids  (Johnson,
1980).   An  adjustment  factor of  3.0/4.8 =  0.625   can  be used  to
adjust the measured BCF from the 4.8 percent lipids  of the bluegill
to the 3.0 percent lipids that is  the weighted average for consumed
fish and  shellfish.   Thus, the  weighted average bioconcentration
factor for acrolein  and  the edible  portion  of all freshwater and
estuarine aquatic organisms consumed by  Americans is  calculated  to
be 344 x 0.625 > 215.
Inhalation                                               .   .,
     Acrolein is generated during oxidation of a variety of organic
substrates.   It has been noted as a combustion product of fuels and
                               C-13

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of  cellulesic  materials (e.g.,  wood and cigarettes)/ as 'an inter-
mediate  product in atmospheric, oxidation of propylene,  and  as a
component of the volatiles produced by  heating organic  substrates.
Actual exposure will depend on general environmental  conditions  and
specific behavior patterns.   Thus,  total  inspiration is the sum of
acrolein inhalations  from the ambient  air,  from local air (e.g.,
occupational considerations,  vehicular  considerations,  side-stream
smoke from cigarettes), and from cigarette smoke.
     Acrolein  as a component of urban smog has been measured in  the
atmosphere of Los Angeles (Renzetti  and  Bryan,  1961;  Altshuller  and
McPherson, 1963).  Renzetti and Bryan collected ambient air in I960
using a series of vapor traps containing  SD-3A alcohol  and quanti-
fied  acrolein  by  absorbance  of   the  4-hexylresorcinol-mercuric
chloride-trichloroacetic acid derivative  (605 ran).   Altshuller  and
McPherson  (1963)  also examined  the atmosphere  in  1961, but col-
lected samples in bubblers  containing the  4-hexylresorcinol  re-
agent; their  results were similar  to those  of Renzetti and Bryan
(1961).   For  10  days  during  the  period from  September through
November 1963,  Altshuller  and McPherson  found that  acrolein aver-
aged 0.012 mg/m  with a peak  concentration of 0.025  mg/m , whereas
Renzetti and  Bryan  found  that acrolein  concentrations for seven
days of  this  period  in 1961 averaged  0.018 mg/m   and peaked at
0.030 mg/m  .   For all of  1961,  acrolein  averaged 0.016 mg/m   and
peaked at 0.032 mg/ra  .                                     *
     Graedel,  et al.  (1976)  developed a mathematical model  for
photochemical processes in the troposphere.   They combined  chemical
                               C-14

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 kinetic measurements and  assumed  values, time-varying sources  of
 trace  contaminants/ solar  flux  variations/  bulk  air  flow/ and  a
 geographical matrix of "reaction volumes" for Hudson  County/  N.J.
                    •*                                     3
 Their  computed peak acrolein concentration  was  0.03 mg/m  .   They
 did  not account for other sources of acrolein or  for  any  degrada-
 tion pathway (McAfee and Gnanadesikan/  1977).   That  their  calcu-
 lated  value  favorably compared with the peak values measured in Los
 Angeles (0.025  to  0.032 mg/m  ) could be  due  to an  artifact.
     Trattner/  et  al. (1977) suggested  that enols are present  in
 the  air of a subway system.   They were measuring airborne  particu-
 lates  by  an  infrared technique.   Samples were collected on a  cas-
 cade impactor containing  a  0.313 u back-up filter.   Potassium  bro-
 mide pellets were prepared from each sample fraction.  Evidence for
 the presence of unsaturated aldehydes were the weak maxima  observed
 at 1,695 cm    (6.90  u) in the pellets prepared from final  impactor
 and  backup  filter  samples.   The  authors  made  no  quantitative
 assessment.
     Acrolein is a common constituent of vehicle exhaust (National
 Academy of Sciences (NAS)/  1976;  Tanimoto and  Uehara,  1975).  The
 exact concentration  depends upon the type of gasoline/ engine/ and
 operating conditions.  Acrolein  concentrations  have been  measured
 by a variety of methods/  and  the consensus of the  studies  suggests
 that the acrolein  concentration  usually does not exceed 23  mg/m  .
Acrolein has been  measured  in emissions of  diesel engines  %t 6.7
 mg/m  and in the emissions of internal combustion engines  at  6.0,
 22.5,  16.1,  14.7,  and about  11.5 mg/m3  (NAS,  1976).  Day,  et al.
 (1971)   reported acrolein  in exhaust from a 1969 model truck oper-
                               C-15

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ated  on  a  dynamometer.  Acrolein  was  measured  (by  the colorimetric
2,4-DNP  method) at 0.05 mg/ra3 at hot idle, 6.4  mg/m3 at  30 mph, and
4.4 mg/m  at  50 mph.
      Bellar  and Sigsby  (1970)  developed a  GC unit which  trapped
organic  substrates  from air directly onto  a GC cutter column  (10
percent  sucrose  octaacetate on  Gas-Chrom  Z)  at  -55°C  and  then
injected the  sample onto  the  analytical column.   Their  unit was
capable  of measuring  acrolein  in the  subpart per million  range.
The unit was  used in measuring, diesel  exhaust,  ambient air in  an
area  of  traffic, and ambient air in the open field.  Diesel  exhaust
contained  12.4  mg/m  acrolein.   No acrolein  was  detected  in the
open  field sample and,  at most, a trace was present in the  sample
from  the traffic area.
      Cigarette  smoke  contains  acrolein.  While a  cigarette  smoker
inspires acrolein directly,  some  questions exist on passive expo-
sure of nonsmokers to acrolein in side-stream smoke (Kusama, et al.
1978;  Horton and Guerin, 1974;  Jermini,  et al.  1976;  Weber-Tschopp,
et al. 1976a).
     Horton and Guerin  (1974)  measured  the  acrolein  content  of
cigarettes by cryogenically trapping smoke  onto a gas chromatog-
raphy column.   A 6-part smoking machine was  used with puffs  set  at
1-minute intervals,  2-second durations,  and 35  ml volume.  Measured
acrolein concentrations for  the tested  cigarettes  are described  in
Table 5.
     Hoffman,  et al.  (1975) measured  acrolein in  marijuana and
tobacco  cigarettes  using gas  chromatography.    Cigarettes  were,
rolled  to a  length  of  85* mm  using  standard cigarette   paper.
                               C-16

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                                        TABLE 5



       Acrolein Delivery  from Some Experimental and Some Commercial Cigarettes*


1
"4
Cigarette
Kentucky Reference
Commercial 85 mm,
Commercial 85 mm,
Experimental 85 mm
filtered
Acrolein Delivery

(IRI)
filtered
non-filtered
, charcoal
Experimental 85 mm (same as
above) , no-charcoal

-
Commercial 85 mm,
Experimental 85 mm
little cigar
, marijuana
iig/cig.
128
102
111
62
103
70
145
tig/puff
12
10
12
7
12
8
14
lig/g tobacco burned
159
153
135
97
155
107
199
^Sources Horton and Guerin,  1974

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 Experimental  details  were  incomplete.    Hoffman,  et  al.  (1975)
 stated that smoking machines  (1  or  20 channel) were employed  and
 contained 10 or fewer  cigarettes.  Error was placed at ±4 to 6 per-
 cent.   They reported  acrolein delivery from mainstream  smoke  was
 92  ug  from marijuana cigarettes and  85 ug from tobacco  cigarettes.
     The  potential exposure of nonsmokers to  side-stream  and  ex-
 haled  cigarette smoke  is  an unresolved question.  Holzer,  et  al.
 (1976)  suggested that passive  exposure  to cigarette smoke  is  not
 important/  while Swiss workers  (Weber-Tschopp,  et al.  1976b;  Jer-
 mini,  et  al. 1976)  have offered evidence  that  passive  exposure is
 an  important inhalation route.
     Holzer,  et al.  (1976)  developed an  absorption tube sampling
 method  to collect  organic materials  (volatiles and "particulate
 matter  associated").   The tubes  (88 mm x 2.5  mm ID)  were  packed
 with Tenax GC or Carbopack BHT.  These tubes had an uncertain capa-
 city  for  substances  of lower retention  than  benzene,  including
 acrolein, so their results were only  qualitative for acrolein.   The
 samples were desorbed and analyzed by GC-MS  (mass  spectral  detec-
 tion) using  a glass capillary  column.  The authors compared  the GC
 chroma tograms  of a  sample  of urban  air  (3.5,1  samples  at  220
ml/min), a standard  cigarette  (IRI,  University of  Kentucky)  (3 ml
of  smoke  taken during a puff  of  2-second duration and 35 ml vol-
 ume) , and air where a cigarette had been smoked  under standard con-
ditions  (same  sampling conditions as for  urban air).    They sug-
gested that  the volatiles  in both air  samples were associated with
gasoline vapor  and  that cigarette smoking did  not  appreciably  add
 to these volatiles.   The journal editor disagreed and in a footnote
                               C-18

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stated that the chromatograms suggested that "a person breathing  in
a room where one cigarette was smoked  inspires  the equivalent of a
3.5 ml puff of cigarette smoke".
     The  Swiss  team  (Jermini, et  al.  1976; Weber-Tschopp, et al.
19765) measured  acrolein concentration from  cigarettes (U.S.)   in
side-stream smoke in a nearly air-tight/ 30-m  climatic room and  in
a  272-liter plexiglass  chamber.   Acrolein  was measured  by gas
chromatography. They  reported acrolein concentrations as  follows:
            3                 33
in the 30-m   room,  0.11 mg/m  and 0.87 mg/m   with  5 and 30 ciga-
rettes, respectively; and  in  the chamber,  0.85  mg/m   for one ciga-
rette.   These  results suggested  that inhalation  of  significant
quantities  of  acrolein can result  from passive exposure to side-
stream smoke.
     Acrolein has been identified as a component of  smoke from wood
burning.   Its  detection in wood smoke  at  commercial smoke houses
(Love and Bratzler, 1966) was discussed in the  Ingestion from Food
section.  Bellar and Sigsby (1970) studied volatile organics by GC
(see above)  in emissions  from a trench incinerator  burning wood.
They published chromatograms  for the wood  smoke emissions but did
not present quantitative data.  An acrolein peak was present in the
chromatogram for  wood smoke  from the  incinerator  without forced
air.   With forced air/ the chromatogram did not contain  a peak for
acrolein/ and the peaks for carbonyl compounds were lower than those
for alcohols.                                               ?
     Hartstein and Forshey (1974) measured  combustion products from
burning four classes of materials:   polyvinyl chloride  (PVC), neo-
prene, rigid urethane foams/ and treated wood.   The materials were
                               C-19

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   burned  by two techniques:   a  sealed system (approximately 370°c)
   and a  stagnation burner  (approximately  400°C).   Cohdensible pro-
   ducts were collected  in  a liquid  nitrogen trap and analyzed by GC
   (thermal  conductivity  detection).    They noted that  the acrolein,
   concentrations measured  were less  than  the  actual  amount present
   since  the tars  and condensed  water  retain  some  acrolein.    They
   never  observed acrolein  in emissions  from  the PVC, neoprene,  or
   urethane  foam  samples.  Acrolein was  present  in emissions from all
   wood samples,  as  summarized  in  Table  6.
   Dermal
       Based upon the  physical properties and known distribution of
  acrolein in the environment,  dermal exposure is  judged to  be negli-
  gible.
                          PHARMACOKINETICS
  Absorption
      Egle  (1972) has  measured the retention of inhaled  acrolein as
 well as formaldehyde  and propionaldehyde in mongrel dogs  anesthe-
 tized with  sodium pentobarbital.  In this  study,  dogs were exposed
 to acrolein concentrations  from  0.4 mg to  0.6 mg/1 for 1 to 3 min-
 utes,  and retention was calculated using  the amount  inhaled and the
 amount recovered.   In measurements  of total respiratory tract ren-
 tention  at ventilatory rates  between 6 and 20/rain.,  81  to 84  per-
 cent of inhaled  acrolein  was retained.  An  increase in tidal volume
 (from  100  ml to 160 ml)  resulted in a significant  (p-^O.OOlf  de-
crease  in  acrolein retention  (from  86  to  77 percent).   This  was
consistent with  findings  that acrolein was  taken up more  readily by*
the upper than the lower  respiratory tract.
                               C-20

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                          TABLE 6           ^_



    Acrolein Produced by Burning Standard Southern Pine*
Acrolein Produced (rag/g
Wood
Treatment
None
None
Pen tachlor ophenol
Creosote
jg\
Koppers fire retardent Type Co/
Koppers waterborne preservative
co®
Sealed
Tube
0.67
0.62
1.21
0.43
unknown
0.47
wood burned)
Stagnation
Burner
0.21

0.70
1 0.59
0.22
0.68
*Source: Hartstein and Forshey, 1974
                          C-21

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 Distribution
      Studies that  were  directly relevant  to the distribution  of
 acrolein upon oral administration were not found.  Munsch, et al.
 (1974b)  have examined the  incorporation of  tritiated  acrolein  in
 rats.   Rats  were  injected  (i.p.) with  acrolein  at  3.36 mg/kg  70
 hours after  partial hepatectomy.   At  24  hours after  injection,
 88.66,  3.13f 1.72,  0.94, and  0.26 percentages  of  the  recovered
 radioactivity-were found in  the acid-soluble, lipid,  protein, RNA,
 and  DNA fractions of the liver,  respectively.   Based  on measure-
 ments taken  10  minutes to 24  hours  after dosing,  the  extent of RNA
 and DNA binding remained relatively constant,  while protein  binding
 increased by about 70 percent.   In  vitro studies  on the binding  of
 acrolein  to nucleic acids are discussed in the Acute,  Subacute, and
 Chronic Toxicity  section.
 Metabolism
     In  terms of  the potential toxicologic effects of  acrolein  in
 drinking water, the instability of acrolein at acid pHs  (see Inges-
 tion  from Water section) may be highly  significant.  As discussed
 by Izard  and Libermann  (1978)  and detailed in the Effects  section
 of this  report, several of the toxic effects of acrolein  are re-
 lated to  the  high reactivity  of the carbon-carbon  double bond.
 However,  the  low pHs encountered  in the  upper portions  of the gas-
 trointestinal  tract would  probably  rapidly  convert  acrolein  to
 saturated  alcohol compounds.   The primary breakdown  product* would
probably  be  beta-propionaldehyde  (see Ingestion  from  Water  sec-
 tion) .  If this is the case,  the toxic effects of  acrolein given  by
oral administration would differ markedly from the effects observed
                               C-22

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following other routes of administration.  No information is avail-
able on the toxic effects of the acrolein breakdown products.  How-
ever,  an  analysis of subchronic and chronic studies suggests that
acrolein  is markedly less toxic when given by oral administration
than when inhaled  (see Basis and Derivation of Criterion section).
     Relatively  little  direct  information  is  available on   the
metabolism of acrolein.   Smith  and Packer  (1972) found  that prepa-
rations of rat  liver mitochrondria  were capable of oxidizing sev-
eral  saturated  aldehydes  but  not unsaturated  aldehydes, such as
acrolein, crotonaldehyde,  and  cinnamaldehyde.   In vitro, acrolein
can  serve as a substrate  for alcohol  dehydrogenases  from human
liver, horse liver,  and  yeast  with  equilibrium constants of 6.5  x
10"11, 8.3 x 10'11,  and  16.7 x  KT11, respectively  (Pietruszko, et
al. 1973).  In vivo studies in  rats  indicate  that a portion of sub-
cutaneously administered  acrolein is converted to 3-hydroxypropyl-
mercapturic acid  (Kaye and Young/ 1972;  Kaye, 1973).  Acrolein  has
also been shown to undergo both spontaneous and enzymatically cata-
lyzed  conjugation  with glutathione  (Boyland  and  Chasseaud,  1967;
Esterbauer, et al. 1975).
     Alarcon (1964,  1970)  has demonstrated that acrolein is formed
during the degradation of  oxidized spermine and spermidine.  Sera-
fini-Cessi (1972) has shown that acrolein  is a probable metabolite
of allyl  alcohol.   Several investigators have  demonstrated that
acrolein  is a metabolite of the anti-tumor agent cyclophospfcamide
(Alarcon, 1976b; Alarcon and Meienhofer, 1971;  Alaroon  and Melen-
dez, 1974; Alarcon,  et al. 1972; Connors,  et al. 1974;  Cox, et  al.
1976a,b; Farmer and Cox, 1975;  Gurtoo, et al.  1978;  Hohorst, et  al.
1976; Thomson and Colvin,  1974).
                               C-23

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 Excretion
                                                     .-
      In rats  given  single subcutaneous injections of acrolein,  10.5
 percent of the  administered dose  was  recovered in  the urine  as
 3-hydroxypropylmercapturic  acid  after  24 hours  (Kaye and Young,
 1972;  Kaye, 1973).
                              EFFECTS
 Acute,  Subacute,  and  Chronic Toxicity
      Acute Effects  on Experimental  Systems:  Several investigators
 have  described  the  toxic effects  of acute  lethal  exposure to acro-
 lein  on experimental  mammals (Boyland,  1940;  Carl, et al. 1939;
 Carpenter, et al. 1949; Skog, 1950; Smyth, et al. 1951;  Pattle and
 Cullumbine, 1956; Philippin, et  al.  1969;  Salem and Cullumbine,
 1960).   Albin (1962)  has summarized some of these  earlier  studies
 as well as unpublished reports (Table  7).   Skog  (1950)  compared the
 pathological  effects  of acute  lethal  subcutaneous  and  inhalation
 exposures  to  acrolein in rats.   After  inhalation  exposures,  the
 rats  evidenced  pathological changes  only  in  the  lungs.   These
 changes included edema, hyperemia, hemorrhages, and  possible degen-
erative changes in  the bronchial  epithelium.  Similar  changes have
 been  noted in mice, guinea pigs, and  rabbits  (Pattle  and Cullum-
bine,  1956;   Salem  and  Cullumbine, 1960).   After administering
 lethal  subcutaneous doses of acrolein to  rats,  Skog  (1950) noted
less  severe  lung damage  (edema  without significant hemorrnaging)
but also  found  pathological  changes  in  the liver  (hyperemfm  and
 fatty degeneration) and kidneys  (focal inflammatory changes).
     Given the probable instability of  acrolein on oral administra-
tion, a quantitative  comparison of  oral exposure  with  other routes
                               C-24

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                                           TABLE 7



                             Acute Lethal Toxicity of Acrolein*





0
ro
in







Species
Mouse
Mouse
Dog
Rat'
Rat
Rat
Mouse
Rabbit
Rabbit
Rabbit
Rabbit
Rabbit
Rabbit
Route
Inhalation
Inhalation
Inhalation
Inhalation
Oral
Oral
Oral
Percutaneous
Percutaneous
Percutaneous
Percutaneous
Percutaneous
Percutaneous
Lethal Dose
LC5Q-875 ppra
LC50-175 ppm
LCgQ-150 ppm
I£50-8 PPm
LD5Q-46 mg/kg
LD5Q-42 mg/kg
LD50-28 mg/kg
LD5Q-200 mg/kg
LD50~562 m9/k9
LD50-335 mg/kg
LD5Q-1022 rag/kg
LD5Q-164 mg/kg
LD5Q-238 mg/kg
Exposure
Time
1 min
10 min
30 min
4 hr
• • •
• • •
• • •
• • •
• * •
• • •
• • •
• • •
* • *
Remarks
Approximate value
Approximate value
Approximate value
Approximate value
Approximate value



Undiluted acrolein
20% acrolein in water
10% acrolein in water
20% acrolein in mineral
10% acrolein in mineral












spirits
spirits
*Source: Albin,  1962

-------
 would  be of particular interest.  In a study by Carl, et al.  (1939),
 rats given  intraperitoneal  injections of  acrolein  at  2.5 mg/kg/day
 died on  the second day.  Single doses of 10 mg/kg given to  two  rats
 by  stomach  tube killed  both  within 24 hours.   However,  six  rats
 tolerated doses of 5 mg/kg/day given by stomach tube for nine days.
 Although  firm conclusions  cannot be made from this limited data,
 these  results suggest  that  acrolein  has a  greater  acute  lethal
 potency when administered intraperitoneally than when given orally.
     The sublethal effects  of acute  acrolein  exposure  on the liver
 have  received considerable  investigation.   In adult  male rats,
 inhalation exposures  to  acrolein or intraperitoneal  injections of
 acrolein cause increases  in hepatic alkaline phosphatase activity
 as well as increases in liver and adrenal weights.  These effects,
 however, occurred only in exposures  causing dyspnea and nasal irri-
 tation (e.g., 4.8 mg/m3 x 40  hours).  Other hepatic enzyme  activi-
 ties, acetylcholine esterase  and glutamic-oxalacetic transaminase,
were not  affected.   Since  similar   patterns  were  seen with other
 respiratory  irritants,  the  alkaline  phosphatase  response  was
attributed  to an alarm  reaction rather   than  specific acrolein-
 induced liver damage (Murphy, et al. 1964).   In subsequent studies
 (Murphy, 1965; Murphy and Porter, 1966),  the  effect of  acrolein on
liver enzymes was  linked to  stimulation  of  the pituitary-adrenal
system resulting in hypersecretion of glucocorticoids and increased
liver enzyme synthesis.   Although these  results  do  not  suggest  that
acrolein is a direct  liver  toxin, Butterworth,  et al.  (1978)  have
shown that intravenous infusions of  acrolein  at doses of 0.85  and
1.70 mg/kg induce periportal  necrosis in  rats.  In further studies
                               C-26

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on the adrenocortical response of rats to acrolein, Scot and Murphy
 (1970)  demonstrated  increased  plasma and  adrenal  corticosterone
levels   in  rats  given  intraperitoneal  injections  of  acrolein.
Unlike similar  effects  caused by DDT and parathion,  the  effect  of
acrolein was  not blocked  by subanesthetic doses of phenobarbital
but  was  blocked by dexamethasone only at lower doses of  acrolein.
The  degree  of increased corticosterone levels is dependent  on the
state of the  adrenocortical secretory cycle  in  which acrolein  as
well as  other toxins  are administered  (Szot and Murphy,  1971).
     Since  acrolein is a  component of cigarette  smoke, the sub-
lethal  effects of  acrolein on  the respiratory  system have been
examined in some detail.  Murphy, et al.  (1963) found that,  in gui-
nea  pigs, inhalation of acrolein at concentrations from 0.92 to 2.3
mg/ra for periods  of  up to 12 hours caused dose-related  increases
in respiratory resistance, along with prolonged and deepened respi-
ratory cycles.  In  tests on  guinea  pigs exposed to  whole  cigarette
smoke from various  types of  cigarettes, Rylander  (1973)  associated
concentrations of  acrolein and  acetaldehyde with decreases  in the
number of free macrophages.  In mice exposed  to acrolein  in  air  at
concentrations  from 2.3 to 4.6 mg/m   for 24  hours there was evi-
dence of decreased pulmonary killing of Staphylococcus aureus and
Proteus mirabilis.  This decrease in intrapulmonary  bacterial kill-
ing  was  further suppressed  in  mice with  viral  pneumonia  (Jakab,
1977).   Kilburn and McKenzie (1978) have shown that acrolein*(13.8
mg/m  x  4 hours) by inhalation is cytotoxic to the  airway cells  of
hamsters, causing  both immediate  and  delayed exfoliation.   When
administered either .with  or adsorbed onto carbon particles, acro-
                               C-27

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lein  induced  leukocyte recruitment to  the  airways,  mimicking the
effect of whole cigarette smoke.  In a  single 10-raihute  inhalation
exposure of mice, acrolein caused dose-related decreases in respi-
ration attributed to sensory  irritation, with an ECgg of 3.9 mg/m3
(Kane and Alarie,  1977).   Formaldehyde caused the same  effect and
exhibited competitive  agonism in combination with acrolein  (Kane
and Alarie, 1978).
     Acrolein has been shown to exert pronounced ciliastatic activ-
ity in a variety of aquatic invertebrates  (see review by Izard and
Libermann, 1978).   As  discussed by Wynder, et al. (1965), impair-
ment of ciliary function in the respiratory tract of mammals may be
involved in the  pathogenesis  of several respiratory diseases, in-
cluding cancer.  Of several respiratory irritants  examined by Car-
son,  et  al.  (1966), acrolein was the  most effective in reducing
mucus flow rates  in cats after short-term  inhalation exposures.  In
in vivo  assays  of chicken trachea  ciliary activity,  acrolein and
hydrogen cyanide were found to be among the most potent  ciliatoxic
components of cigarette smoke  (Battista and Kensler, 1970).  Simi-
larly, in tests on  various types of cigarette smoke, Dalhamn (1972)
associated ciliastasis  in cats with  variations  in the  concentra-
tions of acrolein and tar.
     In in vitro studies  on  the effects of cigarette smoke compo-
nents on rabbit lung alveolar macrophages,  acrolein has  been shown
to inhibit phagocytosis,  adhesiveness,  and calcium-dependant ATP-
ase activity (Low,  et al.  1977)  and to inhibit the  uptake of cyclo-
leucine and cfc-aminoisobutyrate but not 3-0-methylglucose (Low and
                               C-28

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 Bulman,  1977).    However/  acrolein has  been  shown to inhibit  the
 uptake of glucose by  rabbit erythrocytes (Riddick,  et  al.  1968).
      Egle and Hudgins (1974)  noted that low doses  (0.05 mg/kg) of
 acrolein administered by intravenous  injection  to rats caused an
 increase  in blood  pressure/  but higher doses  (0.5 to 5.0  mg/kg)
 caused  marked decreases  in  blood pressure and  bradycardia.   The
 pressor response  was  attributed  to  increased catecholamine release
 from  sympathetic  nerve  endings and the adrenal medulla/ while  the
 depressor response was  attributed to vagal  stimulation.  Depressor
 effects were  noted after  1-minute inhalation exposures to  acrolein
 at 2.5 and  5.0 mg/1.  Acrolein elicited  significant cardiovascular
 effects  at  concentrations  below  those  encountered  in cigarette
 smoke.  Basu/ et al.  (1971)  have also examined  the effects  of acro-
 lein  on  heart rate in  rats.   Tachycardia  was  induced in  animals
 under general (sodium pentobarbital) anesthesia/  while bradycardia
was induced in animals  receiving  both general anesthesia and local
ocular  anesthesia  (2 percent  tetracain hydrochloride)  prior to
acrolein exposure.   Pretreatment with atropine  (0.5  mgAg?  i.v.)
along with  local  and general anesthesia  blocked  the bradycardia
response. Tachycardia was attributed  to  increased sympathetic dis-
charge caused by eye irritation.   Since the bradycardia  response
was blocked  by atropine/ parasympathetic  involvement was suggested.
       *,
     Several  groups  of investigators have examined  the  .general
cytotoxic effects  of acrolein.   Alarcon  (1964)  determine^  the
 inhibitory  activities  of spermine/  spermidine/   and  acrolein to
S-180 cell cultures.  The  concentrations  of  these  compounds causing
50 percent  inhibition were 1.4 to 1.5 x  10" mmol/ml for spermine/
                               C-29

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2.8  to 3.1 x 10   mmol/ml  for  spermidine,  and 2.6  to 3.5 x 10~5
iranol/ml for acrolein.  Since the inhibitory  potencies, of  these com-
pounds  were similar- and  since  only the two amines  required amine
oxidase in  exerting  the  inhibitory  effect,  Alarcon  (1964)  proposed
that  the  inhibitory activity of the  two  amines was due to the  in
vitro  formation of  acrolein.    Two groups of  investigators have
examined  the  role  of acrolein  in the  viricidal  effects of  oxidized
spermine  (Bachrach,  et al.  1971; Bachrach and  Rosenkovitch, 1972;
Nishimura,  et al.  1971,  1972).  Both  groups determined  that  the
antiviral potency  of acrolein  was  substantially less  than that  of
oxidized  spermine  and  that  the  antiviral  effects of  oxidized sper-
mine are  not  attributable to the generation of  acrolein.
     Koerker, et al. (1976)  have examined the cytotoxicity of acro-
lein  and  related  short-chain  aldehydes and  alcohols to  cultured
neuroblastoma cells.   Aldehydes were consistently more  toxic than
the corresponding  alcohols.  Based  on viability of harvested cells
and increase  in the number  of sloughed  cells  after exposure, acro-
lein was  more potent  than  formaldehyde and much more potent than
acetaldehyde  or  propionaldehyde.   Based  on  decreases in neurite
formation and viability of  sloughed  cells, formaldehyde was some-
what more potent  than  acrolein and substantially more potent than
either  acetaldehyde or  propionaldehyde.   In  ir\ vitro tests  on
Ehrlich-Landschutz diploid  ascites  tumor  cells, Holmberg  and Malm-
fors (1974) found acrolein  to be substantially more toxic th|in for-
maldehyde over incubation periods  of 1 to 5 hours.   Both  of these
aldehydes,  however, were  among the  more  toxic  organic  solvents
assayed in  this  study.   Similarly, in in  vitro  tests of tobacco
                               C-30

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smoke  constituents on  mouse ascites  sarcoma BP8  c'ells  (48-hour
exposure  periods), Pilotti, et  al.  (1975)  found  aldehydes to be
among  the most toxic  group of compounds studied.  At a  concentra-
tion of  100 uM, acrolein  caused substantially greater  inhibition
(94 percent) than  formaldehyde  (15 percent).
     Several of the cytotoxicity studies on acrolein  have addressed
the role of acrolein in the antineoplastic effects of cyclophospha-
mide.  Sladek  (1973)  determined the cytotoxicity of cyclophospha-
mide  and  various  cyclophosphamide metabolities,  including acro-
lein,  to  Walker 256 ascites cells.  In this study,  ascites cells
were exposed to the various compounds  jin vitro for one  hour,  then
injected  into  host rats.   The proportion  of viable  ascites cells
was  estimated   from survival times  of  the  rats.    Based on  this
assay, acrolein was found  to be  only marginally cytotoxic (LC9Q of
8.75 uM)  and  did  not account for  a  substantial proportion of the
cytotoxicity of cyclophosphamide  metabolites generated iri vivo.
Cyclophosphamide itself was virtually  nontoxic  (LCgo of^»100  uM).
Similar results on the  cytotoxicity  of acrolein to Walker  ascites
cells was obtained by Phillips (1974)  using an _in vitro  test system
in which cells were exposed to cytotoxic agents  for one  hour,  then
transferred to fresh culture medium. .Cytotoxicity was expressed as
a 72-hour  ICgQ  —  the exposure  concentration causing a  50  percent
decrease  in cell number compared to untreated  cells  72  hours after
treatment.  The ICg0  for  acrolein  was  1.0 ug/ml  (approximately 18
uM) and  the IC5Q  for  cyclophosphamide was 6,000 ug/ml.   Lelieveld
and Van Putten  (1976)  measured  the cytotoxic effects of  cyclophos-
phamide and six possible metabolites, including acrolein, to normal
                               C-31

-------
 hcmatopoietic  stem  cells of  mice/  osteosarcoraa cells,  and L1210
 leukemia cells.  Acrolein was  inactive against normal hematopoietic
 stem cells and osteosarcoma cells, and less active than cyclophos-
 phamide against leukemia cells.  Similarly/ Brock (1976)  has found
 that acrolein is less active than cyclophosphamide against Yoshida
 ascitic sarcoma of the rat.
      The cytotoxic effects of acrolein may be attributed/ at least
 in part/ to direct damage of nucleic acids or impaired nucleic acid
 or protein synthesis.  Using primary cultures of mouse-kidney tis-
 sue exposed to a total  of 70 ug acrolein/ Leuchtenberger/  et  al.
 (1968)  noted  a progressive decrease  in the uptake of tritiated uri-
 dine/  decreased RNA, and pycnosis of  cell nuclei.   Similarly/  in
 cultures of polyoma-transformed  cells  from cell lines of  Chinese
 hamsters exposed to  acrolein  at  concentrations of  0.8  to  2.5 x
 10" M  for one hour, Alarcon (1972)  found  concentration-related
 decreases  in  the  uptake  of tritiated uridine/  tritiated  thymidine,
 and tritiated leucine.   Using similar  methods/ Rimes and  Morris
 (1971)  have also  demonstrated inhibition of DMA/ RNA/ and  protein
 synthesis  by  acrolein in Escherichia coli.
     In jin vitro  studies on  the kinetics of acrolein  inhibition  of
 rat liver  and E.  coli RNA-polymerases/ Moule, et  al.  (1971)  found
 that inhibition was  unaffected by the amount of DNA  in the  medium
 but was partially  offset by  increased  levels  of  RNA-polymerase,
 suggesting that acrolein acts  on RNA-polymerase rather  than DNA.
 In  parallel  studies  on rat  liver and S.  coli  DNA-polymerase/
Munsch, et al.  (1973)  noted  that  acrolein inhibited rat liver DNA-
polymerase but stimulated E. coli DNA-polymerase.  Since the active
                               032

-------
 site  of rat liver  DNA-polymerase  is associated with a  functional
 sulfhydryl group  but  E. coli  DNA-polymerase  is  not  and since  acro-
 lein's  inhibitory  effect  on rat  liver DNA-polymerase  could  be
 antagonized  by 2-raercaptoethanol (see Synergism and/or  Antagonism
 section),  these investigators concluded that, acrolein acts on  rat
 liver DNA-polymerase by reacting with the sulfhydryl group.  Subse-
 quently,  Munsch,  et al.  (1974a) demonstrated that  tritiated  acro-
 lein binds 20  to  30 times more  to rat liver  DNA-polymerase than to
 E.  coli DNA-polymerase.    In partially  hepatectomized rats  given
 intraperitoneal injections of  acrolein  at  doses  of 0.1  to  2.7
 rag/kg,  DNA and RNA synthesis was  inhibited  in both the liver  and
 lungs (Munsch  and Frayssinet, 1971).
     Subacute  Toxicity to  Experimental  Mammals:   Most studies  on
 the subacute toxicity of acrolein  have  involved inhalation  expo-
 sures.   In  1-month inhalation  exposures of rats  to acrolein  at
 1.2 mg/m , Bouley (1973) noted decreases in growth  rates  and in  the
 levels  of oxidation-reduction coenzymes in  the liver (additional
details not  given).  Rats  continously exposed  to  acrolein in  the
 air at 1.27 mg/m3 for up to 77 days  evidenced decreased food intake
accompanied  by decreased  body weight gain.   Between days 7 and  21
of exposure, animals evidenced nasal  irritation.  Changes  in  rela-
 tive lung  and  liver  weights, as well   as serum  acid phosphatase
activity, are summarized  in Table 8.  Respiratory tract irritation,
a decrease  in  the  number of alveolar macrophages, and increased
susceptibility  to respiratory infection by  Salmonella enteritidis
were noted only during the  first three  weeks of exposure  (Bouley,
et al. 1975, 1976).  Philippin,  et  al. (1969) also  noted decreased
                               C-33

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                                                TABLE 8

               Relative Weights of Lungs and Liver, and Serum Level of Acid Phosphatases*
           Parameters
                                  Time
 Control rats
                                                                   Test Rats
Statistical
  Analysis
o
ui
Lungs weight x 100

Body weight
                                15th  and  32nd  days
                                    77th day
no significant difference between 2 x 10 control
            and 2 x 10 test rats
                                                   n « 10
                                                   ra *  0.489
                                                s.d. >  0.087
                    n * 15
                    m *  0.588
                 s.d. »  0.111
                                                                                   t « 2.67
                                                                                 0.02>P>0.01
Liver weight x
body weight
100

15th day
n - 10
m * 5.00
s.d. « 0.14
n - 10
m - 4.55
s.d. » 0.14
t = 7.12
0.001>P
                                32nd and 77th days
                                                no significant difference between 10 and 15 con-
                                                        trol, and 10 and 15 test rats
mil of acid phosphatases
per ml of serum
                                     15th day
                                32nd  and 77th days
                                                   n * 10
                                                   m - 77.87
                                                s.d. = 10.59
                    n - 10
                    m * 62.11
                 s.d. «  6.72
  t = 3.91
  P » 0.001
                                                no significant differences between 10 and 11 con-
                                                        trol,  and 10 and 11 test rats
     *Source:  Bouley,  et al.  1976
     n  =  number  of rats; m =  mean  value;  s.d.  *  standard deviation

-------
 body weight in mice exposed to airborne acrolein at 13.8  rag/m  and
 34.5 mg/m , six hours per day/ five days per week,  for six  weeks.
 Although the decreased body weight was significant (p 0.01),  the
 extent   of  the  decrease  was  neither  substantial  (approximately
 € percent)  nor dose-related.
      Lyon,  et al.  (1970) exposed rats, guinea  pigs,  monkeys,  and
 dogs to  acrolein concentrations of 1.6 and 8.5 rag/m  in the air  for
 eight hours per day, five days per week, for six weeks.   In addi-
 tion, continuous exposures  were conducted at 0.48, 0.53,  2.3,  and
 4.1  mg/m  for 90 days using the same animals.   The following bio-
 logical  endpoints  were  used  to  assess the  effects  of  exposure:
 mortality,  toxic  signs,  whole  body weight  changes, hematologic
 changes  (hemoglobin  concentration,  hematocrit,  and  total  leuko-
 cytes) ,  biochemical  changes  (blood  urea  nitrogen,  alanine  and
 aspartate  aminotransferase  activities),  and  pathological changes
 in heart, lung,  liver, spleen,  and kidney.  Gross effects were  not
 noted in the  continuous  exposures to  acrolein at  0.48  and 0.53
 mg/m  or in  the  repeated exposures to  1.6  mg/m .   In continuous
 exposures  to 2.3 and 4.1 mg/m  and in  repeated exposures to  8.5
 mg/m  ,  dogs  and  monkeys displayed  signs of  eye and respiratory
 tract irritation and rats  evidenced  decreased  weight gain.   All
 animals  exposed  repeatedly to acrolein  at 1.6  mg/m   developed
chronic  inflammatory  changes of the lung.  These changes  were more
pronounced  in dogs and monkeys than in rats and guinea pigs,  /ft  8.5
mg/m  squamous  metaplasia and basal cell  hyperplasia  of  the tra-
cheas of dogs and monkeys were attributed to acrolein exposure.  In
addition, this  exposure  induced necrotizing  bronchitis  and   bron-
                               C-35

-------
 chiolitis with squambus metaplasia in the lungs of 7 of  9  monkeys.
                                                    ;•
 Similar  pathological results were noted in continuous exposures  of
 rats,  guinea pigs,  dogs, and monkeys to 2.3 and 4.1 mg/ra^.
     Feron,  et al.   (1978) exposed hamsters, rats, and  rabbits  to
 acrolein vapor at 0.4,  3.2,  and 11.3 mg/nr six hours per day,  five
 days  per week, for  13  weeks.  At the highest  concentration, all
 animals  displayed signs of eye irritation, decreased food  consump-
 tion,  and decreased  weight gain.   In rats and  rabbits, no  abnormal
 hematological changes were noted.   Female guinea pigs at the high-
 est dose, however,   showed statistically significant increases  in
 the number of erythrocytes,  packed cell volume, hemoglobin concen-
 tration,  number of  lymphocytes,  and a decrease  in the  number  of
 neutrophilic leukocytes.  Additional  changes  noted in  this  study
 are summarized in Table 9.
     Watanabe and Aviado  (1974)   have  demonstrated that  repeated
 inhalation exposures of mice to acrolein (100 mg/ra3 for 30  minutes,
 twice  a  day  for  five weeks) cause  a reduction in pulmonary  com-
 pliance.
     The  subacute oral  toxicity  of acrolein has been examined  in
 less detail.   Albin  (1962) found that rats  exposed  to acrolein  in
drinking  water at concentrations  up to 200 mg/1 for 90 days  evi-
denced only  slight  weight reduction at the highest level  tested.
This was attributed  to unpalatability of the drinking water. Simi-
                                                             *
 lar results have been reported by Newell (1958)  (summarized in  NAS,
1977).   In one study, acrolein was  added  to the drinking  water  of
male and female rats at  5,  13, 32, 80, and 200 mg/1 for 90 days.  No
hematologic,  organ-weight, or pathologic  changes could  be  attrib-
uted to  acrolein  ingestion.   At  the highest concentration, water

                               C-36

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                                               TABLE 9

                  Summary of  Treatment-Related  Effects  in  Hamsters,  Rats  and  Rabbits
                             Repeatedly Exposed to Acrolein  for  13 Weeks*
O
         Criteria
         Affected
   Effects
                                                                  a
                                 Hamsters
                                 Acrolein (ppm)
Rats
Acrolein (ppm)
Rabbits
Acrolein (ppm)

Symptoraa tology
Mortality
Growth
Food intake
Haema tology
Urinary amorphous
material
Urinary crystals
Organ weights
Lungs
Heart
Kidneys
Adrenals
Gross pathology
Lungs
Histopathology
Nasal cavity
Larynx
Trachea
Bronchi + lungs
0.4
0
0
0
NE
0

0
0

0
0
0
0

0

0
0
0
0
1.4
X
0
0
NE
0
•
0
0

0
0
0
0

0

X
0
0
0
4.9
XXX
0
«-.
NE
X

+
. -

ft
+
+
0

0

XXX
X
XX
0
0.4
0
0
-
0
0

0
0

0
0
0
0

0

X
0
0
0
1.4
X
0
—
-
0

0
0

0
0
0
0

0

XX
0
0
0
4.9
XX
+++
	
—
0

+
-

•n-
+
+
+++

X

XXX
XX
XXX
XXX
0.4
-fl
0
0
0
0

0
0

0
0
0
0

0

0
NE
0
0
1.4
X
0
-
-
0

0
0

0
0
0
0

0

0
NE
0
0
j'9
XXX
.0
_._
—
0

•f
0

++
0
0
0

0

XX
NE
X
XX
         *Source: Feron, et al. 1978
          0 =• not affected; x = slightly affected; xx = moderately affected;
         xxx = severely affected; + = slightly increased; ++ = moderately increased;
         +++ - markedly increased; - = slightly decreased;— - moderately decreased;
         	 = markedly decreased; NE - not examined

-------
 consumption was reduced  by one-third  for the first three weeks.  By
 the 12th week,  the rats had  apparently adapted  to'the odor  and
 taste  of acrolein. .  In  a subsequent study, acrolein  was  added to
                    -*
 the drinking water of male  rats  at concentrations of  600,  1,200,
 and 1,800 mg/1  for 60 days.   All  animals died at, the two  higher
 concentrations, and 1 of 5  animals  died at 600 mg/1 concentration.
 Death  was apparently  due to  lack of water intake.  Tissues from the
 animals  surviving 600 mg/1  did not  show any gross or  micropatho-
 logic  abnormalities.
     Chronic Toxicity to Experimental Mammals:  The only published
 chronic  toxicity study on acrolein is  that presented by Feron  and
 Rruysse  (1977).   In this study, male  and female Syrian golden  ham-
 sters  were exposed  to acrolein at 9.2 mg/m  in the air, seven hours
 per day,  five days per week, for 52  weeks.  During the first week of
 exposure, animals evidenced signs of eye irritation, salivated,  had
 nasal  discharge,  and  were very restless.  These signs  disappeared
 during the  second week of exposure.   During the exposure period,
 males  and females  had  reduced body  weight  gains compared  to  the
 control animals but the  survival  rate was  unaffected.   Heraatologi-
 cal changes,  i.e.,  slight but  statistically significant  increased
 hemoglobin  content  and  packed  cell  volume, occurred  only  in  fe-
males.    Similarly, significant  (p
-------
     Effects  on  Humans:   As  summarized  in Table 10, considerable
information is available on the irritant properties of acrolein to
humans.   In studies on  photochemical  smog,  Altshuller (1978) has
estimated that acrolein could cause 35 to 75 percent as much  irri-
tation as formaldehyde.  Schuck and Renzetti (1960)  indicated that
acrolein and  formaldehyde  account for most  of  the eye irritation
caused by the photooxidation of various hydrocarbons.  Acrolein is
also  involved in the  irritant  effect of  cigarette  smoke (Weber-
Tschopp, et al. 1976a,b, 1977).
     Relatively  little information,  however, is  available on the
toxic effects of acrolein in humans.  Henderson and Haggard (1943)
state that  vapor concentrations of 23  mg/m  are lethal in a short
time.
     In  a  study on  irritant dermatitis  induced  by diallylglycol
carbonate monomer,  Lacroix, et al. (1976) conducted patch tests on
humans with acrolein.  In these tests, acrolein solutions in etha-
nol caused  no irritation at  concentrations  (v/v) of 0.01  to 0.1
percent.  At a concentration of 1 percent, 6 of 48 subjects showed
a positive  response (two erythemas  and four serious  edemas  with
bullae).  At a concentration of 10 percent, all eight subjects had
positive responses.  Histological findings of  a  second  series of
tests with 10 percent  acrolein are summarized in Table 11.
     Kaye and Young  (1974)  have  detected 3-hydroxypropylmercap-
turic in  the  urine of patients  receiving cyclophosphamide ,prally
(50 mg tvice or three times daily) but not in the urine of untreated
humans.      Based   on  analogies   to  the  metabolic  patterns  of
                               C-39

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                                              TABLE 10

                              Irritant Properties of Acrolein  to Humans
   Exposure
     Effect
                                                                            Reference
0.58 mg/m  x 5 min.
   2.3 mg/ra^ x  1 min.
   2.3 mg/ra  x  2 to  3 min.

   2.3 mg/m3 x  4 to  5 min.
    4.1 mg/nu  x  30  sec.
    4.1 ag/nu  x  1.0 min.
n   4.1 mg/ra   x  3  to 4 min.
i
*»
0           i
    12.7 mg/m  x 5  sec.

    12.7 mg/m3 x 20 sec.
    12.7 mg/ra  x 1  min.


    50.1 mg/m3 x  1 sec.

    0.48
    2.3 mg/m3
    9.2 mg/mj

    1.8 mg/ra  x  10  min.
    2.8 mg/m  x  5  min.
moderate irritation of sensory
  organs

slight nasal irritation
slight nasal and moderate eye
  irritation
moderate nasal irritation and
  practically intolerable eye
  irritation

odor detectable
slight eye irritation
profuse lachrymation; practically
  intolerable

slight odor; moderate nasal and
  eye irritation
painful eye and nasal irritation
marked lachrymation; vapor prac-
  tically intolerable

intolerable

odor threshold

highly irritating
lacrimation

lacrimation within 20 seconds,
  irritation to exposed mucosal
  surfaces
lacrimation within 5 seconds,
  irritation to exposed mucosal
  surfaces
                                                                            Albin,  1962
                                                                         Reist and Rex,  197?

                                                                         Pattie  and
                                                                           Culluntbine,  1956

                                                                         Sim and Pattle,
                                                                           1957

-------
                         TABLE  11

    Patch Tests with Ten Percent Acrolein in Ethanol on
          Control  Subjects  (Biopsied at 48 Hours)*
No. of
Biopsy
CM 375
CM 376
CN 74
CN 88
CN 89
CN 90
CN 91
CN 178
CN 179
CN 346
CN 347
CN 348
Polymorph. Papillary
Infiltrate Edema Epidermis
+++ ++ 0
+ ++ Necrosis
!,• ^^ Q
•M. ++ Necrosis
+ + 0
* + Necrosis
++ + : 0
+ . •«• Necrosis
* + Necrosis
0 + Bullae
•i»i-* •»• - 0
•M. *+• Bullae
Result
Irritation
Irritation
Irritation
Irritation
Irritation
Irritation
Irritation
Irritation
Irritation
Irritation
Irritation
Irritation
*Source: Lacroix, et al. 1976
                          C-41

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 cyclophosphamide in rats,  these investigators concluded  that  acro-
 lein  is probably a metabolite of cyclophosphamide in man.
      In  studies  014 human  polymorphonuclear  leukocytes  (PMNs),
 Bridges, et al.  (1977) found  that  acrolein was a potent  iri  vitro
 inhibitor  of  PMN chemotaxis (EC5Q of 15 urn)  but had  no significant
 effect on  PMN  integrity  (measured  by  beta-glucurbnidase  release,
 lactic acid dehydrogenase release,   and  cell  viability)  or  glucose
 metabolism (measured by glucose  utilization, lactic  acid  produc-
 tion, and  hexose monophosphate activity).  Cysteine,  at a  concen-
 tration  of  10  mM, completely  blocked  the  inhibitory  effect  of
 160 urn acrolein on PMN chemotaxis.   These results  are  consistent
 with  the assumption that  acrolein inhibits chemotaxis by reacting
 with  one or more  essential thiol groups on  cellular  proteins  in-
 volved in chemotaxis.  These proteins, however, do not appear  to be
 involved in glucose metabolism.
     Schabort (1967) demonstrated that acrolein inhibits human lung
 lactate dehydrogenase.   Inhibition  appeared  to be  noncompetitive
 with respect to  both NAOH  and pyruvate.
     Little  information is  available  on  the  chronic effects  of
 acrolein on humans.  An abstract  of  a Russian study  indicates that
 occupational exposure to acrolein (0.8 to 8.2  mg/nr), methylmercap-
 tan  (0.003 to  5.6 mg/m3),  methylmercaptopropionaldehyde  (0.1  to
 6.0 mg/m3), formaldehyde  (0.05  to  8.1 mg/m3),  and  acetaldehyde
 (0.48 to  22 mg/m )  was associated  with irritation  of  the mucous
membranes.   This effect was most frequent in women working for less
 than one year and greater  than  seven years  (Kantemirova, 1975).
                               C-42

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Synerqism  and/or  Antagonism
     Acrolein is highly  reactive toward  thiol  groups.   Acrolein
rapidly  conjugates with both  glutathione  and  cysteine (Esterbauer,
                   Jf     ,
et  al.  1975,  1976).   Cysteine  has been  shown  to antagonize  the
cytotoxic  effects of  acrolein on  ascites  tumor cells  of mice (Til-
lian,  et al. 1976).   Cysteine also antagonizes the  inhibition  of
                                                          X
acrolein on rabbit alveolar  macrophage calcium-dependent  ATPase,
phagocytosis,  and adhesiveness (Low, et al. 1977).   Both  cysteine
and  ascorbic acid have been  shown to  antagonize the acute  lethal
effects  of orally administered acrolein in male rats (Sprince,  et
al.  1978).   Munsch,  et  al.   (1973,  1974a)  have  demonstrated  that
2-raercaptoethanol antagonizes the inhibitory  effect of  acrolein  on
rat  liver  DNA-polymerase.   The   irritant  effects  of  acrolein  in-
jected into  the footpad of rats were blocked  by  N-acetyl-cysteine,
penicillamide, glutathione,  0-mercaptopropionylglycine, 2-mercap-
toethanol,   and ^^.^dimethylcysteamine   (Whitehouse   and Beck,
1975).
     The effects of acrolein, unlike those of ODT and  parathion,  on
the adrenocortical response of rats  is not inhibited by pretreat-
raent with  phenobarbital  and  is only partially inhibited  by dexa-
methasone  (Szot and Murphy, 1970).
     Pretreatment of  rats with acrolein  (3 mg/kg, i.p.)  signifi-
cantly  prolongs  hexobarbital  and  pentobarbital sleeping times
(Jaeger and Murphy, 1973).
                                                             V
Teratogenicity
     Reports have not been encountered on the potential  teratogeni-
city of acrolein.
                               C-43

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     Bouley, et al.  (1976) exposed male and female rats to acrolein
vapor at 1.3 mg/m  for 26 days and found no significant differences
either  in  the number, of  pregnant  animals or in  the  number and mean
weight  of  fetuses.
Mutagenicity
     In the dominant-lethal  assay for  mutagenicity  in  ICR/Ha Swiss
mice, acrolein did not cause a  significant increase in early fetal
deaths  or  pre-implantation  losses at doses  of 1.5 and  2.2 mg/kg
given in single intraperitoneal injections to male mice prior to an
8-week  mating period  (Epstein,  et al.  1972).
     As summarized by  Izard  and Libermann  (1978) ,  Rapoport  (1948)
assayed several olefinic aldehydes for their ability to induce sex-
linked  mutations in  Drosophila  melanogaster.    Acrolein had the
highest activity, causing   2.23  percent  mutations (IS  mutations
among 671  chromosomes).
     Using a strain  of DNA-polymerase deficient  Escherichia coli,
Bilimoria  (1975)  detected mutagenic activity in  acrolein as well as
cigar,  cigarette, and pipe smoke.  In  a  strain  of E. eoli used for
detecting forward mutations  (from gal Rs to gal* and from 5-methyl-
tryptophan  sensitivity   to  5-methyltryptophan  resistance)  and
reverse mutations (from arg~ to  arg"1") ,  acrolein demonstrated no
mutagenic  activity with  or without activation by mouse liver homo-
genates (Ellenberger and Mohn,  1976, 1977).
     Bignami, et  al.  (1977)   found that  acrolein  induced mutagenic
                                                           B
effects in Salmonella  typhimurium strains TA1538 and  TA98  (inser-
tions and  deletions),  but showed no activity in  strains TA1535 or
TA100  (base-pair substitutions).    Anderson,  et al.   (1972)  were
                               C-44

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 unable  to  induce  point  mutations  in  eight  histidine-requiring
 mutants of  S.  typhimurium.   This  system  also gave  negative  results
 for 109 other  herbicides but was positive for three known mutagens:
 diethyl  sulfate,  N-methyl-N'-nitro-N-nitrosoguanidine,  and  ICR-
      Izard  (1973)  determined the mutagenic effects  of  acrolein  on
 three strains of Saccharomyces  cerevisiae.  In  strain N123,  a  his-
 tidine auxotroph,  acrolein at  320  rag/1 induced twice  the control
 incidence  of respiratory-deficient mutants.   In  two methionine
 auxotroph  haploid  strains used  to  assay for frameshift  mutations
 and base-pair substitutions,  acrolein was inactive.  As  discussed
 by Izard and Libermann  (1978),  these  results  suggest that acrolein
 is not a strong inducer of respiratory deficient mutants and  does
 not appear  to  induce frameshift mutations or  base-pair  substitu-
 tions  in S.  cerevisiae.  However,  this lack  of activity could  be
due to the high toxicity or instability of acrolein or to the in-
ability of these strains to convert acrolein to some other  active
molecule.                     .  .
Carcinogenic!ty
     Ellenberger and Mohn  (1976)  indicated  that acrolein  is  "known
as (a) cytotoxic and  carcinogenic compound."   The  carcinogenicity
of acrolein  has not been  confirmed in this review of  the litera-
ture.   In the chronic inhalation study by Feron and Kruysse  (1977)
acrolein gave no indication of carcinogenic activity, had ho  effect
                                                              »
on the carcinogenic activity of  diethylnitrosamine  (DENA), and had
a minimal  effect on  the carcinogenic activity of  benzo(
-------
Table  12.   Based on  these  results,  Feron and Kruysse  (1977)  con-
cluded that  "...the study produced insufficient  evidence  to  enable
acrolein to  be regarded as an evident cofactor in respiratory tract
carcinogenesis."  Similar results have  been  obtained in a not-yet-
published  bioassay  sponsored  by the  National  Cancer  Institute
(Sharon Feeney,  personal  communication).   In this study,  hamsters
were exposed to acrolein vapor  at 11.5 mg/ra ,  six  hours  per  day,
five days  per  week,  throughout their life span.  Evidence was  not
found  that acrolein was a carcinogen or a cocarcinogen  with  either
benzo(<7*>)pyrene or ferric oxide.  DiMacco (1955)  summarizes a study
by  Savoretti (1954)   indicating  that acrolein  resulted in  an  in-
crease  in  the incidence  of benzopyrene-induced  neoplasms.    This
summary does not provide information on the  species  tested,  doses,
routes  of administration, or  the significance of the observed  in-
crease.
     Boyland  (1940)  found  that  acrolein, at daily  oral  doses  of
0.25 mg/mouse,  had a  marginal  (p^O.l)  inhibitory  effect on  the
growth  of  spontaneous skin  carcinomas  and a  significant  (p-^0.05)
inhibitory effect on  the growth  of grafted sarcomas.
                               C-46

-------
                                    TABLE 12

     Sit*. Type, and Incidence of Respiratory Tract Tumor » In Haaatera Eipoaed to
Air or AeroleIn Vapor and Treated Intratracheally with BP  or  Subcutaneously  with DENA*




Incidence
of TiMora
Inhalation of Air
Site and Type
of TuMora
	
I
* No of anlMala
xj t
examined
Larynx
Papllloaa
Trachea
Polyp
PaplllMa
Squaaoua cell
carcinoma
lUonch!
Polyp
Papiiioma
' Adenocarclnoaia
Squaaioua cell
carcinoma
Lung a
Papillary
adenoaia"
Aclnar adenoaia
Adenoaquaaous
adenoaa
SquaHoua cell
carclnoaa '
Oat cell-like
carcinoma
* 0.91
NaClb |

V
21

0

0
0

0

s
0
0

0


0
0

.9 **

0

0
BPC
1«. 2 •?>


27

1

0
0

0

0
1
0

0


0
0

1

0

0
BP*
|1C. 4


24

0

0
1

2

0
0
1

0


1
2

0

0

0
•g) OBNA*

Feaale*
27

3

0
•

0

0
2
0

0


0
0

0

0

0
* O.M
NaCl"

V
27

0

0
1

0

0
0
0

0


0
0

0

0

0



Inhalation of Acroleln
BPC
(U.2 •«.!


29

0

1
3

Q

0
0
0

0


2
2

0

0

0
BP*
(3C.4 M9>


30

0

0
C

2

0
0
0

1


4
5

2

1

1

DENA*


20

S

0
•

0

1
1
0

0


0
0

0

0

0

-------
TABLE 12 (continued)
Incidence of Tuarora
Inhalation of Air


0
I
4k
OB









-













Site and Type
of Tuaora
No of anl.fla
eiMlned'
Naaal cavity
Polyp
Papllloaa
Adenocarc 1 noaa
taryni
PapllloM
Trachea
Polyp
PaptlloM
Squftaoua cell
carclno.a
Anaplestle
carcinoma
Sarcoaa
Bronchi
Polyp
PapilloM
Adenoaa
Adenocarclno»a
l.ungi
Papillary adendfta
Acinar adeno.a
Adenosqua.oua
adenoaa
Adenocarc Inoaa
8 0.9«
BPC
NaClb (11.2 .9!
V
10

0
0
0

0

0
0

0

0
0

0
0
0
0
0
0

0
0
29

0
0
0

0

0
2

0

0
0

0
I
0
0
0
1

1
0
BPd
, (!«.« .91

DBNA*
Nalea
10 29

0
0
0

1

0
5

1

1
I

0
2
0
I
C
1

2
2

1
0
1

7

2
1

0

0
0

1
2
0
0
0
0

0
0
* 0.9»
NaClb
V
10

0
0
0

0

0
0

0

0
0

0
0
0
0
0
0

0
0
	 	 *«•-
Inhalation of Acroleln
BPC
I1-.2 .91
10

0
0
0

0

1
1

0

0
1

0
1
0
0
0
1

I
0
BP*
(1C. 4 *9l
29

0
0
0

1

2
1

1

2
1

2
0
1
2
4
1

1
0

DBMJt*
10

0
1
0

4

1
S

0

0
0

0
0
0
0
0
0

0
0

-------
                                              TABLE 12  (continued)





Incidence
of TiMora
Inhalation of Air
O
I
Site >and Type
of Tiworp
AdenoequaMoua
carcinoaia
SquMoui cell
carcinoma
Oat cell-like
carclnoM
Anaplaatlc
carcinoaa
* 0.91
MaCl"
0
0
0
0
BPC
III. 2 my}
0
0
0
0
tt*
(16.4 »gj
0
1
0
1
OBHA*
0
0
0
0
* 0.9%
MaClb
0
0
0
0



Inhalation of Acroleln
Hi. 2 B9)
0
1
0
0
(16.4 Kg)
1
1
1
0
DEN A*
o t
0
0
0
•Sources Peron and Kruyaae. 1977
*Ho further treatment
 Given Intratracheally (0.2 all «eek!y during 52 wb
C0lven Intratracheatly In S2 weekly doaea of 0.15 mg
 Given intratracheally In 52 weekly doaea of 0.70 mq
'Given aubcutaneoualy In 17 three-weekly doaea of 0.125 ul
*A few haaaters were loat through canniballa« or autolyala

-------
                      CRITERION FORMULATION
Existing Guidelines  and  Standards
     Th« current  time-weighted average threshold  limit  value  (TLV)
for acrolein established by the American Conference of Governmental
Industrial, Hygienists (ACGIH, 1977) is 0.1 ppm (0.25 mg/m3).  The
same value is enforced by the Occupational Safety  and Health Admin-
istration  (39 FR 23540).  The ACGIH standard was designed to "mini-
mize, but  not entirely prevent, irritation to all  exposed  individ-
uals"  (ACGIH,  1974).   Kane  and  Alarie  (1977) have reviewed the
basis for  this TLV in terms  of both additional data  on  human  irri-
tation and their  own work on the  irritant effects of  acrolein  to
mice (summarized  in  the  Acute, Subacute,  and Chronic Toxicity sec-
tion) .   These investigators concluded that "the  0.1 ppm TLV for
acrolein is  acceptable  but  is close  to  the highest value of the
acceptable  0.02  to 0.2  ppm  range  predicted  by this  animal model"
(Kane and Alarie, 1977).
     The Food and Drug  Administration permits the use  of  acrolein
as a slime-control substance in the manufacture  of  paper and paper-
board for use in  food packaging (27 FR 46) and  in  the treatment  of
food starch at not more  than 0.6 percent  acrolein  (28 FR 2676).
     In the Soviet Union, the maximum  permissible  daily concentra-
tion of  acrolein in  the atmosphere is 0.1  mg/ra   (Gusev, et al.
1966).  This study did  not specify whether this level  is  intended
as an occupational or ambient air quality standard.
Current Levels of Exposure
     As detailed in the Exposure section, quantitative estimates  of
current levels of human exposure  cannot be made  based on the avail-
able data.   Acrolein has  not been  monitored  in  ambient raw  or
finished waters.
                               C-50

-------
Special Groups at Ri^<
     Since acrolein is a component of tobacco and marijuana smoke,
people exposed to  these  smokes  are  a group at increased risk from
inhaled acrolein.  In addition, acrolein is generated by the ther-
mal decomposition of fat, so cooks are probably also at additional
risk (see Exposure .section).  since  acrolein has been shown to sup-
press pulmonary  antibacterial defenses,  individuals with or prone
to pulmonary  infections may also be at greater risk (Jakab, 1977).
Basis and Derivation of Criterion
     Although acrolein is mutagenic in some test systems  (see Muta-
genicity section) and can bind  to mammalian DNA (see Acute Effects
on  Experimental  Systems  section),  current  information indicates
that acrolein is not a  carcinogen or cocarcinogen (see Carcino-
genicity section).   Water quality criteria for  acrolein could be
derived from  the TLV, chronic inhalation studies, or subacute oral
studies using noncarcinogenic biological responses.
     Stokinger and Woodward (1958) have described  a  method for cal-
culating  water  quality  criteria  from TLVs.   Essentially,  this
method consists  of deriving an acceptable  daily  intake (ADI)  for
man  from  the TLV by  making  assumptions  on  breathing  rate  and
absorption.   The ADI is  then  partitioned  into permissible amounts
from drinking water and other sources.  However, because  the TLV is
based on  the prevention  of the  irritant  effects  of  acrolein on
inhalation exposures, such a criterion would.have little, if any,
                                                            «
validity.
     A criterion could  also be  estimated based on chronic inhala-
tion data.  Female hamsters exposed  to acrolein at 9.2 mg/m3  in the
                               C-51

-------
air,  seven hours per  day,  five days per  week,  for 52 weeks  evi-
denced  slight hematologic changes, significant decreases  in  liver
weight,  and  significant  increases  in lung  weights  (Feron .and
Kruysse,  1977).   By making  assumptions of respiratory volume and
retention,  the exposure  data from  this  study  can  be., converted  to  a
mg/kg dose and  an "equivalent" water exposure level can be calcu-
lated.  The average  body weight for  the hamsters  at the end of the
exposure was about 100 g.  Assuming a mean  minute  volume  (amount of
air  exchanged per minute) of 33 ml for a  100 g hamster  (Robinson,
1968) and  a retention  of 0.75,  the average daily  dose  is estimated
at  68.3 ug/animal  (9.2  mg  acrolein/m  x 0.033  1/min x 1  m /1,000
liters  x  60-min/hour x 7 hours/day x 5  days/7 days x 0.75) or 683
ug/kg.  Using an  uncertainty factor  of  1,000  (NAS,  1977),  an esti-
mated "unacceptable" daily  dose for man  is  0.683  ug/kg  or  47.8
ug/man,  assuming  a 70  kg body  weight.
     A criterion  based on this daily dose level would be  unsatis-
factory for two  reasons.  First, the dose data used to derive the
standard  are  not based on a  no-observed-effect  level  (NOEL).   In
this respect, the derived criterion  could  represent an undesirably
high  level in water.    Secondly,  the  estimation is  based  on an
inhalation  study.   Given the  probable  instability of acrolein in
the gastrointestinal tract,  the use of  inhalation data may not be
suitable for deriving  a  criterion.
     In Drinking Water  and  Human  Health,  the National Academy of
Sciences  (NAS, 1977) summarized the study by Newell (1958)  in which
acrolein was added  to  the drinking water of rats  at concentrations
of 5, 13,  32,  80, and 200 mg/1 for  90 days  without apparent adverse
                               C-52

-------
effects   (see  Acute,  Subacutae,  and  Chronic  Toxicity - section) .
Assuming  a  daily water, consumption of 35 ml/day and a  body weight
of 450 g  (ARS Sprague-Dawley, 1974), the chronic no-effect dose for
rats based  on  200 mg/1 in water is estimated at 15.6 mg/kg.   This-
value may be converted into an ADI  for  man by applying  an uncer-
tainty factor.   Since  the study involved only 90-day exposures,  an
uncertainty factor of  1,000 is recommended  (NAS, 1977).  thus,  the
estimated ADI for man is 15.6 ug/kg or 1.09 mg/man,  assuming a  70  kg
body weight.  Therefore, consumption of 2 liters of water daily and
6.5 grams  of fish  having  a bioconcentration factor of  215  would
result  in,   assuming 100  percent gastrointestinal  absorption  of
acrolein, a maximum permissible concentration of '0.32 ug/1  for  the
ingested water:
                                       0.321 mg/1
          21+  (215 x 0.0065) x 1.0
This calculation assumes that 100 percent of man's  exposure  is con-
tributed by  ingesting  water and contaminated fish/shellfish prod-
ucts.   Although  it is desirable  to develop a  criterion based on
total exposure analysis, the data for other exposure are not suffi-
cient to support a factoring of the ADI  level.
     In summary,  based on  the  use of  acute toxicologic data  for
rats and an  uncertainty  factor  of  1,000, the criterion  level cor-
responding to the calculated acceptable  daily intake of  15.6 ug/kg
is 0.32 mg/1.  Drinking water contributes 12 percent of  the  assumed
                                                            *
exposure while eating  contaminated fish products  accounts for 88
percent.   The criterion  level  for acrolein  can alternatively be
expressed as 0.78 mg/1 if exposure is assumed to be from the con-
sumption of  fish and shellfish products  alone.
                               C-53

-------
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                                   C-61

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       IT S GOVERNMENT PRINTING OFftCE :«- ~-:'6«M«
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