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CORNINGHazlcton MUTAGENICITY TEST WITH T-6342 IN THE SALMONELLA - ESCHEPICHL4 COLIMAMMALIAN-MICP,(>SOMt MUTATION ASSAY RE-1@ERSE FINAL REPORT AUTHOR Timothy E.Lawlor,M.A. PERFORMING LABORATORY Coming HazletonInc.(CHV) 9200 LeesburgPike Vienna,Virginia22182 LABORATORY PROJECT ID CHV StudyNo.: 17073-0409 SUBM=ED TO 3M Corporation Building220-2E-02 3M Center St.Paul,MN 55144-1000 STUDY COMPLETION DAIE December 14,1995 CHV StudyNo.: 17073-0409 1 of 30 CORNINGHazleton QUALITY ASSURANCE STATEMENT STUDY TITLE: Salmonel-lEaschericchoilai/Mammalian-MicrRoesvoemresMeutation Assay ASSAY NO.: 17073-0-409 PROTOCOL No.: 409,Edition4,Modifiedfor3M Corporation QualityAssuranceinspectionosfthestudyandreviewofthefinalreportoftheabove referenced projectwere conductedaccordingtotheStandardoperatingProceduresoftheQualityAssurance Unitand accordingtothegeneralrequirementosftheappropriatGeood LaboratoryPractice regulationsF.indingsfrom theinspectionasnd finalreportreviewwerereportedtomanagement and tothestudydirectoorn thefollowingdates: Inspection/Date Plating- 09/19/95 DraftReportReview - 11/06/95 FindingsRep-Qrted 09/19/95 11/07/95 FinalReportReview - 12/14/95 12/14/95 Audito M. Murphy C. Orantes/ S. Ballenger C. Orantes u@ul it@syssursaunr@acnecme@mtt Datre-RJease-d CHV StudyNo.: 17073-0-409 2 CORNINGHazleton STUDY COMPLIANCE AND CERTIFICATION The study was conducted incompliance with theGood LaboratoryPracticeregulationsasset forthintheFood and Drug Administration(FDA) Title21 oftheU.S. Code ofFederal RegulationsPart58, issuedDecember 22, 1978,(effectivJeune 20, 1979) and with any applicableamendments. There were no significandteviationsfrom theaforementioned regulationosrthe signedprotocolthatwould affecttheintegritoyf the studyor theinterpretation of thetestresults.The raw datahave been reviewed by theStudy Director,who certifietshatthe evaluationofthe testarticlaes presentedhereinrepresentsan appropriateconclusionwithinthe contextof thestudy designand evaluationcriteria. Study Director: Timothy E. awlor,M.A. Bacterial utagenesis Genetacan- CellularToxicology Li Study Completion Date CHV Study No.: 17073-0-409 3 TABLE OF CONTENTS CORNINGHazieton Page No. 1. SUMMARY ..........................................5......... ii. STUDY INFORMATION ..................................7.......... III. MATERIALS AND METHODS ...............................9......... IV. RESULTS AND CONCLUSIONS .............................2.3.......... V. DATA TABLES .......................................26.......... CHV StudyNo.: 17073-0-409 4 CORNINGHazleton SECTION 1. SUMMARY INTRODUCTION AND CONCLUSIONS CHV StudyNo.: 17073-0-409 5 CORNINGHazleton SUMMARY A. Introduction At therequesotf3M CorporatioCno,ming HazletoInnc.investigaTt-e6d342for mutageniacctiviitnytheSalmonella-Eschericcohliia/Mammalian-MicrosRoemveerseMutation Assay. This assayevaluatedthetestarticlaend/oritsmetabolitesfortheirabilittyoinduce reversemutationsatthehistidinleocusinthegenome of specifiScalmonella typhimurium tester strainasnd atthe tryptophanlocusinan Escherichiacolitesterstrainboth inthepresenceand absence of an exogenous metabolicactivationsystem of mammalian microsomal enzymes derivedfrom AroclorTm-inducedratliver(S9). The doses testedin themutagenicityassaywere selectedbased on the resultsof a dose rangefindingstudy usingtesterstrainsTA 100 and WP2uvrA and ten doses oftestarticlreanging from 5,000 to 6.67 @Lgper plate,one plateper dose,both in thepresenceand absence of S9 mix. ne testerstrainsused in themutagenicityassaywere Salmonella typhimurium testerstrains TA98, TAIOO, TA1535, TA1537, and EscherichiacolitesterstrainWP2uvrA. Theassaywas conducted with fivedoses oftestarticlienboththepresenceand absence of S9 mix along with concurrentvehicleand positivecontrolsusingthreeplatesper dose. The doses testedwere 5,000,3,330, 1,000,333, and 100 gg per platein both thepresenceand absence of S9 mix. B. Conclusions The resultosftheSalmonella- Escherichiacoli/Mammalian-Microsome Reverse Mutation Assay indicatethat,under theconditionsofthisstudy,3M Corporation'tsestarticle, T-6342, did not cause a positiveincreaseinthe number of revertantpser plateofany of thetester strainseitherinthepresenceor absenceof microsomal enzymes preparedfrom AroclofT'm-inducerdatliver(S9). CHV Study No.: 17073-0409 6 CORNINGHazleton SECTION 11.STUDY INFORMATION CHV StudyNo.: 17073-0409 7 CORNINGHazleton STUDY INFORMATION A. Sponsor: 3M Corporation B. TestArticle:T-6342 I. Physical Description: clear colorless liquid 2. Date Received: 07/21/95 C. Type of Assay: Salmonella-Escherichia coli/Mammalian-Microsome Reverse Mutation Assay I ProtocolNumber: CHV Protocol409,Edition4 Modifiedfor3M Corporation 2. CHV StudyNumber: 17073-0-409 D. Study Dates I. Study InitiatioDnate: 08/28/95 2. ExperimentalStartDate: 09/12/95 3. ExperimentalTerminationDate: 09/22/95 E. Study SupervisoryPersonnel Study Director: Timothy E. Lawlor,M.A. LaboratorySupervisor: Michael S.Mecchi, B.S. CHV Study No.: 17073-0-409 8 I CORNINGHazleton SECTION Ill.MATERIALS AND METHODS CHV Study No.: 17073-0-409 9 CORNINGHazleton MATERIALS AND METHODS The experimentmaalterialmse,thodsandprocedureasrebasedon thosedescribebdy Ames etal(1975)andGreenandMuriel(1976). MATERIALS A. Tester Strains I. Salmonella typhimurium The tester strains used were the Salmonella typhimurium histidine auxotrophs TA98, TAIOO, TA1535, and TA1537 as described by Ames etal (1975). The specificgenotypes of thesestrainsare shown inTable 1. TABLE 1. TEST HistidineMutation hisG46 hisC3076 hisD3052 TA1535 TA1537 TAIOO TA98 R STRAIN GENOTYPES AdditionalMutations LPS Repair R Factor rfa uvrb rfa uvrb +R Inadditiontoa mutation inthe histidinoeperon,thetesterstrainscontaintwo additional mutationswhich enhance theirsensitivittyosome mutagenic compounds. The rfawall mutation resultsinthe lossof one of theenzymes responsibleforthesynthesisofpartofthe lipopolysaccharidbearrierthatforms the surfaceof thebacteriaclellwall.The resultincgellwall deficiencyincreasespermeabilityto certainclassesof chemicalssuch as thosecontaininglarge ringsystems(i.eb.enzo(a)pyrene)thatwould otherwisebe excluded by a normal intactcellwall. The second mutation,a deletionofthe uvrb gene,resultisna deficienDtNA excisionrepair system which greatlyenhances thesensitivitoyf thesestraintsosome mutagens. Since the uvrb deletionextendsthrough thebio gene,allofthe testerstraincsontainingthisdeletionalsorequire thevitaminbiotinforgrowth. StrainsTA98 and TA 100 alsocontainthe R-factorplasmid,pKM 101,which furtherincreases thesensitivitoyf thesestrainstosome mutagens. The mechanism by which thisplasmid increasessensitivittyo mutagens has been suggestedtobe by modifying an existingbacterial DNA repairpolymerase complex involvedwiththemismatch-repairprocess. CHV Study No.: 17073-0-409 10 CORNINGHazleton TestesrtraiTnAs98andTA 1537arerevertferdomhistiddienpeenden(caeuxotropthoy) histidiniendependence(prototrophbyy) frameshifmtutagens.TA1535 isrevertebdy base substitutimountagensand TA 100 isrevertedby mutagenswhich causebothframeshiftasnd base substitutions. 2. Escherichiacoli The testerstrainused was thetryptophanauxotroph WP2uvrA as describebdy Green and Muriel(1976). Inadditiotnoa mutationinthetryptophaonperon,thetestesrtraicnontainsa uvra DNA repair deficiencwyhich enhancesitssensitivittoysome mutageniccompounds. Thisdeficiencayllows thestraitnoshow enhancedmutabilitsyincetheuvra repairsystemwould normallyactto remove thedamaged partoftheDNA moleculeandaccuratelryepairitafterwards. TesterstraiWnP2uvrA isrevertefdrom tryptophadnependence(auxotrophyt)otryptophan independence(prototrophyb)y basesubstitutimountagens. 3. SourceofTesterStrains a. Salmonella typhimurium The testerstrainsin use atCHV were received directlyfrom Dr. BruceAmes, DepartmentofBiochemistryU,niversitoyfCaliforniBae,rkeley. b. Escherichiacoli The testerstrainW,P2uvrA, inuse atCHV was receivedfrom the NationalCollectioonfIndustriaBlacteriaT,orreyResearchStationS,cotland(UnitedKingdom). 4. Storageof the--T-esStterains a. FrozenPermanentStocks Frozenpermanentstockswere preparedby growing fresh overnighctulturesa,ddingDMSO (0.09myml ofculturea)nd freezinsgmallaliquots (0.5-1.m5l)at:5-70*C. CHV StudyNo.: 17073-0409 11 CORNINGHazieton b. MastePrlates Masterplateswere preparedby streakinegachtestesrtraifnrom a frozenpermanentstockontominimalagarappropriatelsyupplementedwith 1)forSalmonella typhimurium,an excessofhistidinaen,d biotina,nd fortestesrtrainTsA 98 and TA 100, ainpicill(i2n5gg/ml),toensurethestablmeaintenanceofthepKM 101plasmid;and 2)for Escherichicaolia,n excessofftyptophanT.esterstraimnasterplatewsere storedat 5 30C. 5. Prel2aratioofnOvernightCultures a. Inoculation Overnightculturefsoruseinalltestinpgrocedureswere inoculated by transferriangcolonyfrom theappropriatmeasterplatetoa flaskcontainincgulturmeedium. Inoculatefdlaskswere placedina shaker/incubatwohrich was programmed tobeginoperation (shaking1,25 25 rpm; incubatio3n7, 2*C) sothattheovernighctulturewsereinlogphaseor latelogphasewhen turbiditmyonitoringbegan. b. Harvest To ensurethatculturewsere harvestedinlatelogphase,thelength ofincubatiownas determinedby spectrophotometrmiocnitoringofculturteurbidityC.ultures were harvestedonce apredeterminedturbiditwyas reachedasdeterminedby a percent transmittanc(e%T) readingon a spectrophotometeTrh.istargeturbiditeynsuresthatcultures have reacheda densityof atleast0.5X 10'cellsperml and thattheculturehsave notovergrown. Overgrown (stationarcyu)lturemsay exhibidtecreasedsensitivittoysome mutagens.Cultures were removed from incubatiownhen thetarge%tT was reachedand wereplacedat5 3OC. 6. ConfirmatioonfTesterStrainGenoilpm Testerstraicnulturewsere checkedforthefollowinggeneticmarkerson theday of theiruse inthemutagenicitayssay: a. Salmonella typhimurium 1) rfa Wall Mutation The presence of the rfa wall mutation was confirmed by demonstratioonfthesensitiviotfytheculturteocrystavlioletA.n aliquootfan overnight CHV StudyNo.: 17073-0-409 12 CORNINGHazieton cultuorfe achstrawiansoverlaoindtpolatceosntainsienlgectmievdeia ndanantibiotic sensitividtiyskcontainin1g0 pg ofcrystavliolewtas added.Sensitiviwtays demonstratedby inhibitiofnbacteriaglrowthina zoneimmediatelysurroundintghedisk. 2) pKM 101 PlasmidR-factor The presenceofthepKM 101plasmidwas confirmedfor testesrtrainTsA98 and TAIOO by demonstratioonfresistancteoampicillinA.n aliquootfan overnightcultureofeachstraiwnas overlaiodntoplatescontaininsgelectivmeedia and an antibiotiscensitividtiyskcontaining10 4g ofaznpicillwians added. Resistancweas demonstratedby bacteriaglrowthinthezoneimmediatelysurroundingthedisk. 3) CharacteristNiucmber ofSpontaneousRevertants T'hemean number of spontaneousrevertantpserplateinthe vehiclecontroltshatarecharacteristoifctherespectivsetrainwsere demonstratedby plating 100 glaliquotosftheculturaelongwiththeappropriatveehicleon selectivmeedia. b. Escherichiacoli 1) CharacteristNiucmber ofSpontaneousRevertants The mean number ofspontaneousrevertantpserplateinthe vehiclecontrolsthatarecharacteristoifctherespectivsetrainwsere demonstratedby plating 100 gl aliquotsoftheV@P2uvrA culturaelongwiththeappropriatveehicleon selectivmeedia. 7. TesterStrainMedia a. CulturinBgroth T'hebrothused togrow overnightcultureosfthetestesrtrainwsas Vogel-Bonnersaltsolutio(nVogeland Bonner,1956)supplementedwith2.5% (w/v)Oxoid NutrienBtrothNo. 2 (drypowder). b. Agar Plates Bottom agar(25ml per15x 100mm petridish)was VogelBonnerminimalmedium E (Vogeland Bonner,1956),supplementedwith1.5% (w/v)agarand 0.2% (w/v)glucose. CHV StudyNo.: 17073-0409 13 CORNINGHazleton C. OverlayAgar forSelectioonf Revertants Overlay(top)agarwas preparedwith 0.7% agar(w/v)and 0.5% NaCl (w/v)and was supplementedwith 10ml of1)0.5MM histidinelbiostoilnutiopner 100 ml agarforselectioonfhistidinreevertantosr,2) 0.5mM tzyptophansolutionper 100 mi of agarforselectioonf tryptophanrevertantsW.hen S9 mix was required2,.0ml of the supplementedtop agarwas used intheoverlay.However, when S9 mix was notrequiredw,ater was added tothesupplementedtopagar(0.5ml ofwaterper2 ml of supplementedtopagar)and theresultin2g.5ml ofdilutedsupplementedtopagarwas used fortheoverlay.Thisdilution ensuredthatthefinaltop agarand amino acidsupplementconcentrationrsemainedthesame both inthepresenceand absenceof S9 mix. B. Liver Microsomal Enzyme Reaction Mixture (S9 Mix) I. S9 Homogenate Livermicrosomalenzymes (S9 homogenate)were purchasedfrom MolecularToxicology,Inc.,Annapolis,MD 21401,Batch 0568 (38.8mg of proteinper ml) and Batch0569 (38.8mg of proteinperml). The homogenate was preparedfrom male SpragueDawley ratsthathad been injecte(di.p.w)ithAroclor@r1m254 (200mg perml incom oil)at 500 mg/kg asdescribedby Ames etal,1975. 2. S9 Mix The S9 mix was preparedimmediatelypriortoitsuse inany experimental procedure.The S9 mix containedthecomponents indicateidnTable Il. TABLE II.S9 Ml' H20 IMNaH2pO4/Na2HP04, pH7.4 0.25M Glucose-6-phosphate 0.1OM NADP 0.825M KCI/0.2M MgCI2 S9 Homogenate 0.70ml 0.10ml 0.02 ml 0.04in] 0.04ml 0.10ml 1.00ml CHV StudyNo.: 17073-0409 14 CORNINGHazleton C. Controls 1. VehicleCon Is Vehiclecontrolswere platedforalltestesrtrainbsoth inthepresenceand absenceof S9 mix. The vehiclecontrolwas plated,usinga 50 Illaliquotof vehicle(equaltothe maximum aliquotoftestarticldeilutiopnlated)a,longwitha 100 pl aliquotoftheappropriate testesrtraiannd a 500 Alaliquotof S9 mix (when necessary)o,n selectivaegar. 2. PositiveControls The combinationsofpositivecontrolsa,ctivatiocnonditionand tester strainpslatedconcurrentlywith theassayareindicatedinTable111. Tester S.M& TA98 TA98 TAIOO TAIOO TA1535 TA1535 TA1537 TA1537 WP2uvrA WP2uvrA TAB] S9 Mix + + + + + TIYE --ds Conc PositiveControl per plate 2-aminoanthracene 2.5pg 2-nitrofluorene 1.0gg 2-aininoanthracene 2.5;ig sodium azide 2.0gg 2-aminoanthracene 2.5gg sodium azide 2.0 pg 2-aminoanthracene 2.5 gg ICR- 191 2.0 gg 2-aminoanthracene 25.0 pg 4-nitroquinoline-N-oxide1.0gg a. Sourceand Grade ofPositiveControlArticles 2-aminoanthracen(eCAS #613-13-8)S,igma Chemical Co.,purity 97.5%;2-nitrofluore(nCeAS #607-57-8)A,ldrichChemicalCo.,purity98%; sodium azide (CAS #26628-22-8),Sigma Chemical Co.,purity>98%; ICR-191 (CAS # 1707-45-0)@ PolyscienceIsnc.p,urity>95%; 4-nitroquinoline-N-ox(iCdAeS #56-57-5),Sigma Chemical Co., purity>99%. CHV StudyNo.: 17073-0409 15 CORNINGHazleton 3. SteriliCtoyn=la a. TestArticle The most concentratetdestarticldeilutiownas checkedforsterility by platinga 50 g] aliquot(thesame volume used intheassay)on selectivaegar. b. S9 Mix agar. The S9 mix was checked forsterilibtyyplating0.5ml on selective METHODS A. Dose RangefindinLyStudy The growth inhibitoryeffect(cytotoxicityo)f thetestarticleto thetestsystem was determinedinordertoallowtheselectioonfappropriatdeosestobe testedinthemutagenicity assay. I. Design The dose rangefindingstudywas performedusingtesterstrainTsA 100 and WP2uvrA both inthepresenceand absenceof S9 mix. Ten dosesof testarticlweere tested atone plateperdose. The testarticlweas checkedforcytotoxicituyp toa maximum concentratioonf5 mg perplate. a. Rationale The cytotoxicitoyfthetestarticloebservedon testerstrainTA 100 isgenerallyrepresentativoef thatobservedon theothertestesrtrainasnd becauseof TA I00's comparativelyhighnumber ofspontaneousrevertantpserplateg,radationsof cytotoxicitcyan be readilydiscernedfrom routineexperimentalvariationT.he Escherichiacolitestesrtrain WP2uvrA does notpossesstherfawallmutationthattheSalmonellatyphimuriumstrainhsave and thus,a differenrtange ofcytotoxicitmyay be observed.Also,thecytotoxicitiynducedby a testarticlienthepresenceof S9 mix may vary greatlyfrom thatobservedintheabsenceof S9 mix. Therefore,thiswould requirethatdifferenttestarticldeoserangesbe testedinthe mutagenicityassaybased on thepresenceor absenceoftheS9 mix. CHV StudyNo.: 17073-0-409 16 CORNINGHazieton 2. Evaluationofthe-Dose-RanizefindSitnugdy Cytotoxicitiysdetectablaesa decreaseinthenumber ofrevertanctolonies perplateand/orby a thinningor disappearancoefthebacteriablackgroundlawn. 3. aelectioonftheMaximum Dose fortheMutaizeniciAtsysU a. No CytotoxicitOybserved Sinceno cytotoxiciwtays observedinthedoserangefindinsgtudy, thehighestdose of testarticluesedinthemutagenicitayssaywas thesame asthattestedinthe rangefindinsgtudy. B. MutageniciijAssay I. Design The assaywas performedusingtestesrtrainTsA98, TA 100,TA 1535, TA1537, and WP2uvrA bothinthepresenceand absenceofS9 mix. Fivedosesoftestarticle weretestedalongwiththeappropriatveehicleand positivceontrolsT.he dosesoftestarticle were selectedbasedon theresultosf thedoserangefindinsgtudy. 2. Frequencyand Routeofadministration The testesrtrainwsere exposedtothetestarticlveiatheplate incorporatiomnethodologyoriginalldyescribedby Ames etal(1975)and Maron and Ames (1983).Thismethodologyhasbeenshown todetecta widerangeofclasseosfchemical mutagens.Intheplateincorporatiomnethodology,thetestarticlteh,etestesrtraiannd theS9 mix (whereappropriatew)ere combinedinmoltenagarwhich was overlaiodntoa minimalagar plate.Followingincubatioant37 2*C for48 8 hr,revertanctoloniewserecounted.All dosesofthetestarticlet,hevehiclecontrolasnd thepositivceontrolwsereplatedintriplicate. C. PlatingProcedures These procedureswere usedinboththedose rangefindinsgtudyand the mutagenicitayssay. Each platewas labeledwitha code which identifietdhetestarticlet,estphase,testesrtrain, activatiocnonditionand dose.The S9 mix and dilutionosfthetestarticlweere prepared immediatelypriortotheiurse. CHV StudyNo.: 17073-0-409 17 CORNINGHazleton When S9 mix was notrequire1d0,0Aloftestesrtraiannd50 Alofvehicloertesatrticdloese was added to2.5 ml ofmolten selectivteop agar(maintainedat45 2 OC). When S9 mix was required,500 pLIof S9 mix, 100 gloftesterstrainand 50 ;ilof vehicleor testarticledose was added to2.0 ml of molten selectivteop agar. Aftertherequiredcomponents had been added, the mixturewas vortexedand overlaidontothe surfaceof 25 ml ofminimal bottom agarcontainedin a 15 x 100 mm petridish.Aftertheoverlayhad solidifietdh,eplateswere invertedand incubatedfor48 8 hrat37 2 *C. Positivecontrolarticlewsere platedusinga 50 glplating aliquot. D. Scoring the Plates Plateswhich were not evaluatedimmediatelyfollowingtheincubationperiod were heldat5 3 *C untilsuch time thatcolony countingand bacteriablackground lawn evaluationcould takeplace. I. BacterialBackeround Lawn Evaluation The conditionofthe bacteriablackground lawn was evaluatedfor evidenceof cytotoxicitaynd testarticlperecipitateE.vidence ofcytotoxicitwyas scoredrelative tothe vehiclecontrolplateand was recordedalong withtherevertanctounts forallplatesatthat dose on the datatablesusing thecode system presentedatthe end of the Materialsand Methods Section. 2. -CountiniRzevertantColonies The number ofrevertanctoloniesper plateforthe vehiclecontrolsand all platescontainingtestarticlweere countedmanually. The number of revertantcoloniesperplate forthe positivecontrolswere countedby automated colonycounter. E. Analysis-ofData For allreplicateplatingst,he mean revertantpser plateand the standarddeviation were calculated.The resultsofthesecalculationasrepresentedintabularform intheData TablesSectionof thisreport. EVALUATION OF TEST RESULTS Before assaydatawere evaluated,thecriterifaora validassayhad tobe met. CHV Study No.: 17073-0-409 18 CORNINGHazleton A. CriterFioarA ValidAssay Thefollowicnrgiterwieareusedtodetermianevaliadssay: I TesterStrainInteg[ity:Salmonella typhimurium a. rfaWall Mutation To demonstrate thepresence of therfawall mutation,testerstrain cultureesxhibitedsensitivittoycrystavliolet. b. PKMIOI Plasmid To demonstratethepresenceof theR-factorplasmid,pKM 101, cultureosftesterstrainTsA98 and TA 100 exhibitedresistancteo ampicillin. C. CharacteristNiucmber of SpontaneousRevertants To demonstratetherequirementforhistidinet,hetestesrtrain culturesexhibiteda characteristniucmber ofspontaneousrevertantpserplatewhen platedalong withthevehicleunder selectivceonditionsT.he acceptablerangesforthevehiclecontrolswere as follows: TA98 8 - 60 TAIOO 60 - 240 TA1535 4 - 45 TA1537 2 - 25 2. TesterStrainIntegrity:Escherichiacoli a. CharacteristNiucmber of SpontaneousRevertants To demonstratetherequirementfortryptophan,thetesterstrain cultureexhibiteda characteristniucmber of spontaneousrevertantpserplatewhen platedalong withthevehicleunder selectivceonditions.The acceptablerangeforWP2uvrA was 5 to 40 revertantpserplate. 3. JesterStrainCultureDenjily To demonstratethatappropriatneumbers of bacteriareplated,thedensity oftesterstraincultureswere greaterthanor equalto0.5x 10"bacteripaerml and/orhad reached CHV StudyNo.: 17073-0409 19 CORNINGHazleton atargelteveolfturbididteymonstratteopdroducceulturweisthadensitgyreattehranorequatlo 0.5x 10'bacteripaer mi. 4. PositiveControlValues a. PositiveControlValuesintheAbsence of S9 Mix To demonstratethatthetestesrtrainwsere capableof identifyinag mutagen,themean valueof a positivecontrolfora respectivteestesrtrainexhibitedatleasta 3-foldincreaseover themean valueofthevehiclecontrolforthatstrain. b. PositiveControlValues inthePresenceof S9 Mix (S9Mix Integrity) To demonstratethattheS9 mix was capableof metabolizinga promutagen to itsmutagenicform(s),themean valueof thepositivceontrolfora respective testerstraininthepresenceof theS9 mix exhibitedatleasta 3-foldincreaseover themean value ofthevehiclecontrolforthatstrain. An acceptablepositivecontrolinthepresenceof S9 fora specifisctrainwas evaluatedas having demonstratedboththeintegritoyftheS9 mix and theabilitoyfthetestesrtrainto detecta mutagen. 2. czotoxiciiy A minimum ofthreenon-toxicdoseswere requiredto evaluateassaydata. B. CriteriaFor A PositiveResponse Once thecriterifaora validassayhad been met,responsesobservedintheassay were evaluatedas follows: I. TesterStrainsTA98.TA 100.and WP2uvrA For a testarticlteo be consideredpositivei,thad toproduceatleasta 2-foldincreasein themean revertantpserplateofatleastone of thesetesterstrainosverthe mean revertantpserplateoftheappropriatveehiclecontrol.Thisincreaseinthemean number of revertantpserplatehad tobe accompanied by a dose responsetoincreasingconcentrationosf the testarticle. CHV StudyNo.: 17073-0409 20 CORNINGHazleton 2. 1TAI537 For a testarticlteobe consideredpositivei,thad toproduceatleasta 3-foldincreaseinthemean revertantpserplateofatleastone ofthesetestesrt-aimoverthe mean revertantpserplateoftheappropriatveehiclecontrol.Thisincreasienthemean number of revertantpserplatehad tobe accompaniedby a dose responsetoincreasincgoncentrationosfthe testarticle. RECORDS TO BE MAINTAINED Allraw data,documentationr,ecordst,heprotocola,nd thefinalreportgeneratedasa resulotf thisstudywillbe archivedinthestoragefacilitioefsComing HazletonInc.,foratleastone year followingsubmissionofthefinalreportotheSponsor.Aftertheone yearperiod,theSponsor may electohavetheaforementionemdaterialrsetaineidnthestoragefacilitioefsComing HazletonInc.,foran additionapleriodoftimeorsenttoa storagefacilitdyesignatebdy the Sponsor. REFERENCES Ames, B.N.,J.McCann, and E.Yamasaki. Methods fordetectincgarcinogenasnd mutagens withtheSalmonella/Mammalian-MicrosomMeutagenicitTyest.MutationResearch 3-L:347-36(41975). BrusickD,.J.,V. F.Simmon, H. S. Rosenkranz,V. A. Ray,andR. S.Stafford. An evaluatioonftheEscherichicaoliWP2 and WP2uvrA reversemutationassay. MutationResearch76:169-190(1980). Green,M.H.L. and W. J.Muriel.Mutagen testinugsingirp'reversioinnEscherichicaoli. MutationResearch31:3-32 (1976). Maron, D.M.,and B. Ames. RevisedMethods fortheSalmonellaMutagenicitTyest. MutationResearchM: 173-215(1983). Vogel,H.J.,andD.M. Bonner.AcetylomithinaosfeE. coli:Partiaplurificatiaonnd some propertieJs.Biol.Chem. M:97-106 (1956). CHV StudyNo.: 17073-0-409 21 CORNINGHazleton BACTF,RIALBACKGRO EVALUATION CODE Theconditiooftnhebackgroubnadcterliaawlnisevaluatbeodthmacroscopicaanldly microscopical(luysinga dissectinmgicroscope)forindicatioonfscytotoxiciatnyd testarticle precipitaatsefollows: CODE DEFMTION CHARACTERISTICS OF BACKGROUND LAWN I Normal A healthymicrocolonylawn. 2 Slightly A noticeabltehinninogfthemicrocolonylawn and an Reduced increaseinthesizeofthemicrocoloniecsompared tothe vehiclecontropllate. 3 Moderately A marked thinninogfthemicrocolonylawn and an Reduced increaseinthesizeofthemicrocoloniecsompared tothe vehiclecontrolplate. 4 Extremely An extremethinningofthemicrocolonylawn and an Reduced increaseinthesizeofthemicrocoloniecsompared tothe vehiclecontrolplate. 5 Absent A completelackofanymicrocolonylawn. 6 Obscured by The backgroundbacterial]awn cannotbe accurately Precipitate evaluatedue tomicroscopicand/ormacroscopictest articlperecipitate. Evidenceofmacroscopictestarticlperecipitaotne theplatesisrecordedby additionofthe followingprecipitatceodetothecodenumber usedtoevaluatteheconditioonfthebackground bacterial]awn. SP Slight Noticeablemacroscopicprecipitaotne theplate, Precipitate however,theprecipitadtoees notinfluenceautomated countingoftheplate. MP Moderate The amount ofmacroscopicprecipitaotne theplate Precipitate would interferweithautomatedcountingt,husrequirintghe platetobe hand counted. hp Heavy The largeamount ofmacroscopicprecipitatoen the Precipitate platemakes therequiredhand countingdifficult. Example:4mp would indicataeplateobservedtohavean extremelyreducedbackgroundlawn which had tobe countedmanuallydue tothemarked amount ofmacroscopictestarticle precipitate. CHV StudyNo.: 17073-0-409 22 CORNINGHazleton SECTION IV.RESULTS AND CONCLUSIONS CHV StudyNo.: 17073-0409 23 CORNINGHazieton RESULTS A. TestArticHlaendha ThetesatrticTl-e6,342w,asstoraetdroomtemperatuDrei.onizweadte(rCHV Lot326)was usedasthevehicle.At 100mg perml,which was themost concentratesdtock dilutiopnreparedt,hetestarticlfeormeda clearc,olorlesssolutionT.he testarticlreemaineda solutioinnallsucceedingdilutionpsreparedforthemutagenicitayssay. B. Dose RangefindingStudy Doses tobe testedinthemutagenicitayssaywereselectebdasedon theresultosf thedoserangefindinsgtudyconductedon thetestarticluesingtestesrtrainTsA 100 and WP2uvrA inboththepresenceand absenceofS9 mix (oneplateperdose).Ten dosesoftest articlfer,om 5,000to6.67gg perplatew,ere testedand theresultasrepresentedinTablesI and 2. These datawere generatedinExperiment17073-AI.No cytotoxicitwyas observedineither thepresenceorabsenceof S9 mix as evidencedby anormal backgroundlawn and no decreasein thenumber ofrevertantpserplate. C. Mutageniciiy Assay The mutagenicityassayresultfsorT-6342 arepresentedinTables3 and 4. These datawere generatedinExperiment17073-B1. The dataarepresentedasmean revertantpser plate standardeviatiofnoreachtreatmenatnd controglroup(Table4 )and asindividuapllate counts(Table3). The resultosf thedose rangefindinsgtudywere usedtoselecftivedosestobe testedinthe mutagenicitayssay.The dosestestedwere 5,000,3,330,1,000,333,and 100 gg perplateinboth thepresenceand absenceof S9 mix. InExperiment17073-BI (Tables3 and 4),alldatawere acceptablaend no positiviencreaseisn thenumber ofrevertantpserplatewere observedwithany ofthetestesrtrainesitheirnthe presenceor absenceof S9 mix. Allcriterfioara validstudyweremet. CHV StudyNo.: 17073-0-409 24 CORNINGHazieton CONCLUSIONS T'heresultosftheSalmonella-Eschericchoilai/Mammalian-MicrosoRmeverseMutationAssay indicattehatu,ndertheconditionosfthisstudy,3M CorporatioetsestarticlTe-,6342,didnot causea positiviencreaseinthenumber of revertantpserplateofany ofthetestesrtrainesitheirn thepresenceorabsenceofmicrosomalenzymes preparedfromAroclorTm-inducerdatliver(S9). CHV StudyNo.: 17073-0-409 25 CORNINGHazleton SECTION V. DATA TABLES CHV Study No.: 17073-0-409 26 CORNINGHazieton TABLE I DOSE RANGEPINDING TEST ARTICLE ID: T-6342 EXPERIMENT ID: 17073-Al VEHICLE: Deionized water STUDY DATE PLATED: DATE COUNTED: 12-Sep-95 15-Sep-95 pg/PLATE REVERTANTS PER PLATE WITH TAIOO REVERTANTS S9 BACKGROUND LAWN EVALUATION* PER PLATE WITHOUT S9 REVERTANTS BACKGROUND PER LAWN PLATE EVALUATION* 0.00 (Vehicle) (50 pi) 127 1 Test Article 6.67 103 1 10.0 100 1 33.3 85 1 66.7 120 1 100 112 1 333 138 667 107 1 1000 119 1 3330 ill 1 5000 118 1 93 1 87 1 81 1 77 1 105 1 98 1 113 1 97 1 79 1 107 1 92 1 Background Lavn Evaluation I - nor-%al 4 - extremely reduced op - &light precipitate Codes: 25up - slightly reduced absent moderate precipitate (requires hand count) 3 - moderately reduced 6 - obscured by precipitate hp - heavy precipitate (requires hand count) CHV Study No.: 17073-0-409 27 CORNINGHazieton TABLE 2 DOSE RANGEPINDING TEST ARTICLE ID: T-6342 EXPERIMENT ID: 17073-Al VEHICLE: Deicnized water STUDY DATE PLATED: DATE COUNTED: 12-Sep-95 15-Sep-95 pg/PLATE REVERTANTS PER PLATE WP2uvrA REVERTANTS WITH S9 BACKGROUND LAWN EVALUATION* PER PLATE WITHOUT S9 REVERTANTS BACKGROUND PER LAWN PLATE EVALUATION* 0.00 (Vehicle) (50 pl) 16 1 Test Article 6.67 24 1 10.0 19 1 33.3 11 1 66.7 12 1 100 23 1 333 20 1 667 8 1 1000 14 1 3330 20 1 5000 18 1 20 1 11 1 16 1 11 1 12 1 24 1 23 1 15 1 19 1 21 1 Background Lawn Evaluation I nor@al 4 extremely reduced op slight precipitate Codes: 2 5 op - slightly reduced - absent - moderate precipitate (requires hand count) 3 - moderately reduced 6 - obscured by precipitate hp - heavy precipitate (requires hand count) CHV Study No.: 17073-0409 28 CORNINGHazieton TEST ARTICLE ID: T-6342 EXPERIMENT ID: 17073-Bl DATE PLATED: 19-Sep-95 DATE COUNTED: 22-Sep-95 TABLE 3 MUTAGENICITY ASSAY INDIVIDUAL PLATE RESULTS COUNTS VEHICLE: Deionizod vater PLATING ALIQUOT: 50 lil REVERTANTS PER PLATE DOSE/ZLATE MICROSOMES: Rat Liver VEHICLE CONTROL TA90 1 2 3 11 25 24 -TAIOO 1 2 3 127 113 128 TA153S 1 2 3 13 15 7 TA1537 1 2 3 la 9 7 TEST ARTICLE POSITIVE CONTROL 100 jig 333 pg 1000 PS 3330 pg 5000 ps 30 36 38 30 27 28 29 34 26 38 31 34 23 19 is 848 995 810 109 115 121 114 III 114 128 123 119 108 112 111 ill IIB 126 16 13 11 5 21 14 13 17 9 13 14 11 15 10 12 926 953 999 110 108 122 6 12 8 7 5 10 10 3 9 10 11 5 10 7 6 107 122 108 WP2uvrA 1 2 BACXGROUND LAW' 3 20 19 19 1 30 14 17 1 IS 21 15 1 12 14 13 1 15 16 16 1 20 29 24 1 201 271 163 1 MICROSOMES: None VEHICLE CONTROL TEST ARTICLE POSITIVE CONTROL 100 pg 333 pg 1000 ps 3330 pg 5000 ps 14 12 13 19 19 10 11 21 17 12 19 14 10 16 15 20 17 9 129 154 156 90 86 86 97 $a 107 103 107 100 104 91 97 82 97 98 92 72 48 841 817 861 7 5 6 5 8 5 13 13 19 6 9 17 6 6 9 9 16 9 582 599 556 7 a 1 3 7 7 10 7 23 5 10 4 4 6 4 12 9 6 202 224 218 10 15 is 1 26 11 15 1 18 15 17 1 27 18 24 1 9 22 19 1 10 16 17 1 39 45 76 2 TA98 TAIOO TAIS35 TAIS37 WP2uvrA 2-aminoanthrac*ne 2-"Inoanthracens 2-aminoanthcacens 2-aminaenthracens 2-aminoanthr&4cono 2.5 2.5 2.5 2.3 25.0 VS/plate pg/p2ate pg/plate Mg/plato pg/plate ... TA98 TAIOO TA1335 TA1337 WP2uvrA 2-nitrefluarone sodium aside sodium aside ZC]t-191 4-nitroquinaline-N-oxide 1.0 pa/plate 2.0 pg/p2at* 2.0 pg/plate 2.0 pa/plate 1.0 Mg/plate Background Lawn Evaluation I - normal 4 - extremely reduced op I slight precipitate Codes: 2 - slightly reduced 5 - absent op - moderate precipitate (requires hand count) 3 - moderately reduced 6 - oucured by precipitate hp - heavy precipitate (requires hand count) CHV StudyNo.: 17073-0-409 29 CORNINGHazleton TABLE 4 MUTAGENICITY ASSAY SUMMARY RESULTS TEST ARTICLE ID: T-6342 F"ERIMENT ID: 17073-BI DATE PLATED: 19-Sep-95 VEHICLE: Dsionized water DATE COUNTED: 22-Sep-95 PLATING ALIQUOT: 50 pl MM REVERTANTS PER PLATS WITH STANDARD DEVIATION DOSE/Pbm MICROSOMES: Rat Liver VEHICLE CONTROL TA98 MEAN S.D. 20 a TA100 MEAN S.D. 117 2 Tkl535 MEAN S.D. 12 4 TA1537 MEAN S.D. 9 2 TEST ARTICLE 100 ps 333 pg 1000 ps 3330 yg 5000 ps 35 4 28 2 30 4h 34 4 20 3 112 3 Ila 4 114 4 123 5 Ila 9 13 3 11 3 13 4 13 2 12 3 9 3 7 3 7 4 9 3 a2 POSITIVE CONTROL 864 99 923 32 113 8 112 a HICROSOMES: None VEHICLE CONTROL TEST ARTICLE POSITIVS CONTROL 100 og 333 pg 1000 P& 3330 pg 5000 ps 13 1 16 5 16 5 15 4 14 3 is 6 146 15 87 2 97 10 203 4 97 7 92 9 84 11 $40 22 6 1 6 2 15 3 11 5 7 2 11 4 579 22 5 4 6 2 10 3 6 3 5 1 9 3 215 11 WP2uvrA MEAN S.D. BACKGROUND LAWN' 19 1 1 20 9 1 17 3 1 13 1 1 16 1 1 24 5 1 178 20 1 14 4 1 17 a 1 17 2 1 23 3 1 17 7 1 14 4 1 53 20 1 TA90 TAIOO TAIS33 TAIS37 WP2uvrA 2-amincenthracene 2-aminaenthracene 2-sainoanthrac*ne 2-aminoonthracene 2-aminoanthracens 2.5 2.5 2.5 2.5 23.0 pS/plate pg/plate pt/plate p$/plate p&/plate ... TA98 TAIOO TA2533 TA1337 WP2uvrA 2-nitrofluorens sodium aside sodium azide ICR-191 4-nitroquinalina-M-axido 1.0 ps/plato 2.0 pa./plate 2.0 pg/plate 2.0 pa/plate 1.0 pg/plate Background Lawn Evaluation 1 - normal 4 m extremely reduced ap m slight precipitate Codes: 2 - slightly reduced 5 - absent up - moderate precipitate (requires hand count) 3 - moderately reduced 6 m obscured by precipitate hp - heavy precipitate (requires hand count) CHV StudyNo.: 17073-0-409 30