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:1000-8020(2009)01-0111-03··房军 杜顺晶综述 金银龙审校, 100021:熊果苷 生理活性 细胞毒性 致突变 化妆品:TQ658 :A:,,,: (Arbutin),[CASNo.497-76-7]4--β-D-,、、、,———。[1],,(tyrosinase),,,,,,,。2090,,,,。,,,。1 ,、、、,、、,:198～201℃,,。,αβ,4--α-D-、4--β-D-。:C12H16O7,:272.25,:,β-、。α-,(hydroquinone,HQ)[CASNo.123-31-9]α-。2 2.1 ,,(Melanin)。(※)(※),[2]。,,,,。。,100mgml。,520%,[3,4]。。NAKAJIMA,0.5～8mmolL,[5],。,。α-β-,4--α-D-。α-,40%,[6],α-β-10[7]。2.2 ECV2304,H2O2ECV2304[8]。3 ,,,。,,。D-HQ[9],HQ。,HQ,HQ,HQ,。3.1 ,,,,。,、、、。,、,、、,,。,38 12009 1 JOURNALOFHYGIENERESEARCH Vol.38 No.1Jan. 2009111 ,。,。3.2 、,。JAHDODARWistar,,1630,,82%100%,90.7%[9]。DEISINGER,HQ,HQ(HQ),,5;HQ,12。HQ,HQ[10]。QUINTUA2005(),、。4。75%24[11]。SCHINDLER,64.8%HQ,66.7%。,Cmax=1.68931.1250mmolml;Tmax=3.604.40h;103.3%。,HQ、、[12]。3.3 3.3.1 ,,,。3.3.1.1 1998CHAKRABORTY,100μgml(0.367mmolL),,300μgml(1.10mmolL)5,48,[13]。。,β-,,[14]。,β-,β-[14]。β-3%,,,,。,VC、VC、HQ、,,[15]。、、BL-99,4,BL-99,70μgml[16]。,,,;3,[17]。3.3.1.2 ITABASHISD,SD,,25、100400mgkg(0.092、0.3671.47mmolkg),100mgkg[18]。3.3.1.3 1996MULLERV79,0.01molL(2.73mgml);β-,≥1mmolL0.3mgml,[19]。β-HQ。2006MICHAEL,,9,2mmolL,HQ[20]。,,(Eubacteriumramulus)、(Enterococcuscasseliflavus)、(Bacteroidesdistasonis)(Bifidobacteriumadolescentis),,21.08、16.62、8.433.59nmol×min-1×(mgprotein)-1。,,,0.500.09nmol(min·mgprot)。MICHAELV79,(E.ramulus)(B.distasonis),β-[20]。β-HQ,。3.3.2 3.3.2.1 ,,、、,,。1988EastmanKodakHQ,F344,HQ25mgkg150mgkg,24,。,HQ。AlbinoDunkin-Hartley,2.0%HQ,0.5%HQ100%,HQ;LLNAHQ[21]。3.3.2.2 ,HQ,。EASTMONDPIROZZIC57BL6、B6C3F1、DBA2,HQ,()[22,23]。KINGHQB[24]。112 383.3.2.3 、 ,HQ、,,HQ。KARIF344NB6,2,25100mgkg。HQ,。HQ,,[25]。3.3.2.4 ,HQ、、、。FISHHQHL6079,57。,CD+34CD-34HQ,CD+34CD-19,HQ75831,8[26,27]。,HQ。3.3.2.5 ,HQ(25、50100mgkg)F344,F344,B6C3F1,,[28]。,HQAmes,(CHO),HQ(S9)(S9);l5178ytk,HQ[28]。,,,,,,。1 ,,.[J].,2004,39(4):266-268.2 IOZUMIK,HOGANSONGE,PENNELLAR.Roleoftyrosinaseasthedeter2minantofpigmentationinculturedhumanmelanocytes[J].JInvestDermatol,1993,100(6):806-811.3 ,,.[J].,2001,22(20):1486-1488.4 CHAKRABORTYAK,FUNAENKAY,KOMOTOM,etal.Effectofarbutinonmelanogenicproteinsinhumanmelanocytes[J].PigmentCellRes,1998,11(4):206-212.5 NAKAJIMAM,SHINODAI,FUKUWATARIY,etal.Arbutinincreasesthepigmentationofculturedhumanmelanocytesthroughmechanismsotherthantheinductionoftyrosinaseactivity[J].PigmentCellRes,1998,11(4):12-17.6 SUGIMOTOK,NISHIMURAT,NOMURAK,etal.Inhibitoryeffectsofalpha-arbutinonmelaninsynthesisinculturedhumanmelanocytescellsandathree-dimensionalhumanskinmodel[J].BioPharmBull,2004,27(4):510-514.7 FUNAYAMAM,ARAKAWAH,YAMAMOTOR,etal.Effectsofalphaandbetaarbutinonactivityoftyrosinasefrommushroomandmousemelanoma[J].BioeciBiotechnolBiochem,1995,59(1):143-144.8 ,,,.H2O2[J].,2005,8(2):241.9 JAHDODARL.Eliminationofarbutinfromtheorganism[J].Pharmazie,1983,38(11):780-781.10 DEISINGERPJ.Humanexposuretonaturallyoccurringhydroquinone[J].ToxicolEnvironHealth,1996,47(1):31-46.11 QUINTUAJ,KOVARKA,LINK,etal.Urinaryexcretionofarbutinmetabolitesafteroraladministrationofbearberryleafextracts[J].PlantaMed,2005,71(2):147-152.12 SCHINDLERG,PATZAKU,BRINKHAUSB,etal.UrinaryexcretionandmetabolismofarbutinafteroraladministrationofArctostaphylosuvaeursiextractasfilm-coatedtabletsandaqueoussolutioninhealthyhumans[J].JClinPharmacol,2002,42(8):920-927.13 CHAKRABORTYAK.Effectofarbutinonmelanogenicproteinsinhumanmelanocytes[J].PigmentCellRes,11(4):206-212.14 ,,,.[J].,2004,26(5):313-316.15 ,,.[J].,2005,26(2):72-75.16 ,,.4[J].,2006,28(2):114-116.17 ,.[J].,2005,35(6):361-363.18 ITABASHIM.Reproductivestudieswitharbutininratsbysubcutaneousadministration(Jpn.)[J].IyakuhinKenkyu,1988,19(2):282-297.19 MULLERL,KASPERP.Themutagenicpotentialofarbutine,anaturallyoccurringhydroquinoneglycoside[J].MutatRes,1996,360(3):291-292.20 MICHAELB.Mutagenicityofarbutininmammaliancellsafteractivationbyhumanintestinalbacteria[J].FoodandChemicalToxicol,2006,44:1940-1947.21 CosmeticIngredientReview(CIR).Addendumtothefinalreportonthesafetyassessmentofhydroquinone[J].JAmCollegeToxicol,1994,13(3):167-230.22 EASTMONDDA.Aninteractionofbenzenemetabolitesreproducesthemyelotoxicityobservedwithbenzeneexposure[J].ToxicolApplPharmacol,1987,91:85-95.23 PRROZZISJ.Preventionofbenzene-inducedmyelotoxicityandprostaglandinsynthesisinbnemarrowofmicebyinhibitorsofprostaglandinHsynthase[J].ImmunoPharmacol,1989,18:39-55.24 KINGAG.Hydroquinoneinhibitsbonemarrowpre-Bcellmaturationinvitro[J].MolPharmacol,1987,32:807-812.25 KARIFW.ToxicityandcarcinogenicityofHydroquinoneinF344NratsandB6C3F1mice[J].FoodChemToxicol,1992,30:737-747.26 SMITHMT.Hydroquinone,abenzenemetatabolite,increasesthelevelofaneusomyofchromosomes7and8inhumanCD34-positivebloodprogenitorcells[J].Carcinogenesis,2000,21(8):1485-1490.27 WAYNESS.Thebenzenemetabolite,hydroquinone,selectivelyinduces5q31-and-7inhumanCD34+CD19-bonemarrowcells[J].ExperimentalHematol,2000,28:169-176.28 NTP(NationalToxicologyProgram).ToxicologyandcarcinogenesisstudiesofhydroquinoneinF344NratsandB6C3F1mice[R].TechRep,1989,366.:2008-10-031,.113