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会计学Keywordsscutellarin;scutellarein;UGT;enzymeinhibition.Contents1.IntroductionIntherecentyears,anotherimportantdrugmetabolizingenzymeUDP-glucuronosyltransferase(UGT)hasbeendemonstratedtoexhibitsignificantcontributiontowardsthemetabolismofclinicaldrugsandherbalcomponents,andmoreandmoreattentionhasbeengiventothisenzymes(MalikandBlack,2012;Lietal.,2012).UGTshavebeendemonstratedtobeinvolvedinthemetaboliceliminationofmanyimportantendogenoussubstances,suchasbilirubin,bileacidandestradiol(Erichsenetal.,2010).Guoetal.showeddeglycosylationprocessofliquiritinstronglyenhancedtheinhibitorycapabilitytowardsUGTs(2012).Huangetal.showedstronginhibitionofglycyrrhetinicacidtowardsUGT1A3and2B7(2012).Liuetal.alsousedinvitroincubationsystemtofindthestronginhibitionofdeoxyschizandrinandschisantherinAtowardsUGT1A3(2012).Chemicalsandreagents.Scutellarin,Scutellarein,4-MU,Tris-HCl,7-hydroxycoumarin,UDPGA(缓冲盐)，重组UGTs亚型（UGT1A1，UGT1A6，UGT1A9，UGT2B7），HPLCreagents.Incubationandanalysismethodsforinhibitionevaluation.After5minpre-incubationat37℃,theUDPGAwasaddedinthemixturetoinitiatethereaction.Theincubationtimewas120minforUGT1A1andUGT2B7,30min,orUGT1A6andUGT1A9,respectively.Thereactionswereterminatedbyadding100mLacetonitrilewith7-hydroxycoumarin(100mM)asinternalstandard.Themixturewascentrifugedat20000×gfor10min,HPLCanalysis.Datafittingfordeterminationofinhibitiontypeandparameters(Ki).Thereactionvelocitywasdeterminedusingvariousconcentrationsof4-MUandscutellarein.ThedatawerefittedusingDixonplotandLineweaver–Burkdoublereciprocalplot.ThesecondplotwiththeslopesfromtheLineweaver–BurkplotversustheconcentrationsofscutellareinwasutilizedtocalculatetheKivalue.Predictionofinvivodrug–druginteractionmagnitude.Predictionofinvivodrug–druginteractionmagnitude.Themostcommonequationfordrug–druginteractionpredictionwasemployedtopredicttheAUCalterationofcoadministereddrugscausedbyco-administrationofscutellarein.3.Resultsanddiscussion图2表明，100mM野黄芩苷对UGT1A1，UGT1A6，UGT1A9，UGT2B7的活性抑制率分别为48.8%、20.
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