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1、ComparisonofInhibitionCapabilityofScutellareinandScutellarinTowardsImportantLiverUDPGlucuronosyltransferase(UGT)isoforms汇报人：..2015.03.18Keywordsscutellarin;scutellarein;UGT;enzymeinhibition.Contents1.Introduction2.Experimentalsection3.Resultsanddiscussion4
2、.Conclusion1.IntroductionIntherecentyears,anotherimportantdrugmetabolizingenzymeUDP-glucuronosyltransferase(UGT)hasbeendemonstratedtoexhibitsignificantcontributiontowardsthemetabolismofclinicaldrugsandherbalcomponents,andmoreandmoreattentionhasbeengiventot
3、hisenzymes(MalikandBlack,2012;Lietal.,2012).UGTshavebeendemonstratedtobeinvolvedinthemetaboliceliminationofmanyimportantendogenoussubstances,suchasbilirubin,bileacidandestradiol(Erichsenetal.,2010).Guoetal.showeddeglycosylationprocessofliquiritinstronglyen
4、hancedtheinhibitorycapabilitytowardsUGTs(2012).Huangetal.showedstronginhibitionofglycyrrhetinicacidtowardsUGT1A3and2B7(2012).Liuetal.alsousedinvitroincubationsystemtofindthestronginhibitionofdeoxyschizandrinandschisantherinAtowardsUGT1A3(2012).Chemicalsand
5、reagents.Scutellarin,Scutellarein,4-MU,Tris-HCl,7-hydroxycoumarin,UDPGA(缓冲盐)，重组UGTs亚型（UGT1A1，UGT1A6，UGT1A9，UGT2B7），HPLCreagents.2.ExperimentalsectionIncubationandanalysismethodsforinhibitionevaluation.After5minpre-incubationat37℃,theUDPGAwasaddedinthemixtu
6、retoinitiatethereaction.Theincubationtimewas120minforUGT1A1andUGT2B7,30min,orUGT1A6andUGT1A9,respectively.Thereactionswereterminatedbyadding100mLacetonitrilewith7-hydroxycoumarin(100mM)asinternalstandard.Themixturewascentrifugedat20000×gfor10min,HPLCanalys
7、is.Datafittingfordeterminationofinhibitiontypeandparameters(Ki).Thereactionvelocitywasdeterminedusingvariousconcentrationsof4-MUandscutellarein.ThedatawerefittedusingDixonplotandLineweaver–Burkdoublereciprocalplot.ThesecondplotwiththeslopesfromtheLineweave
8、r–BurkplotversustheconcentrationsofscutellareinwasutilizedtocalculatetheKivalue.Predictionofinvivodrug–druginteractionmagnitude.Predictionofinvivodrug–druginteractionmagnitude.Themostcommonequationfordrug–dru
