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- 约3.16千字
- 约 20页
- 2026-02-03 发布于山东
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研究生英文文献汇报演示文稿第一页,共20页。
第二页,共20页。
Keywordsscutellarin;scutellarein;UGT;enzymeinhibition.第三页,共20页。
Contents1.Introduction2.Experimentalsection3.Resultsanddiscussion4.Conclusion第四页,共20页。
1.Introduction第五页,共20页。
Intherecentyears,anotherimportantdrugmetabolizingenzymeUDP-glucuronosyltransferase(UGT)hasbeendemonstratedtoexhibitsignificantcontributiontowardsthemetabolismofclinicaldrugsandherbalcomponents,andmoreandmoreattentionhasbeengiventothisenzymes(MalikandBlack,2012;Lietal.,2012).UGTshavebeendemonstratedtobeinvolvedinthemetaboliceliminationofmanyimportantendogenoussubstances,suchasbilirubin,bileacidandestradiol(Erichsenetal.,2010).第六页,共20页。
Guoetal.showeddeglycosylationprocessofliquiritinstronglyenhancedtheinhibitorycapabilitytowardsUGTs(2012).Huangetal.showedstronginhibitionofglycyrrhetinicacidtowardsUGT1A3and2B7(2012).Liuetal.alsousedinvitroincubationsystemtofindthestronginhibitionofdeoxyschizandrinandschisantherinAtowardsUGT1A3(2012).第七页,共20页。
Chemicalsandreagents.Scutellarin,Scutellarein,4-MU,Tris-HCl,7-hydroxycoumarin,UDPGA(缓冲盐),重组UGTs亚型(UGT1A1,UGT1A6,UGT1A9,UGT2B7),HPLCreagents.2.Experimentalsection第八页,共20页。
Incubationandanalysismethodsforinhibitionevaluation.After5minpre-incubationat37℃,theUDPGAwasaddedinthemixturetoinitiatethereaction.Theincubationtimewas120minforUGT1A1andUGT2B7,30min,orUGT1A6andUGT1A9,respectively.Thereactionswereterminatedbyadding100mLacetonitrilewith7-hydroxycoumarin(100mM)asinternalstandard.Themixturewascentrifugedat20000×gfor10min,HPLCanalysis.第九页,共20页。
Datafittingfordeterminationofinhibitiontypeandparameters(Ki).Thereactionvelocitywasdeterminedusingvariousconcentrationsof4-MUandscutellarein.ThedatawerefittedusingDixonplotandLineweaver–Burkdoublereciprocalplot.Thesecondplotwiththeslo
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