:1672—2019(2007)08—0646—04CYP3A4和CYP2B6药物诱导剂体外筛选体系的建立胡东莉,王果,李智,范岚,谭志荣,王丹,周宏灏(中南大学临床药理研究所,湖南长沙410078)?论着?摘要:,将表达载体和报告载体共转染HepG2细胞,,:hPXR;CYP3A4;CYP2B6;荧光素酶报告基因;诱导剂中图分类号::AEstablishmentofinvitroscreeningsystemforCYP3A4andCYP2B6inducersHUDong—li,WANGGuo,LIZhi,FANLan,TANZhi—long,WANGDan,ZHOUHong-hao(InstituteofClinicalPharmacology,CentralSouthUniversity,Changsha,Hunan410078,)Abstract:【0bjeetive】ToestablishaninvitrosystemtoscreendruginducersofCYP450enzymes.【Method】ClongingthepromotersofCYP3A4andCYP2B6whichcontainedtheelementsthathPXR,akindofnuclearrecep-tor,canrecognizeandbind,andinsertingthetrans—elementtotheupstreamoffireflyluciferaserepo~,Co—transfectingthereportvectorandhPXRexpressionvectortoHepG2cellline,andanalyzingluciferaseactivityafterthecelltreatedwithrifampinorDMSO.【Result】ThefoldactivationvalueofluciferaseofrifampingroupwasstatisticallydifferentfromcontrolgroupandDMSOgroup.【Conclusion】essfullyestab—:humanP
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