白花前胡甲素及丙素经hCAR通路诱导UGT1A1的表达  

Induction of UGT1A1 expression by praeruptorin A and praeruptorin C through hCAR pathway

作　　者：周许年[1] 毕惠嫦[1] 金晶[1] 邓蓉蓉[1] 应梦佳[1] 王永涛[1] 黄民[1] 

机构地区：[1]中山大学药学院药物代谢与药动学实验室,广东广州510006

出　　处：《药学学报》2013年第5期794-798,共5页Acta Pharmaceutica Sinica

基　　金：国家"重大新药创制"科技重大专项(2012ZX09506001-004);国家科技支撑计划(2008BAI51B02)

摘　　要：中药前胡为伞形科植物白花前胡（Peucedanum praeruptorumDUNN．）的干燥根，具有宣散风热、降气化痰等功效。其主要活性成分白花前胡甲素（PA）及白花前胡丙素（PC）属于香豆素类化合物，是一对外消旋体。This study is purposed to investigate the effects of praeruptorin A （PA） and praeruptorin C （PC） on UGT1A1 in HepG2 cells through hCAR pathway. PA and PC were incubated with HepG2 cells for 24 h and 48 h, mRNA and protein expressions of UGT1A1 were determined by real-time PCR and Western blotting assays. Additionally, effects of PA and PC on UGT1A1 mRNA and protein expressions were also measured after transient transfection of a specific CAR siRNA for 72 h in HepG2 cells. UGT1A1 mRNA and protein expression levels were significantly increased by PA and PC after incubation for 48 h. Moreover, the mRNA and protein up-regulations of UGT1A1 were attenuated by transient transfection of a specific CAR siRNA, suggesting the induction was mediated by CAR. The results suggest that PA and PC can significantly up-regulate UGT1A1 expression partially via the CAR-mediated pathway.

关 键 词：白花前胡甲素 白花前胡丙素 UGT1A1 CAR 中药-药物相互作用 

分 类 号：R963[医药卫生—微生物与生化药学]