中国药理学通报Issue(7)：926-930,931,6.DOI:10.3969/j.issn.1001-1978.2014.07.010
银杏内酯B通过激活孕烷X受体诱导CYP3 A4的表达
Ginkgolide B induces CYP3 A4 expression through activation of human pregnane X receptor
摘要
Abstract
Aim To study the induction effect of Ginkgolide B on CYP3A4,and further verify the role of pregnane X receptor in CYP3 A4 induction expres-sion. Methods With different concentrations of Ginkgolide B treatment on LS174T cells,the CYP3A4 mRNA expression was detected by Q-PCR assay,fur-ther PXR-CYP3 A4 stable translation HepG2 cell lines were used to test the effect of Ginkgolide B on activity of PXR by reporter gene screening assay.CYP3A4 protein expression was detected by Western blot.PXR was knocked down with transfected with siRNA, CYP3 A4 mRNA and protein were detected in the con-dition of PXR low expression.Results The results revealed that the level of CYP 3 A 4 gene and protein expression were significantly increased by Ginkgolide B,and there was no induction effect on PXR.Reporter gene screening showed that Ginkgolide B could en-hance the transcriptional activity of PXR in a concen-tration-dependent manner.Under conditions of low ex-pression of PXR ,Ginkgolide B could also increase ex-pression of CYP3A4,but the induction folds were low-er than those of normal PXR group.Conclusion Ginkgolide B can signicantly up-regulate CYP3 A4 ex-pression via the PXR-CYP3 A4 pathway,and it has no effects on PXR gene expression.关键词
银杏内酯B/利福平/细胞色素P450 3A4/孕烷X受体/荧光定量PCR技术/小干涉RNAKey words
Ginkgolide B/rifampicin/cytochrome P450 3A4/pregnane X receptor/quantitative PCR/small interfering RNA分类
医药卫生引用本文复制引用
周涛,高月,王宇光,马增春,肖勇,汤响林,梁乾德,胡东华,肖成荣,谭洪玲..银杏内酯B通过激活孕烷X受体诱导CYP3 A4的表达[J].中国药理学通报,2014,(7):926-930,931,6.基金项目
国家科技部“重大新药创制”科技重大专项（No 2009ZX09501-304）；国家重点基础研究发展计划（973计划）项目（No 2011CB505304，2012CB518402）；国家自然科学基金资助项目 （）
