title: [Screening of pregnane X receptor activation from ginsenosides].
abstract: In order to study effects of ginseng on the metabolism of drug belong to CYP3A4 substrate, screening of pregnane X receptor activation from ginsenosides was performed by reporter assay. Based on PXR-CYP3A stable translation cell lines, 13 ginsenosides were screened for pregnane X receptor activation by reporter assays, and RIF as the positive control. The effect of ginsenosides Rg1 onCYP3A4 mRNA expression was also investigated by RT-PCR. The PXR-CYP3A stable translation cell lines had good response to RIF, and the EC50 is 2.51 micro mol x L(-1). When the condition of final concentration was 10 micromol x L(-1), ginsenoside F2 and protopanaxatriol had moderate inductive effects on PXR. Panaxotriol, Rg2, pseudoginsenoside F11, Rg1, ginsenoside and Rb3 had inhibitory effects on PXR. Ginsenoside Rf1, Rg3, Rh2 and protopanaxdiol had no obvious effects on PXR. Rg1 down-regulated CYP3A4 mRNA expression in a concentration-dependent manner. Activation of pregnane X receptor by ginsenosides may influence the metabolism of drug belong to CYP3A4 substrate, and cause ginseng-drug interactions.
authors.affiliation: Beijing Institute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China.
authors.forename: Yu-Guang
authors.initials: YG
authors.lastname: Wang
authors.forename: Hao-Sheng
authors.initials: HS
authors.lastname: Liu
authors.forename: Xian-Xie
authors.initials: XX
authors.lastname: Zhang
authors.forename: Yong
authors.initials: Y
authors.lastname: Xiao
authors.forename: Bei-Bei
authors.initials: BB
authors.lastname: Lu
authors.forename: Zeng-Chun
authors.initials: ZC
authors.lastname: Ma
authors.forename: Qian-De
authors.initials: QD
authors.lastname: Liang
authors.forename: Xiang-Lin
authors.initials: XL
authors.lastname: Tang
authors.forename: Cheng-Rong
authors.initials: CR
authors.lastname: Xiao
authors.forename: Hong-Ling
authors.initials: HL
authors.lastname: Tan
authors.forename: Bo-Li
authors.initials: BL
authors.lastname: Zhang
authors.forename: Yue
authors.initials: Y
authors.lastname: Gao
mesh_terms: D051544:Cytochrome P-450 CYP3A / Q000235:genetics / Q000378:metabolism*; D004347:Drug Interactions; D036145:Ginsenosides / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D000077297:Pregnane X Receptor; D012333:RNA, Messenger / Q000378:metabolism; D011987:Receptors, Steroid / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics; D012502:Sapogenins / Q000494:pharmacology; D014162:Transfection
chemical_list: D036145:Ginsenosides; D000077297:Pregnane X Receptor; D012333:RNA, Messenger; D011987:Receptors, Steroid; D012502:Sapogenins; C407883:ginsenoside F2; C413985:pseudoginsenoside F11; C081552:protopanaxatriol; C026474:ginsenoside Rg2; C044463:ginsenoside Rb3; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human; C035054:ginsenoside Rg1