人参中皂苷成分的孕烷X受体激动特性筛选  

Screening of pregnane X receptor activation from ginsenosides

作　　者：王宇光[1] 刘浩生[1,2] 张娴勰[1] 肖勇[1] 陆倍倍[1] 马增春[1] 梁乾德[1] 汤响林[1] 肖成荣[1] 谭洪玲[1] 张伯礼[3] 高月[1] 

机构地区：[1]军事医学科学院放射与辐射医学研究所,北京100850 [2]安徽医科大学,安徽合肥230032 [3]天津中医药大学,天津300193

出　　处：《药学学报》2013年第1期144-148,共5页Acta Pharmaceutica Sinica

基　　金：国家"重大新药创制"科技重大专项(2009ZX09501-304);国家重点基础研究发展计划(973计划)项目(2011CB505304;2012CB518402);国家自然科学基金资助项目(81073149);北京市自然科学基金资助项目(7112110)

摘　　要：人参（Panax ginseng C.A.）是常见的补益中药,具有大补元气、复脉固脱、生津养血、安神益智之功效,是中医临床常用中药,在中药复方配伍中也使用广泛。现代药理学研究显示,人参具有抗肿瘤、抗抑郁、抗氧化等活性,其药用价值已为世界公认。人参的主要成分是人参皂苷,约占人参组成的4%,具有抗疲劳、神经保护、延缓衰老、抑制肿瘤细胞生长、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 on CYP3A4 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 μmol.L 1.When the condition of final concentration was 10 μmol.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.

关 键 词：CYP3A4 孕烷X受体 人参皂苷 药物相互作用 

分 类 号：R963[医药卫生—微生物与生化药学]