The inhibitory effect of intestinal bacterial metabolite of ginsenosides on CYP3A activity

	The inhibitory effect of intestinal bacterial metabolite of ginsenosides on CYP3A activity
	Liu, Y ; Li, W ; Li, P ; Deng, MC ; Yang, SL ; Yang, L
刊名	biological & pharmaceutical bulletin
	2004-10-01
卷号	27 期号:10 页码:1555-1560
关键词	ginseng-drug interaction intestinal bacterial metabolite ginsenoside CYP3A
产权排序	1;1
英文摘要	the intestinal bacterial metabolites of ginsenosides are responsible for the main pharmacological activities of ginseng. the purpose of this study was to find whether these metabolites influence hepatic metabolic enzymes and to predict the potential for ginseng-prescription drug interactions. utilizing the probe reaction of cyp3a activity, testosterone 6beta-hydroxylation, the effects of derivatives of 20(s)-protopanaxadiol and 20(s)-protopanaxatriol families on cyp3a activity in rat liver microsomes were assayed. our results showed that ginsenosides from the 20(s)-protopanaxadiol and 20(s)-protopanaxatriol family including rb-1, rb-2, rc, compound-k, re, and rg(1), had no inhibitory effect, whereas rg(2), 20(s)-panaxatriol and 20(s)-protopanaxatriol exhibited competitive inhibitory activity against cvp3a activity in these microsomes with the inhibition constants (k) of 86.4+/-0.8mum, 1.7+/-0.1mum, and 3.2+/-0.2 mum, respectively. this finding demonstrates that differences in their chemical structure might influence the effects of ginsenosides on cyp3a activity and that ginseng-derived products might have potential for significant ginseng-drug interactions.
WOS标题词	science & technology ; life sciences & biomedicine
类目[WOS]	pharmacology & pharmacy
研究领域[WOS]	pharmacology & pharmacy
关键词[WOS]	in-vitro ; drug-interactions ; liver-microsomes ; ginseng saponins ; rat-liver ; cytochrome-p450 ; absorption ; excretion ; toxicity ; enzymes
收录类别	SCI
原文出处	true
语种	英语
WOS记录号	WOS:000224522100013
公开日期	2010-11-30
内容类型	期刊论文
源URL	[http://159.226.238.44/handle/321008/80971]
专题	大连化学物理研究所_中国科学院大连化学物理研究所
作者单位	1.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China 2.Chinese Acad Sci, Grad Sch, Dalian 116023, Peoples R China
推荐引用方式 GB/T 7714	Liu, Y,Li, W,Li, P,et al. The inhibitory effect of intestinal bacterial metabolite of ginsenosides on CYP3A activity[J]. biological & pharmaceutical bulletin,2004,27(10):1555-1560.
APA	Liu, Y,Li, W,Li, P,Deng, MC,Yang, SL,&Yang, L.(2004).The inhibitory effect of intestinal bacterial metabolite of ginsenosides on CYP3A activity.biological & pharmaceutical bulletin,27(10),1555-1560.
MLA	Liu, Y,et al."The inhibitory effect of intestinal bacterial metabolite of ginsenosides on CYP3A activity".biological & pharmaceutical bulletin 27.10(2004):1555-1560.