Intestinal bacterial metabolite of naturally occurring 20(S)-protopanaxatriol ginsenosides is the inhibitor of CYP3A - A new biotransformation way with potential for clinical drug-drug interaction

	Intestinal bacterial metabolite of naturally occurring 20(S)-protopanaxatriol ginsenosides is the inhibitor of CYP3A - A new biotransformation way with potential for clinical drug-drug interaction
	Yang, L; Liu, Y
刊名	yakugaku zasshi-journal of the pharmaceutical society of japan
	2004
卷号	124 页码:57-60
关键词	ginseng-drug interaction intestinal bacterial metabolite ginsenoside CYP3A
英文摘要	the intestinal bacterial metabolites of ginsenosides are really responsible for the main pharmacological activities of ginseng. the purpose of this study was to find whether intestinal bacterial metabolites of ginsenosides possess influences on 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 liver microsomes and cdna-expressed human cyp3a4 were assayed. our results showed that either in rat and human liver microsomes or in cdna-expressed cyp3a4, ginsenosides exhibited a similar inhibition profile for testosterone 6 13 -hydroxylation activity. ginsenosides from 20(s)-protopanaxadiol and 20(s)-protopanaxatriol family including rb-1, rb-2, rc, compound-k, re, and rg(1) were no inhibitory effect, whereas the intestinal bacterial metabolite of 20(s)-protopanaxatriol ginsenosides, 20(s)-protopanaxatriol (ppt), exhibited strong competitively inhibitory activity against cyp3a activity in human and rat liver. microsomes and in cdna-expressed cyp3a4. this finding demonstrates that naturally occurring ginsenosides have no inhibitory effects on cyp3a activities, yet their intestinal bacterial metabolite possesses the potential for inhibitory effects on cyp3a activities. it suggests that ginseng-derived products might result in significant ginseng-drug interactions via their intestinal bacterial metabolite.
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]	ginseng saponins ; rat ; absorption ; excretion
收录类别	SCI ; ISTP
语种	英语
WOS记录号	WOS:000225267900015
公开日期	2015-11-10
内容类型	期刊论文
源URL	[http://159.226.238.44/handle/321008/139593]
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	Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China
推荐引用方式 GB/T 7714	Yang, L,Liu, Y. Intestinal bacterial metabolite of naturally occurring 20(S)-protopanaxatriol ginsenosides is the inhibitor of CYP3A - A new biotransformation way with potential for clinical drug-drug interaction[J]. yakugaku zasshi-journal of the pharmaceutical society of japan,2004,124:57-60.
APA	Yang, L,&Liu, Y.(2004).Intestinal bacterial metabolite of naturally occurring 20(S)-protopanaxatriol ginsenosides is the inhibitor of CYP3A - A new biotransformation way with potential for clinical drug-drug interaction.yakugaku zasshi-journal of the pharmaceutical society of japan,124,57-60.
MLA	Yang, L,et al."Intestinal bacterial metabolite of naturally occurring 20(S)-protopanaxatriol ginsenosides is the inhibitor of CYP3A - A new biotransformation way with potential for clinical drug-drug interaction".yakugaku zasshi-journal of the pharmaceutical society of japan 124(2004):57-60.