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题名: Ginsenoside metabolites, rather than naturally occurring ginsenosides, lead to inhibition of human cytochrome P450 enzymes
作者: Liu, Yong;  Zhang, Jiang-Wei;  Li, Wei;  Ma, Hong;  Sun, Jie;  Deng, Mai-Cun;  Yang, Ling
关键词: ginseng-drug interactions ;  ginsenosides ;  intestinal metabolites ;  cytochrome P450
刊名: TOXICOLOGICAL SCIENCES
发表日期: 2006-06-01
DOI: 10.1093/toxsci/kfj164
卷: 91, 期:2, 页:356-364
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Toxicology
研究领域[WOS]: Toxicology
英文摘要: There is still an argument about ginseng-prescription drug interactions. To evaluate the influence on cytochrome P450 (P450) activities of ginseng in the present study, the influence on P450 activities of naturally occurring ginsenosides and their degradation products in human gut lumen was assayed by using human liver microsomes and cDNA-expressed CYP3A4. The results showed that the naturally occurring ginsenosides exhibited no inhibition or weak inhibition against human CYP3A4, CYP2D6, CYP2C9, CYP2A6, or CYP1A2 activities; however, their main intestinal metabolites demonstrated a wide range of inhibition of the P450-mediated metabolism. There was no mechanism-based inhibition found on these P450 isoforms. It is noteworthy that Compound K, protopanaxadiol (Ppd), and protopanaxatriol (Ppt) all exhibited moderate inhibition against CYP2C9 activity, and Ppd and Ppt also exhibited potent competitive inhibition against CYP3A4 activity. We suggest that after oral administration, naturally occurring ginsenosides might influence hepatic P450 activity in vivo via their intestinal metabolites.
关键词[WOS]: ST-JOHNS-WORT ;  INTESTINAL CYP3A4 INHIBITION ;  JUICE COMPONENTS DIFFER ;  LIVER-MICROSOMES ;  IN-VITRO ;  INTERINDIVIDUAL VARIATIONS ;  CATALYTIC-ACTIVITY ;  DRUG INTERACTION ;  FATTY-ACID ;  BACTERIA
语种: 英语
WOS记录号: WOS:000237697300005
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/139954
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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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, Peoples R China
3.Liaoning Normal Univ, Coll Life Sci, Dalian 116029, Peoples R China
4.Dalian Med Univ, Affiliated Hosp 2, Dalian 116027, Peoples R China

Recommended Citation:
Liu, Yong,Zhang, Jiang-Wei,Li, Wei,et al. Ginsenoside metabolites, rather than naturally occurring ginsenosides, lead to inhibition of human cytochrome P450 enzymes[J]. TOXICOLOGICAL SCIENCES,2006,91(2):356-364.
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