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题名: Reversible Inhibition of Three Important Human Liver Cytochrome P450 Enzymes by Tiliroside
作者: Sun, Dong-Xue2;  Lu, Jin-Cai2;  Fang, Zhong-Ze1, 3;  Zhang, Yan-Yan1, 3;  Cao, Yun-Feng2;  Mao, Yu-Xi1, 3;  Zhu, Liang-Liang1, 3;  Yin, Jun2;  Yang, Ling1, 3
关键词: cytochrome P450 (CYP) ;  tiliroside ;  drug-herb interactions
刊名: PHYTOTHERAPY RESEARCH
发表日期: 2010-11-01
DOI: 10.1002/ptr.3189
卷: 24, 期:11, 页:1670-1675
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Chemistry, Medicinal ;  Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: Tiliroside, an active flavonoid extensively found in many medicinal plants including Helichrysum italicum, Geranium mexicanum and Helianthemum glomeratum, has been demonstrated to exert multiple biological effects including antiinflammatory, antimicrobial, antioxidant and antitumor activities. Cytochrome P450 (CYP) enzymes play an important role in the Phase I oxidation metabolism of a wide range of xenobiotics and inhibition of CYP isoforms might influence the elimination of drugs and induce serious adverse drug response. The inhibition of seven CYP isoforms (CYP3A4, CYP1A2, CYP2A6, CYP2D6, CYP2C9, CYP2C8 and CYP2E1) by tiliroside was investigated using in vitro human liver microsomal incubation assays. The results showed that tiliroside strongly inhibited the activity of CYP3A4 (IC(50) = 9.0 +/- 1.7 mu M), CYP2C8 (IC(50) = 12.1 +/- 0.9 mu M) and CYP2C9 (IC(50) = 10.2 +/- 0.9 mu M) with other CYP isoforms negligibly influenced. Further kinetic analysis showed that inhibition of these three CYP isoforms by tiliroside is best fit to a competitive way. The K(i) value was calculated to be 5.5 mu M, 3.3 mu M, 9.4 mu M for CYP3A4, CYP2C9 and CYP2C8, respectively. The relatively low K(i) values suggested that tiliroside might induce drug-drug interactions with many clinically used drugs which are mainly metabolized by these three CYP isoforms. Therefore, attention should be given to the probable drug-drug interaction between tiliroside-containing herbs and substrates of CYP3A4, CYP2C9 and CYP2C8. Copyright (C) 2010 John Wiley & Sons, Ltd.
关键词[WOS]: DRUG-INTERACTIONS ;  DIETARY FLAVONOIDS ;  GRAPEFRUIT JUICE ;  METABOLISM ;  ABSORPTION
语种: 英语
WOS记录号: WOS:000283794300015
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/142174
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, Lab Pharmaceut Resource Discovery, Dalian Inst Chem Phys, Dalian 116023, Peoples R China
2.Shenyang Pharmaceut Univ, Sch Tradit Chinese Med, Shenyang 110016, Peoples R China
3.Chinese Acad Sci, Grad Sch, Beijing 100049, Peoples R China

Recommended Citation:
Sun, Dong-Xue,Lu, Jin-Cai,Fang, Zhong-Ze,et al. Reversible Inhibition of Three Important Human Liver Cytochrome P450 Enzymes by Tiliroside[J]. PHYTOTHERAPY RESEARCH,2010,24(11):1670-1675.
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