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Reversible Inhibition of Three Important Human Liver Cytochrome P450 Enzymes by Tiliroside
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
KeywordCytochrome P450 (Cyp) Tiliroside Drug-herb Interactions
Source PublicationPHYTOTHERAPY RESEARCH
2010-11-01
DOI10.1002/ptr.3189
Volume24Issue:11Pages:1670-1675
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
WOS SubjectChemistry, Medicinal ; Pharmacology & Pharmacy
WOS Research AreaPharmacology & Pharmacy
WOS KeywordDRUG-INTERACTIONS ; DIETARY FLAVONOIDS ; GRAPEFRUIT JUICE ; METABOLISM ; ABSORPTION
AbstractTiliroside, 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.
Language英语
WOS IDWOS:000283794300015
Citation statistics
Cited Times:22[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/142097
Collection中国科学院大连化学物理研究所
Affiliation1.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
GB/T 7714
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.
APA Sun, Dong-Xue.,Lu, Jin-Cai.,Fang, Zhong-Ze.,Zhang, Yan-Yan.,Cao, Yun-Feng.,...&Yang, Ling.(2010).Reversible Inhibition of Three Important Human Liver Cytochrome P450 Enzymes by Tiliroside.PHYTOTHERAPY RESEARCH,24(11),1670-1675.
MLA Sun, Dong-Xue,et al."Reversible Inhibition of Three Important Human Liver Cytochrome P450 Enzymes by Tiliroside".PHYTOTHERAPY RESEARCH 24.11(2010):1670-1675.
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