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题名: Inhibitory Effects of 17 Steroids Towards 6 Major Cytochrome P450 Isoforms
作者: Wang, Guo-En1;  Cao, Yun-Feng3, 4;  Kurihara, Hiroshi1;  Fang, Zhong-Ze2;  He, Rong-Rong1
关键词: Cytochrome P450 (CYP) ;  In vivo drug-drug interaction (DDI) ;  Steroids
刊名: LATIN AMERICAN JOURNAL OF PHARMACY
发表日期: 2014
卷: 33, 期:8, 页:1326-1331
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: The aim of present study was to investigate drug-drug interaction (DDI) potential of 17 steroids by examining their inhibitory effects towards 6 major cytochrome P450 (CYP) isoforms. Inhibitory effects of 17 steroids (aldosterone, androstenedione, corticosterone, cortisol, dehydroepiandrosterone, 11-deoxycortisol, dexamethasone, estrone, 17 alpha-hydroxyprogesterone, medroxyprogesterone, megestrol acetate, methylprednisolone, methyltestosterone, prednisolone, prednisone, pregnenolone, and testosterone) at 100 mu M (25 mu M for estrone) were tested towards 6 major P450 isoforms including CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 in human liver microsomes. The results demonstrated that CYP3A4 was mostly sensitive to the inhibitory effect of the steroids. CYP2C9 and CYP1A2 were moderately affected. CYP2A6 and CYP2D6 were the least inhibited. Instead of inhibition, activation was observed towards CYP2E1 by some steroids. Given the limited inhibition and the potential maximal physiological concentrations, these steroids were considered less likely to lead to serious DDI via the inhibition of P450 in vivo.
关键词[WOS]: HUMAN LIVER-MICROSOMES ;  CYP3A4-MEDIATED DRUG-METABOLISM ;  CYCLOSPORINE-A OXIDASE ;  ENDOGENOUS STEROIDS ;  HUMAN HEPATOCYTES ;  PRIMARY CULTURES ;  IN-VITRO ;  3A4 ;  P450 ;  INDUCERS
语种: 英语
WOS记录号: WOS:000344934100013
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/145574
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.Jinan Univ, Coll Pharm, Antistress & Hlth Res Ctr, Guangzhou 510632, Guangdong, Peoples R China
2.Tianjin Med Univ, Sch Publ Hlth, Dept Toxicol, Tianjin 300070, Peoples R China
3.Chinese Acad Sci, Joint Ctr Translat Med, Dalian Inst Chem Phys, Dalian 116023, Peoples R China
4.Liaoning Med Univ, Affiliated Hosp 1, Dalian 116023, Peoples R China

Recommended Citation:
Wang, Guo-En,Cao, Yun-Feng,Kurihara, Hiroshi,et al. Inhibitory Effects of 17 Steroids Towards 6 Major Cytochrome P450 Isoforms[J]. LATIN AMERICAN JOURNAL OF PHARMACY,2014,33(8):1326-1331.
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