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题名: Inhibition of human CYP3A4 and CYP3A5 enzymes by gomisin C and gomisin G, two lignan analogs derived from Schisandra chinensis
作者: Zhao, Jin1;  Sun, Tao2;  Wu, Jing-Jing3, 4;  Cao, Yun-Feng3, 4, 5;  Fang, Zhong-Ze4, 6;  Sun, Hong-Zhi4;  Zhu, Zhi-Tu4;  Yang, Kun6;  Liu, Yong-Zhe6;  Gonzalez, Frank J.7;  Yin, Jun1
关键词: Gomisin C ;  Gomisin G ;  CYP3A4 ;  CYP3A5 ;  Inhibition ;  Herb-drug interactions
刊名: FITOTERAPIA
发表日期: 2017-06-01
DOI: 10.1016/j.fitote.2017.03.010
卷: 119, 页:26-31
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: Gomisin C (GC) and gomisin G (GG) are two lignan analogs isolated from the Traditional Chinese Medicine Schisandra chinensis which possesses multiple pharmacological activities. However, the potential herb-drug interactions (HDI) between these lignans and other drugs through inhibiting human cytochrome P450 3A4 (CYP3A4) and CYP3A5 remains unclear. In the present study, the inhibitory action of GC and GG on CYP3A4 and CYP3A5 were investigated. The results demonstrated that both GC and GG strongly inhibited CYP3A-mediated midazolam 1 '-hydroxylation, nifedipine oxidation and testosterone 6 beta-hydroxylation. Notably, the inhibitory intensity of GC towards CYP3A4 was stronger than CYP3A5 when using midazolam and nifedipine as substrates. While inhibition of GC towards CYP3A5 was weaker than CYP3A4 when using testosterone as substrate. In contrast, GG showed a stronger inhibitory activity on CYP3A5 than CYP3A4 without substrate-dependent behavior. In addition, docking simulations indicated that the pi-pi interaction between CYP3A4 and GC, and hydrogen-bond interaction between CYP3A5 and GG might result in their different inhibitory actions. Furthermore, the AUC of drugs metabolized by CYP3A was estimated to increase by 8%-321% and 2%-3190% in the presence of GC and GG, respectively. These findings strongly suggested that GC and GG showed high HDI potentials, and the position of methylenedioxy group determined their different inhibitory effect towards CYP3A4 and CYP3A5, which are of significance for the application of Schisandra chinensis-containing herbs. 2017 Elsevier B.V. All rights reserved.
关键词[WOS]: IN-VITRO ;  LIVER-MICROSOMES ;  DRUG-INTERACTIONS ;  METABOLISM ;  MIDAZOLAM ;  TESTOSTERONE ;  NIFEDIPINE ;  PREDICTION ;  EXTRACT ;  PROBE
语种: 英语
WOS记录号: WOS:000404307800005
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/152105
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.Shenyang Pharmaceut Univ, Sch Tradit Chinese Med, Shenyang 110016, Peoples R China
2.Liaoning Canc Hosp & Inst, Dept Breast Med, Shenyang 110042, Peoples R China
3.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China
4.Key Lab Liaoning Tumor Clin Metabol KLLTCM, Jinzhou, Liaoning, Peoples R China
5.Shanghai Inst Planned Parenthood Res, Key Lab Contracept & Devices Res NPFPC, Shanghai Engineer & Technol Res Ctr Reprod Hlth D, Shanghai, Peoples R China
6.Tianjin Med Univ, Sch Publ Hlth, Dept Toxicol, 22 Qixiangtai Rd, Tianjin 300070, Peoples R China
7.NIH, Lab Metab, Ctr Canc Res, Bldg 37,Room 3106, Bethesda, MD 20892 USA

Recommended Citation:
Zhao, Jin,Sun, Tao,Wu, Jing-Jing,et al. Inhibition of human CYP3A4 and CYP3A5 enzymes by gomisin C and gomisin G, two lignan analogs derived from Schisandra chinensis[J]. FITOTERAPIA,2017,119:26-31.
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