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题名: Reversible and Time-Dependent Inhibition of CYP3A4-Mediated Nifedipine Oxidation by Noscapine
作者: Jin, Xue-Li1;  Tang, Shu-Hong3;  Fang, Zhong-Ze2;  Qu, Yan-Qing1;  Liang, Rui1;  Gao, Zhen-Ming1;  Tang, Bo1;  Sun, De-Guang1;  Li, Ming3;  Yang, Ling2;  Wang, Li-Ming1
关键词: Drug-drug interaction (DDI) ;  Nifedipine ;  Noscapine ;  Substrate-dependent inhibition ;  Time-dependent inhibition (TDI) ;  Warfarin
刊名: LATIN AMERICAN JOURNAL OF PHARMACY
发表日期: 2011-11-01
卷: 30, 期:9, 页:1854-1857
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: Substrate-dependent inhibition of CYP3A4 might influence the extrapolation of drug interactions from the in vitro to in vivo situation. The aim of the present study is to investigate reversible and time-dependent inhibition of CYP3A4-mediated nifedipine oxidation by noscapine. Furthermore, in vitro-in vivo extrapolation (IVIVE) was performed using in vitro parameters. The results showed that CYP3A4-mediated nifedipine oxidation activity was strongly inhibited with an IC50 of 25.7 +/- 5.4 mu M. Kinetic analysis showed that inhibition of CYP3A4-mediated nifedipine oxidation by noscapine was best fit to a non-competitive manner with Ki value of 10.9 mu M. IC50 shift experiment showed that IC50 was significantly decreased from 25.7 +/- 5.4 mu M to 0.34 +/- 0.07 mu M after pre-incubation with noscapine for 30 min, which indicated that time-dependent inhibition existed for inhibition of CYP3A4 by noscapine. The AUC of (R)-warfarin was predicted to increase by 0.5 % using C-max or 0.2 % using unbound C-max with reversible inhibition prediction equation, while the AUC of (R)-warfarin was estimated to increase by 23.1 % using C-max or 10.4 % using unbound C-max with TDI prediction equation. Inhibition of CYP3A4 by noscapine showed substrate-dependent inhibition behaviour. However, the results obtained from IVIVE are very similar using testosterone or nifedipine as probe substrates.
关键词[WOS]: DRUG-DRUG INTERACTIONS ;  METABOLISM ;  PREDICTION ;  WARFARIN ;  CYP3A4 ;  APOPTOSIS ;  BINDING ;  CELLS
语种: 英语
WOS记录号: WOS:000301966100029
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/142313
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.Dalian Med Univ, Affiliated Hosp 2, Dalian 116023, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China
3.Fifth Hosp Dalian, Dept Med Oncol, Dalian, Peoples R China

Recommended Citation:
Jin, Xue-Li,Tang, Shu-Hong,Fang, Zhong-Ze,et al. Reversible and Time-Dependent Inhibition of CYP3A4-Mediated Nifedipine Oxidation by Noscapine[J]. LATIN AMERICAN JOURNAL OF PHARMACY,2011,30(9):1854-1857.
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