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Reversible and Time-Dependent Inhibition of CYP3A4-Mediated Nifedipine Oxidation by Noscapine
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
2011-11-01
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
关键词[WOS]DRUG-DRUG INTERACTIONS ; METABOLISM ; PREDICTION ; WARFARIN ; CYP3A4 ; APOPTOSIS ; BINDING ; CELLS
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.
语种英语
WOS记录号WOS:000301966100029
引用统计
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/142313
专题中国科学院大连化学物理研究所
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
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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.
APA Jin, Xue-Li.,Tang, Shu-Hong.,Fang, Zhong-Ze.,Qu, Yan-Qing.,Liang, Rui.,...&Wang, Li-Ming.(2011).Reversible and Time-Dependent Inhibition of CYP3A4-Mediated Nifedipine Oxidation by Noscapine.LATIN AMERICAN JOURNAL OF PHARMACY,30(9),1854-1857.
MLA Jin, Xue-Li,et al."Reversible and Time-Dependent Inhibition of CYP3A4-Mediated Nifedipine Oxidation by Noscapine".LATIN AMERICAN JOURNAL OF PHARMACY 30.9(2011):1854-1857.
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