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学科主题: 物理化学
题名: Inhibitory effects of sanguinarine on human liver cytochrome P450 enzymes
作者: Qi, Xiao-Yi1;  Liang, Si-Cheng2, 3;  Ge, Guang-Bo2;  Liu, Yong2;  Dong, Pei-Pei4;  Zhang, Jiang-Wei2;  Wang, Ao-Xue1;  Hou, Jie4;  Zhu, Liang-Liang2;  Yang, Ling2;  Tu, Cai-Xia1
通讯作者: 杨凌 ;  涂彩霞
关键词: Sanguinarine ;  Human liver microsomes ;  Cytochrome P450 enzyme ;  Drug-drug interaction ;  Time-dependent inhibition
刊名: FOOD AND CHEMICAL TOXICOLOGY
发表日期: 2013-06-01
DOI: 10.1016/j.fct.2013.02.054
卷: 56, 页:392-397
收录类别: SCI
合作性质: 
文章类型: Article
部门归属: 18
项目归属: 1806
产权排名: 待补充
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Food Science & Technology ;  Toxicology
资助者: 2,2
研究领域[WOS]: Food Science & Technology ;  Toxicology
英文摘要: Sanguinarine (SAG) has been recognized as an anticancer drug candidate. However, the drug-drug interactions (DDI) potential for SAG via the inhibition against human cytochrome P450 (CYP) enzymes remains unclear. In the present study, the inhibitory effects of SAG on seven major human CYP isoforms 1A2, 2A6, 2E1, 2D6, 2C8, 2C9 and 3A4 were investigated with human liver microsomes (HLM). The results showed that SAG was a potent noncompetitive inhibitor of CYP2C8 activity (K-i = 8.9 mu M) and competitive inhibitor of CYP1A2, CYP2C9 and CYP3A4 activities (K-i = 2.7, 3.8 and 2.0 mu M, respectively). Furthermore, SAG exhibited time- and NADPH-dependent inhibition towards CYP1A2 and CYP3A4 with K-i/k(inact) values of 13.3/0.087 and 5.58/0.029 min(-1) mu M-1, respectively. Weak inhibition of SAG against CYP2E1, CYP2D6 and CYP2A6 was also observed. In vitro-in vivo extrapolation (IV-IVE) from HLM data showed that more than 35.9% of CYP1A2, CYP2C9, CYP2C8 and CYP3A4 activities in vivo could be inhibited by SAG, suggesting that harmful DDIs could occur when SAG or its medical preparations are co-administered with drugs primarily cleared by these CYP isoforms. Further in vivo studies are needed to evaluate the clinical significance of the data presented herein. (C) 2013 Elsevier Ltd. All rights reserved.
关键词[WOS]: XENOBIOTIC-METABOLIZING ENZYMES ;  ST JOHNS WORT ;  ALKALOID SANGUINARINE ;  DRUG-METABOLISM ;  EPIDEMIC DROPSY ;  CHELERYTHRINE ;  PHARMACOGENOMICS ;  ACTIVATION ;  PREDICTION ;  OXIDATION
语种: 英语
原文出处: 查看原文
WOS记录号: WOS:000318960100046
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/119431
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, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian, Peoples R China
3.Dalian Anim Hlth Supervis Inst, Dalian, Peoples R China
4.Dalian Med Univ, Dalian, Peoples R China

Recommended Citation:
Qi, Xiao-Yi,Liang, Si-Cheng,Ge, Guang-Bo,et al. Inhibitory effects of sanguinarine on human liver cytochrome P450 enzymes[J]. FOOD AND CHEMICAL TOXICOLOGY,2013,56:392-397.
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