Inhibitory effects of sanguinarine on human liver cytochrome P450 enzymes
文献类型：期刊论文
| 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 |
| 刊名 | food and chemical toxicology
 |
| 出版日期 | 2013-06-01 |
| 卷号 | 56页码:392-397 |
| 关键词 | Sanguinarine Human liver microsomes Cytochrome P450 enzyme Drug-drug interaction Time-dependent inhibition |
| 通讯作者 | 杨凌 ; 涂彩霞 |
| 产权排序 | 待补充 |
| 合作状况 | 英 |
| 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. |
| 学科主题 | 物理化学 |
| WOS标题词 | science & technology ; life sciences & biomedicine |
| 类目[WOS] | food science & technology ; toxicology |
| 研究领域[WOS] | food science & technology ; toxicology |
| 关键词[WOS] | xenobiotic-metabolizing enzymes ; st johns wort ; alkaloid sanguinarine ; drug-metabolism ; epidemic dropsy ; chelerythrine ; pharmacogenomics ; activation ; prediction ; oxidation |
| 资助信息 | 2，2 |
| 收录类别 | SCI |
| 原文出处 | 397 |
| 语种 | 英语 |
| WOS记录号 | WOS:000318960100046 |
| 公开日期 | 2014-09-11 |
| 源URL | [http://159.226.238.44/handle/321008/119431]  |
| 专题 | 大连化学物理研究所_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, 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 |
| 推荐引用方式 GB/T 7714 | 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. |
| APA | Qi, Xiao-Yi.,Liang, Si-Cheng.,Ge, Guang-Bo.,Liu, Yong.,Dong, Pei-Pei.,...&Tu, Cai-Xia.(2013).Inhibitory effects of sanguinarine on human liver cytochrome P450 enzymes.food and chemical toxicology,56,392-397. |
| MLA | Qi, Xiao-Yi,et al."Inhibitory effects of sanguinarine on human liver cytochrome P450 enzymes".food and chemical toxicology 56(2013):392-397. |
入库方式： OAI收割
来源：大连化学物理研究所
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