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学科主题: 物理化学
题名: Inhibition of Human Liver Cytochrome P450 2C8 and 3A4 by Sanguinarine
作者: QiXY ;  LiangSC ;  GeGB ;  FangZZ ;  YangL
会议名称: 9th International Meeting of the International-Society-for-the-Study-of-Xenobiotics
会议日期: 2010-9-4
出版日期: 2010-09-04
会议地点: TURKEY
通讯作者: 杨凌
ISSN: 0360-2532
部门归属: 十八室
主办者: 国际药物代谢学会
摘要: Abstract: Sanguinaria, a benzo[c]phenanthridine alkaloid extracted from the root of Sanguinaria canadenis and other poppy-fumaria species, exhibits many biological activities, such as antimicrobial, antiinflammatory, antioxidant, antitumor activities, and singlet oxygen generation potential [1]. As antibiotics or anticancer drug, sanguinaria is likely to be used in combination with various synthetic drug in most case, thus it is necessary to evaluate potential pharmacokinetics drug-drug interactions induced by sanguinaria. An in vitro study revealed that sanguinaria can caused competitive inhibition of human CYP1A2 with Ki of 2 µM [2], but the inhibitory effects on other CYP enzymes remain unreported. In this study, the inhibition of sanguinariato on CYP3A4 and CYP2C8 displayed reversible inhibition. The kinetic parameters of reversible inhibition (Ki) are 2.2 µM for CYP3A4 and 8.82 µM for CYP2C8. Due to the limited pharmacokinetics data of sanguinaria in human, it is nigh impossible to evaluate its potential effects to human from in vitro data, further work will be done in the future. Reference: [1] Curr drug metab, 2007; 8:173-176 [2] Toxicol lett, 2004; 151:375-387
语种: 中文
Citation statistics: 
内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/114340
Appears in Collections:中国科学院大连化学物理研究所_会议论文

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Recommended Citation:
QiXY,LiangSC,GeGB,et al. Inhibition of Human Liver Cytochrome P450 2C8 and 3A4 by Sanguinarine[C]. 见:9th International Meeting of the International-Society-for-the-Study-of-Xenobiotics. TURKEY. 2010-9-4.
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