大蒜素对肝脏药物转运体OATP1B1转运功能的影响

中国临床药理学与治疗学 ›› 2013, Vol. 18 ›› Issue (7): 749-753.

大蒜素对肝脏药物转运体OATP1B1转运功能的影响

杨国营¹, 马凯¹, 吴兰香², 张伟³, 周宏灏^2,3

¹泰山医学院附属邹平医院外科,滨州 256200,山东;
²重庆医科大学生命科学研究院,重庆 400016;
³中南大学临床药理研究所,长沙 400078,湖南

收稿日期:2012-07-16 修回日期:2012-12-06 出版日期:2013-07-26 发布日期:2013-06-20
通讯作者: 吴兰香, 女,医学博士,副研究员,研究方向:临床药理学。Tel: 023-68486875 E-mail: lxwu2008@126.com
作者简介:杨国营,男,本科,主治医师,研究方向:临床药理学。Tel: 0543-4357501 E-mail: yrbing1230@163.com
基金资助:
国家自然科学基金(81102511);重庆市自然科学基金(cstc2011jjA10004);中国博士后科学基金(2011M500669);重庆市博士后科研项目特别资助项目(渝xm201102007)

Influence of allicin on the function of organic anion transporting polypeptide 1B1

YANG Guo-ying¹, MA Kai¹, WU Lan-xiang², ZHANG Wei³, ZHOU Hong-hao^2,3

¹Department of Urology, Taishan Medical University Affiliated Zouping People's Hospital, Binzhou 56200, Shangdong, China;
²Institute of Life Sciences, Chongqing Medical University, Chongqing 400016, China;
³Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University, Changsha 400078, Hunan,China

Received:2012-07-16 Revised:2012-12-06 Online:2013-07-26 Published:2013-06-20

摘要/Abstract

摘要： 目的: 观察大蒜素对肝脏药物转运体-有机阴离子转运多肽1B1(Organic anion transporting polypeptide 1B1, OATP1B1)转运功能的影响。方法: 利用稳定表达人OATP1B1的人胚胎肾293(Human embryonic kidney 293, HEK293)细胞株,以[³H]硫酸雌酮和普伐他汀为底物进行OATP1B1摄取反应,观察大蒜素对OATP1B1摄取功能的影响。结果: 大蒜素对OATP1B1摄取[³H]硫酸雌酮和普伐他汀的功能有竞争性抑制作用,抑制常数K_i值分别为(18.3±5.2) μmol/L 和(15.4±6.8) μmol/L。结论: 大蒜素对肝脏药物转运体OATP1B1转运功能的抑制作用可诱导中药-西药相互作用。

关键词: 大蒜素, OATP1B1, 中药-西药相互作用

Abstract: AIM: To investigate the effect of allicin on organic anion transporting polypeptide 1B1 (OATP1B1) activities.METHODS: Using human embryonic kidney 293 (HEK293) cells stably expressing OATP1B1, to observe the effect of allicin on OATP1B1-mediated uptake of [³H]estrone sulfate and pravastatin.RESULTS: Allicin can competitively inhibit the OATP1B1-mediated uptake of [³H]estrone sulfate and pravastatin, with the K_i values of (18.3±5.2)μmol/L and (15.4±6.8)μmol/L,repectively.CONCLUSION: These data indicate that modification of OATP1B1 transport activity by allicin is a mechanism for herb-drug interactions in human beings.

Key words: Allicin, OATP1B1, Her-drug interaction

中图分类号:

R969.2

杨国营, 马凯, 吴兰香, 张伟, 周宏灏. 大蒜素对肝脏药物转运体OATP1B1转运功能的影响[J]. 中国临床药理学与治疗学, 2013, 18(7): 749-753.

YANG Guo-ying, MA Kai, WU Lan-xiang, ZHANG Wei, ZHOU Hong-hao. Influence of allicin on the function of organic anion transporting polypeptide 1B1[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2013, 18(7): 749-753.

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