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大蒜素对肝脏药物转运体OATP1B1转运功能的影响
引用本文: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].金属学报,2013,18(7):749-753.
作者姓名:杨国营  马凯  吴兰香  张伟  周宏灏
作者单位: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
基金项目: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)
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Ki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  
收稿时间:2012-07-16
修稿时间:2012-12-06

Influence of allicin on the function of organic anion transporting polypeptide 1B1
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].Acta Metallurgica Sinica,2013,18(7):749-753.
Authors:YANG Guo-ying  MA Kai  WU Lan-xiang  ZHANG Wei  ZHOU Hong-hao
Affiliation:1.Department of Urology, Taishan Medical University Affiliated Zouping People's Hospital, Binzhou 56200, Shangdong, China;2.Institute of Life Sciences, Chongqing Medical University, Chongqing 400016, China;3.Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University, Changsha 400078, Hunan,China
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 Ki 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.
Keywords:Allicin  OATP1B1  Her-drug interaction  
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