齐墩果酸对OATP1B1介导药物转运功能的关联性影响

Association Effect of Oleanolic Acid on the Function of OATP1B1

摘要: 目的探讨齐墩果酸对有机阴离子转运多肽1B1（organic anion transporting polypetide1B1，OATP1B1）转运功能的关联性影响。方法利用稳定表达人OATP1B1的人胚胎肾293（hunan embyonic kindney293，HEK293）细胞株，以氟伐他汀为底物进行OATP1B1摄取反应，观察齐墩果酸对OATP1B1摄取功能的影响。结果齐墩果酸对OATP1B1摄取氟伐他汀的功能有竞争性抑制作用，抑制常数Ki值为（20.3±2.1）mmol·L^-1。结论齐墩果酸对肝脏药物转运体OATP1B1转运抑制作用可诱导中西药相互作用。

Abstract: OBJECTIVE To investigate the association effect of oleanolic acid(OA) on organic anion transporting polypeptide1B1(OATP1B1) transport function. METHODS Using human embryonic kidney 293(HEK293) cells stably expressing OATP1B1, to observe the effect of OA on OATP1B1-mediated uptake of fluvastatin(FV). RESULTS OA could competitively inhibit the OATP1B1-mediated uptake of FV, with the ki values of (20.3±2.1)mmol·L^-1. CONCLUSION Inhibitory effect of OA on transporter function of liver drug transporter OATP1B1 can induce hurb-drug interactions.