熊果酸对OATP1B1*1a和OATP1B1*5介导瑞舒伐他汀肝脏摄取的影响
Aim(s)：Chinese herbal medicines such as hawthorn, salvia etc are usually combined withstatins so as to treat cardiovascular diseases more effective. Chinese herbal medicines contain many kindsof active components, which may have drug-drug interactions with statins. This study aims to explore theeffect and mechanism that ursolic acid affect OATPIBl-mediated transport of rosuvastatin in hepatobiliaryat cell and molecular level. Methods：This study will explore the effect of ursolic acid onOAPTIBl-mediated transport of rosuvastatin in the different cell systems. Given the geneticpolymorphisms of OATPIBl, simultaneously, this study will further explore the effect of ursolic acid onOATPIBl(521T>C)-mediated transport of rosuvastatin. Results：When the concentration of ursolic acidwere 1.8 uM and 18 uM, it showed that ursolic acid significantly inhibit the uptake of rosuvastatin in bothOATPIBl*la-HEK 293T cells and OATPIB1*5-HEK 293T cells. The reducing of OATPIBl*la transporton rosuvastatin were 34.60±2.99％ and 66.08±1.83%, and for OATPIB1*5 were 34.27+7.08% and66.95±1.14%. Inhibitory parameters of IC50 were 6.25±0.42 uM and 6.07±0.57uM, respectively. Conclusions：This study suggests that ursolic acid can inhibit the uptake of rosuvastatin in hepatocytes.
熊果酸 瑞舒伐他汀 肝脏摄取 药物相互作用
温金华 魏筱华
南昌大学第一附属医院药学部
国内会议
江苏扬州
中文
96-107
2014-06-20（万方平台首次上网日期，不代表论文的发表时间）