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Aim(s)Chinese herbal medicines such as hawthorn,salvia etc are usually combined with statins so as to treat cardiovascular diseases more effective.Chinese herbal medicines contain many kinds of active components,which may have drug-drug interactions with statins.This study aims to explore the effect and mechanism that ursolic acid affect OATP1B1-mediated transport of rosuvastatin in hepatobiliary at cell and molecular level.Methods This study will explore the effect of ursolic acid on OAPT1B1-mediated transport of rosuvastatin in the different cell systems.Given the genetic polymorphisms of OATP1B1,simultaneously,this study will further explore the effect of ursolic acid on OATP1B1(521T>C)-mediated transport of rosuvastatin.Results When the concentration of ursolic acid were 1.8 uM and 18 uM,it showed that ursolic acid significantly inhibit the uptake of rosuvastatin in both OATP1B1*1a-HEK 293T cells and OATP1B1*5-HEK 293T cells.The reducing of OATP1B1*1a transport on rosuvastatin were 34.60±2.99% and 66.08±1.83%,and for OATP1B1*5 were 34.27±7.08% and 66.95±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.