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European Journal of Drug Metabolism and Pharmacokinetics

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Open Access 01-09-2014 | Short Communication

The influence of herbal medicine ursolic acid on the uptake of rosuvastatin mediated by OATP1B11a and 5

Authors: Wen Jin Hua, Wei Xiao Hua, Fu Yong Nan, Wang An Jiang, Chen Yan

Published in: European Journal of Drug Metabolism and Pharmacokinetics | Issue 3/2014

Abstract

Chinese herbal medicines such as hawthorn, salvia, etc., are frequently combined with statins so as to treat cardiovascular diseases more effectively. 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 by which ursolic acid affects OATP1B1-mediated transport of rosuvastatin. 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. When the concentration of ursolic acid was 1.8 and 18 µM, it showed that ursolic acid significantly inhibits the uptake of rosuvastatin in both OATP1B1*1a-HEK 293T cells and OATP1B1*5-HEK 293T cells. The reduction of OATP1B1*1a transport of 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 and 6.07 ± 0.57 µM, respectively. This study suggests that ursolic acid can affect the uptake of rosuvastatin in hepatocytes by inhibiting the transport of OATP1B1, and gene mutation of OATP1B1 may cause different effects on its transport of rosuvastatin.

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Title: The influence of herbal medicine ursolic acid on the uptake of rosuvastatin mediated by OATP1B1*1a and *5
Authors: Wen Jin Hua
Wei Xiao Hua
Fu Yong Nan
Wang An Jiang
Chen Yan
Publication date: 01-09-2014
Publisher: Springer International Publishing
Published in: European Journal of Drug Metabolism and Pharmacokinetics / Issue 3/2014
Print ISSN: 0378-7966
Electronic ISSN: 2107-0180
DOI: https://doi.org/10.1007/s13318-014-0187-8

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The influence of herbal medicine ursolic acid on the uptake of rosuvastatin mediated by OATP1B11a and 5

Abstract

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