Background: Green tea can inhibit OATPs, so it may interact with the substrate of OATPs, such as rosuvastatin.
Objective: This study aimed to investigate the effects of green tea on the pharmacokinetics of rosuvastatin and its mechanism.
Methods: Male Sprague-Dawley rats received different doses of green tea extract (GTE) and (−)- epigallocatechin-3-gallate (EGCG). Caco-2
cells and OATP1B1-HEK293T cells were used in drug uptake and transport assay. The matrix concentrations of rosuvastatin and catechins were
determined by ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS).
Results: GTE and EGCG were both found to increase the area under the plasma concentration-time curve (AUC0-∞) of rosuvastatin ((p<0.050).
In the Caco-2 cell model, the uptake and transport of rosuvastatin in the GTE groups were 1.94-fold (p<0.001) and 2.11-fold (p<0.050) higher,
respectively, than those of the control group. However, in the EGCG group, the uptake and transport of rosuvastatin were decreased by 22.62%
and 44.19%, respectively (p<0.050). In the OATP1B1- HEK293T cell model, the OATP1B1-mediated rosuvastatin uptake was decreased by
GTE to 35.02% of that in the control (p<0.050) and was decreased by EGCG to 45.61% of that in the control (p<0.050).
Conclusion: GTE increased the systemic rosuvastatin exposure in rats. The mechanism may include an increase in rosuvastatin absorption and a
decrease in liver distribution by inhibiting OATP1B1. EGCG may be the main ingredient of green tea that affects the pharmacokinetic parameters
of rosuvastatin. Our results showed the importance of conducting green tea-rosuvastatin study.