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Among them, kaempferol decreased the concentration most significantly, by 54.17 %, which indicated that flavonoids may alleviate bosentan-induced liver injury by inhibiting OATP1B1-mediated bosentan uptake. Furthermore, the pharmacophore model indicated the hydrogen bond acceptors and hydrogen bond donors may play critical role in the potency of flavonoids inhibition on OATP1B1. Taken together, our findings would provide helpful information for predicting the potential risks of flavonoid-containing food/herb-drug interactions in humans a