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药物转运体和药物代谢酶是影响药物体内处置过程中至关重要的因素。大黄酸作为传统中药大黄的主要活性成分,具有广泛药理活性。研究发现,大黄酸与药物转运体和代谢酶密切相关,能够直接激活或抑制多种转运体的功能及其蛋白表达。而且大黄酸对药物代谢酶细胞色素P450(CYP450)的功能及其蛋白表达同样有抑制作用。因此,大黄酸与其他药物合用时,可能发生基于药动学的药物相互作用(drug-drug interaction,DDI)。从药物转运体和代谢酶的体内分布、大黄酸对转运体及代谢酶的影响等方面进行综述。
Drug transporters and drug-metabolizing enzymes are crucial factors in the drug’s disposal in vivo. Rhein is a major traditional Chinese medicine rhubarb active ingredient, has a wide range of pharmacological activities. The study found that rhein is closely related to drug transporters and metabolic enzymes, and can directly activate or inhibit the function of multiple transporters and their protein expression. Moreover, rhein has the same inhibitory effect on the function and protein expression of the cytochrome P450 (CYP450), a drug metabolizing enzyme. As a result, rhein-based drug-drug interaction (DDI) may occur when used in combination with other drugs. From the in vivo distribution of drug transporters and metabolic enzymes, the effects of rhein on transporters and metabolic enzymes, etc. are reviewed.