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 metabolic enzymes are crucial factors in the process of drug treatment. Rhein, as the main active component of traditional Chinese medicine rhubarb, has a wide range of pharmacological activities. Previous studies have shown that rhein is closely related to drug transporters and metabolic enzymes, and can directly activate or inhibit the functions of a variety of transporters and their protein expression. Furthermore, rhein can inhibit the function and protein expression of cytochrome P450 (CYP450), a drug metabolizing enzyme. Thus, when rhein is combined with other drugs, the drug-drug interaction (DDI) may occur based on pharmacokinetic. This paper focuses on the distribution of drug transporters, metabolic enzymes, and the effects of rhein on transporters and metabolic enzymes.

国家自然科学基金项目（81473280，81603186）