藥物轉(zhuǎn)運(yùn)體和藥物代謝酶是影響藥物體內(nèi)處置過程中至關(guān)重要的因素。大黃酸作為傳統(tǒng)中藥大黃的主要活性成分，具有廣泛藥理活性。研究發(fā)現(xiàn)，大黃酸與藥物轉(zhuǎn)運(yùn)體和代謝酶密切相關(guān)，能夠直接激活或抑制多種轉(zhuǎn)運(yùn)體的功能及其蛋白表達(dá)。而且大黃酸對(duì)藥物代謝酶細(xì)胞色素P450（CYP450）的功能及其蛋白表達(dá)同樣有抑制作用。因此，大黃酸與其他藥物合用時(shí)，可能發(fā)生基于藥動(dòng)學(xué)的藥物相互作用（drug-drug interaction，DDI）。從藥物轉(zhuǎn)運(yùn)體和代謝酶的體內(nèi)分布、大黃酸對(duì)轉(zhuǎn)運(yùn)體及代謝酶的影響等方面進(jìn)行綜述。

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.

國(guó)家自然科學(xué)基金項(xiàng)目（81473280，81603186）