P-糖蛋白(P-gp)是跨膜ATP结合盒(ABC)药物外排转运蛋白之一,在肠道、肝脏、肾脏和血脑屏障等各种人体组织中表达.它通过将药物泵出细胞来减少其细胞内浓度,并影响药物的药代动力学及其治疗效果.P-gp具有广泛的底物特异性,可以泵出多种药物,包括常规药物和中药中的活性成分.越来越多的证据证实了中药在广泛治疗多种疾病以及与西药联合应用方面的显著疗效.中药-西药相互作用引起了极大的关注,其中大多数相互作用涉及转运蛋白如P-gp.本研究系统地阐述了天然产物活性成分对P-gp的抑制或诱导作用以及P-gp的调控机制,以明确基于转运蛋白P-gp的中药药物协同或抑制作用以及联合中药西药的安全问题.“,”P-glycoprotein (P-gp) is an important transmembrane ATP-bind-ing cassette (ABC) drug efflux transporter expressed in various human tissues such as the intestines, liver, kidneys, and blood-brain barrier. It limits the intracellular concentration of xenobiot-ics by pumping them out of the cells, affecting drug pharma-cokinetics and therapeutic effects. With its broad substrate spe-cificity, it has the potential to remove a wide range of drugs from Chinese materia medica (CMM), including conventional medi-cines and active compounds. Increasing evidence has confirmed the superior therapeutic effectiveness of CMM in treating a wide range of diseases worldwide, as well as in conjunction with west-ern drugs. As a result, herbal medicine-drug compounds have prompted widespread concern, with the majority of these inter-actions involving transporters such as P-gp. This review systemat-ically summarizes the inhibition or induction of P-gp expression/function by active CMM compounds and the underly-ing regulatory mechanisms. It will aid in improving understand-ing of the synergistic or inhibiting effects associated with trans-porter P-gp as well as rational safety concerns for using CMM, particularly in combination with drugs.