血脑屏障上的P-糖蛋白及其转运功能研究进展

Current views of transporting role of P-glycoprotein in the blood-brain barrier

P-糖蛋白(P-glycoprotein,P-gp)是一个由分子量170-180KD组成的糖蛋白,其主动的药物外排作用是造成肿瘤细胞产生多药耐药性(Multidrug resistance,MDR)的重要原因。近年来研究发现,P-糖蛋白在机体正常组织如血脑屏障(blood-brain barrier,BBB)也呈高度表达。本文归纳了P-糖蛋白的逆转剂及其底物的特征,系统介绍了血脑屏障上P-糖蛋白的转运功能及其研究方法,期望为P-糖蛋白逆转剂的应用以及中枢神经系统疾病的治疗提供帮助。

P-glyeoprotein （P-gp） is a 170-180 kD cell-surface transporter protein and has been thought to confer multidrug resistance （MDR） to chemotoxins by actively effluxing them from the cell. Recent studies showed that P-gp is highly expressed in many types of normal tissue such as blood-brain barrier （BBB）. The present report provided a summary about the characteristics of substrate and reversal agent of P-gp, the transporting role and research methods about this protein in the BBB were also reviewed, which may be helpful in the application of P-gp reversal agent and treatment of diseases in the central never system.