中药逆转P-糖蛋白介导的肿瘤多药耐药的研究进展

多药耐药（MDR）是导致癌症化疗失败的主要因素。肿瘤产生MDR的机制很多,其中最为常见也研究得较为深入的一种机制是一种ATP依赖跨膜转运蛋白P-糖蛋白（P-gp）在肿瘤细胞中的过度表达。由于相当一部分化疗药物属于P-gp的转运底物,过度表达的P-gp使细胞内药物浓度显著低于有效毒性浓度,从而产生耐药性。P-gp调节剂可通过抑制P-gp的转运功能或者抑制蛋白的表达修复肿瘤细胞对药物的敏感性。本文就近年来在部分中药及中药单体成分逆转肿瘤P-gp-MDR作用方面的研究做一些总结。

Multidrug resistance (MDR) is the major reason for failure of human cancer chemotherapy. One of the main underlying mechanisms of MDR is the over-expression of P-glycoprotein (P-gp), an ATP-dependent membrane transporter protein encoded by MDR1 gene. P-gp extrudes a spectrum of anticancer drugs from cancer cells and decreases effective intracellular drug concentrations, therefore leads to drug tolerance of cancer cells. P-gp modulators restore chemosensitivity of cancer cells through inhibiting transport function or cellular expression of P-gp. Chinese medicines have been used for treatment of cancer for thousand years. This review provides a brief introduction of Chinese medicines that exhibited activity in reversing P-gp-mediated MDR in cancers.