普郎尼克逆转肿瘤细胞MDR的研究进展

Advances in the study of overcoming multidrug resistance in cancer by pluronic block copolymers

肿瘤的多药耐药问题是目前研究的热点问题,P-gp的过度表达是产生多药耐药的主要原因。在临床上主要是通过联合应用P-gp逆转剂或加大化疗药物的用量来解决这个问题。但是,逆转剂的使用会产生许多副作用,这使逆转剂的使用受到抑制。因此,寻找安全有效的P-gp逆转剂倍受关注。普朗尼克这个赋形剂由于对P-gp有明显的抑制作用而被广泛研究。本文从逆转MDR的作用机制,结构和浓度与抑制效果的关系及应用三个方面对普朗尼克在MDR方面的研究进行综述。

Nowadays,lots of investigators draw attention to multidrug resistance（MDR） in cancer.The MDR is mostly due to the overexpressing of P-glycoprotein（P-gp）.In the clinic,strategies for reversing MDR are combined use of P-gp reversal agents or increasing the dose of chemotherapeutics.However,the reversal agents usually lead to many side-effects,which affect the usage of these agents.Therefore,developing a safe and effective reversal agent attracts widespread attention.Pluronic has been extensively investigated because of its inhibition on P-gp activity.This paper describes the mechanism of reversion of MDR by pluronic,the relationship between copolymer molecular structure,concentration and inhibitory activity,and the novel application of the copolymer.