氨氯地平衍生物CJX2对K562/DOX细胞阿霉素耐药的逆转作用  

Reversal effects of CJX2,a amlodipine derivative,on the resistance to doxorubicin by,in doxorubicin-resistant human myelogenous leukemia(K562/DOX) cells

作　　者：张忠泉[1] 纪忠歧[1] 

机构地区：[1]河南大学药学院药理教研室,河南开封475001

出　　处：《河南大学学报（医学版）》2009年第2期96-100,共5页Journal of Henan University:Medical Science

摘　　要：目的:研究氨氯地平衍生物CJX2对K562/DOX细胞阿霉素耐药的逆转作用。方法:应用流式细胞仪和MTT法观察了CJX2对K562/DOX细胞P-糖蛋白(P-glycoprotein,Pgp)的抑制作用及对K562/DOX细胞阿霉素耐药的逆转作用。结果:CJX2能剂量相关性地增加K562/DOX细胞对罗丹明123(rhodamine123,Rh123)的摄取以及细胞内Rh123的累积,明显抑制Pgp介导的Rh123外排,显著增强阿霉素对K562/DOX细胞的细胞毒作用,提高细胞caspase3活性,增加K562/DOX细胞内阿霉素水平。结论:氨氯地平衍生物CJX2能显著抑制Pgp的外排功能,逆转Pgp介导的K562/DOX细胞的多药耐药性。Objective： To study the reversal of resistance to doxorubicin by CJX2, a amlodipine derivative, in doxorubicin-resistant human myelogenous leukemia （K562/DOX） cells. Methods： The effect of CJX2 on （Pglycoprotein, Pgp）function and resistance to doxorubicin in K562/DOX cells were observed by using flow cytometric technology and MTT assay. Results： CJX2 increased intracellular accumulation of Rh123 in K562/DOX cells in a concentration related manner and significantly inhibited the efflux of Rh123 from the cells, the doxorubicin induced cytotoxicity, caspase 3 activity in doxorubicin treated cells and the intracellular accumulation of doxorubicin, was also potentate by CJX2. Conclusion： The reversed effect of CJX2 on resistance to doxorubicin in K562/DOX cells is associated with its inhibitory effect on Pgp function.

关 键 词：CJX2 P-糖蛋白 多药耐药 阿霉素 逆转作用 

分 类 号：R979.1[医药卫生—药品]