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氨氯地平衍生物CJX1对K562/DOX细胞阿霉素耐药的逆转作用
引用本文:姬汴生,何玲,刘国卿.氨氯地平衍生物CJX1对K562/DOX细胞阿霉素耐药的逆转作用[J].中国药科大学学报,2005,36(2):159-163.
作者姓名:姬汴生  何玲  刘国卿
作者单位:中国药科大学药理学教研室,南京,210009
摘    要:目的:研究氨氯地平衍生物CJX1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CJX1对K562/DOX细胞P-糖蛋白(P-gp)的抑制作用及对K562/DOX细胞阿霉素耐药的逆转作用.结果:CJX1能剂量相关性地增加K562/DOX细胞内罗丹明123(Rh 123)的累计,明显抑制P-gp 介导的Rh 123外排,显著增强阿霉素对K562/DOX细胞的细胞毒作用,增加K562/DOX细胞内阿霉素水平.结论:氨氯地平衍生物CJX1能显著抑制P-gp的外排功能,逆转K562/DOX细胞的多药耐药性.

关 键 词:氨氯地平衍生物  P-糖蛋白  多药耐药  阿霉素  逆转作用
文章编号:1000-5048(2005)02-0159-05
修稿时间:2004年7月14日

Reversal of Resistance to Doxorubicin by CJX1,an Amlodipine Derivative,in Doxorubicin-resistant Human Myelogenous Leukemia (K562/ DOX) Cells
JI Bian-Sheng,HE Ling,LIU Guo-Qing.Reversal of Resistance to Doxorubicin by CJX1,an Amlodipine Derivative,in Doxorubicin-resistant Human Myelogenous Leukemia (K562/ DOX) Cells[J].Journal of China Pharmaceutical University,2005,36(2):159-163.
Authors:JI Bian-Sheng  HE Ling  LIU Guo-Qing
Abstract:AIM:To study the reversal of resistance to doxoru bi cin by CJX1,an amlodipine derivative, in doxorubicin-resistant human myelogen o us leukemia(K562/DOX)cells.METHOD:The effect of CJX1 on P-glyco protein function and resistance to doxorubicin in K562/ DOX cells was explored by using flo w cytometric technology and MTT assay.RESULT:CJX1 increased intr acellular accumulation of rhodanmine 123 (Rh 123)in K562/DOX cells in a dose-de pendent manner and significantly inhibited the efflux of Rh 123 from the cells. The doxoru b icin-induced cytotoxicity and apoptosis were significantly potentiated by CJX1 by promoting intracellular doxorubicin.CONCLUSION:The reversed ef fect of CJX1 on multidrug resistance to doxorubicin in K562/ DOX cells could be atlributed to CJX1's inhibitory effect on P-glycoprotein function.
Keywords:CJX1
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