摘要
目的:探讨五味子甲素对表达多药耐药相关蛋白1的肿瘤耐药细胞株的逆转耐药作用及相关机制。方法:FCM测定不同浓度五味子甲素对柔红霉素抑制HL60/ADR生长及同一浓度五味子甲素对不同化疗药物抑制HL60/ADR和HL60/MRP细胞生长的影响;五味子甲素作用前后,HL60/ADR和HL60/MRP细胞内化疗药物柔红霉素和MRP1特异性底物二醋酸羧基荧光素积聚的变化。结果:25μmol/L五味子甲素可有效降低HL60/ADR、HL60/MRP对柔红霉素、长春新碱和依托泊甙的半数抑制浓度,逆转倍数分别是5,11,16和3,3,13倍;五味子甲素能够增加柔红霉素和MRP1特异性底物二醋酸羧基荧光素在细胞内的积聚。结论:五味子甲素可以逆转不同化疗药物对MRP1介导的耐药,其逆转机制与增加化疗药物的积聚能力有关。
Objective To investigate the reversal effect of Schisandrin A(Schisandrin A) on MRP cell lines and its possible mechanisms. Methods Susceptibility of DNR, VCR and VP16 enhanced by Schisandrin A in HL-60/ADR and HL-60/MRP cell lines, were evaluated with flow cytometry. The intracellular concentrations of DNR and CFDA, and a specific fluorescent substrate for MRP1 were detected also with flow cytometry. Results Schisandrin A could increase the drug susceptibility of HL 60/ADR and HL-60/MRP cells to DNR, VCR and VP16 at the concentrations of 25 μM and the reversal folds were 5-, 11-, 16- and 3-, 3 , 13-fold, respectively. Meanwhile, Schisandrin A could significantly increase the intracellular accumulation of DNR in the two cell lines when detected by flow cytometry. Conclusion Schisandrin A could reverse multidrug resistance of different drugs caused by MRP1 in HL60/ADR and HL60/MRP cell lines and this was in a dose-dependent manner. The reversal effect is related to the increase of intracellular accumulation of chemotherapeutic drugs.
出处
《中华实用诊断与治疗杂志》
2009年第9期857-859,共3页
Journal of Chinese Practical Diagnosis and Therapy
关键词
五味子甲素
多药耐药
MRP1
逆转剂
Schisandrin A
muhidrug resistance
muhidrug resistance-associated protein 1
modulator