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目的 :观察环孢霉素 A(Cs A)、维拉帕米 (Ver)、黄体酮 (Prog)对膀胱癌多药耐受相关蛋白 (MRP)介导的多药耐受 (MDR)的逆转作用。方法 :分别采用 MTT方法和流式细胞仪检测观察 Cs A、Ver和 Prog逆转化疗药物 VCR对 MRP高表达的膀胱癌细胞的细胞毒性作用的逆转效果 ,以及对细胞内柔红霉素 (DNR)聚集、外排的影响。结果 :Cs A和 Ver作为多药耐受糖蛋白 (P- gp)的良好剂同样可以显著逆转 VCR对 MRP高表达的 EJ/MRP细胞毒性作用 ,具有增加 EJ/ MRP细胞内 DNR的聚集和减少外排的作用 ,剂量越大作用越强 ;而 Prog则无类似作用。结论 :Cs A和 Ver对人膀胱癌 MRP介导的 MDR具有良好的逆转作用 ,可通过增加细胞内的药物聚集和减少外排已进入细胞内的药物起作用 ,这种作用存在剂量依从关系。
OBJECTIVE: To observe the reversal of multidrug resistance-associated protein (MRP) -mediated multidrug resistance (MDR) induced by cyclosporin A (CsA), verapamil (Ver) and progesterone effect. Methods: MTT and flow cytometry were used to detect the reversal effect of CsA, Ver and Prog on reversing the cytotoxicity of MRP-overexpressing bladder cancer cells by VCR. The effects of daunorubicin (DNR) Agglomeration, the impact of efflux. Results: Cs A and Ver, as good agents of multi-drug tolerance glycoprotein (P-gp), could also significantly reverse the cytotoxic effect of VCR on EJ / MRP cells with high expression of MRP, and increase the accumulation and decrease of DNR in EJ / MRP cells The role of efflux, the greater the role of the greater dose; and Prog no similar effect. CONCLUSIONS: CsA and Ver have a good reversal effect on MRP-mediated MDR in human bladder cancer and may play a dose-dependent role by increasing intracellular drug accumulation and decreasing efflux into the cells.