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目的:建立灵敏、快速、稳定的检测P-糖蛋白(P-gp)功能的高内涵筛选模型,寻找高效、低毒的肿瘤多药耐药逆转剂。方法:以荧光探针JC-1在耐药细胞内蓄积实验为基础,建立基于细胞的高内涵筛选模型。结果:JC-1的最佳使用浓度为0.5μmol.L-1,为RHO123浓度的1/10;同时,JC-1染色稳定性好、所建模型Z因子达0.8,明显优于RHO123组。利用该模型筛选获得了多个能抑制P-gp功能的化合物。结论:所建立的P-gp蛋白功能抑制剂高内涵筛选模型具有灵敏、简便与稳定等特点,可用于药物筛选。
OBJECTIVE: To establish a sensitive, rapid and stable high-content screening model for detecting P-glycoprotein (P-gp) function in order to find efficient and low toxic multidrug resistance reversal agents. Methods: Based on the accumulation experiment of fluorescent probe JC-1 in drug-resistant cells, a cell-based high content screening model was established. Results: The optimal concentration of JC-1 was 0.5μmol.L-1, which was 1/10 of that of RHO123. Meanwhile, the staining stability of JC-1 was good. The Z-factor of model was 0.8, which was significantly better than that of RHO123 group. A number of compounds that can inhibit P-gp function were screened by this model. Conclusion: The established high-content screening model of P-gp protein inhibitor is sensitive, simple and stable and can be used for drug screening.