小分子化合物S1抑制K562细胞增殖及其机理研究

The study of effect and mechanism of small molecular compound S1 inhibiting proliferation of K562 cell

目的:探讨小分子化合物S1对K562细胞的抑制作用及机理,为S1治疗慢性粒细胞白血病(chronic myeloid leukemia,CML)提供理论与实验基础。方法:MTT法检测不同浓度S1对K562细胞增殖的抑制作用;应用Chou-Talalay计算联合指数,观察单独应用S1与S1联合阿糖胞苷对K562细胞增殖抑制的协同作用;Western-blotting方法检测不同浓度S1作用后K562细胞系中Bcl-2蛋白表达水平的变化。结果:与对照组相比,S1可以抑制K562细胞的增殖(P<0.05);S1与阿糖胞苷联合应用对K562细胞的生长抑制具有协同作用,联合指数CI<1;S1可下调K562细胞系中抗凋亡蛋白Bcl-2的表达。结论:小分子化合物可通过下调抗凋亡蛋白Bcl-2的表达抑制K652细胞的增殖,并与阿糖胞苷具有协同作用。

Objective：To investigate its therapeutic potential as a novel small-molecule inhibitor of Bcl-2 for the treatment of chronic myeloid leukemia （CML）.Methods：K562 cells proliferation was measured by MTT assay.We used the Chou-Talalay method to determine the compound combination synergism.The expression of Bcl-2 protein was examined with Western-blotting.Results：Compared with control group，S1 can decrease the survival rate of K562 cells （P〈0.05）.S1 showed a synergistic effect when combined with cytosine arabinoside hydrochloride （Ara-c） in inhibiting K562 cell proliferation，CI〈1.S1 down-regulated the Bcl-2 protein in K562 cell line.Conclusion：S1 can inhibit proliferation of K562 cell through down-regulating the expression of Bcl-2 protein.Meanwhile，it can demonstrate a synergistic combination effect with cytosine arabinoside.