化合物2G2抑制K562细胞增殖并诱导凋亡

The small molecule compound 2G2 inhibits K562 proliferation and induces apoptosis

目的建立基于白血病细胞K562生长活力的小分子化合物筛选的高通量筛选模型,筛选特异性针对慢性粒细胞白血病(CML)增殖抑制的先导化合物。方法以K562细胞系为实验对象,在96孔板上,利用MTS/PMS比色实验测定化合物对细胞活力的影响,建立具有抑制K562细胞活性的化合物筛选模型,并应用该模型完成了1000多种小分子化合物的筛选,对筛选得到的活性化合物通过3H-TdR掺入实验、细胞生长曲线、细胞周期和凋亡检测等实验进行验证和分析。结果建立并利用96孔板药物筛选模型,筛选获得一个具有一定特异性抑制K562细胞增殖的化合物——2G2。结论成功建立了抗白血病药物的筛选方法,为白血病治疗药物的开发研究提供了新的筛选模型。

Objective To find the small molecule compounds, and establish a drug screening model according to proliferation of the leukemia cell line K562. Methods The K562 cells were cultured in the 96-well plate and dealed with more than 1000 small molecule compounds 48 h,then the OD value at 492nm was detected by MTS assay which could determine the number of viable ceils in proliferation. Asmall molecule compound 2G2 which has the effect of inhibitory proliferation to leukemia cell was got. The growth curve, division cycle and apoptosis of K562 to 2G2 were also studied. Results Asmall molecule compound 2G2 which could inhibit the proliferation of K562 cells by the model was found. Conclusion The model of leukemia drug screening can be performed by highthroughput drug screening for effective extraction of small molecule pre-compounds.