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目的:建立以白血病细胞系K562为靶点的高通量抗肿瘤药物筛选模型。方法:在96孔细胞培养板上,运用四唑氮化合物(MTS)和电子耦联剂(PMS)连用的方法,对K562细胞增殖情况进行检测。对在化合物影响下K562细胞增殖变化的检测条件进行了优化。结果:采用这一细胞水平的高通量抗肿瘤药物筛选模型,完成了800个小分子有机化合物的筛选,每个化合物的用量是500ng。11个化合物在浓度为5mg/L时可抑制细胞增殖达80％以上,其中9个通过多浓度复筛得到了确认。抑制活性最强的化合物的IC_(50)为170nmol/L,共有7个化合物显示IC_(50)低于10μmol/L。结论:采用K562细胞系进行高通量筛选是快速、经济、有效、实用的发现新型抗肿瘤药物的方法。
Objective: To establish a high-throughput antitumor drug screening model targeting leukemia cell line K562. Methods: The proliferation of K562 cells was detected in 96-well cell culture plates by using tetrazolium compound (MTS) and electron coupling agent (PMS). The detection conditions of the proliferation of K562 cells under the influence of compound were optimized. RESULTS: Using this cellular level high-throughput antitumor drug screening model, 800 small molecule organic compounds were screened for 500ng of each compound. Eleven compounds inhibited cell proliferation by more than 80% at a concentration of 5 mg / L, of which nine were confirmed by multi-concentration rescreening. The IC 50 of the compounds with the most inhibitory activity was 170 nmol / L, and a total of 7 compounds showed IC 50 less than 10 μmol / L. Conclusion: High-throughput screening using K562 cell line is a rapid, economical, effective and practical method to discover new anti-tumor drugs.