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目的合成新型有机锗喹啉酯倍半氧化物,研究它们对体外培养PC-3M细胞的抑制作用,分析作用机理,研究分子结构和抗癌活性之间的关系。方法利用氧化还原、加成、酰化、水解等反应合成了2种新型有机锗喹啉酯化合物。用MTT方法研究化合物分别在10μM,30μM和60μM对PC-3M癌细胞的抑制作用。显微镜下观察药物作用后的PC-3M细胞形态,应用流式细胞光度术检测药物对PC-3M细胞周期的影响。结果2种化合物对PC-3M的IC50分别为10μM和30μM;10～30μM浓度的药物能使细胞皱缩,碎片增加,药物不仅强烈抑制了细胞的增值,而且对细胞形态也产生了严重影响。细胞生长过程中,G0/G1和G2/M期细胞数量减少而S期细胞数量明显增多。结论合成的新化合物对体外培养PC-3M癌细胞的增殖具有很强的抑制作用,药物与细胞核内DNA发生了相互作用。化合物中甲基的存在不利于抗癌作用的发挥。
OBJECTIVE To synthesize quinolinol ester sesquioxide, study their inhibitory effect on PC-3M cells cultured in vitro, analyze the mechanism of action, and study the relationship between molecular structure and anti-cancer activity. Methods Two novel organic germanium quinoline ester compounds were synthesized by redox reaction, addition reaction, acylation reaction and hydrolysis reaction. Compounds were tested for their inhibitory effects on PC-3M cancer cells at 10, 30 and 60 μM, respectively, using the MTT method. The morphology of PC-3M cells was observed under the microscope. The effect of drugs on the cell cycle of PC-3M cells was detected by flow cytometry. Results The IC50 values of PC-3M and PC-3M were 10μM and 30μM, respectively. The drug concentration of 10μM and 30μM increased the cell shrinkage and debris. The drug not only strongly inhibited the cell proliferation, but also had a serious effect on cell morphology. During cell growth, the number of G0 / G1 and G2 / M phase cells decreased and the number of S phase cells increased significantly. Conclusion The new compounds have a strong inhibitory effect on the proliferation of PC-3M cells cultured in vitro. Drugs interact with DNA in the nucleus. The presence of methyl in the compound is not conducive to the anticancer effect of play.