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芪类化合物在癌的起始、促进和发展阶段均有化学抗癌活性,对其化学结构进行改造并进行作用机制研究,提高其抗肿瘤活性,有可能发现新的抗肿瘤药物.在合成23种芪类化合物的基础上,以MTT法测定其对9种肿瘤细胞系的抑制作用,发现多种化合物对SMMC-7721、BGC-823、HepG2、Bel-7402、MCF-7、SGC-7901细胞系具有较明显的抑制活性.以细胞周期分析、Hoechst33258荧光染色及线粒体膜电位变化进行检测,发现经抑制作用较强的化合物HCQ-10处理后的Bel-7402细胞发生G2/M期阻滞,并继发细胞凋亡.实验结果说明,合成芪类化合物对SMMC-7721、BGC-823、HepG2、Bel-7402、MCF-7、SGC-7901细胞具有较为明显的增殖抑制作用,其抑制Bel-7402细胞增殖的作用机制为阻滞细胞于G2/M期并诱导细胞继发凋亡.
Stilbene compounds have chemical anticancer activity in the initiation, promotion and development stages of cancer, and their chemical structures are modified and their mechanism of action is studied to improve their antitumor activity, so that new antitumor drugs may be found. On the basis of the stilbene compounds, the inhibitory effect of these compounds on 9 tumor cell lines was determined by MTT assay. It was found that SMMC-7721, BGC-823, HepG2, Bel-7402, MCF-7, SGC-7901 cells The cell cycle analysis, Hoechst33258 fluorescence staining and mitochondrial membrane potential changes were detected, the inhibition of the compound HCQ-10 treated Bel-7402 cells in G2 / M phase arrest, And secondary to apoptosis.Experimental results show that the synthesis of stilbene compound on SMMC-7721, BGC-823, HepG2, Bel-7402, MCF-7, SGC-7901 cells have a more significant inhibition of proliferation, inhibition of Bel- 7402 cell proliferation mechanism of action is to block cells in G2 / M phase and induce apoptosis of cells.