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首页> 外文期刊>Cytotechnology >Cytotoxic, tubulin-interfering and proapoptotic activities of 4′-methylthio- trans -stilbene derivatives, analogues of trans -resveratrol
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Cytotoxic, tubulin-interfering and proapoptotic activities of 4′-methylthio- trans -stilbene derivatives, analogues of trans -resveratrol

机译：反式白藜芦醇类似物4'-甲硫基-反式-二苯乙烯衍生物的细胞毒，微管蛋白干扰和促凋亡活性

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The aim of this study was to evaluate the cytotoxicity of a series of seven 4′-methylthio- trans -stilbene derivatives against cancer cells: MCF7 and A431 in comparison with non-tumorigenic MCF12A and HaCaT cells. The mechanism of anti-proliferative activity of the most cytotoxic trans -resveratrol analogs: 3,4,5-trimethoxy-4′-methylthio- trans -stilbene (3,4,5-MTS) and 2,4,5-trimethoxy-4′-methylthio- trans -stilbene (2,4,5-MTS) was analyzed and compared with the effect of trans -resveratrol. All the compounds that were studied exerted a stronger cytotoxic effect than trans -resveratrol did. MCF7 cells were the most sensitive to the cytotoxic effect of trans -resveratrol analogs with IC _(50) in the range of 2.1–6.0?μM. Comparing the cytotoxicity of 3,4,5-MTS and 2,4,5-MTS, a significantly higher cytotoxic activity of these compounds against MCF7 versus MCF12A was observed, whereas no significant difference was observed in cytotoxicity against A431 and HaCaT. In the series of 4′-methylthio- trans -stilbenes, 3,4,5-MTS and 2,4,5-MTS were the most promising compounds for further mechanistic studies. The proapoptotic activity of 3,4,5-MTS and 2,4,5-MTS, estimated with the use of annexin-V/propidium iodide assay, was comparable to that of trans -resveratrol. An analysis of cell cycle distribution showed a significant increase in the percentage of apoptotic cells and G2/M phase arrest in MCF7 and A431 as a result of treatment with 3,4,5-MTS, whereas trans -resveratrol tended to increase the percentage of cells in S phase, particularly in epithelial breast cells MCF12A and MCF7. Both trans -stilbene derivatives enhanced potently tubulin polymerization in a dose-dependent manner with sulfur atom participating in the interactions with critical residues of the paclitaxel binding site of β-tubulin.
机译：这项研究的目的是评估与非致瘤性MCF12A和HaCaT细胞相比，一系列七个7'4'-甲硫基-反式-二苯乙烯衍生物对癌细胞的细胞毒性：MCF7和A431。大多数细胞毒性反式白藜芦醇类似物的抗增殖活性的机制：3,4,5-三甲氧基-4'-甲硫基-反式-二苯乙烯（3,4,5-MTS）和2,4,5-三甲氧基-分析了4'-甲硫基-反式-二苯乙烯（2,4,5-MTS）并将其与反式白藜芦醇的作用进行了比较。所有研究的化合物都比反式白藜芦醇具有更强的细胞毒性作用。 MCF7细胞对反式白藜芦醇类似物的IC _（50）范围为2.1–6.0？M的细胞毒性作用最敏感。比较3,4,5-MTS和2,4,5-MTS的细胞毒性，观察到这些化合物对MCF7的细胞毒性活性明显高于MCF12A，而对A431和HaCaT的细胞毒性没有显着差异。在一系列的4'-甲硫基-反式-苯乙烯基苯甲酸中，3,4,5-MTS和2,4,5-MTS是用于进一步机理研究的最有希望的化合物。用膜联蛋白-V /碘化丙啶测定法估计的3,4,5-MTS和2,4,5-MTS的促凋亡活性与反式白藜芦醇相当。细胞周期分布分析表明，使用3,4,5-MTS处理后，MCF7和A431中凋亡细胞的百分比和G2 / M期阻滞显着增加，而反式白藜芦醇则倾向于增加S期中的细胞，特别是上皮性乳腺癌细胞MCF12A和MCF7。两种反式-二苯乙烯衍生物均以剂量依赖性方式有效地增强了微管蛋白的聚合，其中硫原子参与了与β-微管蛋白的紫杉醇结合位点的关键残基的相互作用。

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