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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Hydroxychalcones induce apoptosis in B16-F10 melanoma cells via GSH and ATP depletion.
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Hydroxychalcones induce apoptosis in B16-F10 melanoma cells via GSH and ATP depletion.

机译:羟基查耳酮通过GSH和ATP消耗诱导B16-F10黑色素瘤细胞凋亡。

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摘要

Searching for leading compounds of new drugs for cancer therapy, we studied the toxicity of 13 hydroxychalcones never tested before toward melanoma cell line (B16-F10). The compounds were obtained by aldolic condensation between aldehydes and hydroxylated acetophenones, in alkaline conditions. Three of them showed cytotoxicity to the cell line. Two of them induced mitochondrial GSH and ATP depletion and promoted cell death through apoptosis in melanoma cells. One of the compounds induced cell death through necrosis but did not significantly decrease the intracellular mitochondrial GSH and ATP levels in melanoma cells. The results suggest that the predominant factor for the activity is the molecule shape, and secondarily the number of hydroxyl groups.
机译:在寻找用于癌症治疗的新药的领先化合物时,我们研究了13种以前从未测试过的羟基查耳酮对黑素瘤细胞系(B16-F10)的毒性。该化合物是通过在碱性条件下醛与羟基化的苯乙酮之间的醛缩合获得的。其中三个对细胞系显示出细胞毒性。其中两个诱导线粒体GSH和ATP耗竭,并通过黑色素瘤细胞凋亡促进细胞死亡。其中一种化合物通过坏死诱导细胞死亡,但并未显着降低黑色素瘤细胞的细胞内线粒体GSH和ATP水平。结果表明,活性的主要因素是分子形状,其次是羟基数。

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