Hydroxychalcones induce apoptosis in B16-F10 melanoma cells via GSH and ATP depletion
Hydroxychalcones induce apoptosis in B16-F10 melanoma cells via GSH and ATP depletion
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DOI：
10.1016/j.ejmech.2008.09.009
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发表时间：
2009-04-01
影响因子：
6.7
通讯作者：
Creczynski-Pasa, Tania Beatriz
中科院分区：
文献类型：
--
作者：
Formento Navarini, Andreia Lilian;Chiaradia, Louise Domeneghini;Creczynski-Pasa, Tania Beatriz
为了寻找新型抗癌药物的先导化合物，我们研究了13种以前从未测试过的羟基查耳酮对黑色素瘤细胞系（B16-F10）的毒性。这些化合物是在碱性条件下由醛与羟基苯乙酮发生羟醛缩合反应得到的。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，但未显著降低黑色素瘤细胞中的细胞内线粒体GSH和ATP水平。结果表明，影响活性的主要因素是分子的形状，其次是羟基的数量。(c)2008年由Elsevier Masson SAS出版。
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. (c) 2008 Published by Elsevier Masson SAS.