Hydroxychalcones induce apoptosis in B16-F10 melanoma cells via GSH and ATP depletion

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• 作者：André ; ia Lilian Formento Navarini ; Louise Domeneghini Chiaradia ; Aless ; ra Mascarello ; Má ; rcio Fritzen ; Ricardo José ; Nunes ; Rosendo Augusto Yunes ; Tâ ; nia Beatriz Creczynski-Pasa
• 关键词：Hydroxychalcones ; Melanoma ; Antitumoral ; Apoptosis ; GSH ; ATP
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：April 2009
• 年：2009
• 卷：44
• 期：4
• 页码：1630-1637
• 全文大小：473 K

文摘

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.