4.7 Article

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

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 4, 页码 1630-1637

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.09.009

关键词

Hydroxychalcones; Melanoma; Antitumoral; Apoptosis; GSH; ATP

资金

  1. CNPq (Conselho Nacional de Desenvolvimento Cientifico e Tecnologico)
  2. CAPES (Coordenacao de Pessoal de Nivel Superior)
  3. FAPESC (Fundacao de Amparo a Ciencia e Tecnologia de Santa Catarina)

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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.

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