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

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.

Graphical abstractHydroxychalcones were tested toward a melanoma cell line. The compounds induced mitochondrial GSH and ATP depletion, and cell apoptosis. The molecule shape and the number of hydroxyl groups are important for the activity.Figure optionsDownload full-size imageDownload as PowerPoint slide