Methoxy- and Fluoro-chalcone Derivatives Arrest Cell Cycle Progression and Induce Apoptosis in Human Melanoma Cell A375

Henmi Kayo, Hiwatashi Yoko, Hikita Eri, Toyama Naoya, Hirano Toshihiko

doi:10.1248/bpb.32.1109

Because of the lack of efficacious treatments for advanced melanoma, new approaches are necessary. Chalcones are contained in fruits and vegetables, and have been suggested to be cancer-preventive. In this study, effects of synthetic chalcone derivatives were investigated especially on the proliferation of human melanoma cells and peripheral blood mononuclear cells (PBMCs). Four out of the 12 synthetic chalcones: 4-trifluoromethyl-4′-methoxychalcone (CH-1), 4-trifluoromethyl-2′-methoxychalcone (CH-3), 3-trifluoromethyl-2′,4′-dimethoxychalcone (CH-4) and 3-trifluoromethyl-4′-methoxychalcone (CH-7) exhibited significant antiproliferative efficacies against the cultured cells of the human melanoma cell line A375. CH-1, CH-3, CH-4, and CH-7 induced cell cycle arrest at the S-G₂/M phase within 24 h after the treatment. CH-3, CH-4, and CH-7 significantly activated caspase-3 at 12 h, subsequently induced apoptosis at 72 h. All chalcones inhibited concanavalin A-induced proliferation of PBMCs dose-dependently. Our results suggest that some methoxy- and/or fluoro-chalcones have antitumor efficacy by inducing apoptosis and the cell-cycle arrest.

Methoxy- and Fluoro-chalcone Derivatives Arrest Cell Cycle Progression and Induce Apoptosis in Human Melanoma Cell A375

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Methoxy- and Fluoro-chalcone Derivatives Arrest Cell Cycle Progression and Induce Apoptosis in Human Melanoma Cell A375

書誌事項

この論文をさがす

説明

収録刊行物

被引用文献 (2)*注記

参考文献 (18)*注記

キーワード

詳細情報 詳細情報について

書き出し

問題の指摘

詳細情報詳細情報について