Apoptotic effect of chalcone derivatives of 2-acetylthiophene in human breast cancer cells

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• 作者：Tatiana B. Fogaç ; a^a ; ¹ ; Rosiane M. Martins^a ; ¹ ; Karine R. Begnini^a ; Caroline Carapina^b ; Marina Ritter^b ; Claudio M.P. de Pereira^b ; Fabiana K. Seixas^a ; Tiago Collares^a ; ^{collares.t@gmail.com}
• 关键词：Anticancer ; Cytotoxicity ; Chalcone ; Apoptosis
• 刊名：Pharmacological Reports
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：69
• 期：1
• 页码：156-161
• 全文大小：1799 K
• 卷排序：69

文摘

A variety of chalcones have demonstrated cytotoxic activity toward several cancer cell lines. This study aimed to investigate the cytotoxicity of four chalcones derivatives of 2-acetylthiophene in human breast cancer cell lines.MethodsMCF-7 and MDA-MB-231 cells were treated with synthesized chalcones and the cytotoxicity was evaluated by tetrazolium dye (MTT), live/dead, and DAPI assays.ResultsChalcones significantly decreased MCF-7 and MDA-MB-231 cells viability in vitro in a dose dependent manner. After 48 h treatment, the IC50 values ranging from 5.52 to 34.23 μM. Chalcone 3c displayed the highest cytotoxic activity from all the tested compounds. Cytotoxic effects of compounds were confirmed in the live/dead assay. In addition, DAPI staining revealed that these compounds induce death by apoptosis.ConclusionThe data speculate that chalcone derivatives of 2-acetylthiophene may represent a source of therapeutic agents for human breast cancer.