Doctoral Program, Faculty of Medicine, Public Health and Nursing (FKKMK), Universitas Gadjah Mada, Yogyakarta, Indonesia.
Department of Biomedicine, Faculty of Medicine, Universitas Mataram, Indonesia.
Asian Pac J Cancer Prev. 2023 Feb 1;24(2):683-691. doi: 10.31557/APJCP.2023.24.2.683.
Chalcone-3 has been shown to be cytotoxic and selective against luminal subtype breast cancer cell lines, which are suspected to occur through the mechanism of epidermal growth factor receptors (EGFR) inhibition. However, the cytotoxic effect has never been tested on cell strains from patients with triple negative breast cancer (TNBC), where EGFR expression is known to increase. This study aimed to identify the role of chalcone-3 in one of the downstream targets of EGFR as an antiproliferative agent.
Chalcone-3 was examined for its effect on proliferation in human breast cancer MDA-MB-231 cell lines. The percentage of proliferation inhibition was analyzed using methyl-thiazol tetrazolium assay. Flow cytometry was used to analyze the population of cell cycle distribution and the expression of cyclin-D1 and pEGFR.
Chalcone-3 inhibited the proliferation of MDA-MB-231 cells in a dose and time-dependent manner with an IC50 value of 17.98±6.36 µg/mL by inducing cell cycle arrest at the G2/M phase. Flow cytometry assays showed that chalcone-3 significantly reduced the expression of pEGFR and cyclin-D1, contributing to cell cycle arrest.
Chalcone-3 might have potential as an anti-proliferative drug to treat TNBC.
查尔酮-3 已被证明具有细胞毒性，并对腔型乳腺癌细胞系具有选择性，其作用机制疑似为抑制表皮生长因子受体 (EGFR)。然而，这种细胞毒性作用从未在三阴性乳腺癌 (TNBC) 患者的细胞株上进行过测试，已知 EGFR 表达在 TNBC 中增加。本研究旨在确定查尔酮-3 作为一种抗增殖剂在 EGFR 的下游靶标之一中的作用。
研究了查尔酮-3 对人乳腺癌 MDA-MB-231 细胞系增殖的影响。使用甲基噻唑四唑测定法分析增殖抑制百分比。流式细胞术用于分析细胞周期分布和细胞周期蛋白 D1 和 pEGFR 的表达。
查尔酮-3 以剂量和时间依赖的方式抑制 MDA-MB-231 细胞的增殖，IC50 值为 17.98±6.36µg/mL，通过诱导 G2/M 期细胞周期停滞。流式细胞术分析表明，查尔酮-3 显著降低了 pEGFR 和细胞周期蛋白 D1 的表达，导致细胞周期停滞。
查尔酮-3 可能具有作为治疗三阴性乳腺癌的抗增殖药物的潜力。
