Department of Chemistry, College of Chemistry and Materials Science, Jinan University, Guangzhou 510632, China.
Mar Drugs. 2022 Feb 22;20(3):158. doi: 10.3390/md20030158.
In this paper, eight new galaxamide analogues (~) were synthesized and evaluated for their cytotoxic activities against five cancer cell lines, MCF-7, MD-MBA-231, HepG2, Hela, and A549, using MTT assays. The modified analogue displayed broad spectrum cytotoxic activity toward each tested cell line with IC values of 1.65 ± 0.30 (MCF-7), 2.91 ± 0.17 (HepG2), 4.59 ± 0.27 (MD-MBA-231), 5.69 ± 0.37 (Hela), and 5.96 ± 0.41 (A549) μg/mL, respectively. The galaxamides and induced concentration-dependent apoptosis of the MCF-7 cells after 72 h as evaluated by the flow cytometry experiment. The results showed that these compounds could induce MCF-7 cell apoptosis by arresting the G0/G1 phase of the cell cycle and finally achieving the effect of inhibiting the proliferation of MCF-7 cells.
在这项研究中，合成了 8 种新的半乳糖胺类似物（~），并通过 MTT 法评估了它们对 MCF-7、MD-MBA-231、HepG2、Hela 和 A549 这 5 种癌细胞系的细胞毒性。经测试，结构修饰后的类似物 对每种测试的细胞系均表现出广谱的细胞毒性，其 IC 值分别为 1.65 ± 0.30（MCF-7）、2.91 ± 0.17（HepG2）、4.59 ± 0.27（MD-MBA-231）、5.69 ± 0.37（Hela）和 5.96 ± 0.41（A549）μg/mL。半乳糖胺类似物 和 可诱导 MCF-7 细胞凋亡，其浓度依赖性在 72 h 后通过流式细胞术实验得到证实。结果表明，这些化合物可通过将细胞周期的 G0/G1 期阻滞并最终达到抑制 MCF-7 细胞增殖的效果来诱导 MCF-7 细胞凋亡。
