In Vitro and In Vivo Effects of Synthesis Novel Phenoxyacetamide Derivatives as Potent Apoptotic Inducer against HepG2 Cells through PARP-1 Inhibition
作者:Mai M. Sayed、Zohour I. Nabil、Nahla S. El-Shenawy、Rasha A. Al-Eisa、Mohamed S. Nafie
DOI:10.3390/ph16111524
日期:——
potential cytotoxic agents, new semi-synthetic phenoxy acetamide derivatives, compound I and compound II, were synthesized, characterized, and screened for their cytotoxic activity against breast cancer (MCF-7) and liver cancer (HepG2) cell lines. The two compounds were more promising against HepG2 than the MCF-7 cell line according to IC50 values. When tested against the HepG2 cell line, compound I, and
为了发现潜在的细胞毒剂,我们合成、表征了新的半合成苯氧基乙酰胺衍生物化合物 I 和化合物 II,并筛选了它们对乳腺癌 (MCF-7) 和肝癌 (HepG2) 细胞系的细胞毒活性。根据 IC50 值,这两种化合物比 MCF-7 细胞系更有希望对抗 HepG2。当针对 HepG2 细胞系进行测试时,与参考药物 5-氟尿嘧啶 (5-FU) 相比,化合物 I 和化合物 II 均具有显着增加的细胞毒活性,化合物的 IC50 值为 1.43 M、5.32 M 和 6.52 M分别为1、5-FU和化合物II。此外,与正常细胞相比,化合物 I 对癌细胞表现出一定程度的选择性。化合物I显着增强HepG2总凋亡细胞死亡,增加约24.51倍。根据细胞周期分析,化合物 I 诱导细胞周期 G1/S 期停滞并阻断 HepG2 细胞的进展。应用 RT-PCR 技术实现了促凋亡基因的高度显着上调。抗凋亡基因显着下调。有内