PDF(Pubmed)
Abstract：
The purpose of the current investigation was to produce cinammaldehyde-based chalcone derivatives (3a-k) to evaluate their potential effectiveness as antioxidant and inhibitory agents versus human Caco-2 cancer cells. The findings obtained using the DPPH assay showed that compound 3e had the highest effective antioxidant activity with the best IC50 value compared with the other compounds. Moreover, the cytotoxic findings revealed that compound 3e was the best compound for inhibiting Caco-2 development in contrast to all other produced derivatives, with the lowest IC50 concentration (32.19 ± 3.92 µM), and it also had no detrimental effects on healthy human lung cells (wi38 cells). Exposure of Caco-2 cells with this IC50 value of compound 3e resulted in a substantial rise in the number of early and late cells that are apoptotic with a significant comet nucleus when compared with control cells employing the annexin V/PI and comet evaluations, respectively. Furthermore, qRT-PCR and ELISA examinations indicated that compound 3e significantly altered the expression of genes and their relative proteins related to apoptosis in the treated Caco-2 cells, thus significantly inhibiting Caco-2 growth through activating Caspase-3 via an intrinsic apoptotic pathway. As a result, compound 3e could serve as an effective therapy for human colon cancer.
摘要：
当前研究的目的是生产基于甲醛的查尔酮衍生物（3a-k），以评估其作为抗氧化剂和抑制剂对人Caco-2癌细胞的潜在有效性。使用DPPH测定获得的发现表明,与其他化合物相比,化合物3e具有最高的有效抗氧化活性和最佳的IC50值。此外，细胞毒性研究结果表明，与所有其他产生的衍生物相比，化合物3e是抑制Caco-2发育的最佳化合物，具有最低IC50浓度（32.19±3.92µM），它对健康的人肺细胞（wi38细胞）也没有有害影响。与使用膜联蛋白V/PI和彗星评估的对照细胞相比，将Caco-2细胞暴露于化合物3e的此IC50值导致早期和晚期细胞的数量大幅增加，并具有显著的彗星核凋亡。分别。此外，qRT-PCR和ELISA检测表明，化合物3e显著改变了Caco-2细胞凋亡相关基因及其相关蛋白的表达，从而通过内在凋亡途径激活Caspase-3显著抑制Caco-2生长。因此,化合物3e可以作为人类结肠癌的有效疗法。
