Karaosmanoğlu Oğuzhan, Berber Halil, Sivas Hülya, Uysal Ulku Dilek
Department of Biology, Faculty of Science, Eskişehir Technical University, Eskişehir, Turkey. Department of Biology, Kamil Özdağ Faculty of Science, Karamanoğlu Mehmetbey University, Karaman, Turkey.
Department of Chemistry, Faculty of Science, Eskişehir Technical University, Eskişehir, Turkey.
Cell Biochem Biophys. 2025 Jul 16. doi: 10.1007/s12013-025-01826-y.
Chemotherapy resistance is a major obstacle in cancer; thus, the development of new anticancer agents is being studied with great importance. Schiff bases containing an azomethine group have been widely used in various pharmaceutical applications. Here, five Schiff base derivatives of 2-hydroxybenzaldehyde (8S1-8S5) were synthesized and characterized. Their cytotoxicity was screened against six cancerous and two normal cell lines using a neutral red uptake assay. The apoptotic mechanism of the compound 8S3 in MCF-7 cells was evaluated through a combination of cell cycle analysis, measurement of mitochondrial membrane potential, reactive oxygen species levels, caspase activity, analysis of gene expression in the mitogen-activated protein kinase (MAPK) signalling pathway, and in silico analysis studies. Treatment of the cells with 8S3 resulted in an increase in sub-G0/G1 populations and MMP disruption. The expressions of 30 genes involved in MAPK signalling were upregulated, while 10 genes were downregulated in these cells. This transcriptional profile supports a MAPK-mediated apoptotic response and highlights 8S3's potential to overcome chemoresistance by disrupting key survival MAPK signalling pathways. 8S3 might induces apoptosis through a mechanism involving modulation of MAPK pathway and mitochondrial dysfunction, in a ROS-independent manner. Results highlight 8S3's potential as a candidate for further development of anti-cancer drugs in cancer therapy.
化疗耐药是癌症治疗中的一个主要障碍;因此,新型抗癌药物的研发正受到高度重视。含有甲亚胺基团的席夫碱已广泛应用于各种药物领域。在此,合成并表征了2-羟基苯甲醛的五种席夫碱衍生物(8S1 - 8S5)。使用中性红摄取试验对六种癌细胞系和两种正常细胞系进行了细胞毒性筛选。通过细胞周期分析、线粒体膜电位测量、活性氧水平、半胱天冬酶活性测定、丝裂原活化蛋白激酶(MAPK)信号通路基因表达分析以及计算机模拟分析研究相结合的方式,评估了化合物8S3在MCF - 7细胞中的凋亡机制。用8S3处理细胞导致亚G0/G1期细胞群体增加和线粒体膜电位破坏。参与MAPK信号传导的30个基因的表达上调,而这些细胞中有10个基因表达下调。这种转录谱支持MAPK介导的凋亡反应,并突出了8S3通过破坏关键的存活MAPK信号通路来克服化疗耐药的潜力。8S3可能通过一种不依赖活性氧的机制,通过调节MAPK途径和线粒体功能障碍来诱导细胞凋亡。结果突出了8S3作为癌症治疗中抗癌药物进一步开发候选物的潜力。