Bakar-Ates Filiz, Ozkan Erva
Faculty of Pharmacy, Department of Biochemistry, Ankara University, Anadolu, Ankara, 06560, Turkey.
Faculty of Pharmacy, Department of Biochemistry, Ankara Medipol University, Altindag, Ankara, 06050, Turkey.
Naunyn Schmiedebergs Arch Pharmacol. 2025 Apr;398(4):3985-3994. doi: 10.1007/s00210-024-03523-8. Epub 2024 Oct 11.
Ferroptosis is an important regulated cell death mechanism characterized by iron-dependent lipid peroxidation and oxidative stress. In this study, we examined the ferroptosis-inducing effect of the combined use of Paclitaxel, a microtubule-stabilizing agent, and Erastin, a ferroptosis inducer, in breast cancer cells. In this context, the combination of the compounds in question was applied to the cells and the presence of a synergistic effect was determined by calculating the combination index. Glutathione (GSH) levels and glutathione peroxidase (GPX) activity were determined by commercial assay kits, and the effect of the compounds on lipid peroxidation was determined by measurement of malondialdehyde (MDA) levels. Additionally, the effect of combination treatment on ferroptotic protein expression was determined by western blot. Our findings revealed that the combination treatment caused a significant change in mitochondrial function by causing an increase in the depolarized/viable cell population. Additionally, there was a significant increase in intracellular reactive oxygen species (ROS) levels compared to single applications of the compounds. The significant increase observed in malondialdehyde (MDA) levels revealed that the combination treatment increased lipid peroxidation. Moreover, intracellular GSH levels and glutathione peroxidase (GPX) activity significantly decreased by Paclitaxel-Erastin combination. The expression of ferroptosis-regulating proteins was significantly downregulated. The findings showed that the Paclitaxel-Erastin combination synergistically contributed to the accumulation of lipid reactive oxygen species and induced the ferroptotic cell death pathway in breast cancer cells.
铁死亡是一种重要的程序性细胞死亡机制,其特征为铁依赖性脂质过氧化和氧化应激。在本研究中,我们检测了微管稳定剂紫杉醇与铁死亡诱导剂艾拉司丁联合使用对乳腺癌细胞的铁死亡诱导作用。在此背景下,将上述化合物组合应用于细胞,并通过计算组合指数来确定协同效应的存在。使用商业检测试剂盒测定谷胱甘肽(GSH)水平和谷胱甘肽过氧化物酶(GPX)活性,并通过测量丙二醛(MDA)水平来确定化合物对脂质过氧化的影响。此外,通过蛋白质印迹法确定联合治疗对铁死亡相关蛋白表达的影响。我们的研究结果显示,联合治疗通过增加去极化/活细胞群体导致线粒体功能发生显著变化。此外,与单独应用化合物相比,细胞内活性氧(ROS)水平显著升高。丙二醛(MDA)水平的显著升高表明联合治疗增加了脂质过氧化。此外,紫杉醇-艾拉司丁组合显著降低了细胞内GSH水平和谷胱甘肽过氧化物酶(GPX)活性。铁死亡调节蛋白的表达显著下调。研究结果表明,紫杉醇-艾拉司丁组合协同促进了脂质活性氧的积累,并诱导了乳腺癌细胞的铁死亡细胞死亡途径。