In vitro and in silico investigations of the pro-apoptotic activity of Opuntia ficus-indica cladode extracts against K562 cells

Şule Öncül, E. Becer, Pınar Mega Tiber, K. Teralı, A. Aykaç
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Abstract

Cladodes of Opuntia ficus-indica (OFI) are thought to be an excellent source of bioactive compounds, making them an aspirant for the manufacture of health-promoting compounds. This study aims at exploring the pro-apoptotic effects of spiny and thornless OFI cladode extracts on the human immortalized myelogenous leukemia cell line (K562). The ethanol extraction method was used for preparing cladode extract. Cytotoxicity was evaluated by MTT assays. Membrane permeability/damage was detected by annexin V-binding assays, and mitochondrial damage/alteration was detected by mitochondrial membrane potential measurements. The protein expression quantities of Bax and Bcl-2 were assessed by Western blotting. The pro-apoptotic potentials of the main spiny and thornless OFI extract constituents were investigated structurally and mechanistically using protein–ligand docking and interaction profiling. Spiny OFI extract displayed a stronger cytotoxic effect than thornless OFI extract on K562 cells. In silico findings agreed with the pro-apoptotic action observed in vitro. Finally, our findings imply that OFI extracts cause apoptosis in K562 cells in order to have anti-cancer effects.
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欧蓬荚果提取物对 K562 细胞促凋亡活性的体外和硅学研究
据认为,Opuntia ficus-indica(OFI)的苞片是生物活性化合物的极佳来源,使其成为生产促进健康的化合物的理想原料。本研究旨在探究有刺和无刺蝙蝠蛾科植物苞片提取物对人类永生化骨髓性白血病细胞系(K562)的促凋亡作用。 采用乙醇萃取法制备药材提取物。细胞毒性通过 MTT 试验进行评估。膜通透性/损伤通过附件素 V 结合试验进行检测,线粒体损伤/改变通过线粒体膜电位测量进行检测。Bax 和 Bcl-2 的蛋白表达量通过 Western 印迹法进行评估。通过蛋白质配体对接和相互作用分析,从结构和机理上研究了有刺和无刺 OFI 提取物主要成分的促凋亡潜能。 与无刺 OFI 提取物相比,有刺 OFI 提取物对 K562 细胞具有更强的细胞毒性作用。硅学研究结果与体外观察到的促凋亡作用一致。 最后,我们的研究结果表明,OFI 提取物会导致 K562 细胞凋亡,从而产生抗癌作用。
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