Gamal Nourhan M, Bakly Wesam El, Saad Sherin S T, Waseef Dalia A A El, El-Shal Amal S, Ezzat Wessam, Magdy Yosra M
Clinical Pharmacology Department, Faculty of Medicine, Ain-Shams University, Cairo, Egypt.
Clinical Pharmacology Department, Armed Forces College of Medicine, Cairo, Egypt.
Naunyn Schmiedebergs Arch Pharmacol. 2025 May 21. doi: 10.1007/s00210-025-04136-5.
Chronic stress is recognized as a risk factor for neurodegeneration. Sodium glucose co-transporter 2 receptors (SGLT2) have been found in various brain regions, suggesting the potential neuroprotective properties of SGLT2 inhibitors as dapagliflozin (DGF). This study aimed to investigate the effect of DGF on behavioral, and neurodegenerative changes in chronic restraint stress (CRS) as an animal model of cognitive impairment. Forty-eight male rats were allocated into four groups: Control; CRS-subjected group, rats were subjected to chronic restraint stress for 6 weeks to induce cognitive impairment; DGF-treated CRS group, dapagliflozin was given daily by oral gavage; and DGF-administered group. Behavioral tests were performed and fasting serum glucose, insulin, and corticosterone levels were measured. Hippocampal oxidative markers, insulin signaling, mitochondrial function, amyloid beta, p-tau, and brain-derived neurotrophic factor (BDNF) gene expression were evaluated. DGF significantly prevented CRS-induced cognitive dysfunction (Y maze and Morris water maze tests). Also, DGF ameliorated hippocampal neurodegenerative changes by decreasing tau and amyloid beta levels, while increasing BDNF gene expression. DGF reduced hippocampal phosphorylated mammalian target of rapamycin (p-mTOR) and protein kinase B (p-Akt) levels. In addition to its antioxidant effects, DGF increased ATP levels and cytochrome C oxidase activity. These findings were confirmed by transmission electron microscopic (TEM) examination. The current study demonstrates a biological link between chronic stress, insulin resistance, and cognitive impairment. Dapagliflozin has therapeutic potential in alleviating cognitive deficits and neurodegeneration primarily due to its insulin-sensitizing and antioxidant properties, along with its capacity to enhance mitochondrial function.
慢性应激被认为是神经退行性变的一个危险因素。已在多个脑区发现钠葡萄糖协同转运蛋白2受体(SGLT2),这表明SGLT2抑制剂(如达格列净,DGF)具有潜在的神经保护特性。本研究旨在探讨DGF对作为认知障碍动物模型的慢性束缚应激(CRS)中行为及神经退行性变的影响。48只雄性大鼠被分为四组:对照组;CRS组,大鼠接受6周的慢性束缚应激以诱导认知障碍;DGF治疗的CRS组,每天经口灌胃给予达格列净;以及DGF给药组。进行行为测试并测量空腹血清葡萄糖、胰岛素和皮质酮水平。评估海马体氧化标志物、胰岛素信号传导、线粒体功能、β淀粉样蛋白、磷酸化tau蛋白(p-tau)和脑源性神经营养因子(BDNF)基因表达。DGF显著预防了CRS诱导的认知功能障碍(Y迷宫和莫里斯水迷宫测试)。此外,DGF通过降低tau蛋白和β淀粉样蛋白水平,同时增加BDNF基因表达,改善了海马体神经退行性变。DGF降低了海马体中磷酸化的雷帕霉素靶蛋白(p-mTOR)和蛋白激酶B(p-Akt)水平。除了其抗氧化作用外,DGF还增加了ATP水平和细胞色素C氧化酶活性。这些发现通过透射电子显微镜(TEM)检查得到证实。本研究证明了慢性应激、胰岛素抵抗和认知障碍之间的生物学联系。达格列净在减轻认知缺陷和神经退行性变方面具有治疗潜力,这主要归因于其胰岛素增敏和抗氧化特性,以及增强线粒体功能的能力。