Kaur Darshpreet, Grewal Amarjot Kaur, Almasoudi Suad Hamdan, Almehmadi Ahmad H, Alsfouk Bshra A, Kumar Amit, Singh Varinder, Alexiou Athanasios, Papadakis Marios, Welson Nermeen N, Singh Thakur Gurjeet, El-Saber Batiha Gaber
Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India.
Department of Biology, College of Sciences, Umm Al-Qura University, 21955, Makkah, Saudi Arabia.
Sci Rep. 2025 Aug 7;15(1):28963. doi: 10.1038/s41598-025-13920-5.
Alzheimer's disease (AD) is responsible for more than 80% of cases of dementia in senior individuals globally. In the current study, the role of modulation of the FGF1/PI3K/Akt pathway in the protective effect of tozasertib was evaluated. Experimental dementia was induced in mice by injecting streptozotocin (STZ) intracerebroventricularly. Various biochemical parameters for oxidative stress & lipid peroxidation (SOD, GSH, catalase, TBARS), neuroinflammation (MPO, IL-6, IL-1 β, TNF-α, NFκB), apoptotic markers (Bax, Bcl-2, Caspase-3), and memory parameters (AChE activity, β1-40 levels) were assessed. The behavioral parameters evaluated included the Morris Water Maze test and the step-down passive avoidance test. Histological changes were assessed using H&E staining. ICV STZ-induced AD resulted in increased oxidative stress, lipid peroxidation, neuroinflammation, apoptosis, and decreased learning and memory. The results showed that administration of tozasertib improved memory, decreased levels of oxidative stress, inflammatory parameters, and apoptotic markers, and improved histological parameters in a dose-dependent manner. Pre-administration of LY294002, a PI3K/Akt pathway inhibitor, partially reversed the protective effects of Tozasertib, suggesting possible involvement of this pathway. However, as the mechanism was inferred primarily through pharmacological antagonism, further studies including direct molecular assessments (e.g. p-Akt/t-Akt) are warranted to confirm the role of FGF1/PI3K/Akt signaling in Tozasertib's action.
阿尔茨海默病(AD)导致了全球老年人群中80%以上的痴呆病例。在本研究中,评估了FGF1/PI3K/Akt通路调节在托扎司他保护作用中的作用。通过脑室内注射链脲佐菌素(STZ)在小鼠中诱导实验性痴呆。评估了氧化应激和脂质过氧化的各种生化参数(超氧化物歧化酶、谷胱甘肽、过氧化氢酶、硫代巴比妥酸反应物)、神经炎症(髓过氧化物酶、白细胞介素-6、白细胞介素-1β、肿瘤坏死因子-α、核因子κB)、凋亡标志物(Bax、Bcl-2、半胱天冬酶-3)以及记忆参数(乙酰胆碱酯酶活性、β1-40水平)。评估的行为参数包括莫里斯水迷宫试验和被动回避试验。使用苏木精-伊红染色评估组织学变化。脑室内注射STZ诱导的AD导致氧化应激增加、脂质过氧化、神经炎症、细胞凋亡,并导致学习和记忆能力下降。结果表明,托扎司他给药可改善记忆,降低氧化应激水平、炎症参数和凋亡标志物,并以剂量依赖方式改善组织学参数。PI3K/Akt通路抑制剂LY294002的预先给药部分逆转了托扎司他的保护作用,提示该通路可能参与其中。然而,由于该机制主要是通过药理学拮抗作用推断出来的,因此需要进一步的研究,包括直接的分子评估(如磷酸化Akt/总Akt),以确认FGF1/PI3K/Akt信号在托扎司他作用中的作用。