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使用计算机模拟、体外和体内方法评估紫红素的散发性抗阿尔茨海默病活性。

Evaluation of the Sporadic Anti-Alzheimer's Activity of Purpurin Using In Silico, In Vitro, and In Vivo Approaches.

作者信息

Rustage Kajol, Rai Nitish, Sinha Saurabh Kumar, Goyal Juhi, Chouhan Pragati, Baniya Bhuvanesh, Dubey Deepti, Singhal Runjhun, Malani Pooja, Pareek Aaushi, Pant Malvika, Jain Smita, Bisht Akansha, Pareek Ashutosh, Ratan Yashumati, Ashraf Ghulam Md, Jain Vivek

机构信息

Department of Pharmaceutical Sciences, Mohan Lal Sukhadia University, Udaipur, 313001, India.

Department of Biotechnology, Mohan Lal Sukhadia University, Udaipur, 313001, India.

出版信息

Mol Neurobiol. 2025 Apr 10. doi: 10.1007/s12035-025-04910-9.

Abstract

Purpurin, a naturally occurring compound found in certain plants, has demonstrated promising neuroprotective effects in the context of Alzheimer's disease (AD). This study investigated the efficacy of purpurin in mitigating neurodegenerative changes induced by streptozotocin (3 mg/kg ICV) and amyloid beta (20 μM) in murine models. Neuroprotective effects were assessed through in vitro and in vivo experiments complemented by in silico simulation studies. SH-SY5Y cell viability, behavioral, biochemical, and histopathological studies were also conducted. The results revealed that purpurin interacts with acetylcholinesterase (AChE) and amyloid-beta (Aβ), exhibiting glide scores of - 10.72 and - 3.05 kcal/mol, respectively. Purpurin (8 μM) significantly alleviated Aβ-induced cellular damage by decreasing malondialdehyde production and enhancing superoxide dismutase and Thio barbituric acid reactive substances levels in a dose-dependent manner. Intraperitoneal administration of purpurin at 50 mg/kg significantly improved both long-term and short-term memory and enhanced social interactions. These benefits were linked to the reductions in AChE activity and oxidative and inflammatory marker levels triggered by streptozotocin. Neuroprotective effects were also supported by restoring neuronal DNA content in the hippocampus, cerebellum and prefrontal cortex. Histological findings further corroborated the reduction in neurodegenerative marker levels. In silico simulations supported these findings by indicating that purpurin primarily binds to the Trp 286 and Tyr 341 residues of AChE, inhibiting its catalytic activity at the peripheral anionic site. In conclusion, the neuroprotective activity of purpurin in AD models is attributed to its inhibitory effects on AChE, coupled with reductions in inflammation and oxidative stress and the restoration of neuronal DNA integrity in critical brain regions.

摘要

紫红素是一种存在于某些植物中的天然化合物,在阿尔茨海默病(AD)背景下已显示出有前景的神经保护作用。本研究调查了紫红素在减轻链脲佐菌素(3 mg/kg脑室内注射)和β-淀粉样蛋白(20 μM)诱导的小鼠模型神经退行性变化方面的功效。通过体外和体内实验,并辅以计算机模拟研究来评估神经保护作用。还进行了SH-SY5Y细胞活力、行为、生化和组织病理学研究。结果显示,紫红素与乙酰胆碱酯酶(AChE)和β-淀粉样蛋白(Aβ)相互作用,其滑行分数分别为-10.72和-3.05 kcal/mol。紫红素(8 μM)通过降低丙二醛生成并以剂量依赖方式提高超氧化物歧化酶和硫代巴比妥酸反应性物质水平,显著减轻了Aβ诱导的细胞损伤。以50 mg/kg腹腔注射紫红素可显著改善长期和短期记忆,并增强社交互动。这些益处与链脲佐菌素引发的AChE活性以及氧化和炎症标志物水平降低有关。海马体、小脑和前额叶皮质中神经元DNA含量的恢复也支持了神经保护作用。组织学结果进一步证实了神经退行性标志物水平的降低。计算机模拟通过表明紫红素主要与AChE的Trp 286和Tyr 341残基结合,在周边阴离子位点抑制其催化活性,支持了这些发现。总之,紫红素在AD模型中的神经保护活性归因于其对AChE的抑制作用,以及炎症和氧化应激的减轻以及关键脑区神经元DNA完整性的恢复。

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