New Tacrine Dimers Alleviate the Intracellular Amyloid-β-induced Cognitive Disturbance and Oxidative Stress in Mice.

IF 1.1 4区综合性期刊 Q3 MULTIDISCIPLINARY SCIENCES

Anais da Academia Brasileira de Ciencias Pub Date : 2025-07-25 DOI:10.1590/0001-3765202520241163

Ana Elisa Gonçalves, Otto Spigariol, Luísa M DA Silva, Yuri F Rego, Clara Herrera-Arozamena, María Isabel Rodríguez-Franco, Ângelo DE Fátima, Thiago Henrique Doring, Lucas Augusto Araujo, Maria Lígia R Macedo, Sumbal Saba, Jamal Rafique, Aldo S DE Oliveira, Márcia Maria DE Souza

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引用次数: 0

Abstract

This study aimed to investigate in vivo and ex-vivo the effects of tacrine dimers (TD1, TD2, TD3 and TD4) in mice with Alzheimer's disease (AD) induced by amyloid peptide (Aβ42) and, respectively, evaluated in behavioral tests of cognition, oxidative stress and neuroinflammation. All dimers reduced the cognitive deficit caused by Aβ42, oxidative stress and neuroinflammation, especially the compound TD4. By ADMET analysis (SwissADME and pkCSM 2.10 platforms), TD4 exhibited favorable pharmacokinetic properties with the control drug. The results suggest a therapeutic potential for AD for these compounds, given their distinct cognitive and neuroprotective effects in AD models induced by Aβ42.

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新塔克林二聚体减轻细胞内淀粉样蛋白β诱导的小鼠认知障碍和氧化应激。

本研究旨在探讨他林二聚体（TD1, TD2， TD3和TD4）对淀粉样肽（Aβ42）诱导的阿尔茨海默病（AD）小鼠的体内和体外作用，并分别在认知、氧化应激和神经炎症的行为测试中进行评估。所有二聚体均能降低a - β42引起的认知缺陷、氧化应激和神经炎症，尤其是化合物TD4。通过ADMET分析（SwissADME和pkCSM 2.10平台），TD4与对照药物表现出良好的药动学特性。鉴于这些化合物在a β42诱导的AD模型中具有明显的认知和神经保护作用，研究结果表明这些化合物具有治疗AD的潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Anais da Academia Brasileira de Ciencias 综合性期刊-综合性期刊

CiteScore

2.20

自引率

0.00%

发文量

347

审稿时长

1 months

期刊介绍： The Brazilian Academy of Sciences (BAS) publishes its journal, Annals of the Brazilian Academy of Sciences (AABC, in its Brazilianportuguese acronym ), every 3 months, being the oldest journal in Brazil with conkinuous distribukion, daking back to 1929. This scienkihic journal aims to publish the advances in scienkihic research from both Brazilian and foreigner scienkists, who work in the main research centers in the whole world, always looking for excellence. Essenkially a mulkidisciplinary journal, the AABC cover, with both reviews and original researches, the diverse areas represented in the Academy, such as Biology, Physics, Biomedical Sciences, Chemistry, Agrarian Sciences, Engineering, Mathemakics, Social, Health and Earth Sciences.