Suppr超能文献

三疣棱子蟹酚类化合物富分组分的分子对接及对东莨菪碱诱导的阿尔茨海默病样条件下认知障碍的影响。

Molecular Docking and Cognitive Impairment Attenuating Effect of Phenolic Compound Rich Fraction of Trianthema portulacastrum in Scopolamine Induced Alzheimer's Disease Like Condition.

机构信息

Bioorganic & Medicinal Chemistry Research Laboratory, Department of Pharmaceutical Sciences, Sam Higginbottom University of Agriculture, Technology & Sciences (SHUATS), Allahabad, 211007, India.

Bharat Technology, Uluberia, Howrah, 711316, India.

出版信息

Neurochem Res. 2019 Jul;44(7):1665-1677. doi: 10.1007/s11064-019-02792-7. Epub 2019 Apr 4.

Abstract

Dementia is considered as the frequent cause of neurodegenerative mental disorder such as Alzheimer's disease (AD) amongst elderly people. Free radicals as well as cholinergic deficit neurons within nucleus basalis magnocellularis demonstrated to attribute with aggregation of β amyloid which further acts as an essential hallmark in AD. Various phenolic phytoconstituents exists in Trianthema portulastrum (TP) leaves have been reported as active against various neurological disorders. The current investigation was undertaken to evaluate the antiamnesic potential of butanol fraction of TP hydroethanolic extract (BFTP) by utilizing rodent models of elevated plus maze (EPM) and Hebbs William Maze (HWM) along with in vitro and in vivo antioxidant as well as acetylcholinesterase (AChE) inhibition studies. Molecular docking studies were also performed for evaluation of molecular interaction of existed phenolic compounds in BFTP. In vitro antioxidant study revealed concentration dependant strong ability of BFTP to inhibit free radicals. In vitro AChE inhibition study showed competitive type of inhibition kinetics. BFTP significantly reversed (p < 0.005 versus scopolamine) the damaging effect of scopolamine by reducing TL (Transfer Latency) and TRC (Time taken to recognize the reward chamber) in the EPM and HWM, respectively. BFTP also contributed towards increased (p < 0.005 versus scopolamine) enzymatic antioxidant as well as hippocampal acetylcholine (ACh) levels. Histological studies also supported the results as BFTP pretreated mice significantly reversed the scopolamine induced histological changes in hippocampal region. Docking studies confirmed chlorogenic acid has the most significant binding affinity towards AChE. This research finding concludes that BFTP could be a beneficial agent for management of cognition and behavioral disorders associated with AD.

摘要

痴呆被认为是老年人神经退行性精神障碍(如阿尔茨海默病(AD))的常见原因。自由基本以及基底核大细胞神经胆碱能缺陷被证明与β淀粉样蛋白的聚集有关,β淀粉样蛋白进一步成为 AD 的重要标志。三角叶车前草(TP)叶中存在的各种酚类植物成分已被报道对各种神经障碍具有活性。本研究旨在通过利用高架十字迷宫(EPM)和 Hebbs William Maze(HWM)的啮齿动物模型,以及体外和体内抗氧化和乙酰胆碱酯酶(AChE)抑制研究,评估 TP 水醇提取物的丁醇部分(BFTP)的抗健忘潜力。还进行了分子对接研究,以评估 BFTP 中存在的酚类化合物的分子相互作用。体外抗氧化研究表明,BFTP 具有浓度依赖性的强能力,可抑制自由基。体外 AChE 抑制研究显示出竞争性抑制动力学。BFTP 显著逆转了东莨菪碱对 EPM 和 HWM 中转移潜伏期(TL)和识别奖励室时间(TRC)的损害作用(与东莨菪碱相比,p <0.005)。BFTP 还增加了(与东莨菪碱相比,p <0.005)酶抗氧化剂和海马乙酰胆碱(ACh)水平。组织学研究也支持了这一结果,因为 BFTP 预处理的小鼠显著逆转了海马区域中东莨菪碱诱导的组织学变化。对接研究证实绿原酸对 AChE 具有最显著的结合亲和力。这项研究结果表明,BFTP 可能是管理与 AD 相关的认知和行为障碍的有益药物。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验