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天然来源的非碱性胆碱酯酶抑制剂化合物。

Non-Alkaloid Cholinesterase Inhibitory Compounds from Natural Sources.

机构信息

School of Chemical Engineering and Mineral Industries, University of Ngaoundere, 454 Ngaoundere, Cameroon.

Department of Chemistry, Mugla Sitki Kocman University, Mugla 48000, Turkey.

出版信息

Molecules. 2021 Sep 14;26(18):5582. doi: 10.3390/molecules26185582.

DOI:10.3390/molecules26185582
PMID:34577053
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8472022/
Abstract

Alzheimer's disease (AD) is a severe neurodegenerative disorder of different brain regions accompanied by distresses and affecting more than 25 million people in the world. This progressive brain deterioration affects the central nervous system and has negative impacts on a patient's daily activities such as memory impairment. The most important challenge concerning AD is the development of new drugs for long-term treatment or prevention, with lesser side effects and greater efficiency as cholinesterases inhibitors and the ability to remove amyloid-beta(Aβ) deposits and other related AD neuropathologies. Natural sources provide promising alternatives to synthetic cholinesterase inhibitors and many have been reported for alkaloids while neglecting other classes with potential cholinesterase inhibition. This review summarizes information about the therapeutic potential of small natural molecules from medicinal herbs, belonging to terpenoids, coumarins, and phenolic compounds, and others, which have gained special attention due to their specific modes of action and their advantages of low toxicity and high efficiency in the treatment of AD. Some show superior drug-like features in comparison to synthetic cholinesterase inhibitors. We expect that the listed phytoconstituents in this review will serve as promising tools and chemical scaffolds for the discovery of new potent therapeutic leads for the amelioration and treatment of Alzheimer's disease.

摘要

阿尔茨海默病(AD)是一种严重的神经退行性疾病,影响着全球超过 2500 万人。这种进行性的大脑恶化影响着中枢神经系统,对患者的日常活动如记忆力产生负面影响。AD 面临的最重要的挑战是开发新的药物进行长期治疗或预防,这些药物的副作用更小、效率更高,如乙酰胆碱酯酶抑制剂,以及清除淀粉样蛋白-β(Aβ)沉积和其他相关 AD 神经病理学的能力。天然来源为合成乙酰胆碱酯酶抑制剂提供了有前途的替代品,许多生物碱已被报道,而其他具有潜在乙酰胆碱酯酶抑制作用的类别的报道却很少。本文综述了来自药用植物的小分子天然化合物的治疗潜力,这些化合物属于萜类、香豆素和酚类化合物等,由于其特定的作用模式以及在治疗 AD 方面毒性低、效率高的优点,引起了人们的特别关注。一些化合物在药物样特征方面优于合成的乙酰胆碱酯酶抑制剂。我们期望本文中列出的植物成分将成为发现新的、有效的治疗阿尔茨海默病的潜在治疗靶点的有前途的工具和化学支架。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e688/8472022/86d9a3320a9d/molecules-26-05582-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e688/8472022/86d9a3320a9d/molecules-26-05582-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e688/8472022/86d9a3320a9d/molecules-26-05582-g001.jpg

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