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Naturally Occurring Acetylcholinesterase Inhibitors and Their Potential Use for Alzheimer's Disease Therapy

机译:天然存在的乙酰胆碱酯酶抑制剂及其在阿尔茨海默氏病治疗中的潜在用途

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摘要

Alzheimer's disease (AD) is a main cause of dementia, accounting for up to 75% of all dementia cases. Pathophysiological processes described for AD progression involve neurons and synapses degeneration, mainly characterized by cholinergic impairment. This feature makes acetylcholinesterase inhibitors (AChEi) the main class of drugs currently used for the treatment of AD dementia phase, among which galantamine is the only naturally occurring substance. However, several plant species producing diverse classes of alkaloids, coumarins, terpenes, and polyphenols have been assessed for their anti-AChE activity, becoming potential candidates for new anti-AD drugs. Therefore, this mini-review aimed to recapitulate last decade studies on the anti-AChE activity of plant species, their respective extracts, as well as isolated compounds. The anti-AChE activity of extracts prepared from 54 plant species pertaining 29 families, as well as 36 isolated compounds were classified and discussed according to their anti-AChE pharmacological potency to highlight the most prominent ones. Besides, relevant limitations, such as proper antioxidant assessment, and scarcity of toxicological and clinical studies were also discussed in order to help researchers out with the bioprospection of potentially new AChEi.
机译:阿尔茨海默氏病(AD)是痴呆症的主要原因,占所有痴呆症病例的75%。描述为AD进展的病理生理过程涉及神经元和突触变性,其主要特征在于胆碱能障碍。此功能使乙酰胆碱酯酶抑制剂(AChEi)成为当前用于治疗AD痴呆期的主要药物,其中加兰他敏是唯一的天然物质。但是,已经评估了几种产生不同种类的生物碱,香豆素,萜烯和多酚的植物物种的抗AChE活性,成为新的抗AD药物的潜在候选者。因此,本小型综述旨在概述植物物种,其各自提取物以及分离出的化合物的抗AChE活性的最新十年研究。从29个科的54种植物中提取的提取物以及36种分离的化合物的抗AChE活性根据其抗AChE药理效力进行了分类和讨论,以突出最突出的化合物。此外,还讨论了相关的局限性,例如适当的抗氧化剂评估以及缺乏毒理学和临床研究,以帮助研究人员摆脱潜在的新型AChEi的生物勘探。

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