Abstract

A few organic synthetic drugs, such as donepezil, rivastigmine and tacrine, are used for inhibition of acetylcholinesterase (AChE) can provide palliative treatment without generally affecting the progression of the disease, however, sometimes at the cost of severe side effects. Flavonoids and flavonoid glycosides are the potential natural compounds from plants and foods for the treatment of Alzheimer’s disease (AD). In this study, the affinity of nine kaempferol and its glycosides on AChE were evaluated, and their interactions with flavonoids by molecular docking were predicted. Results indicated that Kaempferol exhibited the highest affinity to inhibit the activity of AChE. Besides, kaempferol-3-O-rhamnoside showed good AChE affinity among kaempferol monoglycosides. Kaempferol-3-O-glucorhamnoside and kaempferol-3-O-gentiobioside showed some AChE affinity among kaempferol diglycosides. We can conclude that these compounds are a promising class of AChE inhibitors for the treatment of AD and deserve further study.

中文翻译：

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类黄酮和类黄酮糖苷中乙酰胆碱酯酶抑制剂的探索

摘要

一些有机合成药物，例如多奈哌齐，利凡斯的明和他克林，被用于抑制乙酰胆碱酯酶（AChE），可以在不影响疾病进展的情况下提供姑息治疗，但有时会以严重的副作用为代价。类黄酮和类黄酮糖苷是来自植物和食品的潜在天然化合物，可用于治疗阿尔茨海默氏病（AD）。在这项研究中，评估了九种山emp酚及其糖苷对AChE的亲和力，并通过分子对接预测了它们与类黄酮的相互作用。结果表明，Kaempferol对抑制AChE的活性具有最高的亲和力。此外，山奈酚-3-O-鼠李糖苷在山奈酚单糖苷之间显示出良好的AChE亲和力。Kaempferol-3-O-glucorhamnoside和Kaempferol-3-O-gentiobioside显示在Kaempferol diglycosides之间有一些AChE亲和力。我们可以得出结论，这些化合物是用于治疗AD的有前途的AChE抑制剂，值得进一步研究。