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PMID: 41864079 已发表 · ppublish 英语

Acetylcholine-protective activity of chemo-enzymatically synthesized aryl vicinal diols and hydroxy ketones.

Bioorganic chemistry ·第 175 卷 ·2026-07-05

Grzelczyk J, Pérez-Sánchez H, Carmena-Bargueño M, Gałązka-Czarnecka I, Budryn G, Hernik D, Brenna E, Boratyński F

摘要

Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are the main enzymes responsible for the development and progression of Alzheimer's disease (AD). AChE and BChE hydrolyze acetylcholine (ACh), disrupting its management in neurotransmitters. In order to prevent and alleviate the symptoms of AD, the use of new compounds, chemo-enzymatically synthesized in environmentally friendly method from propenylbenzene derivatives as AChE and BChE inhibitors has been proposed. Molecular modeling and isothermal titration calorimetry were used to determine the AChE and BChE inhibition parameters. It has been observed that diols and hydroxy ketones have a significant inhibitory effect. In particular, 1-(4-hydroxy-3-methoxyphenyl)propane-1,2-diol showed inhibitory effects in both research models. The results indicate that diols and hydroxy ketones bind to AChE and BChE at the active site. This further suggests that these compounds could potentially be used in supplements or functional foods to prevent AD.

关键词
Acetylcholinesterase Alzheimer's disease Butyrylcholinesterase Green synthesis Inhibition Isothermal titration calorimetry
文献信息
期刊
Bioorganic chemistry
期刊简称
Bioorg Chem
ISSN
1090-2120
发表日期
2026-07-05
语言
英语
国家/地区
United States
NLM ID
1303703
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