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基于碘化丙啶的多胺配体作为乙酰胆碱酯酶和乙酰胆碱酯酶诱导的β-淀粉样蛋白聚集的有效抑制剂。

Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.

作者信息

Bolognesi Maria Laura, Andrisano Vincenza, Bartolini Manuela, Banzi Rita, Melchiorre Carlo

机构信息

Alma Mater Studiorum, University of Bologna, Department of Pharmaceutical Sciences, Via Belmeloro 6, 40126 Bologna, Italy.

出版信息

J Med Chem. 2005 Jan 13;48(1):24-7. doi: 10.1021/jm049156q.

DOI:10.1021/jm049156q
PMID:15633997
Abstract

Heterodimers 4 and 5 were effective inhibitors of acetylcholinesterase (AChE) activity and AChE-induced amyloid-beta (A beta) aggregation. The peculiar biological profile of 4 can be relevant in studying the molecular basis underlying the nonclassical action of AChE and in addressing the question whether AChE inhibitors can affect the neurotoxic cascade leading to Alzheimer's disease. Compound 4 emerged as the most potent heterodimer so far available to inhibit AChE-induced A beta aggregation.

摘要

异二聚体4和5是乙酰胆碱酯酶（AChE）活性及AChE诱导的β-淀粉样蛋白（Aβ）聚集的有效抑制剂。4独特的生物学特性可能与研究AChE非经典作用的分子基础以及解答AChE抑制剂是否能影响导致阿尔茨海默病的神经毒性级联反应这一问题相关。化合物4是目前已知抑制AChE诱导的Aβ聚集最有效的异二聚体。

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