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β-倒捻子素衍生物的设计、合成及乙酰胆碱酯酶抑制活性。

Design, synthesis and cholinesterase inhibitory activity of -mangostin derivatives.

机构信息

State Key Laboratory of Phytochemistry and Plant Resources in West China, and Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, People' s Republic of China.

University of Chinese Academy of Sciences, Beijing, People's Republic of China.

出版信息

Nat Prod Res. 2020 May;34(10):1380-1388. doi: 10.1080/14786419.2018.1510925. Epub 2018 Nov 20.

Abstract

-mangostin, a polyphenol xanthone derivative, was mainly isolated from pericarps of the mangosteen fruit ( L.). In present investigation, a series of derivatives were designed, synthesised and evaluated for their inhibitory activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among the synthesised xanthones, compounds , , and showed AChE selective inhibitory activity, was a BuChE selective inhibitor while , , , , , and were dual inhibitors. The most potent inhibitor of AChE was while was the most potent inhibitor of BuChE with IC values of 5.26 M and 7.55 M respectively.

摘要

-山竹素,一种多酚类的呫吨酮衍生物,主要从山竹果皮(L.)中分离得到。在目前的研究中,设计、合成了一系列衍生物,并对其乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BuChE)抑制活性进行了评价。在所合成的呫吨酮中,化合物 、 、 和 对乙酰胆碱酯酶具有选择性抑制活性, 是丁酰胆碱酯酶的选择性抑制剂,而 、 、 、 、 、 是双重抑制剂。对乙酰胆碱酯酶抑制活性最强的化合物是 ,对丁酰胆碱酯酶抑制活性最强的化合物是 ,IC 值分别为 5.26 μM 和 7.55 μM。

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