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