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

Abstract

α-mangostin, a polyphenol xanthone derivative, was mainly isolated from pericarps of the mangosteen fruit (Garcinia mangostana L.). In present investigation, a series of derivatives were designed, synthesised and evaluated in vitro for their inhibitory activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among the synthesised xanthones, compounds 1, 9, 13 and 16 showed AChE selective inhibitory activity, 15 was a BuChE selective inhibitor while 2, 3, 5, 6, 7, 12 and 14 were dual inhibitors. The most potent inhibitor of AChE was 16 while 5 was the most potent inhibitor of BuChE with IC₅₀ values of 5.26 μM and 7.55 μM respectively.

Graphical Abstract

Keywords:

• Garcinia mangostana
• α-Mangostin
• Synthesis
• Cholinesterase inhibitors
• AChE
• BuChE

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was financially supported by grants from Yunnan Provincial Science and Technology Department (2017ZF003, 2015HB093, 2015FB168 and provincial academician free exploration project).