Design, synthesis and cholinesterase inhibitory activity of α-mangostin derivatives.
Nat Prod Res
; 34(10): 1380-1388, 2020 May.
Article
in En
| MEDLINE
| ID: mdl-30456989
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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Cholinesterase Inhibitors
/
Garcinia mangostana
/
Xanthones
Language:
En
Journal:
Nat Prod Res
Year:
2020
Document type:
Article