Acetylcholinesterase and monoamine oxidase-B inhibitory activities by ellagic acid derivatives isolated from Castanopsis cuspidata var. sieboldii.

ABSTRACT: Among 276 herbal extracts, a methanol extract of Castanopsis cuspidata var. sieboldii stems was selected as an experimental source for novel acetylcholinesterase (AChE) inhibitors. Five compounds were isolated from the extract by activity-guided screening, and their inhibitory activities against butyrylcholinesterase (BChE), monoamine oxidases (MAOs), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1) were also evaluated. Of these compounds, 4'-O-(α-L-rhamnopyranosyl)-3,3',4-tri-O-methylellagic acid (3) and 3,3',4-tri-O-methylellagic acid (4) effectively inhibited AChE with IC₅₀ values of 10.1 and 10.7 µM, respectively. Ellagic acid (5) inhibited AChE (IC₅₀ = 41.7 µM) less than 3 and 4. In addition, 3 effectively inhibited MAO-B (IC₅₀ = 7.27 µM

SUBMITTER: Oh JM 

PROVIDER: S-EPMC8260592 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature