An aporphine alkaloid from Nelumbo nucifera as an acetylcholinesterase inhibitor and the primary investigation for structure-activity correlations.

Abstract:

:N-methylasimilobine (1), a new-found strong acetylcholinesterase (AChE) inhibitor, along with two weakly active aporphine alkaloids, nuciferine (2) and nornuciferine (3) were separated from Nelumbo nucifera. N-methylasimilobine (1) inhibited 50% of AChE activity at the concentrations of 1.5 ± 0.2 µg mL(-1) when the standard IC(50) value of Physostigmine was 0.013 ± 0.002 µg mL(-1). The mode of AChE inhibition by 1 was reversible and non-competitive. In addition, molecular modelling was performed to explore the binding mode of inhibitor 1 at the active site of AChE.

journal_name

Nat Prod Res

journal_title

Natural product research

authors

Yang ZD,Zhang X,Du J,Ma ZJ,Guo F,Li S,Yao XJ

doi

10.1080/14786419.2010.487188

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

387-92

issue

5

eissn

1478-6419

issn

1478-6427

journal_volume

26

pub_type

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