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

Authors
  • Yang, Zhong-duo
  • Zhang, Xu
  • Du, Juan
  • Ma, Zhao-jian
  • Guo, Feng
  • Li, Shuo
  • Yao, Xiao-jun
Type
Published Article
Journal
Natural product research
Publication Date
Jan 01, 2012
Volume
26
Issue
5
Pages
387–392
Identifiers
DOI: 10.1080/14786419.2010.487188
PMID: 21732870
Source
Medline
License
Unknown

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.

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