An aporphine alkaloid from Nelumbo nucifera as an acetylcholinesterase inhibitor and the primary investigation for structure–activity correlations
2012
Yang, Zhong-duo | Zhang, Xu | Du, Juan | Ma, Zhao-jian | Guo, Feng | Li, Shuo | Yao, Xiao-jun
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 IC₅₀ 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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