Geissoschizine methyl ether, a corynanthean-type indole alkaloid from Uncaria rhynchophylla as a potential acetylcholinesterase inhibitor |
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Authors: | Yang Zhong-Duo Duan Dong-Zhu Du Juan Yang Ming-Jun Li Shuo Yao Xiao-Jun |
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Institution: | School of Life Science and Engineering , Lanzhou University of Technology, Lanzhou, P.R. China. |
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Abstract: | Geissoschizine methyl ether (1), a newly discovered strong acetylcholinesterase (AChE) inhibitor, along with six weakly active alkaloids, vallesiachotamine (2), hisuteine (3), hirsutine (4), isorhynchophylline (5), cisocorynoxeine (6) and corynoxeine (7) have been isolated from Uncaria rhynchophylla. Geissoschizine methyl ether (1) inhibited 50% of AChE activity at concentrations of 3.7?±?0.3?μg?mL(-1) while the IC(50) value of physostigmine as a standard 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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