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Acetylcholinesterase inhibitory activity and neuroprotection in vitro, molecular docking, and improved learning and memory functions of demethylcurcumin in scopolamine-induced amnesia ICR mice

Abstract

In this study, demethylcurcumin (DC), the minor constituent in curcuminoids, showed better than those of curcumin in anti-acetylcholinesterase (anti-AChE) activities, anti-amyloid β peptide aggregations, neuroprotective activities in 6-hydroxydopamine-treated SH-SY5Y cell models, and anti-nitric oxide productions in lipopolysaccharide-treated RAW 264.7 macrophages. Based on molecular docking analyses with AChE, the meta-hydroxyl group in DC, nonexistent in curcumin, showed the formation of hydrogen bonds with Ser293 and Tyr341 in the binding sites of AChE. For animal experiments, the scopolamine-induced amnesia ICR mice were used to analyze the learning and memory functions of DC in comparisons with positive control of donepezil. Mice fed with DC (50 mg/kg) or donepezil (5 mg/kg) demonstrated to improve and showed a significant difference compared to those in the control group (P < 0.05, 0.01, or 0.001) in a passive avoidance test and in a water maze probe test. The brain extracts of the mice in the DC or donepezil group showed reduced AChE activities and higher ORAC activities and also showed a significant difference compared to those in the control group (P < 0.05, 0.01, or 0.001). DC might be beneficial to develop functional foods or as a lead compound for degenerative disorders.

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Article information


Submitted
07 Oct 2019
Accepted
10 Feb 2020
First published
11 Feb 2020

Food Funct., 2020, Accepted Manuscript
Article type
Paper

Acetylcholinesterase inhibitory activity and neuroprotection in vitro, molecular docking, and improved learning and memory functions of demethylcurcumin in scopolamine-induced amnesia ICR mice

Y. Liu, C. Lee, L. Chen, T. Lee, Y. Hsieh, C. Han, C. Yang, W. Huang and W. Hou, Food Funct., 2020, Accepted Manuscript , DOI: 10.1039/C9FO02339A

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