Abstract

Based on our continuous effort to investigate chemistry and biology of the plant secondary metabolites, we were able to isolate a glycosidal flavonoid 1 from the Wild Egyptian Artichoke. The activity of dihydromyricetin 3-O-rhamnoside (sin. dihydromyricitrin, ampelopsin 3-O-rhamnoside) (1) against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE); its absolute configuration using X-ray crystallography were determined for the first time. Inhibitory activity of 1 against AChE and BChE enzymes were determined using a slightly modified version of Ellman’s method. Compound 1 was revealed to have a potent inhibition against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 0.070 ± 0.008 and 0.071 ± 0.004 mM, respectively, where IC50 values of the reference drug (galanthamine) were 0.023 ± 0.15 and 0.047 ± 0.91 mM. Compound 1 could be a promising molecule against Alzheimer’s disease.

Details

Title
X-ray crystalographic data, absolute configuration, and anticholinesterase effect of dihydromyricitrin 3-O-rhamnoside
Author
Elsebai, Mahmoud Fahmi 1 ; Ghabbour, Hazem A. 2 ; Salmas, Ramin Ekhteiari 3 ; Orhan, Ilkay Erdogan 4 ; Senol Deniz, Fatma Sezer 4 

 Mansoura University, Department of Pharmacognosy, Faculty of Pharmacy, Mansoura, Egypt (GRID:grid.10251.37) (ISNI:0000000103426662) 
 Mansoura University, Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura, Egypt (GRID:grid.10251.37) (ISNI:0000000103426662) 
 Britannia House, King’s College London, Department of Chemistry, London, UK (GRID:grid.13097.3c) (ISNI:0000 0001 2322 6764) 
 Gazi University, Department of Pharmacognosy, Faculty of Pharmacy, Ankara, Türkiye (GRID:grid.25769.3f) (ISNI:0000 0001 2169 7132) 
Publication year
2022
Publication date
2022
Publisher
Nature Publishing Group
e-ISSN
20452322
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2730914963
Copyright
© The Author(s) 2022. This work is published under http://creativecommons.org/licenses/by/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.