X-ray crystalographic data, absolute configuration, and anticholinesterase effect of dihydromyricitrin 3-O-rhamnoside.

Autor: Elsebai MF; Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt. elsebai72@yahoo.com., Ghabbour HA; Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt., Salmas RE; Department of Chemistry, Britannia House, King's College London, London, UK., Orhan IE; Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, 06330, Ankara, Türkiye., Senol Deniz FS; Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, 06330, Ankara, Türkiye.
Jazyk: angličtina
Zdroj: Scientific reports [Sci Rep] 2022 Nov 01; Vol. 12 (1), pp. 18351. Date of Electronic Publication: 2022 Nov 01.
DOI: 10.1038/s41598-022-23240-7
Abstrakt: 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 IC 50 values of 0.070 ± 0.008 and 0.071 ± 0.004 mM, respectively, where IC 50 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.
(© 2022. The Author(s).)
Databáze: MEDLINE
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