Emetine and Indirubin- 3- monoxime interaction with human brain acetylcholinesterase: A computational and statistical analysis.
Journal
Cellular and molecular biology (Noisy-le-Grand, France)
ISSN: 1165-158X
Titre abrégé: Cell Mol Biol (Noisy-le-grand)
Pays: France
ID NLM: 9216789
Informations de publication
Date de publication:
02 Jan 2022
02 Jan 2022
Historique:
received:
31
12
2021
entrez:
9
7
2022
pubmed:
10
7
2022
medline:
14
7
2022
Statut:
epublish
Résumé
Alzheimer's disease is a chronic neurodegenerative ailment and the most familiar type of dementia in the older population with no effective cure to date. It is characterized by a decrease in memory, associated with the mutilation of cholinergic neurotransmission. Presently, acetylcholinesterase inhibitors have emerged as the most endorsed pharmacological medications for the symptomatic treatment of mild to moderate Alzheimer's disease. This study aimed to research the molecular enzymatic inhibition of human brain acetylcholinesterase by a natural compound emetine and I3M. Molecular docking studies were used to identify superior interaction between enzyme acetylcholinesterase and ligands. Furthermore, the docked acetylcholinesterase-emetine complex was validated statistically using an analysis of variance in all tested conformers. In this interaction, H-bond, hydrophobic interaction, pi-pi, and Cation-pi interactions played a vital function in predicting the accurate conformation of the ligand that binds with the active site of acetylcholinesterase. The conformer with the lowest free energy of binding was further analyzed. The binding energy for acetylcholinesterase complex with emetine and I3M was -9.72kcal/mol and -7.09kcal/mol, respectively. In the current study, the prediction was studied to establish a relationship between binding energy and intermolecular energy (coefficient of determination [R2 linear = 0.999), and intermolecular energy and Van der wall forces (R2 linear = 0.994). These results would be useful in gaining structural insight for designing novel lead compounds against acetylcholinesterase for the effective management of Alzheimer's disease.
Identifiants
pubmed: 35809297
doi: 10.14715/cmb/2021.67.4.12
doi:
Substances chimiques
Cholinesterase Inhibitors
0
Indoles
0
Ligands
0
Acetylcholinesterase
EC 3.1.1.7
indirubin
V86L8P74GI
Emetine
X8D5EPO80M
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM