Cargando…

Docking and Molecular Dynamic Investigations of Phenylspirodrimanes as Cannabinoid Receptor-2 Agonists

Cannabinoid receptor ligands are renowned as being therapeutically crucial for treating diverse health disorders. Phenylspirodrimanes are meroterpenoids with unique and varied structural scaffolds, which are mainly reported from the Stachybotrys genus and display an array of bioactivities. In this w...

Descripción completa

Detalles Bibliográficos
Autores principales: Omar, Abdelsattar M., Aljahdali, Anfal S., Safo, Martin K., Mohamed, Gamal A., Ibrahim, Sabrin R. M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9821895/
https://www.ncbi.nlm.nih.gov/pubmed/36615238
http://dx.doi.org/10.3390/molecules28010044
_version_ 1784865811103481856
author Omar, Abdelsattar M.
Aljahdali, Anfal S.
Safo, Martin K.
Mohamed, Gamal A.
Ibrahim, Sabrin R. M.
author_facet Omar, Abdelsattar M.
Aljahdali, Anfal S.
Safo, Martin K.
Mohamed, Gamal A.
Ibrahim, Sabrin R. M.
author_sort Omar, Abdelsattar M.
collection PubMed
description Cannabinoid receptor ligands are renowned as being therapeutically crucial for treating diverse health disorders. Phenylspirodrimanes are meroterpenoids with unique and varied structural scaffolds, which are mainly reported from the Stachybotrys genus and display an array of bioactivities. In this work, 114 phenylspirodrimanes reported from Stachybotrys chartarum were screened for their CB2 agonistic potential using docking and molecular dynamic simulation studies. Compound 56 revealed the highest docking score (−11.222 kcal/mol) compared to E3R_6KPF (native agonist, gscore value −12.12 kcal/mol). The molecular docking and molecular simulation results suggest that compound 56 binds to the putative binding site in the CB2 receptor with good affinity involving key interacting amino acid residues similar to that of the native ligands, E3R. The molecular interactions displayed π–π stacking with Phe183 and hydrogen bond interactions with Thr114, Leu182, and Ser285. These findings identified the structural features of these metabolites that might lead to the design of selective novel ligands for CB2 receptors. Additionally, phenylspirodrimanes should be further investigated for their potential as a CB2 ligand.
format Online
Article
Text
id pubmed-9821895
institution National Center for Biotechnology Information
language English
publishDate 2022
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-98218952023-01-07 Docking and Molecular Dynamic Investigations of Phenylspirodrimanes as Cannabinoid Receptor-2 Agonists Omar, Abdelsattar M. Aljahdali, Anfal S. Safo, Martin K. Mohamed, Gamal A. Ibrahim, Sabrin R. M. Molecules Article Cannabinoid receptor ligands are renowned as being therapeutically crucial for treating diverse health disorders. Phenylspirodrimanes are meroterpenoids with unique and varied structural scaffolds, which are mainly reported from the Stachybotrys genus and display an array of bioactivities. In this work, 114 phenylspirodrimanes reported from Stachybotrys chartarum were screened for their CB2 agonistic potential using docking and molecular dynamic simulation studies. Compound 56 revealed the highest docking score (−11.222 kcal/mol) compared to E3R_6KPF (native agonist, gscore value −12.12 kcal/mol). The molecular docking and molecular simulation results suggest that compound 56 binds to the putative binding site in the CB2 receptor with good affinity involving key interacting amino acid residues similar to that of the native ligands, E3R. The molecular interactions displayed π–π stacking with Phe183 and hydrogen bond interactions with Thr114, Leu182, and Ser285. These findings identified the structural features of these metabolites that might lead to the design of selective novel ligands for CB2 receptors. Additionally, phenylspirodrimanes should be further investigated for their potential as a CB2 ligand. MDPI 2022-12-21 /pmc/articles/PMC9821895/ /pubmed/36615238 http://dx.doi.org/10.3390/molecules28010044 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Omar, Abdelsattar M.
Aljahdali, Anfal S.
Safo, Martin K.
Mohamed, Gamal A.
Ibrahim, Sabrin R. M.
Docking and Molecular Dynamic Investigations of Phenylspirodrimanes as Cannabinoid Receptor-2 Agonists
title Docking and Molecular Dynamic Investigations of Phenylspirodrimanes as Cannabinoid Receptor-2 Agonists
title_full Docking and Molecular Dynamic Investigations of Phenylspirodrimanes as Cannabinoid Receptor-2 Agonists
title_fullStr Docking and Molecular Dynamic Investigations of Phenylspirodrimanes as Cannabinoid Receptor-2 Agonists
title_full_unstemmed Docking and Molecular Dynamic Investigations of Phenylspirodrimanes as Cannabinoid Receptor-2 Agonists
title_short Docking and Molecular Dynamic Investigations of Phenylspirodrimanes as Cannabinoid Receptor-2 Agonists
title_sort docking and molecular dynamic investigations of phenylspirodrimanes as cannabinoid receptor-2 agonists
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9821895/
https://www.ncbi.nlm.nih.gov/pubmed/36615238
http://dx.doi.org/10.3390/molecules28010044
work_keys_str_mv AT omarabdelsattarm dockingandmoleculardynamicinvestigationsofphenylspirodrimanesascannabinoidreceptor2agonists
AT aljahdalianfals dockingandmoleculardynamicinvestigationsofphenylspirodrimanesascannabinoidreceptor2agonists
AT safomartink dockingandmoleculardynamicinvestigationsofphenylspirodrimanesascannabinoidreceptor2agonists
AT mohamedgamala dockingandmoleculardynamicinvestigationsofphenylspirodrimanesascannabinoidreceptor2agonists
AT ibrahimsabrinrm dockingandmoleculardynamicinvestigationsofphenylspirodrimanesascannabinoidreceptor2agonists