Cargando…

Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids

An anti-neurodegeneration activity study was carried out for 80 flavonoid compounds. The structure–activity analysis of the structures was carried out by performing three different anti-neurodegeneration screening tests, showing that in these structures, the presence of a hydroxy substituent group a...

Descripción completa

Detalles Bibliográficos
Autores principales: Preet, Gagan, Haj Hasan, Ahlam, Ramlagan, Piteesha, Fawdar, Shameem, Boulle, Fabien, Jaspars, Marcel
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10609304/
https://www.ncbi.nlm.nih.gov/pubmed/37894669
http://dx.doi.org/10.3390/molecules28207188
_version_ 1785127982278377472
author Preet, Gagan
Haj Hasan, Ahlam
Ramlagan, Piteesha
Fawdar, Shameem
Boulle, Fabien
Jaspars, Marcel
author_facet Preet, Gagan
Haj Hasan, Ahlam
Ramlagan, Piteesha
Fawdar, Shameem
Boulle, Fabien
Jaspars, Marcel
author_sort Preet, Gagan
collection PubMed
description An anti-neurodegeneration activity study was carried out for 80 flavonoid compounds. The structure–activity analysis of the structures was carried out by performing three different anti-neurodegeneration screening tests, showing that in these structures, the presence of a hydroxy substituent group at position C3′ as well as C5′ of ring B and a methoxy substituent group at the C7 position of ring A play a vital role in neuroprotective and antioxidant as well as anti-inflammatory activity. Further, we found structure (5) was the top-performing active structure out of 80 structures. Subsequently, a molecular docking study was carried out for the 3 lead flavonoid compounds (4), (5), and (23) and 21 similar hypothetical proposed structures to estimate the binding strength between the tested compounds and proteins potentially involved in disease causation. Ligand-based pharmacophores were generated to guide future drug design studies.
format Online
Article
Text
id pubmed-10609304
institution National Center for Biotechnology Information
language English
publishDate 2023
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-106093042023-10-28 Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids Preet, Gagan Haj Hasan, Ahlam Ramlagan, Piteesha Fawdar, Shameem Boulle, Fabien Jaspars, Marcel Molecules Article An anti-neurodegeneration activity study was carried out for 80 flavonoid compounds. The structure–activity analysis of the structures was carried out by performing three different anti-neurodegeneration screening tests, showing that in these structures, the presence of a hydroxy substituent group at position C3′ as well as C5′ of ring B and a methoxy substituent group at the C7 position of ring A play a vital role in neuroprotective and antioxidant as well as anti-inflammatory activity. Further, we found structure (5) was the top-performing active structure out of 80 structures. Subsequently, a molecular docking study was carried out for the 3 lead flavonoid compounds (4), (5), and (23) and 21 similar hypothetical proposed structures to estimate the binding strength between the tested compounds and proteins potentially involved in disease causation. Ligand-based pharmacophores were generated to guide future drug design studies. MDPI 2023-10-20 /pmc/articles/PMC10609304/ /pubmed/37894669 http://dx.doi.org/10.3390/molecules28207188 Text en © 2023 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
Preet, Gagan
Haj Hasan, Ahlam
Ramlagan, Piteesha
Fawdar, Shameem
Boulle, Fabien
Jaspars, Marcel
Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids
title Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids
title_full Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids
title_fullStr Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids
title_full_unstemmed Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids
title_short Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids
title_sort anti-neurodegenerating activity: structure–activity relationship analysis of flavonoids
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10609304/
https://www.ncbi.nlm.nih.gov/pubmed/37894669
http://dx.doi.org/10.3390/molecules28207188
work_keys_str_mv AT preetgagan antineurodegeneratingactivitystructureactivityrelationshipanalysisofflavonoids
AT hajhasanahlam antineurodegeneratingactivitystructureactivityrelationshipanalysisofflavonoids
AT ramlaganpiteesha antineurodegeneratingactivitystructureactivityrelationshipanalysisofflavonoids
AT fawdarshameem antineurodegeneratingactivitystructureactivityrelationshipanalysisofflavonoids
AT boullefabien antineurodegeneratingactivitystructureactivityrelationshipanalysisofflavonoids
AT jasparsmarcel antineurodegeneratingactivitystructureactivityrelationshipanalysisofflavonoids