2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus

Detalhes bibliográficos
Autor(a) principal: Santos, Clementina M.M.
Data de Publicação: 2024
Outros Autores: Proença, Carina, Freitas, Marisa, Araújo, Alberto N., Silva, Artur, Fernandes, Eduarda
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)
Texto Completo: http://hdl.handle.net/10198/29737
Resumo: alpha-amylase and alpha-glucosidase are key enzymes implicated in carbohydrate digestion and their inhibition has been suggested as a powerful approach for regulating blood glucose levels. The present work describes for the first time their inhibition by a group of twelve hydroxylated 2-styrylchromones (2-SC). Our findings revealed that 2-SC display strong systematic inhibition of alpha-glucosidase rather than alpha-amylase activity. The number and position of the hydroxy groups in the chromone moiety further modulate the inhibitory profile of the studied compounds, and the derivatives bearing one catechol unit are efficient inhibitors of both enzymes. Enzyme kinetic studies indicate that all active compounds act as competitive inhibitors of alpha-amylase while most of them behave as non-competitive inhibitors of alpha-glucosidase. The results are promising and pave the way to further deciphering the potential of this class of compounds as a suitable alternative for the management of type 2 diabetes and its complications.
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spelling 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitusAlpha-amylaseAlpha-glucosidaseDiabetesKinetics2-Styrylchromonesalpha-amylase and alpha-glucosidase are key enzymes implicated in carbohydrate digestion and their inhibition has been suggested as a powerful approach for regulating blood glucose levels. The present work describes for the first time their inhibition by a group of twelve hydroxylated 2-styrylchromones (2-SC). Our findings revealed that 2-SC display strong systematic inhibition of alpha-glucosidase rather than alpha-amylase activity. The number and position of the hydroxy groups in the chromone moiety further modulate the inhibitory profile of the studied compounds, and the derivatives bearing one catechol unit are efficient inhibitors of both enzymes. Enzyme kinetic studies indicate that all active compounds act as competitive inhibitors of alpha-amylase while most of them behave as non-competitive inhibitors of alpha-glucosidase. The results are promising and pave the way to further deciphering the potential of this class of compounds as a suitable alternative for the management of type 2 diabetes and its complications.This work received support from national funds (FCT/ MCTES, Fundação para a Ciência e Tecnologia and Ministério da Ciência, Tecnologia e Ensino Superior) through the projects of CIMO (UIDB/00690/2020 and), SusTEC (LA/P/0007/2021) and REQUIMTE (UIDB/50006/2020 and UIDP/50006/2020). This work also received financial support from the project EXPL/MED-QUI/ 0815/2021, with funding from FCT/MCTES through national funds, and “Programa Operacional Competitividade e Internacionalização” (COMPETE). Open access funding provided by FCT|FCCN (b-on).SpringerBiblioteca Digital do IPBSantos, Clementina M.M.Proença, CarinaFreitas, MarisaAraújo, Alberto N.Silva, ArturFernandes, Eduarda2024-05-09T14:09:05Z20242024-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10198/29737engSantos, Clementina M. M.; Proença, Carina; Freitas, Marisa; Araújo, Alberto N.; Silva, Artur M. S.; Fernandes, Eduarda (2024). 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus. Medicinal Chemistry Research. ISSN 1054-2523. 33:4, p. 600-6101054-252310.1007/s00044-024-03200-81554-8120info:eu-repo/semantics/openAccessreponame:Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)instname:FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologiainstacron:RCAAP2025-02-25T12:21:21Zoai:bibliotecadigital.ipb.pt:10198/29737Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireinfo@rcaap.ptopendoar:https://opendoar.ac.uk/repository/71602025-05-28T16:35:58.095622Repositórios Científicos de Acesso Aberto de Portugal (RCAAP) - FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologiafalse
dc.title.none.fl_str_mv 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
title 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
spellingShingle 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
Santos, Clementina M.M.
Alpha-amylase
Alpha-glucosidase
DiabetesKinetics
2-Styrylchromones
title_short 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
title_full 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
title_fullStr 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
title_full_unstemmed 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
title_sort 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
author Santos, Clementina M.M.
author_facet Santos, Clementina M.M.
Proença, Carina
Freitas, Marisa
Araújo, Alberto N.
Silva, Artur
Fernandes, Eduarda
author_role author
author2 Proença, Carina
Freitas, Marisa
Araújo, Alberto N.
Silva, Artur
Fernandes, Eduarda
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Biblioteca Digital do IPB
dc.contributor.author.fl_str_mv Santos, Clementina M.M.
Proença, Carina
Freitas, Marisa
Araújo, Alberto N.
Silva, Artur
Fernandes, Eduarda
dc.subject.por.fl_str_mv Alpha-amylase
Alpha-glucosidase
DiabetesKinetics
2-Styrylchromones
topic Alpha-amylase
Alpha-glucosidase
DiabetesKinetics
2-Styrylchromones
description alpha-amylase and alpha-glucosidase are key enzymes implicated in carbohydrate digestion and their inhibition has been suggested as a powerful approach for regulating blood glucose levels. The present work describes for the first time their inhibition by a group of twelve hydroxylated 2-styrylchromones (2-SC). Our findings revealed that 2-SC display strong systematic inhibition of alpha-glucosidase rather than alpha-amylase activity. The number and position of the hydroxy groups in the chromone moiety further modulate the inhibitory profile of the studied compounds, and the derivatives bearing one catechol unit are efficient inhibitors of both enzymes. Enzyme kinetic studies indicate that all active compounds act as competitive inhibitors of alpha-amylase while most of them behave as non-competitive inhibitors of alpha-glucosidase. The results are promising and pave the way to further deciphering the potential of this class of compounds as a suitable alternative for the management of type 2 diabetes and its complications.
publishDate 2024
dc.date.none.fl_str_mv 2024-05-09T14:09:05Z
2024
2024-01-01T00:00:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10198/29737
url http://hdl.handle.net/10198/29737
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Santos, Clementina M. M.; Proença, Carina; Freitas, Marisa; Araújo, Alberto N.; Silva, Artur M. S.; Fernandes, Eduarda (2024). 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus. Medicinal Chemistry Research. ISSN 1054-2523. 33:4, p. 600-610
1054-2523
10.1007/s00044-024-03200-8
1554-8120
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Springer
publisher.none.fl_str_mv Springer
dc.source.none.fl_str_mv reponame:Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)
instname:FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologia
instacron:RCAAP
instname_str FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologia
instacron_str RCAAP
institution RCAAP
reponame_str Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)
collection Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)
repository.name.fl_str_mv Repositórios Científicos de Acesso Aberto de Portugal (RCAAP) - FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologia
repository.mail.fl_str_mv info@rcaap.pt
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