2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2024 |
| Outros Autores: | , , , , |
| 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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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 |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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article |
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publishedVersion |
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http://hdl.handle.net/10198/29737 |
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http://hdl.handle.net/10198/29737 |
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eng |
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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 |
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openAccess |
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application/pdf |
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Springer |
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Springer |
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