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

2024Journal article Open access
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dc.contributor.authorSantos, Clementina M.M.
dc.contributor.authorProença, Carina
dc.contributor.authorFreitas, Marisa
dc.contributor.authorAraújo, Alberto N.
dc.contributor.authorSilva, Artur
dc.contributor.authorFernandes, Eduarda
dc.date.accessioned2024-05-09T14:09:05Z
dc.date.available2024-05-09T14:09:05Z
dc.date.issued2024
dc.description.abstractalpha-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.pt_PT
dc.description.sponsorshipThis 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).pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationSantos, 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. 600-610pt_PT
dc.identifier.doi10.1007/s00044-024-03200-8pt_PT
dc.identifier.eissn1554-8120
dc.identifier.issn1054-2523
dc.identifier.urihttp://hdl.handle.net/10198/29737
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherSpringerpt_PT
dc.relationLA/P/0007/2021pt_PT
dc.relationMountain Research Center
dc.relationAssociated Laboratory for Green Chemistry - Clean Technologies and Processes
dc.relationAssociated Laboratory for Green Chemistry - Clean Technologies and Processes
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectAlpha-amylasept_PT
dc.subjectAlpha-glucosidasept_PT
dc.subjectDiabetesKineticspt_PT
dc.subject2-Styrylchromonespt_PT
dc.title2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellituspt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleMountain Research Center
oaire.awardTitleAssociated Laboratory for Green Chemistry - Clean Technologies and Processes
oaire.awardTitleAssociated Laboratory for Green Chemistry - Clean Technologies and Processes
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F00690%2F2020/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F50006%2F2020/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDP%2F50006%2F2020/PT
oaire.citation.endPage610pt_PT
oaire.citation.issue4pt_PT
oaire.citation.startPage600pt_PT
oaire.citation.titleMedicinal Chemistry Researchpt_PT
oaire.citation.volume33pt_PT
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStream6817 - DCRRNI ID
person.familyNameSantos
person.givenNameClementina M.M.
person.identifier.ciencia-id9018-DB9C-C590
person.identifier.orcid0000-0003-4380-7990
person.identifier.scopus-author-id7201458663
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
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relation.isAuthorOfPublication.latestForDiscovery64f662b6-775d-4ea0-bfd7-f527af0ac1a0
relation.isProjectOfPublication29718e93-4989-42bb-bcbc-4daff3870b25
relation.isProjectOfPublication0d71ca47-dd95-4204-8a34-d28377654df3
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