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A study towards drug discovery for the management of type 2 diabetes: Mellitus through inhibition of the carbohydrate-hydrolyzing enzymes α-amylase and α-glucosidase by chalcone derivatives

2019Journal article Open access
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dc.contributor.authorRocha, Sónia
dc.contributor.authorSousa, Adelaide
dc.contributor.authorRibeiro, Daniela
dc.contributor.authorCorreia, Catarina M.
dc.contributor.authorSilva, Vera L.M.
dc.contributor.authorSantos, Clementina
dc.contributor.authorSilva, Artur
dc.contributor.authorAraújo, Alberto N.
dc.contributor.authorFernandes, Eduarda
dc.contributor.authorFreitas, Marisa
dc.date.accessioned2018-02-19T10:00:00Z
dc.date.accessioned2020-01-06T14:10:12Z
dc.date.available2018-01-19T10:00:00Z
dc.date.available2020-01-06T14:10:12Z
dc.date.issued2019
dc.description.abstractThe inhibition of carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, is one of the major therapeutic strategies for the treatment of type 2 diabetes mellitus. Chalcones have been recognized for their multiple biological activities, including antidiabetic properties, through unclear mechanisms. In the present work, a panel of chalcones bearing hydroxy, methoxy, methyl, nitro, chloro, fluoro and bromo substituents were evaluated against α-amylase and α-glucosidase activities, most of them for the first time. The results showed that the substitution patterns and the type of substituents of chalcones influence their inhibitory activity. The presence of hydroxy groups at C-2’- and C-4’ of the A ring and at C-3 and C-4 of the B ring favors the intended effect. Chalcones holding nitro groups and chloro substituents, together with a hydroxy group in the chalcone scaffold, showed strong inhibition of the α-glucosidase activity. The present study provides related scaffolds that may serve as the basis for the design and synthesis of new structures in order to obtain the ideal antidiabetic chalcone.
dc.description.sponsorshipThis work received financial support from the European Union (FEDER funds POCI/01/0145/FEDER/007265) and National Funds (FCT/MEC, Fundação para a Ciência e Tecnologia and Ministério da Educação e Ciência) under the Partnership Agreement PT2020 UID/QUI/50006/2013, and “Programa Operacional Competitividade e Internacionalização” (COMPETE) (POCI-01-0145-FEDER-029241). Thanks are due to University of Aveiro, Instituto Politécnico de Bragança, FCT/ MEC for the financial support to the QOPNA (FCT UID/QUI/ 00062/2013) and CIMO (UID/AGR/00690/2013) research Units through national funds and where applicable co-financed by the FEDER, within the PT2020 Partnership Agreement, and also to the Portuguese NMR Network. Sónia Rocha acknowledges FCT the financial support for the PhD grant (PD/BD/ 145169/2019), in the ambit of “QREN – POPH – Tipologia 4.1 – Formação Avançada”, co-sponsored by Fundo Social Europeu (FSE) and by national funds of Ministério da Ciência, Tecnologia e Ensino Superior (MCTES).
dc.description.versioninfo:eu-repo/semantics/publishedVersionen_EN
dc.identifier.citationRocha, Sónia; Sousa, Adelaide; Ribeiro, Daniela; Correia, Catarina M.; Silva, Vera L.M.; Santos, Clementina M.M.; Silva, Artur M.S.; Araújo, Alberto N.; Fernandes, Eduarda; Freitas, Marisa (2019). A study towards drug discovery for the management of type 2 diabetes: Mellitus through inhibition of the carbohydrate-hydrolyzing enzymes α-amylase and α-glucosidase by chalcone derivatives. Food and Function. ISSN 2042-6496. 10, p. 5510-5520en_EN
dc.identifier.doi10.1039/c9fo01298ben_EN
dc.identifier.issn2042-6496
dc.identifier.urihttp://hdl.handle.net/10198/20264
dc.language.isoeng
dc.peerreviewedyesen_EN
dc.titleA study towards drug discovery for the management of type 2 diabetes: Mellitus through inhibition of the carbohydrate-hydrolyzing enzymes α-amylase and α-glucosidase by chalcone derivativesen_EN
dc.typejournal article
dspace.entity.typePublication
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876/UID%2FAGR%2F00690%2F2013/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876/UID%2FQUI%2F50006%2F2013/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876/UID%2FQUI%2F00062%2F2013/PT
oaire.fundingStream5876
oaire.fundingStream5876
oaire.fundingStream5876
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.rightsopenAccessen_EN
rcaap.typearticleen_EN
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