Publicação
Exploring the inhibitory potential of 2-styrylchromones on pancreatic α- amylase
| datacite.subject.fos | Engenharia e Tecnologia::Biotecnologia Industrial | |
| datacite.subject.sdg | 09:Indústria, Inovação e Infraestruturas | |
| dc.contributor.author | Santos, Clementina M.M. | |
| dc.contributor.author | Proença, Carina | |
| dc.contributor.author | Freitas, Marisa | |
| dc.contributor.author | Araújo, Alberto N. | |
| dc.contributor.author | Silva, Artur M.S. | |
| dc.contributor.author | Fernandes, Eduarda | |
| dc.contributor.editor | XVIIIENSPQ | |
| dc.date.accessioned | 2026-05-14T15:02:24Z | |
| dc.date.available | 2026-05-14T15:02:24Z | |
| dc.date.issued | 2023 | |
| dc.description.abstract | Diabetes mellitus is a metabolic disorder that afflicts about 537 million people worldwide and this number is predicted to rise to 643 million by 2030, according to the International Diabetes Federation.1 It is characterized by hyperglycemia, caused by the deficiency in the secretion of insulin and/or in the action of this pancreatic hormone. To date, the best therapeutic strategy known consists of inhibiting carbohydrate-hydrolyzing enzymes, namely the α-amylase enzyme. The currently marketed inhibitors (e.g., acarbose, miglitol, and voglibose) are based on carbohydrate-related structures, with moderate affinity for the enzyme and with disturbing side effects.2 Thus, an active pursuit for novel and more effective anti-diabetic drugs has been carried out and a wide variety of structurally diverse heterocyclic compounds has been studied. Chromones are among the oxygenated 6-membered heterocycles evaluated and the results exhibited by some 2-arylchromones point out the relevance of this class of compounds in the inhibition of α‐amylase enzymatic activity.3 Nonetheless, a detailed investigation of the effects of the restricted group of chromones known as 2-styrylchromones (2-SC) has not been conducted to date. With this rationale in mind and as part of our on-going project, the aim of the present study is to investigate the effect of a panel of twelve 2-SC 1 on pancreatic α-amylase activity and their mechanism of inhibition, to infer about the importance of this class of compounds in the management of type 2 diabetes and its complications. α-Amylase was exposed to different concentrations of 2-SC 1 and the hydrolysis of the substrate 2-chloro-p-nitrophenyl-α-D-maltotriose was monitored spectrophotometrically at 405 nm. Acarbose was used as the standard inhibitor. In addition, the study of the inhibition type was carried out through nonlinear regression Michaelis-Menten enzymatic kinetics and the corresponding Lineweaver-Burk plot.4 The results showed that the IC50 values obtained ranged from 26 to 174 μM, considerably higher than the positive control acarbose (IC50 = 0.62 ± 0.07 μM). All active compounds revealed a competitive type of inhibition while for the positive control a mixed type of inhibition was obtained. More details concerning the structure-activity relationship will be presented and discussed in this communication. | eng |
| dc.description.sponsorship | Thiswork receivedsupport fromnational funds (FCT/MCTES, FundaçãoparaaCiênciae TecnologiaandMinistériodaCiência,TecnologiaeEnsinoSuperior) throughtheprojectsof CIMO (UIDB/00690/2020 and UIDP/00690/2020), SusTEC (LA/P/0007/2021), REQUIMTE (UIDB/50006/2020andUIDP/50006/2020)andthroughtheprojectwiththereferenceEXPL/MEDQUI/0815/2021. Carina Proença acknowledges funding from FCT through the project, EXPL/MEDQUI/0815/2021. MarisaFreitasacknowledgeshercontractundertheScientificEmploymentStimulus-IndividualCall(CEECIndividual)2020.04126.CEECIND/CP159CT0006andLAQV-REQUIMTEforhercontractunderthereferenceLA/P/0008/2020. | |
| dc.identifier.citation | Santos, Clementina M.M.; Proença, Carina; Freitas, Marisa; Araújo, Alberto N.; Silva, Artur M.S.; Fernandes, Eduarda (2023). Exploring the inhibitory potential of 2-styrylchromones on pancreatic α- amylase. In XVIII National Meeting of the Portuguese Society of Chemistry. Aveiro | |
| dc.identifier.uri | http://hdl.handle.net/10198/36667 | |
| dc.language.iso | eng | |
| dc.peerreviewed | yes | |
| dc.relation | Mountain Research Center - UIDB/00690/2020 | |
| dc.relation | Associated Laboratory for Green Chemistry - Clean Technologies and Processes | |
| dc.relation | UIDP/50006/2020 | |
| dc.rights.uri | N/A | |
| dc.subject | 2-styrylchromones | |
| dc.subject | Pancreatic α-amylase | |
| dc.subject | Enzymatic inhibition | |
| dc.subject | Diabetes mellitus | |
| dc.subject | Chromones | |
| dc.title | Exploring the inhibitory potential of 2-styrylchromones on pancreatic α- amylase | eng |
| dc.type | conference poster | |
| dspace.entity.type | Publication | |
| oaire.awardNumber | UIDB/00690/2020 | |
| oaire.awardNumber | UIDB/50006/2020 | |
| oaire.awardTitle | Mountain Research Center - UIDB/00690/2020 | |
| oaire.awardTitle | Associated Laboratory for Green Chemistry - Clean Technologies and Processes | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F00690%2F2020/PT | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F50006%2F2020/PT | |
| oaire.citation.conferenceDate | 2023 | |
| oaire.citation.conferencePlace | Aveiro | |
| oaire.citation.title | XVIII Encontro Nacional da SPQ | |
| oaire.fundingStream | 6817 - DCRRNI ID | |
| oaire.fundingStream | 6817 - DCRRNI ID | |
| oaire.version | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |
| person.familyName | Santos | |
| person.givenName | Clementina M.M. | |
| person.identifier.ciencia-id | 9018-DB9C-C590 | |
| person.identifier.orcid | 0000-0003-4380-7990 | |
| person.identifier.scopus-author-id | 7201458663 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
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