IAF, QGF, and QDF peptides exhibit cholesterol-lowering activity through a statin-like HMG-CoA reductase regulation mechanism: In silico and in vitro approach

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Autor(es): dc.contributorUniversidade Federal da Bahia (UFBA)-
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.creatorSilva, Mariana-
Autor(es): dc.creatorPhiladelpho, Biane-
Autor(es): dc.creatorSantos, Johnnie-
Autor(es): dc.creatorSouza, Victória-
Autor(es): dc.creatorSouza, Caio-
Autor(es): dc.creatorSantiago, Victória-
Autor(es): dc.creatorSilva, Jaff-
Autor(es): dc.creatorSouza, Carolina-
Autor(es): dc.creatorAzeredo, Francine-
Autor(es): dc.creatorCastilho, Marcelo-
Autor(es): dc.creatorCilli, Eduardo-
Autor(es): dc.creatorFerreira, Ederlan-
Data de aceite: dc.date.accessioned2025-08-21T23:12:28Z-
Data de disponibilização: dc.date.available2025-08-21T23:12:28Z-
Data de envio: dc.date.issued2022-05-01-
Data de envio: dc.date.issued2022-05-01-
Data de envio: dc.date.issued2021-10-01-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.3390/ijms222011067-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/233668-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/233668-
Descrição: dc.descriptionIn this study, in silico approaches are employed to investigate the binding mechanism of peptides derived from cowpea β-vignin and HMG-CoA reductase. With the obtained information, we designed synthetic peptides to evaluate their in vitro enzyme inhibitory activity. In vitro, the total protein extract and <3 kDa fraction, at 5000 µg, support this hypothesis (95% and 90% inhibition of HMG-CoA reductase, respectively). Ile-Ala-Phe, Gln-Gly-Phe, and Gln-Asp-Phe peptides were predicted to bind to the substrate binding site of HMGCR via HMG-CoAR. In silico, it was established that the mechanism of HMG-CoA reductase inhibition largely entailed mimicking the interactions of the decalin ring of simvastatin and via H-bonding; in vitro studies corroborated the predictions, whereby the HMG-CoA reductase activity was decreased by 69%, 77%, and 78%, re-spectively. Our results suggest that Ile-Ala-Phe, Gln-Gly-Phe, and Gln-Asp-Phe peptides derived from cowpea β-vignin have the potential to lower cholesterol synthesis through a statin-like regulation mechanism.-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
Descrição: dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)-
Descrição: dc.descriptionSchool of Pharmacy Federal University of Bahia-
Descrição: dc.descriptionChemistry Institute Sao Paulo State University-
Descrição: dc.descriptionChemistry Institute Sao Paulo State University-
Descrição: dc.descriptionFAPESP: 13/07600-3-
Descrição: dc.descriptionFAPESP: 14/50926-0-
Descrição: dc.descriptionCNPq: 426235/2016-9-
Idioma: dc.languageen-
Relação: dc.relationInternational Journal of Molecular Sciences-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectCompetitive HMG-CoA reductase inhibitor-
Palavras-chave: dc.subjectCowpea peptides-
Palavras-chave: dc.subjectMolecular docking-
Palavras-chave: dc.subjectPharmacokinetic properties-
Título: dc.titleIAF, QGF, and QDF peptides exhibit cholesterol-lowering activity through a statin-like HMG-CoA reductase regulation mechanism: In silico and in vitro approach-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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