| Texto completo | |
| Autor(es): Mostrar menos - |
Silva, Mariana
[1, 2]
;
Philadelpho, Biane
[2]
;
Santos, Johnnie
[2]
;
Souza, Victoria
[2]
;
Souza, Caio
[2]
;
Santiago, Victoria
[2]
;
Silva, Jaff
[1, 2]
;
Souza, Carolina
[2]
;
Azeredo, Francine
[2]
;
Castilho, Marcelo
[2]
;
Cilli, Eduardo
[1]
;
Ferreira, Ederlan
[2]
Número total de Autores: 12
|
| Afiliação do(s) autor(es): | [1] Sao Paulo State Univ, Chem Inst, BR-14800900 Araraquara, SP - Brazil
[2] Univ Fed Bahia, Sch Pharm, BR-40170115 Salvador, BA - Brazil
Número total de Afiliações: 2
|
| Tipo de documento: | Artigo Científico |
| Fonte: | INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES; v. 22, n. 20 OCT 2021. |
| Citações Web of Science: | 1 |
| Resumo | |
In this study, in silico approaches are employed to investigate the binding mechanism of peptides derived from cowpea beta-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 mu g, 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%, respectively. Our results suggest that Ile-Ala-Phe, Gln-Gly-Phe, and Gln-Asp-Phe peptides derived from cowpea beta-vignin have the potential to lower cholesterol synthesis through a statin-like regulation mechanism.</p> (AU) | |
| Processo FAPESP: | 14/50926-0 - INCT 2014: biodiversidade e produtos naturais |
| Beneficiário: | Vanderlan da Silva Bolzani |
| Modalidade de apoio: | Auxílio à Pesquisa - Programa BIOTA - Temático |
| Processo FAPESP: | 13/07600-3 - CIBFar - Centro de Inovação em Biodiversidade e Fármacos |
| Beneficiário: | Glaucius Oliva |
| Modalidade de apoio: | Auxílio à Pesquisa - Centros de Pesquisa, Inovação e Difusão - CEPIDs |