In vitro and in silico studies of 3-hydroxy-3-methyl-glutaryl coenzyme A reductase inhibitory activity of the cowpea Gln-Asp-Phe peptide

Autor(es)

de Cerqueira e Silva, Mariana Barros ^[1] ; da Cruz Souza, Caio Alexandre ^[1] ; Philadelpho, Biane Oliveira ^[1] ; Novais da Cunha, Mariana Mota ^[1] ; Reis Batista, Fabiana Pacheco ^[1] ; da Silva, Jaff Ribeiro ^[1] ; Druzian, Janice Izabel ^[1] ; Castilho, Marcelo Santos ^[1] ; Cilli, Eduardo Maffud ^[2] ; Ferreira, Ederlan S. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Fed Bahia, Sch Pharm, Barao de Jeremoabo St, BR-40170115 Salvador, BA - Brazil

^[2] Sao Paulo State Univ UNESP, Inst Chem, Rua Prof Francisco Swgni, BR-14800060 Araraquara, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Food Chemistry; v. 259, p. 270-277, SEP 1 2018.
• Citações Web of Science: 1

Resumo

Previous studies have shown that cowpea protein positively interferes with cholesterol metabolism. In this study, we evaluated the ability of the fraction containing peptides of < 3 kDa, as well as that of the Gln-Asp-Phe (QDF) peptide, derived from cowpea beta-vignin protein, to inhibit HMG-CoA reductase activity. We established isolation and chromatography procedures to effectively obtain the protein with a purity above 95%. In silico predictions were performed to identify peptide sequences capable of interacting with HMG-CoA reductase. In vitro experiments showed that the fraction containing peptides of < 3 kDa displayed inhibition of HMG-CoA reductase activity. The tripeptide QDF inhibits HMG-CoA reductase (IC50 = 12.8 mu M) in a dose-dependent manner. Furthermore, in silico studies revealed the binding profile of the QDF peptide and hinted at the molecular interactions that are responsible for its activity. Therefore, this study shows, for the first time, a peptide from cowpea beta-vignin protein that inhibits HMG-CoA reductase and the chemical modifications that should be investigated to evaluate its binding profile. (AU)

• 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