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Inhibitory Potential of Synthetic Amino Acid Derivatives against Digestive Enzymes as Promising Hypoglycemic and Anti-Obesity Agents.
Silva, Franciane Campos da; Santos, Bruna Celeida Silva; Castro, Pedro Pôssa de; Amarante, Giovanni Wilson; Sousa, Orlando Vieira de.
Afiliação
  • Silva FCD; Departamento de Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal de Juiz de Fora, Campus Universitário, São Pedro, Juiz de Fora 36036-900, MG, Brazil.
  • Santos BCS; Departamento de Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal de Juiz de Fora, Campus Universitário, São Pedro, Juiz de Fora 36036-900, MG, Brazil.
  • Castro PP; Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Campus Universitário, São Pedro, Juiz de Fora 36036-900, MG, Brazil.
  • Amarante GW; Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Campus Universitário, São Pedro, Juiz de Fora 36036-900, MG, Brazil.
  • Sousa OV; Departamento de Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal de Juiz de Fora, Campus Universitário, São Pedro, Juiz de Fora 36036-900, MG, Brazil.
Biomolecules ; 13(6)2023 06 07.
Article em En | MEDLINE | ID: mdl-37371533
Over the last decades, the increased incidence of metabolic disorders, such as type two diabetes and obesity, has motivated researchers to investigate new enzyme inhibitors. In this study, the inhibitory effects of synthetic amino acid derivatives (PPC80, PPC82, PPC84, PPC89, and PPC101) on the activity of digestive enzymes were assessed using in vitro assays. The inhibitory effect was determined by the inhibition percentage and the 50% inhibitory concentration (IC50), and the mechanism of action was investigated using kinetic parameters and Lineweaver-Burk plots. PPC80, PPC82, and PPC84 inhibited pancreatic lipase (IC50 of 167-1023 µM) via competitive or mixed mechanisms. The activity of pancreatic α-amylase was suppressed by PPC80, PPC82, PPC84, PPC89, and PPC101 (IC50 of 162-519 µM), which acted as competitive or mixed inhibitors. Finally, PPC84, PPC89, and PPC101 also showed potent inhibitory effects on α-glucosidase (IC50 of 51-353 µM) as competitive inhibitors. The results suggest that these synthetic amino acid derivatives have inhibitory potential against digestive enzymes and may be used as therapeutic agents to control metabolic disorders.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fármacos Antiobesidade / Hipoglicemiantes Idioma: En Revista: Biomolecules Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Brasil País de publicação: Suíça
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fármacos Antiobesidade / Hipoglicemiantes Idioma: En Revista: Biomolecules Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Brasil País de publicação: Suíça