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Inhibitory Potential of Synthetic Amino Acid Derivatives against Digestive Enzymes as Promising Hypoglycemic and Anti-Obesity Agents.
| Content Provider | Europe PMC |
|---|---|
| Author | da Silva, Franciane Campos Santos, Bruna Celeida Silva de Castro, Pedro Pôssa Amarante, Giovanni Wilson de Sousa, Orlando Vieira |
| Editor | Youssef, Diaa Shaala, Lamiaa |
| Copyright Year | 2023 |
| Abstract | 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. |
| Journal | Biomolecules |
| Volume Number | 13 |
| PubMed Central reference number | PMC10296036 |
| Issue Number | 6 |
| PubMed reference number | 37371533 |
| e-ISSN | 2218273X |
| DOI | 10.3390/biom13060953 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2023-06-07 |
| Access Restriction | Open |
| Rights License | Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). © 2023 by the authors. |
| Subject Keyword | amino acid derivatives digestive enzymes pancreatic lipase pancreatic α-amylase α-glucosidase metabolic disorders |
| Content Type | Text |
| Resource Type | Article |
| Subject | Biochemistry Molecular Biology |
