Antidiabeticin vitroandin vivoevaluation of cyclodipeptides isolated fromPseudomonas fluorescensIB-MR-66e
| Autor: | Rachel Mata, Claudia Tovar-Palacio, Berenice Ovalle-Magallanes, M. Rangel-Grimaldo, S. De la Torre-Zavala, Mariana Lozano-Gonzalez, Armando R. Tovar, Lilia G. Noriega |
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| Rok vydání: | 2019 |
| Předmět: |
chemistry.chemical_classification
biology Insulin medicine.medical_treatment Insulin tolerance test Pseudomonas fluorescens Peptide 02 engineering and technology General Chemistry Pharmacology 010402 general chemistry 021001 nanoscience & nanotechnology biology.organism_classification 01 natural sciences Catalysis In vitro 0104 chemical sciences Postprandial Enzyme chemistry In vivo Materials Chemistry medicine 0210 nano-technology |
| Zdroj: | New Journal of Chemistry. 43:7756-7762 |
| ISSN: | 1369-9261 1144-0546 |
| Popis: | Three cyclodipeptides [cyclo(L-Pro-L-Leu), 1; cyclo(L-Pro-L-Val), 2; and cyclo(L-Pro-L-Phe), 3] were isolated from Pseudomonas fluorescens IB-MR-66e. The structures were established by spectral means and corroborated by synthesis. The antidiabetic potential of compounds 1–3 was explored in vivo, in vitro and in silico. The three peptides showed important inhibitory activity against the α-glucosidase enzyme. Further analysis in vivo using a sucrose tolerance test corroborated that compounds 1 and 3 (1–30 mg kg−1) significantly reduced the postprandial state. Peptide 1 (1–30 mg kg−1) also reduced the postprandial peak after a glucose challenge and exhibited significant hypoglycemia during an insulin tolerance test; thus, its antidiabetic action involved also an improvement of insulin utilization not related to Akt phosphorylation nor to an increment in mitochondrial bioenergetics nor insulin secretion. |
| Databáze: | OpenAIRE |
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