| Autor: |
Azzurra Stefanucci, Marilisa Pia Dimmito, Giancarlo Tenore, Stefano Pieretti, Paola Minosi, Gokhan Zengin, Chiara Sturaro, Girolamo Calò, Ettore Novellino, Angelo Cichelli, Adriano Mollica |
| Jazyk: |
angličtina |
| Rok vydání: |
2020 |
| Předmět: |
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| Zdroj: |
Journal of Functional Foods, Vol 73, Iss , Pp 104154- (2020) |
| Druh dokumentu: |
article |
| ISSN: |
1756-4646 |
| DOI: |
10.1016/j.jff.2020.104154 |
| Popis: |
The aim of this work is to investigate the pharmacokinetic properties, antinociceptive and antioxidant activities of rubiscolin-6, soymorphin-6 and their C-terminal amides; The four peptides were synthesized following Fmoc-SPPS strategy to give the final peptides in excellent overall yields and purity following analytical RP-HPLC analysis. None of them shows antioxidant activity and α-tyrosinase inhibition in vitro. All compounds are able to activate G-protein coupled receptor at the δ-opioid receptor (DOR) at 100 μM concentration however, rubiscolin-6-amide exhibits significative antinociceptive effect after i.c.v. administration in the tail flick test (TF) and s.c. administration in the formalin test (FT). Rubiscolin-6 shows the best in vitro intestinal bioavailability in CaCo2 cell monolayer and stability to the brush border exopeptidases in the apical compartment. In silico experiments show the interaction of rubiscolin-6 and rubiscolin-6 amide at the binding cavity of DOR compared with the crystallographic ligand TIPP-NH2. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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Full Text from ScienceDirect