Scopus
🔓 Açık Erişim
Plant-derived peptides rubiscolin-6, soymorphin-6 and their c-terminal amide derivatives: Pharmacokinetic properties and biological activity
Journal of Functional Foods · Ekim 2020
Makale Bilgileri
DergiJournal of Functional Foods
Yayın TarihiEkim 2020
Cilt / Sayfa73
Scopus ID2-s2.0-85089438717
Erişim🔓 Açık Erişim
Özet
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.
Yazarlar (11)
1
Azzurra Stefanucci
2
Marilisa Pia Dimmito
3
Giancarlo Tenore
4
Stefano Pieretti
5
Paola Minosi
6
Gokhan Zengin
ORCID: 0000-0001-6548-7823
7
Chiara Sturaro
8
Girolamo Calò
9
Ettore Novellino
10
Angelo Cichelli
11
Adriano Mollica
Anahtar Kelimeler
Antinociception
Antioxidant activity
Opioid peptides
Rubiscolin-6
Soymorphin-6
Kurumlar
Istituto Superiore Di Sanita
Rome Italy
Selçuk Üniversitesi
Selçuklu Turkey
Università degli Studi di Napoli Federico II
Naples Italy
University of Ferrara
Ferrara Italy
University of G. d'Annunzio Chieti and Pescara
Chieti Italy
Metrikler
23
Atıf
11
Yazar
5
Anahtar Kelime