Abstract
This study aims to investigate the pharmacokinetic properties, antinociceptive, and antioxidant activities of rubiscolin-6, soymorphin-6, and their C-terminal amides. Rubiscolin-6 and soymorphin-6 are two exhorphins derived from spinach and soybean, respectively. The four peptides were synthesized following Fmoc-SPPS strategy to give the final peptides in excellent overall yields, and purity following an analytical RP-HPLC analysis. Rubiscolin-6-amide exhibits a significative antinociceptive effect after i.c.v. and s.c. administration. Rubiscolin-6 shows the best in vitro intestinal bioavailability in the 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.
Supplementary Materials
The following supporting information can be downloaded at: https://www.mdpi.com/article/10.3390/Foods2021-11060/s1. Poster: Plant-Derived Peptides Rubiscolin-6, Soymorphin-6 and Their C-Terminal Amide Derivatives: Pharmacokinetic Properties and Biological Activity.
Author Contributions
Conceptualization, A.M. and A.S.; methodology, E.N.; validation, G.Z., C.S.; G.C.; investigation, S.P. and P.M.; data curation, G.T.; writing-original draft preparation, A.S.; writing-review and editing, A.M. and A.C. All authors have read and agreed to the published version of the manuscript.
Funding
This research received no external funding.
Institutional Review Board Statement
Not applicable.
Data Availability Statement
Not applicable.
Informed Consent Statement
Not applicable.
Conflicts of Interest
The authors declare no conflict of interest.
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