Synthesis and Bioactivity Evaluation of Peptides Derived from Crassostrea rivularis as Bioactive Functional Food Components

Abstract

Peptides derived from marine organisms represent promising candidates for functional food components because of their diverse bioactivities and favorable safety profiles. This study aimed to synthesize three peptides, AWVDY, YAKRCFR, and MSFRFY, from Crassostrea rivularis and assess their antimicrobial and non-toxic potential as bioactive ingredients. Peptide synthesis was carried out using the solid-phase method based on the Fmoc/tBu strategy, employing resin loadings of 0.469, 0.424, and 0.635 mmol/g for AWVDY, YAKRCFR, and MSFRFY, respectively. Chain elongation utilized HATU/HOAt/DIPEA for YAKRCFR and DIC/Oxyma for AWVDY and MSFRFY, followed by TFA-mediated cleavage. Structural characterization was confirmed by LC-MS and NMR analyses. Cytotoxicity assays using A549 and CV-1 cell lines showed that AWVDY exhibited moderate cytotoxicity toward A549 cells and weak cytotoxicity toward CV-1 cells, whereas YAKRCFR and MSFRFY were non-cytotoxic. Antimicrobial evaluation against Candida albicans, Staphylococcus aureus, Staphylococcus epidermidis, Salmonella typhimurium, and Escherichia coli revealed selective inhibition by AWVDY and broader activity by YAKRCFR, while MSFRFY exhibited minimal activity. These results indicate that YAKRCFR possesses the most favorable combination of antimicrobial activity and safety, whereas AWVDY shows moderate cytotoxicity but retains selective antimicrobial potential.