J Agric Food Chem. , 2019., Jan 10. doi: 10.1021/acs.jafc.8b06299.

Transport, Bioavailability, Safety and Calmodulin-Dependent Phosphodiesterase-Inhibitory Properties of Flaxseed-derived Bioactive Peptides.

Nwachukwu I Alashi AM Zahradka P Aluko RE.

Abstract

The aim of this work was to determine bioavailability and in vivo calmodulin-dependent phosphodiesterase (CaMPDE)-inhibitory activity of six flaxseed protein-derived peptides (AGA, AKLMS, QIAK, RWIQ, QQAKQ and KQLSTGC) after oral administration to Wistar rats. Initial experiments tested the cytotoxicity and cellular transport potential of the peptides using Caco-2 cells. The cytotoxicity assay indicated that none of the six peptides had an adverse effect on the proliferation and viability of the Caco-2 cells while transport assay confirmed peptide translocation across the cell membrane. However, only two of the peptides (AGA and RWIQ) were detected in the rat serum up to 90 min post-gavage with traces of RWIQ persisting in serum one week after oral gavage. The six peptides inhibited plasma activity of CaMPDE with AGA (34.63%), QIAK (36.66%) and KQLSTGC (34.21%) being the most effective 30 min after gavage. In contrast, only the AGA maintained a significant plasma CaMPDE activity inhibition (44.35%) after 60 min.

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