Pharmacokinetics and Transport of an Osteogenic Dodecapeptide.

Abstract

A dodecapeptide with the amino acid sequence of IEELEEELEAER (PIE), identified from Mytilus edulis proteolysis hydrolysates, has shown good bone-forming activity in previous studies. The pharmacokinetics and transport of the PIE peptide in vivo or in vitro were investigated in this study. The results showed that the PIE peptide can be transported into monolayer Caco-2 cells, and the PIE peptide was identified in the serum after the mice reached the highest value of 173.60 ± 60.30 ng/mL, in which it was quantified by an optimized mass spectrometry method. In addition, the PIE peptide has a promoting effect on the bone morphogenetic protein pathway at the gene and protein levels. According to the distribution of PIE-FITC in ovariectomized mice after orally administrated PIE-FITC, it was confirmed that it can enter the gastrointestinal tract and serum, and reach the bones. Taken together, the PIE peptide can be absorbed well both in vitro and in vivo, and it could promote pre-osteoblast differentiation factors.