title: The (193-209) 17-residues peptide of bovine β-casein is transported through Caco-2 monolayer.
abstract: Although the bioavailability of large peptides with biological activity is of great interest, the intestinal transport has been described for peptides up to only nine residues. β-casein (β-CN, 193-209) is a long and hydrophobic peptide composed of 17 amino acid residues (molecular mass 1881 Da) with immunomodulatory activity. The present work examined the transport of the β-CN (193-209) peptide across Caco-2 cell monolayer. In addition, we evaluated the possible routes of the β-CN (193-209) peptide transport, using selective inhibitors of the different routes for peptide transfer through the intestinal barrier. The results showed that the β-CN (193-209) peptide resisted the action of brush-border membrane peptidases, and that it was transported through the Caco-2 cell monolayer. The main route involved in transepithelial transport of the β-CN (193-209) peptide was transcytosis via internalized vesicles, although the paracellular transport via tight-junctions could not be excluded. Our results demonstrated the transport of an intact long-chain bioactive peptide in an in vitro model of intestinal epithelium, as an important step to prove the evidence for bioavailability of this peptide.
authors.affiliation: Department of Experimental Veterinary Science, University of Padua, Viale dell'Università, Legnaro, Padua, Italy.
authors.forename: Daniela
authors.initials: D
authors.lastname: Regazzo
authors.forename: Daniel
authors.initials: D
authors.lastname: Mollé
authors.forename: Gianfranco
authors.initials: G
authors.lastname: Gabai
authors.forename: Daniel
authors.initials: D
authors.lastname: Tomé
authors.forename: Didier
authors.initials: D
authors.lastname: Dupont
authors.forename: Joëlle
authors.initials: J
authors.lastname: Leonil
authors.forename: Rachel
authors.initials: R
authors.lastname: Boutrou
mesh_terms: D000818:Animals; D018938:Caco-2 Cells; D002364:Caseins / Q000032:analysis / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism; D002417:Cattle; D012085:Chymosin / Q000378:metabolism; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007155:Immunologic Factors / Q000032:analysis / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism*; D007408:Intestinal Absorption; D049990:Membrane Transport Modulators / Q000494:pharmacology; D026901:Membrane Transport Proteins / Q000378:metabolism; D008871:Microvilli / Q000378:metabolism; D009994:Osmolar Concentration; D010446:Peptide Fragments / Q000032:analysis / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism*; D000074011:Peptide Transporter 1; D020033:Protein Isoforms / Q000378:metabolism; D027981:Symporters / Q000037:antagonists & inhibitors; D019108:Tight Junctions / Q000187:drug effects; D013997:Time Factors; D057900:Transcytosis / Q000187:drug effects
chemical_list: D002364:Caseins; D007155:Immunologic Factors; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins; D010446:Peptide Fragments; D000074011:Peptide Transporter 1; D020033:Protein Isoforms; C082186:SLC15A1 protein, human; D027981:Symporters; C475729:casein hydrolysate; D012085:Chymosin