title: Transport across Caco-2 cell monolayer and sensitivity to hydrolysis of two anxiolytic peptides from αs1-casein, α-casozepine, and αs1-casein-f91-97: effect of bile salts.
abstract: α-Casozepine and f91-97, peptides from α(s1)-casein, display anxiolytic activity in rats and may have to cross the intestinal epithelium to exert this central effect. We evaluated their resistance to hydrolysis by the peptidases of Caco-2 cells and their ability to cross the cell monolayer. To mimic physiological conditions, two preparations of bile salts were used in noncytotoxic concentrations: porcine bile extract and an equimolar mixture of taurocholate, cholate, and deoxycholate. The presence and composition of bile salts appeared to modulate the peptidase activities of the Caco-2 cells involved (i) in the hydrolysis of α-casozepine, leading to much higher formation of fragments f91-99, f91-98, and f91-97, and (ii) in the hydrolysis of f91-97, leading to lower degradation of this peptide. Transport of α-casozepine across Caco-2 monolayer increased significantly, in the presence of bile extract, and of fragment f91-97, in the presence of bile salts.
authors: Unité de Recherche, Animal & Fonctionnalités des Produits Animaux (UR AFPA)-Équipe, Protéolyse & Biofonctionnalités des Protéines et des Peptides, Nancy-Université, Vandœuvre-lès-Nancy, France.
authors: Céline
authors: C
authors: Cakir-Kiefer
authors: Laurent
authors: L
authors: Miclo
authors: Frédérique
authors: F
authors: Balandras
authors: Annie
authors: A
authors: Dary
authors: Claire
authors: C
authors: Soligot
authors: Yves
authors: Y
authors: Le Roux
mesh_terms: D000818:Animals; D014151:Anti-Anxiety Agents / Q000378:metabolism*; D001647:Bile Acids and Salts / Q000494:pharmacology*; D001692:Biological Transport / Q000187:drug effects; D018938:Caco-2 Cells; D002364:Caseins / Q000737:chemistry* / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism*; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects; D007413:Intestinal Mucosa / Q000378:metabolism*; D007422:Intestines / Q000187:drug effects; D008954:Models, Biological; D010446:Peptide Fragments / Q000378:metabolism*; D010447:Peptide Hydrolases / Q000737:chemistry; D013552:Swine
chemical_list: D014151:Anti-Anxiety Agents; D001647:Bile Acids and Salts; D002364:Caseins; D010446:Peptide Fragments; D010447:Peptide Hydrolases