title: In vitro digestibility of α-casozepine, a benzodiazepine-like peptide from bovine casein, and biological activity of its main proteolytic fragment.
abstract: α-Casozepine is a peptide, corresponding to the sequence 91-100 of the bovine α(s1)-casein, displaying anxiolytic activity in the rat. The α(s1)-casein tryptic hydrolysate containing this peptide decreases stress effects after oral administration in various species including man. Therefore, the stability of this peptide toward gastric and pancreatic proteases has been assessed by using pepsin, chymotrypsin/trypsin, Corolase PP, pepsin followed by chymotrypsin/trypsin or pepsin followed by Corolase PP. α-Casozepine was slowly degraded by chymotrypsin, much more sensitive to pepsin and Corolase PP but not completely destroyed after 4 h kinetics. The bonds in the region 91 to 95 of the α-casozepine were totally resistant to hydrolysis by all studied proteases. Surprisingly, a fragment, corresponding to the sequence 91-97 and found in all the hydrolysis media in significant amount, possessed an anxiolytic activity in three behavioral tests measuring this parameter. This peptide could participate in the in vivo activity of α-casozepine.
authors.affiliation: Unité de Recherche Animal & Fonctionnalités des Produits Animaux (UR AFPA), Équipe Protéolyse & Biofonctionnalités des Protéines et des Peptides (PB2P), Nancy-Université, Vandoeuvre-lès-Nancy, France.
authors.forename: Céline
authors.initials: C
authors.lastname: Cakir-Kiefer
authors.forename: Yves
authors.initials: Y
authors.lastname: Le Roux
authors.forename: Frédérique
authors.initials: F
authors.lastname: Balandras
authors.forename: Marie
authors.initials: M
authors.lastname: Trabalon
authors.forename: Annie
authors.initials: A
authors.lastname: Dary
authors.forename: François
authors.initials: F
authors.lastname: Laurent
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Gaillard
authors.forename: Laurent
authors.initials: L
authors.lastname: Miclo
mesh_terms: D000818:Animals; D002364:Caseins / Q000737:chemistry* / Q000378:metabolism; D002417:Cattle; D002918:Chymotrypsin / Q000378:metabolism; D004063:Digestion; D006801:Humans; D006868:Hydrolysis; D008297:Male; D008954:Models, Biological; D010446:Peptide Fragments / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D014357:Trypsin / Q000378:metabolism
chemical_list: D002364:Caseins; D010446:Peptide Fragments; D002918:Chymotrypsin; D014357:Trypsin