title: Lactoferricin-related peptides with inhibitory effects on ACE-dependent vasoconstriction.
abstract: A selection of lactoferricin B (LfcinB)-related peptides with an angiotensin I-converting enzyme (ACE) inhibitory effect have been examined using in vitro and ex vivo functional assays. Peptides that were analyzed included a set of sequence-related antimicrobial hexapeptides previously reported and two representative LfcinB-derived peptides. In vitro assays using hippuryl-L-histidyl-L-leucine (HHL) and angiotensin I as substrates allowed us to select two hexapeptides, PACEI32 (Ac-RKWHFW-NH2) and PACEI34 (Ac-RKWLFW-NH2), and also a LfcinB-derived peptide, LfcinB17-31 (Ac-FKCRRWQWRMKKLGA-NH2). Ex vivo functional assays using rabbit carotid arterial segments showed PACEI32 (both D- and L-enantiomers) and LfcinB17-31 have inhibitory effects on ACE-dependent angiotensin I-induced contraction. None of the peptides exhibited in vitro ACE inhibitory activity using bradykinin as the substrate. In conclusion, three bioactive lactoferricin-related peptides exhibit inhibitory effects on both ACE activity and ACE-dependent vasoconstriction with potential to modulate hypertension that deserves further investigation.
authors.affiliation: Departamento de Biotecnología de Alimentos, Instituto de Agroquímica y Tecnología de Alimentos, Consejo Superior de Investigaciones Científicas, Burjassot, and Centro de Investigación, Hospital Universitario La Fe, Valencia, Spain.
authors.forename: José M
authors.initials: JM
authors.lastname: Centeno
authors.forename: María C
authors.initials: MC
authors.lastname: Burguete
authors.forename: María
authors.initials: M
authors.lastname: Castelló-Ruiz
authors.forename: María
authors.initials: M
authors.lastname: Enrique
authors.forename: Salvador
authors.initials: S
authors.lastname: Vallés
authors.forename: Juan B
authors.initials: JB
authors.lastname: Salom
authors.forename: Germán
authors.initials: G
authors.lastname: Torregrosa
authors.forename: José F
authors.initials: JF
authors.lastname: Marcos
authors.forename: Enrique
authors.initials: E
authors.lastname: Alborch
authors.forename: Paloma
authors.initials: P
authors.lastname: Manzanares
mesh_terms: D000803:Angiotensin I / Q000494:pharmacology; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000494:pharmacology*; D000818:Animals; D017536:Carotid Artery, Common / Q000187:drug effects / Q000502:physiology; D066298:In Vitro Techniques; D007781:Lactoferrin / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*; D007703:Peptidyl-Dipeptidase A / Q000502:physiology; D011817:Rabbits; D014661:Vasoconstriction / Q000187:drug effects*
chemical_list: D000806:Angiotensin-Converting Enzyme Inhibitors; D010455:Peptides; C082171:lactoferricin B; D000803:Angiotensin I; D007703:Peptidyl-Dipeptidase A; D007781:Lactoferrin