title: A Tetrameric Peptide Derived from Bovine Lactoferricin Exhibits Specific Cytotoxic Effects against Oral Squamous-Cell Carcinoma Cell Lines.
abstract: Several short linear peptides derived from cyclic bovine lactoferricin were synthesized and tested for their cytotoxic effect against the oral cavity squamous-cell carcinoma (OSCC) cell lines CAL27 and SCC15. As a control, an immortalized and nontumorigenic cell line, Het-1A, was used. Linear peptides based on the RRWQWR core sequence showed a moderate cytotoxic effect and specificity towards tumorigenic cells. A tetrameric peptide, LfcinB(20-25)4, containing the RRWQWR motif, exhibited greater cytotoxic activity (>90%) in both OSCC cell lines compared to the linear lactoferricin peptide or the lactoferrin protein. Additionally, this tetrameric peptide showed the highest specificity towards tumorigenic cells among the tested peptides. Interestingly, this effect was very fast, with cell shrinkage, severe damage to cell membrane permeability, and lysis within one hour of treatment. Our results are consistent with a necrotic effect rather than an apoptotic one and suggest that this tetrameric peptide could be considered as a new candidate for the therapeutic treatment of OSCC.
authors.affiliation: Cellular and Molecular Physiology Group, Biomedical Research Institute, Faculty of Medicine, Universidad Nacional de Colombia, Bogotá 111321, Colombia.
authors.forename: Víctor A
authors.initials: VA
authors.lastname: Solarte
authors.affiliation: Department of Pharmacy, Faculty of Sciences, Universidad Nacional de Colombia, Bogotá 111321, Colombia.
authors.forename: Jaiver E
authors.initials: JE
authors.lastname: Rosas
authors.affiliation: Department of Chemistry, Faculty of Sciences, Universidad Nacional de Colombia, Bogotá 111321, Colombia.
authors.forename: Zuly J
authors.initials: ZJ
authors.lastname: Rivera
authors.affiliation: Centro de Medicina Regenerativa, Faculty of Medicine, Clínica Alemana, Universidad del Desarrollo, 7690000 Santiago, Chile.
authors.forename: Martha L
authors.initials: ML
authors.lastname: Arango-Rodríguez
authors.affiliation: Department of Pharmacy, Faculty of Sciences, Universidad Nacional de Colombia, Bogotá 111321, Colombia.
authors.forename: Javier E
authors.initials: JE
authors.lastname: García
authors.affiliation: Cellular and Molecular Physiology Group, Biomedical Research Institute, Faculty of Medicine, Universidad Nacional de Colombia, Bogotá 111321, Colombia.
authors.forename: Jean-Paul
authors.initials: JP
authors.lastname: Vernot
mesh_terms: D000818:Animals; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy*; D002417:Cattle; D045744:Cell Line, Tumor; D002463:Cell Membrane Permeability / Q000187:drug effects; D003603:Cytotoxins / Q000494:pharmacology*; D006801:Humans; D007781:Lactoferrin / Q000494:pharmacology*; D009062:Mouth Neoplasms / Q000188:drug therapy*; D009336:Necrosis / Q000188:drug therapy; D010455:Peptides / Q000494:pharmacology*
chemical_list: D003603:Cytotoxins; D010455:Peptides; C082171:lactoferricin B; D007781:Lactoferrin