title: Antitumor effect of the antimicrobial peptide GLI13-8 derived from domain of the avian β-defensin-4.
abstract: We previously reported that GLI13-8, one of cationic antimicrobial peptides from linear avian β-defensin-4 (RL38) analogs, exhibited high antimicrobial activities against both Gram-negative and Gram-positive bacteria. In the present study, we reported the in vitro cytotoxicity of GLI13-8 using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Results showed that the cytotoxicity of GLI13-8 in three human carcinoma cells (HepG2, SGC7901, and A375) was in a dose-dependent manner. When the concentration of GLI13-8 is <128 μM, it had no toxicity towards the normal human fibroblasts (MRC-5). The Annexin-V-FITC/PI staining assay, the Hoechst 33258/PI staining assay, the permeability of fluorescein macromolecules and scanning electron microscope assays, mitochondrial membrane potential assay, caspases-3 and poly ADP-ribose polymerase (PARP) assays have been carried out. Results indicated that apoptosis was induced by GLI13-8 in HepG2 cells, and demonstrated that GLI13-8 induced loss of mitochondrial membrane potential, disruption of HepG2 cell membranes, and activation of caspase-3 and PARP. These findings suggested that GLI13-8 may be an effective agent for HepG2 cells.
authors.affiliation: Laboratory of Molecular Nutrition and Immunity, Institute of Animal Nutrition, Northeast Agricultural University, Harbin 150030, China.
authors.forename: Yao
authors.initials: Y
authors.lastname: Gu
authors.forename: Na
authors.initials: N
authors.lastname: Dong
authors.forename: Anshan
authors.initials: A
authors.lastname: Shan
authors.forename: Qingquan
authors.initials: Q
authors.lastname: Ma
authors.forename: Jianping
authors.initials: J
authors.lastname: Li
authors.forename: Baojing
authors.initials: B
authors.lastname: Cheng
mesh_terms: D000818:Animals; D023181:Antimicrobial Cationic Peptides / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis; D001717:Birds; D053148:Caspase 3 / Q000378:metabolism; D002463:Cell Membrane Permeability; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D019793:Fluorescein / Q000493:pharmacokinetics; D056945:Hep G2 Cells; D006801:Humans; D053078:Membrane Potential, Mitochondrial; D008855:Microscopy, Electron, Scanning; D011065:Poly(ADP-ribose) Polymerases / Q000378:metabolism; D023083:beta-Defensins / Q000737:chemistry*
chemical_list: D023181:Antimicrobial Cationic Peptides; D000970:Antineoplastic Agents; C000588577:GLI13-8 peptide; D023083:beta-Defensins; D011065:Poly(ADP-ribose) Polymerases; D053148:Caspase 3; D019793:Fluorescein
keywords: AvBD-4 derivative; antimicrobial peptide; apoptosis; carcinoma