title: Interaction of pleurocidin and its analogs with phospholipid membrane and their antibacterial activity.
abstract: A 25-mer cationic peptide pleurocidin, isolated from the winter flounder, has broad antibacterial activity. To clarify the structure-activity relationship, its properties and biological activity were examined. CD measurements showed that pleurocidin took an alpha-helical structure in the presence of DOPC/DOPG (3:1, anionic) vesicles. Very weak hemolytic activity of pleurocidin was observed and its antibacterial activity was moderate. Tryptophan fluorescence shift measurements showed that pleurocidin interacted weakly with a neutral phospholipid, but strongly with an acidic phospholipid. The peptide exhibited weak dye-leakage activity for DOPC (neutral) vesicles and moderate activity for acidic vesicles. From experiments on dye-leakage activity and membrane translocation of the peptide, it seemed likely that pleurocidin, like magainin 2, forms pores in the lipid membrane. A study of amino acid substitution in pleurocidin revealed that alpha-helicity, rather than hydrophobicity, affects the properties and activity of the peptide.
authors.affiliation: Department of Applied Chemistry, Faculty of Engineering, Nagasaki University, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Yoshida
authors.forename: Y
authors.initials: Y
authors.lastname: Mukai
authors.forename: T
authors.initials: T
authors.lastname: Niidome
authors.forename: C
authors.initials: C
authors.lastname: Takashi
authors.forename: Y
authors.initials: Y
authors.lastname: Tokunaga
authors.forename: T
authors.initials: T
authors.lastname: Hatakeyama
authors.forename: H
authors.initials: H
authors.lastname: Aoyagi
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D002942:Circular Dichroism; D029941:Fish Proteins; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D008567:Membranes, Artificial; D008826:Microbial Sensitivity Tests; D010455:Peptides / Q000378:metabolism; D010743:Phospholipids / Q000378:metabolism*; D021381:Protein Transport; D011506:Proteins / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D011817:Rabbits; D013050:Spectrometry, Fluorescence; D014364:Tryptophan / Q000737:chemistry
chemical_list: D000900:Anti-Bacterial Agents; D029941:Fish Proteins; D008567:Membranes, Artificial; D010455:Peptides; D010743:Phospholipids; D011506:Proteins; C105851:pleurocidin; D014364:Tryptophan