In vitro activity of dermaseptin S1 derivatives against genital pathogens.
The aim of this study was to evaluate the biological activity of nine dermaseptin-S1 (DRS-S1) derivatives (synthesized by solid-phase methods and purified) against different pathogens causing genital infections (Trichomonas vaginalis, Herpes simplex virus, Papillomavirus). The in vitro activity on T. vaginalis was determined by counting the protozoon in a hemocytometer after vital staining with trypan blue; antiviral activity of the compounds was tested on monolayers of Vero cells for Herpes simplex virus-1 (GFP) and on 293TT cells for human papillomavirus (HPV-16) pseudovirions (GFP). The cytotoxicity of the derivatives was assessed by evaluating both the hemolytic activity and the effect on Vero and 293TT cells. The DRS-S1 longer peptides demonstrated a superior activity on T. vaginalis but also a certain cytopathic effect. The compounds with 29 amino acids exhibited activity against the two viruses tested at concentrations not toxic to cells. The results obtained show that some of the synthetic peptides assessed have inhibitory activity against the pathogens tested, indicating a potential for the development of new molecules for use as topical microbicides to prevent the sexual transmission of microorganisms.
Savoia
Dianella
D
Department of Clinical and Biological Sciences, University of Torino, S. Luigi Gonzaga Hospital, Orbassano, Piedmont, Italy. dianella.savoia@unito.it
Donalisio
Manuela
M
Civra
Andrea
A
Salvadori
Severo
S
Guerrini
Remo
R
D029845:Amphibian Proteins / Q000627:therapeutic use*; D000818:Animals; D000890:Anti-Infective Agents / Q000627:therapeutic use; D023181:Antimicrobial Cationic Peptides / Q000627:therapeutic use*; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D012777:Cottontail rabbit papillomavirus / Q000187:drug effects; D004912:Erythrocytes / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D011528:Protozoan Infections / Q000188:drug therapy; D018139:Simplexvirus / Q000187:drug effects; D014244:Trichomonas / Q000187:drug effects; D014709:Vero Cells
D029845:Amphibian Proteins; D000890:Anti-Infective Agents; D023181:Antimicrobial Cationic Peptides; C070905:dermaseptin