title: In vitro amoebicidal activity of a ceragenin, cationic steroid antibiotic-13, against Acanthamoeba castellanii and its cytotoxic potential.
abstract: Acanthamoeba is a free-living amoeba causing a potentially blinding infection of the cornea. Acanthamoeba keratitis is difficult to treat, without total efficacy in some patients because of cysts that are less susceptible than trophozoites to the usual treatments. Contact lens wearers are most at risk and account for some 95% of cases. Cationic steroid antibiotic (CSA)-13 is a small molecule aminosterol that has been shown to mimic the activity of endogenous antimicrobial peptides and has bactericidal activity based on membrane disruption. We investigated here the in vitro effectiveness of CSA-13 with a concentration of 100, 75, 50, and 25  mg/mL on proliferation of Acanthamoeba castellanii trophozoites and cysts and cytotoxic potential. CSA-13 was evaluated for its amoebicidal activity using an inverted light microscope at 1, 2, 4, 8, 12, and 24  h. For the determination of cytotoxicity of the CSA-13 on L929 cells, agar diffusion tests were performed. CSA-13 inhibited trophozoite growth in dose- and time-dependent ways. At 1  h, no viable trophozoites were observed in the presence of CSA-13 solution in a concentration 100  mg/mL in phosphate-buffered saline. Results of cytotoxicity experiments demonstrated that CSA-13 solution had mild toxicity at 100  mg/mL concentration on cells, whereas it had no toxicity at 75  mg/mL concentration. The findings of this experiment as in vitro ameboebicidal activity for Acanthamoeba suggest that CSA-13 has a potential to be used as a new agent in lens solutions to prevent Acanthamoeba growth and infections.
authors.affiliation: Research Center of Cumhuriyet University School of Medicine, Sivas, Turkey. zubeydeakin@yahoo.com
authors.forename: Zubeyde Akın
authors.initials: ZA
authors.lastname: Polat
authors.forename: Paul B
authors.initials: PB
authors.lastname: Savage
authors.forename: Carl
authors.initials: C
authors.lastname: Genberg
mesh_terms: D048248:Acanthamoeba castellanii / Q000187:drug effects*; D000563:Amebicides / Q000494:pharmacology*; D000818:Animals; D004305:Dose-Response Relationship, Drug; D005779:Immunodiffusion; D066298:In Vitro Techniques; D009994:Osmolar Concentration; D013256:Steroids / Q000008:administration & dosage / Q000494:pharmacology*; D013997:Time Factors; D018675:Toxicity Tests; D053058:Trophozoites / Q000187:drug effects / Q000254:growth & development
chemical_list: D000563:Amebicides; D013256:Steroids; C521528:ceragenin CSA-13