Research Center of Cumhuriyet University School of Medicine, Sivas, Turkey.
J Ocul Pharmacol Ther. 2011 Feb;27(1):1-5. doi: 10.1089/jop.2010.0041. Epub 2010 Dec 13.
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.
棘阿米巴是一种自由生活的阿米巴原虫,可引起角膜的潜在致盲性感染。棘阿米巴角膜炎难以治疗,在某些患者中疗效不理想,因为囊包对常用治疗方法的敏感性不如滋养体。隐形眼镜佩戴者风险最高,占病例的约 95%。阳离子类固醇抗生素(CSA)-13 是一种小分子氨基固醇,已被证明可以模拟内源性抗菌肽的活性,并具有基于膜破坏的杀菌活性。我们在此研究了 CSA-13 在浓度为 100、75、50 和 25mg/ml 时对棘阿米巴包囊和滋养体增殖的体外有效性和细胞毒性。使用倒置显微镜在 1、2、4、8、12 和 24 小时评估 CSA-13 的杀阿米巴活性。为了确定 CSA-13 对 L929 细胞的细胞毒性,进行了琼脂扩散试验。CSA-13 以剂量和时间依赖的方式抑制滋养体生长。在 1 小时时,在含有 100mg/ml CSA-13 的磷酸盐缓冲液中不存在存活的滋养体。细胞毒性实验结果表明,CSA-13 溶液在 100mg/ml 浓度下对细胞具有轻度毒性,而在 75mg/ml 浓度下则没有毒性。该实验的结果表明 CSA-13 具有体外杀阿米巴活性,有望作为隐形眼镜溶液中的一种新药物,用于预防棘阿米巴生长和感染。