In Vitro Amoebicidal Activity of Imidazolium Salts Against Trophozoites

Several strains of the free-living genus Acanthamoeba can cause granulomatous amoebic encephalitis (GAE), a rare chronic and slowly progressive infection of the central nervous system (CNS), and Acanthamoeba keratitis (AK), a sight-threatening eye infectious disease. AK incidence has increased with the popularization of the contact lens wear and its treatment is currently limited and frequently unsuccessful. As imidazolium salts (IS), cationic imidazole derivatives, have promising antimicrobial potential.

The present study evaluated the amoebicidal activity of four IS; 1-n-hexadecyl-3-methylimidazolium methanesulfonate (C₁₆MImMeS), chloride (C₁₆MImCl) and bis (triluoromethylsulfonyl) imide (C₁₆MImNTf2 ), and 1-methyl-3-n-octadecylimidazolium chloride (C₁₈MImCl), against the Acanthamoeba castellanii (ATCC30010) environmental strain and a clinical isolate (genotype T4).

Three IS showed being lethal to 100% of the Acanthamoeba trophozoites at the minimum inhibitory concentrations of 125 and 62.5 μg/mL (C₁₆MImMeS), 31.25 and 62.5 μg/mL (C₁₆MImCl), and 125 and 125 μg/mL (C₁₈MImCl) for ATCC30010 and isolate T4, respectively. C₁₆MImNTf2 did not demonstrate amoebicidal activity. All active IS caused the hemolysis of erythrocytes. The cytotoxic effect of the IS was tested in RAW macrophages and human brain microvascular endothelial cells, which demonstrated cytotoxicity in all concentrations tested against both cell lines. As a consequence, these IS with amoebicidal activity presented low selectivity index values (SI) (SI < 1.0), demonstrating lack of parasite selectivity.

Thus, C₁₆MImMeS, C₁₆MImCl, and C18MImCl seem to hold greater promise as components for contact lens cleaning and disinfection solutions, instead of direct human application.