In Vitro Amoebicidal Activity of Imidazolium Salts Against Trophozoites

Abstract

Introduction

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.

Materials and Methods

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).

Results

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.

Conclusion

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

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Acknowledgements

This study was financed in part by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior—Brasil (CAPES)—Finance Code 001; and the Conselho Nacional de Desenvolvimento Científico e Tecnológico—Brasil (CNPq). Dr. Julio Scharfstein (Instituto de Biofísica Carlos Chagas Filho, UFRJ) is kindly acknowledged for the donation of human brain microvascular endothelial cells.

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Fabres, L.F., da Costa Gonçalves, F., Duarte, E.O.S. et al. In Vitro Amoebicidal Activity of Imidazolium Salts Against Trophozoites. Acta Parasit. 65, 317–326 (2020). https://doi.org/10.2478/s11686-019-00161-6

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Keywords

  • Acanthamoeba
  • Imidazolium ionic liquids
  • Clinical and environmental isolates
  • Keratitis
  • Amoebic encephalitis
  • In vitro cytotoxicity