Journal
JOURNAL OF APPLIED MICROBIOLOGY
Volume 134, Issue 1, Pages -Publisher
OXFORD UNIV PRESS
DOI: 10.1093/jambio/lxac030
Keywords
Acanthamoeba castellanii; anti-amoebic activity; amoebicidal; encystation; excystation; cytotoxicity; cytopathogenicity
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The study found that benzofuran/benzothiophene derivatives have significant anti-amoebic activity against Acanthamoeba castellanii of the T4 genotype. Compounds 1p and 1e showed the highest amoebicidal activity, eliminating 68% and 64% of the amoebae, respectively. These compounds also effectively suppressed the encystation and excystation processes in A. castellanii. Furthermore, the compounds exhibited minimal cytotoxic properties against human cells and reduced amoeba-mediated cytopathogenicity.
Aims To determine the anti-amoebic activity of benzofuran/benzothiophene-possessing compounds against Acanthamoeba castellanii of the T4 genotype. Method and results A series of benzofuran/benzothiophene-possessing compounds were tested for their anti-amoebic activities, in particular, to block encystation and excystation processes in amoebae. Cytotoxicity of the compounds were evaluated using lactate dehydrogenase (LDH) assays. The amoebicidal assay results revealed significant anti-amoebic effects against A. castellanii. Compounds 1p and 1e showed the highest amoebicidal activity, eliminating 68% and 64% of the amoebae, respectively. These compounds remarkably repressed both the encystation and excystation processes in A. castellanii. Furthermore, the selected compounds presented minimal cytotoxic properties against human cells, as well as considerably abridged amoeba-mediated cytopathogenicity when compared to the amoebae alone. Conclusions Our findings show that benzofuran/benzothiophene derivatives depict potent anti-amoebic activities; thus these compounds should be used as promising and novel agents in the rationale development of therapeutic strategies against Acanthamoeba infections.
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