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1.
Mem Inst Oswaldo Cruz ; 115: e190348, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32049098

RESUMO

BACKGROUND: It was previously demonstrated that CMC-20, a nitazoxanide and N-methyl-1H-benzimidazole hybrid molecule, had higher in vitro activity against Giardia intestinalis WB strain than metronidazole and albendazole and similar to nitazoxanide. OBJETIVES: To evaluate the in vitro activity of CMC-20 against G. intestinalis strains with different susceptibility/resistance to albendazole and nitazoxanide and evaluate its effect on the distribution of parasite cytoskeletal proteins and its in vivo giardicidal activity. METHODS: CMC-20 activity was tested against two isolates from patients with chronic and acute giardiasis, an experimentally induced albendazole resistant strain and a nitazoxanide resistant clinical isolate. CMC-20 effect on the distribution of parasite cytoskeletal proteins was analysed by indirect immunofluorescence and its activity was evaluated in a murine model of giardiasis. FINDINGS CMC-20: showed broad activity against susceptible and resistant strains to albendazole and nitaxozanide. It affected the parasite microtubule reservoir and triggered the parasite encystation. In this process, alpha-7.2 giardin co-localised with CWP-1 protein. CMC-20 reduced the infection time and cyst load in feces of G. muris infected mice similar to albendazole. MAIN CONCLUSIONS: The in vitro and in vivo giardicidal activity of CMC-20 suggests its potential use in the treatment of giardiasis.


Assuntos
Albendazol/farmacologia , Antiprotozoários/farmacologia , Proteínas do Citoesqueleto/efeitos dos fármacos , Giardia lamblia/efeitos dos fármacos , Tiazóis/farmacologia , Albendazol/química , Animais , Antiprotozoários/química , Técnica Indireta de Fluorescência para Anticorpo , Humanos , Camundongos , Nitrocompostos , Testes de Sensibilidade Parasitária , Tiazóis/química , Fatores de Tempo
2.
Mem. Inst. Oswaldo Cruz ; 115: e190348, 2020. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1091246

RESUMO

BACKGROUND It was previously demonstrated that CMC-20, a nitazoxanide and N-methyl-1H-benzimidazole hybrid molecule, had higher in vitro activity against Giardia intestinalis WB strain than metronidazole and albendazole and similar to nitazoxanide. OBJETIVES To evaluate the in vitro activity of CMC-20 against G. intestinalis strains with different susceptibility/resistance to albendazole and nitazoxanide and evaluate its effect on the distribution of parasite cytoskeletal proteins and its in vivo giardicidal activity. METHODS CMC-20 activity was tested against two isolates from patients with chronic and acute giardiasis, an experimentally induced albendazole resistant strain and a nitazoxanide resistant clinical isolate. CMC-20 effect on the distribution of parasite cytoskeletal proteins was analysed by indirect immunofluorescence and its activity was evaluated in a murine model of giardiasis. FINDINGS CMC-20 showed broad activity against susceptible and resistant strains to albendazole and nitaxozanide. It affected the parasite microtubule reservoir and triggered the parasite encystation. In this process, alpha-7.2 giardin co-localised with CWP-1 protein. CMC-20 reduced the infection time and cyst load in feces of G. muris infected mice similar to albendazole. MAIN CONCLUSIONS The in vitro and in vivo giardicidal activity of CMC-20 suggests its potential use in the treatment of giardiasis.


Assuntos
Humanos , Animais , Camundongos , Tiazóis/farmacologia , Albendazol/farmacologia , Giardia lamblia/efeitos dos fármacos , Proteínas do Citoesqueleto/efeitos dos fármacos , Antiprotozoários/farmacologia , Tiazóis/química , Fatores de Tempo , Albendazol/química , Técnica Indireta de Fluorescência para Anticorpo , Testes de Sensibilidade Parasitária , Antiprotozoários/química
3.
Mem. Inst. Oswaldo Cruz ; 115: e190348, 2020. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1056773

RESUMO

BACKGROUND It was previously demonstrated that CMC-20, a nitazoxanide and N-methyl-1H-benzimidazole hybrid molecule, had higher in vitro activity against Giardia intestinalis WB strain than metronidazole and albendazole and similar to nitazoxanide. OBJETIVES To evaluate the in vitro activity of CMC-20 against G. intestinalis strains with different susceptibility/resistance to albendazole and nitazoxanide and evaluate its effect on the distribution of parasite cytoskeletal proteins and its in vivo giardicidal activity. METHODS CMC-20 activity was tested against two isolates from patients with chronic and acute giardiasis, an experimentally induced albendazole resistant strain and a nitazoxanide resistant clinical isolate. CMC-20 effect on the distribution of parasite cytoskeletal proteins was analysed by indirect immunofluorescence and its activity was evaluated in a murine model of giardiasis. FINDINGS CMC-20 showed broad activity against susceptible and resistant strains to albendazole and nitaxozanide. It affected the parasite microtubule reservoir and triggered the parasite encystation. In this process, alpha-7.2 giardin co-localised with CWP-1 protein. CMC-20 reduced the infection time and cyst load in feces of G. muris infected mice similar to albendazole. MAIN CONCLUSIONS The in vitro and in vivo giardicidal activity of CMC-20 suggests its potential use in the treatment of giardiasis.


Assuntos
Humanos , Animais , Camundongos , Tiazóis/farmacologia , Albendazol/farmacologia , Giardia lamblia/efeitos dos fármacos , Proteínas do Citoesqueleto/efeitos dos fármacos , Antiprotozoários/farmacologia , Tiazóis/química , Fatores de Tempo , Albendazol/química , Técnica Indireta de Fluorescência para Anticorpo , Testes de Sensibilidade Parasitária , Antiprotozoários/química
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