Revista: | Memorias do Instituto Oswaldo Cruz |
Base de datos: | PERIÓDICA |
Número de sistema: | 000437143 |
ISSN: | 0074-0276 |
Autors: | Matadamas Martínez, Félix1 Nogueda Torres, Benjamín2 Castillo, Rafael1 Hernández Campos, Alicia1 Barrera Valdes, María de la Luz2 León Avila, Gloria2 Hernández, José Manuel3 Yépez Mulia, Lilián4 |
Institucions: | 1Universidad Nacional Autónoma de México, Facultad de Química, Ciudad de México. México 2Instituto Politécnico Nacional, Escuela Nacional de Ciencias Biológicas, Ciudad de México. México 3Instituto Politécnico Nacional, Centro de Investigación y de Estudios Avanzados, Ciudad de México. México 4Instituto Mexicano del Seguro Social, Centro Médico Nacional Siglo XXI, Ciudad de México. México |
Any: | 2020 |
Volum: | 115 |
País: | Brasil |
Idioma: | Inglés |
Tipo de documento: | Artículo |
Enfoque: | Experimental, aplicado |
Resumen en inglés | 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 |
Disciplines | Medicina |
Paraules clau: | Farmacología, Antiparasitarios, Moleculas hibridas, Nitazoxanida, Benzimidazol, Cepas resistentes, Giardia intestinalis |
Keyword: | Pharmacology, Antiparasitic agents, Nitazoxanide, Benzimidazole, Hybrid molecules, Resistant strains, Giardia intestinalis |
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