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Characterisation of the in vitro activity of a Nitazoxanide-N-methyl-1H-benzimidazole hybrid molecule against albendazole and nitazoxanide susceptible and resistant strains of Giardia intestinalis and its in vivo giardicidal activity.
Matadamas-Martínez, Félix; Nogueda-Torres, Benjamín; Castillo, Rafael; Hernández-Campos, Alicia; Barrera-Valdes, María de la Luz; León-Ávila, Gloria; Hernández, José Manuel; Yépez-Mulia, Lilián.
Afiliação
  • Matadamas-Martínez F; Universidad Nacional Autónoma de México, Facultad de Química, Departamento de Farmacia, Mexico City, Mexico.
  • Nogueda-Torres B; Instituto Mexicano del Seguro Social, Centro Médico Siglo XXI, Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, Hospital de Pediatría, Mexico City, Mexico.
  • Castillo R; Escuela Nacional de Ciencias Biológicas-Instituto Politécnico Nacional, Departamento de Parasitología, Mexico City, Mexico.
  • Hernández-Campos A; Universidad Nacional Autónoma de México, Facultad de Química, Departamento de Farmacia, Mexico City, Mexico.
  • Barrera-Valdes ML; Universidad Nacional Autónoma de México, Facultad de Química, Departamento de Farmacia, Mexico City, Mexico.
  • León-Ávila G; Escuela Nacional de Ciencias Biológicas-Instituto Politécnico Nacional, Departamento de Parasitología, Mexico City, Mexico.
  • Hernández JM; Instituto Mexicano del Seguro Social, Centro Médico Siglo XXI, Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, Hospital de Pediatría, Mexico City, Mexico.
  • Yépez-Mulia L; Escuela Nacional de Ciencias Biológicas-Instituto Politécnico Nacional, Departamento de Zoología, Laboratorio de Genética, Mexico City, Mexico.
Mem Inst Oswaldo Cruz ; 115: e190348, 2020.
Article em En | MEDLINE | ID: mdl-32049098
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

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiazóis / Albendazol / Giardia lamblia / Proteínas do Citoesqueleto / Antiprotozoários Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Revista: Mem Inst Oswaldo Cruz Ano de publicação: 2020 Tipo de documento: Article País de afiliação: México País de publicação: Brasil

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiazóis / Albendazol / Giardia lamblia / Proteínas do Citoesqueleto / Antiprotozoários Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Revista: Mem Inst Oswaldo Cruz Ano de publicação: 2020 Tipo de documento: Article País de afiliação: México País de publicação: Brasil