Your browser doesn't support javascript.
loading
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.
  • Matadamas-Martínez, Félix; Universidad Nacional Autónoma de México. Facultad de Química. Departamento de Farmacia. Mexico City. MX
  • Nogueda-Torres, Benjamín; Escuela Nacional de Ciencias Biológicas-Instituto Politécnico Nacional. Departamento de Parasitología. Mexico City. MX
  • Castillo, Rafael; Universidad Nacional Autónoma de México. Facultad de Química. Departamento de Farmacia. Mexico City. MX
  • Hernández-Campos, Alicia; Universidad Nacional Autónoma de México. Facultad de Química. Departamento de Farmacia. Mexico City. MX
  • Barrera-Valdes, María de la Luz; Escuela Nacional de Ciencias Biológicas-Instituto Politécnico Nacional. Departamento de Parasitología. Mexico City. MX
  • León-Ávila, Gloria; Escuela Nacional de Ciencias Biológicas-Instituto Politécnico Nacional. Departamento de Zoología. Laboratorio de Genética. Mexico City. MX
  • Hernández, José Manuel; Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional. Departamento de Biología Celular. Mexico City. MX
  • Yépez-Mulia, Lilián; Instituto Mexicano del Seguro Social. Centro Médico Siglo XXI. Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, Hospital de Pediatría. Mexico City. MX
Mem. Inst. Oswaldo Cruz ; 115: e190348, 2020. tab, graf
Article in English | LILACS | ID: biblio-1091246
ABSTRACT
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.
Subject(s)


Full text: Available Index: LILACS (Americas) Main subject: Thiazoles / Albendazole / Giardia lamblia / Cytoskeletal Proteins / Antiprotozoal Agents Type of study: Prognostic study Limits: Animals / Humans Language: English Journal: Mem. Inst. Oswaldo Cruz Journal subject: Tropical Medicine / Parasitology Year: 2020 Type: Article Affiliation country: Mexico Institution/Affiliation country: Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional/MX / Escuela Nacional de Ciencias Biológicas-Instituto Politécnico Nacional/MX / Instituto Mexicano del Seguro Social/MX / Universidad Nacional Autónoma de México/MX

Similar

MEDLINE

...
LILACS

LIS


Full text: Available Index: LILACS (Americas) Main subject: Thiazoles / Albendazole / Giardia lamblia / Cytoskeletal Proteins / Antiprotozoal Agents Type of study: Prognostic study Limits: Animals / Humans Language: English Journal: Mem. Inst. Oswaldo Cruz Journal subject: Tropical Medicine / Parasitology Year: 2020 Type: Article Affiliation country: Mexico Institution/Affiliation country: Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional/MX / Escuela Nacional de Ciencias Biológicas-Instituto Politécnico Nacional/MX / Instituto Mexicano del Seguro Social/MX / Universidad Nacional Autónoma de México/MX