title: Analysis of the effect of a 2-(trifluoromethyl)-1H-benzimidazole derivative on Trichinella spiralis muscle larvae.
abstract: Albendazole and mebendazole are widely used in the treatment of trichinellosis; however, chemotherapy failure has been reported. In an effort to develop new anthelminthic compounds, we examined a previously synthesized 2-(trifluoromethyl)-1H-benzimidazole derivative (1) that showed good in vitro activity against Trichinella spiralis muscle larvae but low in vivo efficacy. In order to improve the solubility of compound 1, an inclusion complex with 2-hydroxypropyl-β-cyclodextrin (1/HP-βCD) was prepared. When 1/HP-βCD was tested in vivo, it significantly reduced the ML burden (84%). In addition, a proteomic analysis of T. spiralis ML treated with 1 revealed significant changes in the expression levels of proteins involved in energy metabolism and the cytoskeleton of the parasite. Compound (1) also induced extensive ultrastructural changes in the cuticle, hypodermis and midgut of the parasite.
authors: UIMEIP-Pediatría, Centro Médico Nacional Siglo XXI, IMSS, México, DF 06720, Mexico.
authors: Félix
authors: F
authors: Matadamas-Martínez
authors: Benjamín
authors: B
authors: Nogueda-Torres
authors: Alicia
authors: A
authors: Hernández-Campos
authors: Francisco
authors: F
authors: Hernández-Luis
authors: Rafael
authors: R
authors: Castillo
authors: Guillermo
authors: G
authors: Mendoza
authors: Javier R
authors: JR
authors: Ambrosio
authors: Gabriela
authors: G
authors: Andrés-Antonio
authors: Lilián
authors: L
authors: Yépez-Mulia
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000818:Animals; D000871:Anthelmintics / Q000494:pharmacology*; D001562:Benzimidazoles / Q000494:pharmacology*; D015180:Electrophoresis, Gel, Two-Dimensional; D005786:Gene Expression Regulation / Q000187:drug effects; D007814:Larva; D013058:Mass Spectrometry; D051379:Mice; D008807:Mice, Inbred BALB C; D046529:Microscopy, Electron, Transmission; D009132:Muscles / Q000469:parasitology; D040901:Proteomics; D017160:Trichinella spiralis / Q000187:drug effects* / Q000648:ultrastructure; D014235:Trichinellosis / Q000188:drug therapy / Q000469:parasitology*; D047392:beta-Cyclodextrins / Q000494:pharmacology*
chemical_list: D000871:Anthelmintics; D001562:Benzimidazoles; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin