Analysis of the effect of a 2-(trifluoromethyl)-1H-benzimidazole derivative on Trichinella spiralis muscle larvae

作者：Matadamas Martinez Felix; Nogueda Torres Benjamin; Hernandez Campos Alicia; Hernandez Luis Francisco; Castillo Rafael; Mendoza Guillermo; Ambrosio Javier R; Andres Antonio Gabriela; Yepez Mulia Lilian^*

来源：Veterinary Parasitology, 2013, 194(2-4): 193-197.

DOI：10.1016/j.vetpar.2013.01.054

• Trichinella spiralis
• Benzimidazole derivative
• Anthelminthic activity
• Proteomic analysis

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-beta-cyclodextrin (1/HP-beta CD) was prepared. When 1/HP-beta CD 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.

• 出版日期2013-5-20