TY - JOUR
T1 - Analysis of the effect of a 2-(trifluoromethyl)-1H-benzimidazole derivative on Trichinella spiralis muscle larvae
AU - Matadamas-Martínez, Félix
AU - Nogueda-Torres, Benjamín
AU - Hernández-Campos, Alicia
AU - Hernández-Luis, Francisco
AU - Castillo, Rafael
AU - Mendoza, Guillermo
AU - Ambrosio, Javier R.
AU - Andrés-Antonio, Gabriela
AU - Yépez-Mulia, Lilián
N1 - Funding Information:
Authors thank Olivia Reynoso and María Esther Sánchez for their technical assistance. Matadamas-Martínez was the recipient of a fellowship from the IMSS and CONACyT-México (Grants 2010021 and 231497 ). This work was supported by grants from CONACyT Mexico ( 80093 ) and the IMSS ( FIS/IMSS/PROT/G09/764 ).
PY - 2013
Y1 - 2013
N2 - 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)-1. H-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.
AB - 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)-1. H-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.
KW - Anthelminthic activity
KW - Benzimidazole derivative
KW - Proteomic analysis
KW - Trichinella spiralis
UR - http://www.scopus.com/inward/record.url?scp=84877799945&partnerID=8YFLogxK
U2 - 10.1016/j.vetpar.2013.01.054
DO - 10.1016/j.vetpar.2013.01.054
M3 - Artículo
C2 - 23462252
SN - 0304-4017
VL - 194
SP - 193
EP - 197
JO - Veterinary Parasitology
JF - Veterinary Parasitology
IS - 2-4
ER -