title: Study of the activity of 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin-2-one against Schistosomiasis mansoni in mice.
abstract: Previous studies conducted with the imidazolidinic derivative 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin-2-one (LPSF-PT05) show outstanding activity against adult Schistosoma mansoni worms in vitro. In the first phase of this study, S. mansoni-infected mice were treated, orally, with 100 mg/Kg of the LPSF-PT05 in three formulations: Tween 80 and saline solution, oil/water (70 : 30) emulsion, and solid dispersion with polyethylene glycol (PEG). In the second phase, three other doses of the LPSF-PT05 in PEG were tested: 3, 10, 30 mg/kg. These treatment regimens significantly reduced the number of recovered worms due to increases in the solubility of the compound in this formulation; the greatest reduction (70.5%) was observed at the dose of 100 mg/kg. There was no changes in the pattern of mature egg compared to immature eggs; however there was a significant increase in the number of dead eggs. Histopathological analysis of liver tissue showed changes in morphological aspects of the hepatic parenchyma with decrease exudative-productive hepatic granuloma stages, although we found no significant differences in IFN-γ, IL-4, IL-10, or NO production in response to the specific antigen SEA. The results show the derivative LPSF-PT05 to be a potential candidate in the etiological treatment of schistosomiasis with a possible dampening effect of the granulomatous process.
authors.affiliation: Laboratório de Planejamento e Síntese de Fármacos, Universidade Federal de Pernambuco, Avenida Professors Moraes Rego 1265, Cidade Universitária, Recife, PE, Brazil.
authors.forename: Andréa Cristina Apolinário
authors.initials: AC
authors.lastname: da Silva
authors.forename: Juliana Kelle de Andrade Lemoine
authors.initials: JK
authors.lastname: Neves
authors.forename: João Inácio
authors.initials: JI
authors.lastname: Irmão
authors.forename: Vláudia Maria Assis
authors.initials: VM
authors.lastname: Costa
authors.forename: Valdênia Maria Oliveira
authors.initials: VM
authors.lastname: Souza
authors.forename: Paloma Lys
authors.initials: PL
authors.lastname: de Medeiros
authors.forename: Eliete Cavalcanti
authors.initials: EC
authors.lastname: da Silva
authors.forename: Maria do Carmo Alves
authors.initials: Mdo C
authors.lastname: de Lima
authors.forename: Ivan da Rocha
authors.initials: Ida R
authors.lastname: Pitta
authors.forename: Mônica Camelo Pessoa de Azevedo
authors.initials: MC
authors.lastname: Albuquerque
authors.forename: Suely Lins
authors.initials: SL
authors.lastname: Galdino
mesh_terms: D000818:Animals; D000871:Anthelmintics / Q000494:pharmacology*; D005260:Female; D008099:Liver / Q000187:drug effects / Q000276:immunology / Q000473:pathology; D051379:Mice; D010063:Ovum / Q000187:drug effects; D012550:Schistosoma mansoni / Q000187:drug effects*; D012555:Schistosomiasis mansoni / Q000188:drug therapy*; D013867:Thiohydantoins / Q000494:pharmacology*
chemical_list: D000871:Anthelmintics; C575334:LPSF-PT05; D013867:Thiohydantoins