Biological and immunological activity of new imidazolidines against adult worms of Schistosoma mansoni.
The only drug available for treating schistosomiasis is praziquantel, however there are already reports of resistance to its use in treatment, making it necessary to search and develop new compounds to combat schistosomiasis. We tested, in vitro, two new products, Laboratório de Planejamento de Síntese de Fármacos (LPSF)/5-(4-chloro-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one (RZS-2) and LPSF/5-(4-fluoride-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one (RZS-5) imidazolidines, against adult worms of Schistosoma mansoni. Efficacy and safety of these compounds were analyzed through IC50 cytotoxicity, immune response and cell viability tests. At different concentrations ranging from 40-640 microM, the imidazolidines produced motor abnormalities, inhibition of pairing and oviposition and mortality within 24 h at the higher concentrations. Although not triggering changes in IFN-gamma and IL-10, LPSF/RZS-2 and LPSF/RZS-5 induced production of nitric oxide and showed similar behavior to praziquantel in the cell death test.
Neves
Juliana Kelle de Andrade Lemoine
JK
Laboratório de Planejamento e Síntese de Fármacos (LPSF) do Departamento de Antibióticos-UFPE, Recife, Pernambuco, Brazil. lemoineju@gmail.com
Botelho
Sandra Paula Sarinho
SP
de Melo
Cristiane Moutinho Lagos
CM
Pereira
Valéria Rêgo Alves
VR
de Lima
Maria do Carmo Alves
Mdo C
Pitta
Ivan da Rocha
Ida R
Albuquerque
Mônica Camelo Pessoa de Azevedo
MC
Galdino
Suely Lins
SL
D000818:Animals; D005260:Female; D048289:Imidazolidines / Q000008:administration & dosage / Q000276:immunology / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D021261:Parasitic Sensitivity Tests; D012550:Schistosoma mansoni / Q000187:drug effects*; D012555:Schistosomiasis mansoni / Q000188:drug therapy / Q000469:parasitology; D012556:Schistosomicides / Q000008:administration & dosage / Q000276:immunology / Q000494:pharmacology*
C553638:5-(4-chloro-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one); C553639:5-(4-fluoride-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one); D048289:Imidazolidines; D012556:Schistosomicides