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Parasitology Research

, Volume 107, Issue 3, pp 531–538 | Cite as

Biological and immunological activity of new imidazolidines against adult worms of Schistosoma mansoni

  • Juliana Kelle de Andrade Lemoine Neves
  • Sandra Paula Sarinho Botelho
  • Cristiane Moutinho Lagos de Melo
  • Valéria Rêgo Alves Pereira
  • Maria do Carmo Alves de Lima
  • Ivan da Rocha Pitta
  • Mônica Camelo Pessoa de Azevedo Albuquerque
  • Suely Lins Galdino
Original Paper

Abstract

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 µM, 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-γ 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.

Keywords

Nitric Oxide Schistosomiasis Adult Worm Praziquantel Schistosoma Mansoni 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Abbreviations

LPSF

Laboratório de Planejamento de Síntese de Fármacos

PZQ

Praziquantel

RZS

5-benzylidene-3-benzyl-4-thioxo-imidazolidin-2-one

RZS-2

5-(4-chloro-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one

RSZ-5

5-(4-fluoride-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one

Notes

Acknowledgements

This work was supported by grants from the Financiadora de Estudos e Projetos (FINEP), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), and Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq).

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Copyright information

© Springer-Verlag 2010

Authors and Affiliations

  • Juliana Kelle de Andrade Lemoine Neves
    • 1
    • 4
  • Sandra Paula Sarinho Botelho
    • 1
  • Cristiane Moutinho Lagos de Melo
    • 2
  • Valéria Rêgo Alves Pereira
    • 2
  • Maria do Carmo Alves de Lima
    • 1
  • Ivan da Rocha Pitta
    • 1
  • Mônica Camelo Pessoa de Azevedo Albuquerque
    • 3
  • Suely Lins Galdino
    • 1
  1. 1.Laboratório de Planejamento e Síntese de Fármacos (LPSF) do Departamento de Antibióticos-UFPERecifeBrazil
  2. 2.Departamento de Imunologia do Centro de Pesquisas Aggeu Magalhães—CPqAM/FIOCRUZ-UFPERecifeBrazil
  3. 3.Departamento de Medicina Tropical-UFPERecifeBrazil
  4. 4.Departamento de Antibióticos, Centro de Ciências BiológicasUniversidade Federal de PernambucoRecifeBrazil

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