Antischistosomal action of thioxo-imidazolidine compounds: an ultrastructural and cytotoxicity study |
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| Authors: | Neves Juliana Kelle A L de Lima Maria do Carmo Alves Pereira Valéria Rego Alves de Melo Cristiane Moutinho Lagos Peixoto Christina Alves Pitta Ivan da Rocha Albuquerque Mônica Camelo Pessoa Azevedo Galdino Suely Lins |
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| Affiliation: | aLaboratório de Planejamento e Síntese de Fármacos (LPSF), Departamento de Antibióticos, Centro de Ciências Biológicas, Universidade Federal de Pernambuco (UFPE), Av. Prof. Moraes Rego s/n, Cidade Universitária, 50670-901 Recife, PE, Brazil;bLaboratório de Imunogenética, Departamento de Imunologia, Centro de pesquisas Aggeu Magalhães, Fundação Oswaldo Cruz (FIOCRUZ), 50670-420 Recife, PE, Brazil;cLaboratório de Ultraestrutura, Departamento de Entomologia, Centro de Pesquisas Aggeu Magalhães, Fundação Oswaldo Cruz (FIOCRUZ), 50670-420 Recife, PE, Brazil;dLaboratório de Imunopatologia Keizo Asami (LIKA), Universidade Federal de Pernambuco, Av. Prof. Moraes Rego s/n, Cidade Universitária, 50670-901 Recife, PE, Brazil |
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| Abstract: | Schistosomiasis is a disease caused by helminthes of the genus Schistosoma, which threatens approximately 207 million people worldwide. Recently, strains of Schistosoma mansoni appear to be developing tolerance and resistance against Praziquantel, the most commonly available drug on the market used in the treatment of disease. This worrisome development justifies studies that seek alternatives for the prevention, treatment and cure of this disease. This study aimed to evaluate the in vitro activity of new imidazolidine compounds 1-benzyl-4-[(4-chloro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one (LPSF/PT-5) and 1-(4-chloro-benzyl)-4-[(4-fluoro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one (LPSF/PT-11) against adult worms of S. mansoni. LPSF/PT-5 and LPSF/PT-11 imidazolidine derivatives showed relevant schistosomicidal activity in vitro and induced significant ultrastructural alterations in worms and cell death: results similar to praziquantel. Thus, it is possible that these imidazolidine derivatives can be future candidates as schistosomotic drugs, but further studies are needed to elucidate the induced mechanisms behind this response. |
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| Keywords: | Schistosomiasis Schistosoma mansoni Praziquantel Imidazolidinone derivatives in vitro |
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