Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2014 |
| Outros Autores: | , , , , , , , , , , , , , |
| Tipo de documento: | Artigo |
| Idioma: | eng |
| Título da fonte: | Repositório Institucional da FIOCRUZ (ARCA) |
| Texto Completo: | https://www.arca.fiocruz.br/handle/icict/25583 |
Resumo: | Conselho Nacional de Desenvolvimento Científico e Tecnológico (CPNq) and Fundação Oswaldo Cruz (FIOCRUZ). FAPESB postdoctoral scholarship. |
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Santiago, Edna de FariasOliveira, Sheilla Andrade deOliveira Filho, Gevânio Bezerra deMoreira, Diogo Rodrigo MagalhaesGomes, Paulo André TeixeiraSilva, Anekécia Lauro daBarros, Andréia Ferreira deSilva, Aline Caroline daSantos, Thiago André Ramos dosPereira, Valéria Rêgo AlvesGonçalves, Gabriel Gazzoni AraújoBrayner, Fábio AndréAlves, Luiz CarlosWanderley, Almir GonçalvesLeite, Ana Cristina Lima2018-04-03T14:24:14Z2018-04-03T14:24:14Z2014SANTIAGO, E. F. et al. Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles. Antimicrobial Agents and Chemotherapy, v. 58, n. 1, p. 352–363, 2014.0066-4804https://www.arca.fiocruz.br/handle/icict/2558310.1128/AAC.01900-13Conselho Nacional de Desenvolvimento Científico e Tecnológico (CPNq) and Fundação Oswaldo Cruz (FIOCRUZ). FAPESB postdoctoral scholarship.Federal University of Pernambuco. Department of Pharmacy. Recife, PE, Brazil / Federal University of Pernambuco. Laboratory of Immunopathology. Recife, PE, BrazilFederal University of Pernambuco. Laboratory of Immunopathology. Recife, PE, BrazilFederal University of Pernambuco. Department of Pharmacy. Recife, PE, BrazilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilFederal University of Pernambuco. Department of Pharmacy. Recife, PE, BrazilFederal University of Pernambuco. Laboratory of Immunopathology. Recife, PE, BrazilFederal University of Pernambuco. Laboratory of Immunopathology. Recife, PE, BrazilFederal University of Pernambuco. Laboratory of Immunogenetics. Recife, PE, BrazilFederal University of Pernambuco. Laboratory of Immunogenetics. Recife, PE, BrazilFederal University of Pernambuco. Laboratory of Immunogenetics. Recife, PE, BrazilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilFederal University of Pernambuco. Department of Physiology and Pharmacology. Recife, PE, BrazilFederal University of Pernambuco. Department of Pharmacy. Recife, PE, BrazilSchistosomiasis is a chronic and debilitating disease caused by a trematode of the genus Schistosoma and affects over 207 million people. Chemotherapy is the only immediate recourse for minimizing the prevalence of this disease and involves predominately the administration of a single drug, praziquantel (PZQ). Although PZQ has proven efficacy, there is a recognized need to develop new drugs as schistosomicides since studies have shown that repeated use of this drug in areas of endemicity may cause a temporary reduction in susceptibility in isolates of Schistosoma mansoni. Hydrazones, thiosemicarbazones, phthalimides, and thiazoles are thus regarded as privileged structures used for a broad spectrum of activities and are potential candidates for sources of new drug prototypes. The present study determined the in vitro schistosomicidal activity of 10 molecules containing these structures. During the assays, parameters such motility and mortality, oviposition, morphological changes in the tegument, cytotoxicity, and immunomodulatory activity caused by these compounds were evaluated. The results showed that compounds formed of thiazole and phthalimide led to higher mortality of worms, with a significant decline in motility, inhibition of pairing and oviposition, and a mortality rate of 100% starting from 144 h of exposure. These compounds also stimulated the production of nitric oxide and tumor necrosis factor alpha (TNF-α), thereby demonstrating the presence of immunomodulatory activity. The phthalyl thiazole LpQM-45 caused significant ultrastructural alterations, with destruction of the tegument in both male and female worms. According to the present study, phthalyl thiazole compounds possess antischistosomal activities and should form the basis for future experimental and clinical trials.engAmerican Society for MicrobiologySchistosoma mansoniEsquistossomicidasPraziquantelTiazóisQuimioterapiaDrogaSchistosoma mansoniSchistosomicidesPraziquantelThiazolesChemotherapyDrugsEvaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazolesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://www.arca.fiocruz.br/bitstream/icict/25583/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALSantiago EF Evaluation of the anti-Schistosoma ....pdfSantiago EF Evaluation of the anti-Schistosoma 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| dc.title.pt_BR.fl_str_mv |
Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles |
| title |
Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles |
| spellingShingle |
Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles Santiago, Edna de Farias Schistosoma mansoni Esquistossomicidas Praziquantel Tiazóis Quimioterapia Droga Schistosoma mansoni Schistosomicides Praziquantel Thiazoles Chemotherapy Drugs |
| title_short |
Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles |
| title_full |
Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles |
| title_fullStr |
Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles |
| title_full_unstemmed |
Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles |
| title_sort |
Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles |
| author |
Santiago, Edna de Farias |
| author_facet |
Santiago, Edna de Farias Oliveira, Sheilla Andrade de Oliveira Filho, Gevânio Bezerra de Moreira, Diogo Rodrigo Magalhaes Gomes, Paulo André Teixeira Silva, Anekécia Lauro da Barros, Andréia Ferreira de Silva, Aline Caroline da Santos, Thiago André Ramos dos Pereira, Valéria Rêgo Alves Gonçalves, Gabriel Gazzoni Araújo Brayner, Fábio André Alves, Luiz Carlos Wanderley, Almir Gonçalves Leite, Ana Cristina Lima |
| author_role |
author |
| author2 |
Oliveira, Sheilla Andrade de Oliveira Filho, Gevânio Bezerra de Moreira, Diogo Rodrigo Magalhaes Gomes, Paulo André Teixeira Silva, Anekécia Lauro da Barros, Andréia Ferreira de Silva, Aline Caroline da Santos, Thiago André Ramos dos Pereira, Valéria Rêgo Alves Gonçalves, Gabriel Gazzoni Araújo Brayner, Fábio André Alves, Luiz Carlos Wanderley, Almir Gonçalves Leite, Ana Cristina Lima |
| author2_role |
author author author author author author author author author author author author author author |
| dc.contributor.author.fl_str_mv |
Santiago, Edna de Farias Oliveira, Sheilla Andrade de Oliveira Filho, Gevânio Bezerra de Moreira, Diogo Rodrigo Magalhaes Gomes, Paulo André Teixeira Silva, Anekécia Lauro da Barros, Andréia Ferreira de Silva, Aline Caroline da Santos, Thiago André Ramos dos Pereira, Valéria Rêgo Alves Gonçalves, Gabriel Gazzoni Araújo Brayner, Fábio André Alves, Luiz Carlos Wanderley, Almir Gonçalves Leite, Ana Cristina Lima |
| dc.subject.other.pt_BR.fl_str_mv |
Schistosoma mansoni Esquistossomicidas Praziquantel Tiazóis Quimioterapia Droga |
| topic |
Schistosoma mansoni Esquistossomicidas Praziquantel Tiazóis Quimioterapia Droga Schistosoma mansoni Schistosomicides Praziquantel Thiazoles Chemotherapy Drugs |
| dc.subject.en.pt_BR.fl_str_mv |
Schistosoma mansoni Schistosomicides Praziquantel Thiazoles Chemotherapy Drugs |
| description |
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CPNq) and Fundação Oswaldo Cruz (FIOCRUZ). FAPESB postdoctoral scholarship. |
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2014 |
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2014 |
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2018-04-03T14:24:14Z |
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2018-04-03T14:24:14Z |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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article |
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publishedVersion |
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SANTIAGO, E. F. et al. Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles. Antimicrobial Agents and Chemotherapy, v. 58, n. 1, p. 352–363, 2014. |
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https://www.arca.fiocruz.br/handle/icict/25583 |
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0066-4804 |
| dc.identifier.doi.none.fl_str_mv |
10.1128/AAC.01900-13 |
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SANTIAGO, E. F. et al. Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles. Antimicrobial Agents and Chemotherapy, v. 58, n. 1, p. 352–363, 2014. 0066-4804 10.1128/AAC.01900-13 |
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American Society for Microbiology |
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American Society for Microbiology |
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