Author | Santiago, Edna de Farias | |
Author | Oliveira, Sheilla Andrade de | |
Author | Oliveira Filho, Gevânio Bezerra de | |
Author | Moreira, Diogo Rodrigo Magalhaes | |
Author | Gomes, Paulo André Teixeira | |
Author | Silva, Anekécia Lauro da | |
Author | Barros, Andréia Ferreira de | |
Author | Silva, Aline Caroline da | |
Author | Santos, Thiago André Ramos dos | |
Author | Pereira, Valéria Rêgo Alves | |
Author | Gonçalves, Gabriel Gazzoni Araújo | |
Author | Brayner, Fábio André | |
Author | Alves, Luiz Carlos | |
Author | Wanderley, Almir Gonçalves | |
Author | Leite, Ana Cristina Lima | |
Access date | 2018-04-03T14:24:14Z | |
Available date | 2018-04-03T14:24:14Z | |
Document date | 2014 | |
Citation | 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. | pt_BR |
ISSN | 0066-4804 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/25583 | |
Sponsorship | Conselho Nacional de Desenvolvimento Científico e Tecnológico (CPNq) and Fundação Oswaldo
Cruz (FIOCRUZ). FAPESB postdoctoral scholarship. | pt_BR |
Language | eng | pt_BR |
Publisher | American Society for Microbiology | pt_BR |
Rights | open access | pt_BR |
Subject in Portuguese | Schistosoma mansoni | pt_BR |
Subject in Portuguese | Esquistossomicidas | pt_BR |
Subject in Portuguese | Praziquantel | pt_BR |
Subject in Portuguese | Tiazóis | pt_BR |
Subject in Portuguese | Quimioterapia | pt_BR |
Subject in Portuguese | Droga | pt_BR |
Title | Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles | pt_BR |
Type | Article | pt_BR |
DOI | 10.1128/AAC.01900-13 | |
Abstract | Schistosomiasis 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. | pt_BR |
Affilliation | Federal University of Pernambuco. Department of Pharmacy. Recife, PE, Brazil / Federal University of Pernambuco. Laboratory of Immunopathology. Recife, PE, Brazil | pt_BR |
Affilliation | Federal University of Pernambuco. Laboratory of Immunopathology. Recife, PE, Brazil | pt_BR |
Affilliation | Federal University of Pernambuco. Department of Pharmacy. Recife, PE, Brazil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
Affilliation | Federal University of Pernambuco. Department of Pharmacy. Recife, PE, Brazil | pt_BR |
Affilliation | Federal University of Pernambuco. Laboratory of Immunopathology. Recife, PE, Brazil | pt_BR |
Affilliation | Federal University of Pernambuco. Laboratory of Immunopathology. Recife, PE, Brazil | pt_BR |
Affilliation | Federal University of Pernambuco. Laboratory of Immunogenetics. Recife, PE, Brazil | pt_BR |
Affilliation | Federal University of Pernambuco. Laboratory of Immunogenetics. Recife, PE, Brazil | pt_BR |
Affilliation | Federal University of Pernambuco. Laboratory of Immunogenetics. Recife, PE, Brazil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, Brasil | pt_BR |
Affilliation | Federal University of Pernambuco. Department of Physiology and Pharmacology. Recife, PE, Brazil | pt_BR |
Affilliation | Federal University of Pernambuco. Department of Pharmacy. Recife, PE, Brazil | pt_BR |
Subject | Schistosoma mansoni | pt_BR |
Subject | Schistosomicides | pt_BR |
Subject | Praziquantel | pt_BR |
Subject | Thiazoles | pt_BR |
Subject | Chemotherapy | pt_BR |
Subject | Drugs | pt_BR |