In Vitro and in Vivo Antischistosomal Activities of Chalcones

Autor(es):Mostrar menos -

Pereira, Vinicius R. D. ^[1] ; Alves Junior, Ismael J. ^[1] ; da Silveira, Ligia S. ^[2] ; Geraldo, Reinaldo B. ^[1] ; Pinto, Priscila de F. ^[3] ; Teixeira, Fernanda S. ^[4] ; Salvadori, Maria C. ^[4] ; Silva, Marcos P. ^[5] ; Alves, Lara A. ^[6] ; Capriles, Priscila V. S. Z. ^[6] ; Almeida, Ayla das C. ^[7] ; Coimbra, Elaine S. ^[7] ; Pinto, Pedro L. S. ^[8] ; Couri, Mara R. C. ^[2] ; de Moraes, Josue ^[5] ; Da Silva Filho, Ademar A. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Fed Juiz De Fora, Dept Ciencias Farmaceut, Fac Farm, R Jose Lourenco Kelmer S-N, Campus Univ, BR-36036900 Juiz De Fora, MG - Brazil

^[2] Univ Fed Juiz de Fora, Dept Quim, Juiz De Fora, MG - Brazil

^[3] Univ Fed Juiz De Fora, Inst Ciencias Biol, Dept Bioquim, Juiz De Fora, MG - Brazil

^[4] Univ Sao Paulo, Inst Fis, Sao Paulo, SP - Brazil

^[5] Univ Guarulhos, Nucleo Pesquisa Doencas Negligenciadas, Guarulhos, SP - Brazil

^[6] Univ Fed Juiz De Fora, Dept Ciencia Comp, Programa Posgrad Modelagem Comp, ICE, Juiz De Fora, MG - Brazil

^[7] Univ Fed Juiz De Fora, Inst Ciencias Biol, Dept Parasitol Microbiol & Imunol, Juiz De Fora, MG - Brazil

^[8] Adolfo Lutz Inst, Nucleo Enteroparasitas, Sao Paulo, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: CHEMISTRY & BIODIVERSITY; v. 15, n. 12 DEC 2018.
• Citações Web of Science: 1

Resumo

In this study, we evaluated the in vitro and in vivo schistosomicidal activities of chalcones against Schistosoma mansoni worms. In vitro assays revealed that chalcones 1 and 3 were the most active compounds, without affecting significantly mammalian cells. Confocal laser scanning microscopy and scanning electron microscopy studies revealed reduction on the numbers of tubercles and morphological alterations in the tegument of S. mansoni worms after in vitro incubation with chalcones 1 and 3. In a mouse model of schistosomiasis, the oral treatment (400 mg/kg) with chalcone 1 or 3 significantly caused a total worm burden reduction in mice. Chalcone 1 showed significant inhibition of the S. mansoni ATP diphosphohydrolase activity, which was corroborated by molecular docking studies. The results suggested that chalcones could be explored as lead compounds with antischistosomal properties. (AU)

• Processo FAPESP: 16/22488-3 - Reposicionamento de fármacos para doenças negligenciadas: identificação de novos agentes anti-helmínticos
• Beneficiário: Josué de Moraes
• Modalidade de apoio: Auxílio à Pesquisa - Regular