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In Vitro and in Vivo Antischistosomal Activities of Chalcones

2018; Wiley; Volume: 15; Issue: 12 Linguagem: Inglês

10.1002/cbdv.201800398

1612-1880

Vinícius R. D. Pereira, Ismael José Alves, Lígia S. da Silveira, Reinaldo Barros Geraldo, Priscila de Faria Pinto, F. S. Teixeira, M. C. Salvadori, Marcos P. Silva, Lara A. Alves, Priscila Vanessa Zabala Capriles Goliatt, Ayla das Chagas Almeida, Elaine Soares Coimbra, Pedro Luiz Silva Pinto, Mara Rúbia Costa Couri, Josué de Moraes, Ademar Alves da Silva Filho,

Synthesis and biological activity

Abstract 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.