Chemistry & biodiversity · 2018
In Vitro and in Vivo Antischistosomal Activities of Chalcones.
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Pereira Vinícius R D, Junior Ismael J Alves, da Silveira Lígia S, Geraldo Reinaldo B, de F Pinto Priscila, Teixeira Fernanda S, Salvadori Maria C, Silva Marcos P, Alves Lara A, Capriles Priscila V S Z, das C Almeida Ayla, Coimbra Elaine S, Pinto Pedro L S, Couri Mara R C, de Moraes Josué, Da Silva Filho Ademar A
Аннотация
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.