Cardamonin Presents in Vivo Activity against Schistosoma mansoni and Inhibits Potato Apyrase

Autor(es)

Aleixo de Carvalho, Lara Soares ^[1] ; Silva, Livia Mara ^[1] ; de Souza, Vinicius Carius ^[2] ; Nascimento da Silva, Marcos Paulo ^[3] ; Capriles, Priscila V. S. Z. ^[2] ; Pinto, Priscila de Faria ^[4] ; de Moraes, Josue ^[3] ; Da Silva Filho, Ademar Alves ^[1]

Afiliação do(s) autor(es)

^[1] Univ Fed Juiz de Fora, Fac Pharm, Dept Pharmaceut Sci, BR-36036900 Juiz De Fora, MG - Brazil

^[2] Univ Fed Juiz de Fora, Programa Posgrad Modelagem Computac, Dept Ciencia Comp, ICE, BR-36036900 Juiz De Fora, MG - Brazil

^[3] Univ Guarulhos, Res Ctr Neglected Dis, BR-07025000 Guarulhos, SP - Brazil

^[4] Univ Fed Juiz de Fora, Inst Biol Sci, Dept Biochem, BR-36036900 Juiz De Fora, MG - Brazil

• Tipo de documento: Artigo Científico
• Fonte: CHEMISTRY & BIODIVERSITY; v. 18, n. 11 OCT 2021.
• Citações Web of Science: 0

Resumo

Schistosomiasis, a neglected tropical disease caused by Schistosoma species, harms over 250 million people in several countries. The treatment is achieved with only one drug, praziquantel. Cardamonin, a natural chalcone with in vitro schistosomicidal activity, has not been in vivo evaluated against Schistosoma. In this work, we evaluated the in vivo schistosomicidal activities of cardamonin against Schistosoma mansoni worms and conducted enzymatic apyrase inhibition assay, as well as molecular docking analysis of cardamonin against potato apyrase, S. mansoni NTPDase 1 and S. mansoni NTPDase 2. In a mouse model of schistosomiasis, the oral treatment with cardamonin (400 mg/kg) showed efficacy against S. mansoni, decreasing the total worm load in 46.8 % and reducing in 54.5 % the number of eggs in mice. Cardamonin achieved a significant inhibition of the apyrase activity and the three-dimensional structure of the potato apyrase, obtained by homology modeling, showed that cardamonin may interact mainly through hydrogen bonds. Molecular docking studies corroborate with the action of cardamonin in binding and inhibiting both potato apyrase and S. mansoni NTPDases. (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