| Affiliation: | 1. Departamento de Bioquímica, Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Juiz de Fora, MG Brazil;2. Departamento de Química, Universidade Federal de Juiz de Fora, Juiz de Fora, MG Brazil;3. Núcleo de Pesquisa em Doenças Negligenciadas, Universidade Guarulhos, Guarulhos, SP Brazil;4. Faculdade de Farmácia, Departamento de Ciências Farmacêuticas, Universidade Federal de Juiz de Fora, Juiz de Fora, MG Brazil;5. Laboratório de Esquistossomose, Centro de Pesquisas René Rachou, Fundação Oswaldo, Cruz, FIOCRUZ, Belo Horizonte, MG Brazil;6. EMBRAPA – Gado de Leite, Juiz de Fora, MG Brazil;7. Grupo de Modelagem Computacional Aplicada (GMCA), Universidade Federal de Juiz de Fora, Juiz de Fora, MG Brazil |
| Abstract: | In this work, two synthetic aurones revealed moderate schistosomicidal potential in in vitro and in vivo assays. Aurones ( 1 ) and ( 2 ) promoted changes in tegument integrity and motor activity, leading to death of adult Schistosoma mansoni worms in in vitro assays. When administered orally (two doses of 50 mg/kg) in experimentally infected animals, synthetic aurones ( 1 ) and ( 2 ) promoted reductions of 56.20 % and 57.61 % of the parasite load and stimulated the displacement towards the liver of the remaining adult worms. The oogram analysis revealed that the treatment with both aurones interferes with the egg development kinetics in the intestinal tissue. Seeking an action target for compounds ( 1 ) and ( 2 ), the connection with NTPDases enzymes, recognized as important therapeutic targets for S. mansoni, was evaluated. Molecular docking studies have shown promising results. The dataset reveals the anthelmintic character of these compounds, which can be used in the development of new therapies for schistosomiasis. |
