Article
Synthetic Aurones: New Features for Schistosoma mansoni Therapy
Registro en:
TORRES, Daniel Silva et al. Synthetic Aurones: New Features for Schistosoma mansoni Therapy. Chem Biodivers., v. 18, n. 11, e2100439, 2021. doi: 10.1002/cbdv.202100439.
1612-1872
10.1002/cbdv.202100439
Autor
Torres, Daniel Silva
Oliveira, Bruna Alves de
Silveira, Lígia Souza D
Silva, Marcos Paulo da
Pereira, Vinícius Rodrigues Durães
Moraes, Josué
Couri, Mara Rúbia Costa
Queiroz, Rafaella Fortini Grenfell e
Parreiras, Patrícia Martins
Silva, Márcio Roberto
Alves, Lara Azevedo
Souza, Vinícius Carius de
Goliatt, Priscila Vanessa Zabala Capriles
Vasconcelos, Eveline Gomes
Silva Filho, Ademar Alves da
Pinto, Priscila de Faria
Resumen
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.