ynthetic Aurones: New Features for Schistosoma mansoni Therap

Author(s):Show less -

Silva Torres, Daniel ^[1] ; Alves de Oliveira, Bruna ^[1] ; Silveira, Ligia d Souza ^[2] ; Paulo da Silva, Marcos ^[3] ; Rodrigues Duraes Pereira, Vinicius ^[4] ; Moraes, Josue ^[3] ; Rubia Costa Couri, Mara ^[2] ; Queiroz, Rafaella Fortini Grenfell e ^[5] ; Martins Parreiras, Patricia ^[5] ; Roberto Silva, Marcio ^[6] ; Azevedo Alves, Lara ^[7] ; Carius de Souza, Vinicius ^[7] ; Vanessa Zabala Capriles Goliatt, Priscila ^[7] ; Gomes Vasconcelos, Eveline ^[1] ; Alves da Silva Filho, Ademar ^[4] ; de Faria Pinto, Priscila ^[1]

Affiliation

^[1] Univ Fed Juiz De Fora, Inst Ciencias Biol, Dept Bioquim, Juiz De Fora, MG - Brazil

^[2] Univ Fed Juiz de Fora, Dept Quim, Juiz De Fora, MG - Brazil

^[3] Univ Guarulhos, Nucleo Pesquisa Doencas Negligenciadas, Guarulhos, SP - Brazil

^[4] Univ Fed Juiz de Fora, Dept Ciencias Farmaceut, Fac Farm, Juiz De Fora, MG - Brazil

^[5] Fiocruz MS, Fundacao Oswaldo Cruz, Ctr Pesquisas Rene Rachou, Lab Esquistossomose, Belo Horizonte, MG - Brazil

^[6] Embrapa Gado Leite, Juiz De Fora, MG - Brazil

^[7] Univ Fed Juiz De Fora, Grp Modelagem Computac Aplicada GMCA, Juiz De Fora, MG - Brazil

• Document type: Journal article
• Source: CHEMISTRY & BIODIVERSITY; v. 18, n. 11 OCT 2021.
• Web of Science Citations: 1

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. (AU)

• FAPESP's process: 16/22488-3 - Drug repositioning for neglected diseases: identification of novel anthelmintic agents
• Grantee: Josué de Moraes
• Support Opportunities: Regular Research Grants