In Vitroandin VivoAntischistosomal Activities of Chalcones
| Autor: | Mara R.C. Couri, Marcos P. Silva, Ayla das Chagas Almeida, Lígia S. da Silveira, Vinícius R. D. Pereira, Josué de Moraes, Reinaldo B. Geraldo, Lara de Azevedo Alves, Priscila V. S. Z. Capriles, Ismael J. Alves Junior, Priscila de Faria Pinto, Ademar A. da Silva Filho, Maria Cecília Barbosa da Silveira Salvadori, Fernanda de Sá Teixeira, Pedro Luiz Silva Pinto, Elaine Soares Coimbra |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Chalcone Administration Oral Bioengineering Schistosomiasis 01 natural sciences Biochemistry Mice Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Chalcones In vivo parasitic diseases medicine Animals Cytotoxicity Molecular Biology Anthelmintics Binding Sites Microscopy Confocal biology 010405 organic chemistry Apyrase In vitro toxicology Biological activity Helminth Proteins Schistosoma mansoni General Chemistry General Medicine medicine.disease biology.organism_classification Schistosomiasis mansoni In vitro Protein Structure Tertiary 0104 chemical sciences Molecular Docking Simulation Disease Models Animal 030104 developmental biology chemistry Microscopy Electron Scanning Molecular Medicine |
| Zdroj: | Chemistry & Biodiversity. |
| ISSN: | 1612-1880 1612-1872 |
| DOI: | 10.1002/cbdv.201800398 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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