In vitro and in silico evaluation of the schistosomicidal activity of eugenol derivatives using biochemical, molecular, and morphological tools.

dc.contributor.authorSouza, Isabella Maria Monteiro de
dc.contributor.authorNovaes, Rômulo Dias
dc.contributor.authorGonçalves, Reggiani Vilela
dc.contributor.authorFialho, Felipe Leonardo Bley
dc.contributor.authorCarvalho, Diogo Teixeira
dc.contributor.authorSouza, Thiago Belarmino de
dc.contributor.authorDias, Danielle Ferreira
dc.contributor.authorLavorato, Stefânia Neiva
dc.contributor.authorSouza, Raquel Lopes Martins
dc.contributor.authorMarques, Marcos José
dc.contributor.authorCastro, Aline Pereira
dc.date.accessioned2023-10-18T17:35:43Z
dc.date.available2023-10-18T17:35:43Z
dc.date.issued2022pt_BR
dc.description.abstractBackground: Eugenol shows both antibacterial and antiparasitic activities, suggesting that it might be evaluated as an option for the treatment of praziquantel-resistant schistosome. Methods: The in vitro activities of three eugenol derivatives (FB1, FB4 and FB9) on adult worms from Schistosoma mansoni were examined by fluorescence and scanning electron microscopy to analyze effects on the excretory system and integument damage, respectively. Biochemical tests with verapamil (a calcium channel antagonist) and ouabain (a Na+ /K+-ATPase pump inhibitor) were used to characterize eugenol derivative interactions with calcium channels and the Na+/K+-ATPase, while in silico analysis identified potential Na+/K+-ATPase binding sites. Results: The compounds showed effective doses (ED50) of 0.324 mM (FB1), 0.167 mM (FB4), and 0.340 mM (FB9). In addition, FB4 (0.322 mM), which showed the lowest ED50, ED90 and ED100 (p < 0.05), caused the most damage to the excretory system and integument, according to both fluorescence and scanning electron microscopy analysis. The death of adult worms was delayed by ouabain treatment plus FB1 (192 versus 72 hours) and FB9 (192 versus 168 hours), but the response to FB4 was the same in the presence or absence of ouabain. Besides, no changes were noted when all of the eugenol derivatives were combined with verapamil. Moreover, FB1 and FB9 inhibited Na+/K+-ATPase activity according to in silico analysis but FB4 did not show a time- dependent relationship and may act on targets other than the parasite Na+/K+-ATPase. Conclusion: Eugenol derivatives, mainly FB4 when compared to FB1 and FB9, seem to act more effectively on the integument of adult S. mansoni worms.pt_BR
dc.identifier.citationSOUZA, I. M. M. de et al. In vitro and in silico evaluation of the schistosomicidal activity of eugenol derivatives using biochemical, molecular, and morphological tools. Journal of Venomous Animals and Toxins Including Tropical Diseases, v. 28, artigo e20210108, 2022. Disponível em: <https://www.scielo.br/j/jvatitd/a/m5FQpQLh53JqVTxdss3Kn4v/abstract/?lang=en>. Acesso em: 01 ago. 2023.pt_BR
dc.identifier.doihttps://doi.org/10.1590/1678-9199-JVATITD-2021-0108pt_BR
dc.identifier.issn1678-9199
dc.identifier.urihttp://www.repositorio.ufop.br/jspui/handle/123456789/17598
dc.language.isoen_USpt_BR
dc.rightsabertopt_BR
dc.rights.licenseThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http:// creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. Fonte: PDF do artigo.pt_BR
dc.subjectSchistosoma mansonipt_BR
dc.subjectEugenolpt_BR
dc.subjectSchistosomiasispt_BR
dc.subjectMechanism of actionpt_BR
dc.titleIn vitro and in silico evaluation of the schistosomicidal activity of eugenol derivatives using biochemical, molecular, and morphological tools.pt_BR
dc.typeArtigo publicado em periodicopt_BR

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