Please use this identifier to cite or link to this item:
https://hdl.handle.net/10316/113355
DC Field | Value | Language |
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dc.contributor.author | Rigo, Graziela Vargas | - |
dc.contributor.author | Cardoso, Fernanda Gomes | - |
dc.contributor.author | Pereira, Matheus Mendonça | - |
dc.contributor.author | Devereux, Michael | - |
dc.contributor.author | McCann, Malachy | - |
dc.contributor.author | Santos, André L. S. | - |
dc.contributor.author | Tasca, Tiana | - |
dc.date.accessioned | 2024-02-16T11:50:40Z | - |
dc.date.available | 2024-02-16T11:50:40Z | - |
dc.date.issued | 2023-05-22 | - |
dc.identifier.issn | 2076-0817 | pt |
dc.identifier.uri | https://hdl.handle.net/10316/113355 | - |
dc.description.abstract | Trichomonas vaginalis is responsible for 156 million new cases per year worldwide. When present asymptomatically, the parasite can lead to serious complications, such as development of cervical and prostate cancer. As infection increases the acquisition and transmission of HIV, the control of trichomoniasis represents an important niche for the discovery and development of new antiparasitic molecules. This urogenital parasite synthesizes several molecules that allow the establishment and pathogenesis of infection. Among them, peptidases occupy key roles as virulence factors, and the inhibition of these enzymes has become an important mechanism for modulating pathogenesis. Based on these premises, our group recently reported the potent anti-T. vaginalis action of the metal-based complex [Cu(phendione)3](ClO4)2.4H2O (Cu-phendione). In the present study, we evaluated the influence of Cu-phendione on the modulation of proteolytic activities produced by T. vaginalis by biochemical and molecular approaches. Cu-phendione showed strong inhibitory potential against T. vaginalis peptidases, especially cysteine- and metallo-type peptidases. The latter revealed a more prominent effect at both the post-transcriptional and post-translational levels. Molecular Docking analysis confirmed the interaction of Cu-phendione, with high binding energy (-9.7 and -10.7 kcal·mol-1, respectively) at the active site of both TvMP50 and TvGP63 metallopeptidases. In addition, Cu-phendione significantly reduced trophozoite-mediated cytolysis in human vaginal (HMVII) and monkey kidney (VERO) epithelial cell lineages. These results highlight the antiparasitic potential of Cu-phendione by interaction with important T. vaginalis virulence factors. | pt |
dc.language.iso | eng | pt |
dc.publisher | MDPI | pt |
dc.relation | UIDB/EQU/00102/2020 | pt |
dc.rights | openAccess | pt |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | pt |
dc.subject | Trichomonas vaginalis | pt |
dc.subject | metallopeptidases | pt |
dc.subject | cytolysis | pt |
dc.subject | proteolytic activity | pt |
dc.subject | copper-phendione | pt |
dc.title | Peptidases Are Potential Targets of Copper(II)-1,10-Phenanthroline-5,6-dione Complex, a Promising and Potent New Drug against Trichomonas vaginalis | pt |
dc.type | article | - |
degois.publication.firstPage | 745 | pt |
degois.publication.issue | 5 | pt |
degois.publication.title | Pathogens | pt |
dc.peerreviewed | yes | pt |
dc.identifier.doi | 10.3390/pathogens12050745 | pt |
degois.publication.volume | 12 | pt |
dc.date.embargo | 2023-05-22 | * |
uc.date.periodoEmbargo | 0 | pt |
item.openairetype | article | - |
item.fulltext | Com Texto completo | - |
item.languageiso639-1 | en | - |
item.grantfulltext | open | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
crisitem.project.grantno | CIEPQPF- Chemical Engineering and Renewable Resources for Sustainability | - |
crisitem.author.researchunit | CIEPQPF – Chemical Process Engineering and Forest Products Research Centre | - |
crisitem.author.parentresearchunit | Faculty of Sciences and Technology | - |
crisitem.author.orcid | 0000-0003-3524-6900 | - |
Appears in Collections: | FCTUC Eng.Química - Artigos em Revistas Internacionais I&D CIEPQPF - Artigos em Revistas Internacionais |
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File | Description | Size | Format | |
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Peptidases-Are-Potential-Targets-of-CopperII110Phenanthroline56dione-Complex-a-Promising-and-Potent-New-Drug-against-Trichomonas-vaginalisPathogens.pdf | 1.91 MB | Adobe PDF | View/Open |
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