Anthelmintic activity of 1,10-phenanthroline-5,6-dione-based metallodrugs
Abstract Parasitic worm infections impose a significant public health burden, affecting over 2 billion people, particularly in low-income regions. The limited efficacy of current treatments highlights the urgent need for new anthelmintic agents. This study investigates the potential antiparasitic ac...
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Nature Portfolio
2025-02-01
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| Series: | Scientific Reports |
| Online Access: | https://doi.org/10.1038/s41598-025-88484-5 |
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| author | Maria E. Cirino Thainá R. Teixeira Alessandro M. H. Silva Ana C. C. Borges Lucas Fukui-Silva Luis G. Wagner Christiane Fernandes Malachy McCann André L. S. Santos Josué de Moraes |
| author_facet | Maria E. Cirino Thainá R. Teixeira Alessandro M. H. Silva Ana C. C. Borges Lucas Fukui-Silva Luis G. Wagner Christiane Fernandes Malachy McCann André L. S. Santos Josué de Moraes |
| author_sort | Maria E. Cirino |
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| description | Abstract Parasitic worm infections impose a significant public health burden, affecting over 2 billion people, particularly in low-income regions. The limited efficacy of current treatments highlights the urgent need for new anthelmintic agents. This study investigates the potential antiparasitic activity of 1,10-phenanthroline-5,6-dione (phendione) and its metal complexes, [Cu(phendione)3](ClO4)2.8H2O and [Ag(phendione)2](ClO4), against Schistosoma mansoni, the causative agent of intestinal schistosomiasis, and Angiostrongylus cantonensis, responsible for eosinophilic meningitis in humans. Additionally, the compounds were tested on Caenorhabditis elegans, a model organism for drug discovery. All compounds exhibited strong antiparasitic activity, with Cu-phendione showing the greatest potency (EC50 = 2.3 µM for S. mansoni and 6.4 µM for A. cantonensis). Ag-phendione also demonstrated significant activity, achieving EC₅₀ values of 6.5 µM against S. mansoni and 12.7 µM against A. cantonensis. The lethal dose (LD50) values in C. elegans were over 40 times higher, indicating selective antiparasitic effects. Cytotoxicity assays using Vero cells revealed a low toxicity profile and a high selectivity index. Given the promising biological properties of phendione and its metal complexes, these findings contribute to the growing body of research seeking to address the urgent need for new anthelmintic therapies. |
| format | Article |
| id | doaj-art-fb9a7551578848d0b3d399eb7127948b |
| institution | Kabale University |
| issn | 2045-2322 |
| language | English |
| publishDate | 2025-02-01 |
| publisher | Nature Portfolio |
| record_format | Article |
| series | Scientific Reports |
| spelling | doaj-art-fb9a7551578848d0b3d399eb7127948b2025-02-09T12:28:43ZengNature PortfolioScientific Reports2045-23222025-02-011511810.1038/s41598-025-88484-5Anthelmintic activity of 1,10-phenanthroline-5,6-dione-based metallodrugsMaria E. Cirino0Thainá R. Teixeira1Alessandro M. H. Silva2Ana C. C. Borges3Lucas Fukui-Silva4Luis G. Wagner5Christiane Fernandes6Malachy McCann7André L. S. Santos8Josué de Moraes9Núcleo de Pesquisas em Doenças Negligenciadas, Universidade GuarulhosNúcleo de Pesquisas em Doenças Negligenciadas, Universidade GuarulhosNúcleo de Pesquisas em Doenças Negligenciadas, Instituto Científico e Tecnológico, Universidade BrasilNúcleo de Pesquisas em Doenças Negligenciadas, Universidade GuarulhosNúcleo de Pesquisas em Doenças Negligenciadas, Universidade GuarulhosDepartamento de Química, Universidade Federal de Santa CatarinaDepartamento de Química, Universidade Federal de Santa CatarinaDepartment of Chemistry, Maynooth University, National University of IrelandLaboratório de Estudos Avançados de Microrganismos Emergentes e Resistentes, Instituto de Microbiologia Paulo de Góes, Universidade Federal do Rio de JaneiroNúcleo de Pesquisas em Doenças Negligenciadas, Universidade GuarulhosAbstract Parasitic worm infections impose a significant public health burden, affecting over 2 billion people, particularly in low-income regions. The limited efficacy of current treatments highlights the urgent need for new anthelmintic agents. This study investigates the potential antiparasitic activity of 1,10-phenanthroline-5,6-dione (phendione) and its metal complexes, [Cu(phendione)3](ClO4)2.8H2O and [Ag(phendione)2](ClO4), against Schistosoma mansoni, the causative agent of intestinal schistosomiasis, and Angiostrongylus cantonensis, responsible for eosinophilic meningitis in humans. Additionally, the compounds were tested on Caenorhabditis elegans, a model organism for drug discovery. All compounds exhibited strong antiparasitic activity, with Cu-phendione showing the greatest potency (EC50 = 2.3 µM for S. mansoni and 6.4 µM for A. cantonensis). Ag-phendione also demonstrated significant activity, achieving EC₅₀ values of 6.5 µM against S. mansoni and 12.7 µM against A. cantonensis. The lethal dose (LD50) values in C. elegans were over 40 times higher, indicating selective antiparasitic effects. Cytotoxicity assays using Vero cells revealed a low toxicity profile and a high selectivity index. Given the promising biological properties of phendione and its metal complexes, these findings contribute to the growing body of research seeking to address the urgent need for new anthelmintic therapies.https://doi.org/10.1038/s41598-025-88484-5 |
| spellingShingle | Maria E. Cirino Thainá R. Teixeira Alessandro M. H. Silva Ana C. C. Borges Lucas Fukui-Silva Luis G. Wagner Christiane Fernandes Malachy McCann André L. S. Santos Josué de Moraes Anthelmintic activity of 1,10-phenanthroline-5,6-dione-based metallodrugs Scientific Reports |
| title | Anthelmintic activity of 1,10-phenanthroline-5,6-dione-based metallodrugs |
| title_full | Anthelmintic activity of 1,10-phenanthroline-5,6-dione-based metallodrugs |
| title_fullStr | Anthelmintic activity of 1,10-phenanthroline-5,6-dione-based metallodrugs |
| title_full_unstemmed | Anthelmintic activity of 1,10-phenanthroline-5,6-dione-based metallodrugs |
| title_short | Anthelmintic activity of 1,10-phenanthroline-5,6-dione-based metallodrugs |
| title_sort | anthelmintic activity of 1 10 phenanthroline 5 6 dione based metallodrugs |
| url | https://doi.org/10.1038/s41598-025-88484-5 |
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