Ru-terpyridine complexes containing clotrimazole as potent photoactivatable selective antifungal agents
The overuse of antimicrobial agents in medical and veterinary applications has led to the development ofantimicrobial resistance in some microorganisms and this is now one of the major concerns in modern society. Inthis context, the use of transition metal complexes with photoactivatable properties,...
| Autores: | , , , , , , , , |
|---|---|
| Tipo de documento: | artigo |
| Data de publicação: | 2024 |
| País: | España |
| Recursos: | Universidad de Castilla-La Mancha |
| Repositório: | RUIdeRA. Repositorio Institucional de la UCLM |
| OAI Identifier: | oai:ruidera.uclm.es:10578/39446 |
| Acesso em linha: | https://www.sciencedirect.com/science/article/pii/S0162013424002162?via%3Dihub https://hdl.handle.net/10578/39446 |
| Access Level: | Acceso aberto |
| Palavra-chave: | Antifungal ruthenium complexes Antimicrobial Clotrimazole PhotoActivated therapy PACT Photodissociation Substituted terpyridine ligands |
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Ru-terpyridine complexes containing clotrimazole as potent photoactivatable selective antifungal agentsGonzalo Navarro, CarlosTroyano Saez, Antonio JGarcía-Béjar Bermejo, BeatrizMassaguer , AnnaOrganero Gallego, Juan ÁngelSantos Peinado, LucíaRodríguez Fernández-Pacheco, Ana MaríaManzano Manrique, Blanca Rosa LourdesDurá Gracia, GemaAntifungal ruthenium complexesAntimicrobialClotrimazolePhotoActivated therapy PACTPhotodissociationSubstituted terpyridine ligandsThe overuse of antimicrobial agents in medical and veterinary applications has led to the development ofantimicrobial resistance in some microorganisms and this is now one of the major concerns in modern society. Inthis context, the use of transition metal complexes with photoactivatable properties, which can act as drugdelivery systems triggered by light, could become a potent strategy to overcome the problem of resistance. In thiswork several Ru complexes with terpyridine ligands and the clotrimazole fragment, which is a potent antimycoticdrug, were synthesized. The main goal was to explore the potential photoactivated activity of the complexes asantifungal agents and evaluate the effect of introducing different substituents on the terpyridine ligand. Thecomplexes were capable of delivering the clotrimazole unit upon irradiation with visible light in a short period oftime. The influence of the substituents on the photodissociation rate was explained by means of TD-DFT cal-culations. The complexes were tested against three different yeasts, which were selected based on their preva-lence in fungal infections. The complex in which a carboxybenzene unit was attached to the terpyridine ligandshowed the best activity against the three species under light, with minimal inhibitory concentration values of0.88 µM and a phototoxicity index of 50 achieved. The activity of this complex was markedly higher than that offree clotrimazole, especially upon irradiation with visible light (141 times higher). The complexes were moreactive on yeast species than on cancer cell lines.The overuse of antimicrobial agents in medical and veterinary applications has led to the development ofantimicrobial resistance in some microorganisms and this is now one of the major concerns in modern society. Inthis context, the use of transition metal complexes with photoactivatable properties, which can act as drugdelivery systems triggered by light, could become a potent strategy to overcome the problem of resistance. In thiswork several Ru complexes with terpyridine ligands and the clotrimazole fragment, which is a potent antimycoticdrug, were synthesized. The main goal was to explore the potential photoactivated activity of the complexes asantifungal agents and evaluate the effect of introducing different substituents on the terpyridine ligand. Thecomplexes were capable of delivering the clotrimazole unit upon irradiation with visible light in a short period oftime. The influence of the substituents on the photodissociation rate was explained by means of TD-DFT cal-culations. The complexes were tested against three different yeasts, which were selected based on their preva-lence in fungal infections. The complex in which a carboxybenzene unit was attached to the terpyridine ligandshowed the best activity against the three species under light, with minimal inhibitory concentration values of0.88 µM and a phototoxicity index of 50 achieved. The activity of this complex was markedly higher than that offree clotrimazole, especially upon irradiation with visible light (141 times higher). The complexes were moreactive on yeast species than on cancer cell lines.Elsevier202420242024info:eu-repo/semantics/articleapplication/pdfapplication/pdfapplication/pdfhttps://www.sciencedirect.com/science/article/pii/S0162013424002162?via%3Dihubhttps://hdl.handle.net/10578/39446reponame:RUIdeRA. Repositorio Institucional de la UCLMinstname:Universidad de Castilla-La ManchaInglésinfo:eu-repo/semantics/openAccessoai:ruidera.uclm.es:10578/394462026-05-27T07:36:41Z |
| dc.title.none.fl_str_mv |
Ru-terpyridine complexes containing clotrimazole as potent photoactivatable selective antifungal agents |
| title |
Ru-terpyridine complexes containing clotrimazole as potent photoactivatable selective antifungal agents |
| spellingShingle |
Ru-terpyridine complexes containing clotrimazole as potent photoactivatable selective antifungal agents Gonzalo Navarro, Carlos Antifungal ruthenium complexes Antimicrobial Clotrimazole PhotoActivated therapy PACT Photodissociation Substituted terpyridine ligands |
| title_short |
Ru-terpyridine complexes containing clotrimazole as potent photoactivatable selective antifungal agents |
| title_full |
Ru-terpyridine complexes containing clotrimazole as potent photoactivatable selective antifungal agents |
| title_fullStr |
Ru-terpyridine complexes containing clotrimazole as potent photoactivatable selective antifungal agents |
| title_full_unstemmed |
Ru-terpyridine complexes containing clotrimazole as potent photoactivatable selective antifungal agents |
| title_sort |
Ru-terpyridine complexes containing clotrimazole as potent photoactivatable selective antifungal agents |
| dc.creator.none.fl_str_mv |
Gonzalo Navarro, Carlos Troyano Saez, Antonio J García-Béjar Bermejo, Beatriz Massaguer , Anna Organero Gallego, Juan Ángel Santos Peinado, Lucía Rodríguez Fernández-Pacheco, Ana María Manzano Manrique, Blanca Rosa Lourdes Durá Gracia, Gema |
| author |
Gonzalo Navarro, Carlos |
| author_facet |
Gonzalo Navarro, Carlos Troyano Saez, Antonio J García-Béjar Bermejo, Beatriz Massaguer , Anna Organero Gallego, Juan Ángel Santos Peinado, Lucía Rodríguez Fernández-Pacheco, Ana María Manzano Manrique, Blanca Rosa Lourdes Durá Gracia, Gema |
| author_role |
author |
| author2 |
Troyano Saez, Antonio J García-Béjar Bermejo, Beatriz Massaguer , Anna Organero Gallego, Juan Ángel Santos Peinado, Lucía Rodríguez Fernández-Pacheco, Ana María Manzano Manrique, Blanca Rosa Lourdes Durá Gracia, Gema |
| author2_role |
author author author author author author author author |
| dc.subject.none.fl_str_mv |
Antifungal ruthenium complexes Antimicrobial Clotrimazole PhotoActivated therapy PACT Photodissociation Substituted terpyridine ligands |
| topic |
Antifungal ruthenium complexes Antimicrobial Clotrimazole PhotoActivated therapy PACT Photodissociation Substituted terpyridine ligands |
| description |
The overuse of antimicrobial agents in medical and veterinary applications has led to the development ofantimicrobial resistance in some microorganisms and this is now one of the major concerns in modern society. Inthis context, the use of transition metal complexes with photoactivatable properties, which can act as drugdelivery systems triggered by light, could become a potent strategy to overcome the problem of resistance. In thiswork several Ru complexes with terpyridine ligands and the clotrimazole fragment, which is a potent antimycoticdrug, were synthesized. The main goal was to explore the potential photoactivated activity of the complexes asantifungal agents and evaluate the effect of introducing different substituents on the terpyridine ligand. Thecomplexes were capable of delivering the clotrimazole unit upon irradiation with visible light in a short period oftime. The influence of the substituents on the photodissociation rate was explained by means of TD-DFT cal-culations. The complexes were tested against three different yeasts, which were selected based on their preva-lence in fungal infections. The complex in which a carboxybenzene unit was attached to the terpyridine ligandshowed the best activity against the three species under light, with minimal inhibitory concentration values of0.88 µM and a phototoxicity index of 50 achieved. The activity of this complex was markedly higher than that offree clotrimazole, especially upon irradiation with visible light (141 times higher). The complexes were moreactive on yeast species than on cancer cell lines. |
| publishDate |
2024 |
| dc.date.none.fl_str_mv |
2024 2024 2024 |
| dc.type.none.fl_str_mv |
info:eu-repo/semantics/article |
| format |
article |
| dc.identifier.none.fl_str_mv |
https://www.sciencedirect.com/science/article/pii/S0162013424002162?via%3Dihub https://hdl.handle.net/10578/39446 |
| url |
https://www.sciencedirect.com/science/article/pii/S0162013424002162?via%3Dihub https://hdl.handle.net/10578/39446 |
| dc.language.none.fl_str_mv |
Inglés |
| language_invalid_str_mv |
Inglés |
| dc.rights.none.fl_str_mv |
info:eu-repo/semantics/openAccess |
| eu_rights_str_mv |
openAccess |
| dc.format.none.fl_str_mv |
application/pdf application/pdf application/pdf |
| dc.publisher.none.fl_str_mv |
Elsevier |
| publisher.none.fl_str_mv |
Elsevier |
| dc.source.none.fl_str_mv |
reponame:RUIdeRA. Repositorio Institucional de la UCLM instname:Universidad de Castilla-La Mancha |
| instname_str |
Universidad de Castilla-La Mancha |
| reponame_str |
RUIdeRA. Repositorio Institucional de la UCLM |
| collection |
RUIdeRA. Repositorio Institucional de la UCLM |
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15,812429 |