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Insight on the Structure-to-Activity of Carbosilane Metallodendrimers in the Fight against Staphylococcus aureus Biofilms

Biofilm formation is a critical health concern, involved in most human bacterial infections. Combatting this mechanism, which increases resistance to traditional antibiotics and host immune defences, requires novel therapeutic approaches. The remarkable biocide activity and the monodispersity of car...

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Autores principales: Llamazares, Celia, Sanz del Olmo, Natalia, Soliveri, Juan, de la Mata, F. Javier, Copa-Patiño, José Luis, García-Gallego, Sandra
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8156651/
https://www.ncbi.nlm.nih.gov/pubmed/34067558
http://dx.doi.org/10.3390/antibiotics10050589
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author Llamazares, Celia
Sanz del Olmo, Natalia
Soliveri, Juan
de la Mata, F. Javier
Copa-Patiño, José Luis
García-Gallego, Sandra
author_facet Llamazares, Celia
Sanz del Olmo, Natalia
Soliveri, Juan
de la Mata, F. Javier
Copa-Patiño, José Luis
García-Gallego, Sandra
author_sort Llamazares, Celia
collection PubMed
description Biofilm formation is a critical health concern, involved in most human bacterial infections. Combatting this mechanism, which increases resistance to traditional antibiotics and host immune defences, requires novel therapeutic approaches. The remarkable biocide activity and the monodispersity of carbosilane metallodendrimers make them excellent platforms to evaluate the impact of different structural parameters on the biological activity. In this work, we explore the influence of iminopyridine ring substituents on the antibacterial activity against planktonic and biofilm Staphylococcus aureus. New families of first-generation Ru(II) and Cu(II) metallodendrimers were synthesised and analysed, in comparison to the non-substituted counterparts. The results showed that the presence of methyl or methoxy groups in meta position to the imine bond decreased the overall positive charge on the metal ion and, subsequently, the activity against planktonic bacteria. However, it seemed a relevant parameter to consider for the prevention of biofilm formation, if they contribute to increasing the overall lipophilicity. An optimum balance of the charge and lipophilicity of the metallodrug, accomplished through structural design, will provide effective biocide agents against bacteria biofilms.
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spelling pubmed-81566512021-05-28 Insight on the Structure-to-Activity of Carbosilane Metallodendrimers in the Fight against Staphylococcus aureus Biofilms Llamazares, Celia Sanz del Olmo, Natalia Soliveri, Juan de la Mata, F. Javier Copa-Patiño, José Luis García-Gallego, Sandra Antibiotics (Basel) Article Biofilm formation is a critical health concern, involved in most human bacterial infections. Combatting this mechanism, which increases resistance to traditional antibiotics and host immune defences, requires novel therapeutic approaches. The remarkable biocide activity and the monodispersity of carbosilane metallodendrimers make them excellent platforms to evaluate the impact of different structural parameters on the biological activity. In this work, we explore the influence of iminopyridine ring substituents on the antibacterial activity against planktonic and biofilm Staphylococcus aureus. New families of first-generation Ru(II) and Cu(II) metallodendrimers were synthesised and analysed, in comparison to the non-substituted counterparts. The results showed that the presence of methyl or methoxy groups in meta position to the imine bond decreased the overall positive charge on the metal ion and, subsequently, the activity against planktonic bacteria. However, it seemed a relevant parameter to consider for the prevention of biofilm formation, if they contribute to increasing the overall lipophilicity. An optimum balance of the charge and lipophilicity of the metallodrug, accomplished through structural design, will provide effective biocide agents against bacteria biofilms. MDPI 2021-05-17 /pmc/articles/PMC8156651/ /pubmed/34067558 http://dx.doi.org/10.3390/antibiotics10050589 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Llamazares, Celia
Sanz del Olmo, Natalia
Soliveri, Juan
de la Mata, F. Javier
Copa-Patiño, José Luis
García-Gallego, Sandra
Insight on the Structure-to-Activity of Carbosilane Metallodendrimers in the Fight against Staphylococcus aureus Biofilms
title Insight on the Structure-to-Activity of Carbosilane Metallodendrimers in the Fight against Staphylococcus aureus Biofilms
title_full Insight on the Structure-to-Activity of Carbosilane Metallodendrimers in the Fight against Staphylococcus aureus Biofilms
title_fullStr Insight on the Structure-to-Activity of Carbosilane Metallodendrimers in the Fight against Staphylococcus aureus Biofilms
title_full_unstemmed Insight on the Structure-to-Activity of Carbosilane Metallodendrimers in the Fight against Staphylococcus aureus Biofilms
title_short Insight on the Structure-to-Activity of Carbosilane Metallodendrimers in the Fight against Staphylococcus aureus Biofilms
title_sort insight on the structure-to-activity of carbosilane metallodendrimers in the fight against staphylococcus aureus biofilms
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8156651/
https://www.ncbi.nlm.nih.gov/pubmed/34067558
http://dx.doi.org/10.3390/antibiotics10050589
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