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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...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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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. |
format | Online Article Text |
id | pubmed-8156651 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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