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New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents
Pyrrolomycins (PMs) are polyhalogenated antibiotics known as powerful biologically active compounds, yet featuring high cytotoxicity. The present study reports the antibacterial and antitumoral properties of new chemically synthesized PMs, where the three positions of the pyrrolic nucleus were repla...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7345095/ https://www.ncbi.nlm.nih.gov/pubmed/32486200 http://dx.doi.org/10.3390/antibiotics9060292 |
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author | Raimondi, Maria Valeria Presentato, Alessandro Li Petri, Giovanna Buttacavoli, Miriam Ribaudo, Agnese De Caro, Viviana Alduina, Rosa Cancemi, Patrizia |
author_facet | Raimondi, Maria Valeria Presentato, Alessandro Li Petri, Giovanna Buttacavoli, Miriam Ribaudo, Agnese De Caro, Viviana Alduina, Rosa Cancemi, Patrizia |
author_sort | Raimondi, Maria Valeria |
collection | PubMed |
description | Pyrrolomycins (PMs) are polyhalogenated antibiotics known as powerful biologically active compounds, yet featuring high cytotoxicity. The present study reports the antibacterial and antitumoral properties of new chemically synthesized PMs, where the three positions of the pyrrolic nucleus were replaced by nitro groups, aiming to reduce their cytotoxicity while maintaining or even enhancing the biological activity. Indeed, the presence of the nitro substituent in diverse positions of the pyrrole determined an improvement of the minimal bactericidal concentration (MBC) against Gram-positive (i.e., Staphylococcus aureus) or -negative (i.e., Pseudomonas aeruginosa) pathogen strains as compared to the natural PM-C. Moreover, some new nitro-PMs were as active as or more than PM-C in inhibiting the proliferation of colon (HCT116) and breast (MCF 7) cancer cell lines and were less toxic towards normal epithelial (hTERT RPE-1) cells. Altogether, our findings contribute to increase the knowledge of the mode of action of these promising molecules and provide a basis for their rationale chemical or biological manipulation. |
format | Online Article Text |
id | pubmed-7345095 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-73450952020-07-09 New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents Raimondi, Maria Valeria Presentato, Alessandro Li Petri, Giovanna Buttacavoli, Miriam Ribaudo, Agnese De Caro, Viviana Alduina, Rosa Cancemi, Patrizia Antibiotics (Basel) Article Pyrrolomycins (PMs) are polyhalogenated antibiotics known as powerful biologically active compounds, yet featuring high cytotoxicity. The present study reports the antibacterial and antitumoral properties of new chemically synthesized PMs, where the three positions of the pyrrolic nucleus were replaced by nitro groups, aiming to reduce their cytotoxicity while maintaining or even enhancing the biological activity. Indeed, the presence of the nitro substituent in diverse positions of the pyrrole determined an improvement of the minimal bactericidal concentration (MBC) against Gram-positive (i.e., Staphylococcus aureus) or -negative (i.e., Pseudomonas aeruginosa) pathogen strains as compared to the natural PM-C. Moreover, some new nitro-PMs were as active as or more than PM-C in inhibiting the proliferation of colon (HCT116) and breast (MCF 7) cancer cell lines and were less toxic towards normal epithelial (hTERT RPE-1) cells. Altogether, our findings contribute to increase the knowledge of the mode of action of these promising molecules and provide a basis for their rationale chemical or biological manipulation. MDPI 2020-05-30 /pmc/articles/PMC7345095/ /pubmed/32486200 http://dx.doi.org/10.3390/antibiotics9060292 Text en © 2020 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Raimondi, Maria Valeria Presentato, Alessandro Li Petri, Giovanna Buttacavoli, Miriam Ribaudo, Agnese De Caro, Viviana Alduina, Rosa Cancemi, Patrizia New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents |
title | New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents |
title_full | New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents |
title_fullStr | New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents |
title_full_unstemmed | New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents |
title_short | New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents |
title_sort | new synthetic nitro-pyrrolomycins as promising antibacterial and anticancer agents |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7345095/ https://www.ncbi.nlm.nih.gov/pubmed/32486200 http://dx.doi.org/10.3390/antibiotics9060292 |
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