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.

Maria Valeria Raimondi, A.P. (2020). New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents. ANTIBIOTICS, 9(6), 1-19 [10.3390/antibiotics9060292].

New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents

Maria Valeria Raimondi;Alessandro Presentato;Giovanna Li Petri
;
Miriam Buttacavoli;Agnese Ribaudo;Viviana De Caro;Rosa Alduina
;
Patrizia Cancemi
2020-01-01

Abstract

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.
2020
Settore CHIM/08 - Chimica Farmaceutica
Settore BIO/19 - Microbiologia Generale
Settore BIO/06 - Anatomia Comparata E Citologia
Maria Valeria Raimondi, A.P. (2020). New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents. ANTIBIOTICS, 9(6), 1-19 [10.3390/antibiotics9060292].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/424688
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