Many bacterial strains are developing mechanism of resistance to antibiotics, rendering last-resort antibiotics inactive. Therefore, new drugs are needed and in particular metal-based compounds represent a valid starting point to explore new antibiotic classes. In this study, we have chosen to investigate gallium(III) complexes for their potential antimicrobial activity against different strains of Klebsiella pneumoniae, Escherichia coli, and Pseudomonas aeruginosa which have developed different type of resistance mechanism, including the expression of beta-lactamases (NDM-1, ES beta L, or AmpC) or the production of biofilm. We studied a series of thiosemicarbabazones derived from pyridoxal, their related Ga(III) complexes, and the speciation in solution of the Ga(III)/ligand systems as a function of the pH. Proton dissociation constants and conditional stability constants of Ga(III) complexes were evaluated by UV/Vis spectroscopy, and the most relevant species at physiological pH were identified. The compounds are active against resistant Gram-negative strain with minimal inhibitory concentration in the mu M range, while no cytotoxicity was detected in eukaryotic cells.

Gallium(III)-pyridoxal thiosemicarbazone derivatives as nontoxic agents against Gram-negative bacteria / Scaccaglia, Mirco; Rega, Martina; Vescovi, Marianna; Pinelli, Silvana; Tegoni, Matteo; Bacci, Cristina; Pelosi, Giorgio; Bisceglie, Franco. - In: METALLOMICS. - ISSN 1756-5901. - 14:10(2022). [10.1093/mtomcs/mfac070]

Gallium(III)-pyridoxal thiosemicarbazone derivatives as nontoxic agents against Gram-negative bacteria

Scaccaglia, Mirco;Rega, Martina;Vescovi, Marianna;Pinelli, Silvana;Tegoni, Matteo;Bacci, Cristina;Pelosi, Giorgio;Bisceglie, Franco
2022-01-01

Abstract

Many bacterial strains are developing mechanism of resistance to antibiotics, rendering last-resort antibiotics inactive. Therefore, new drugs are needed and in particular metal-based compounds represent a valid starting point to explore new antibiotic classes. In this study, we have chosen to investigate gallium(III) complexes for their potential antimicrobial activity against different strains of Klebsiella pneumoniae, Escherichia coli, and Pseudomonas aeruginosa which have developed different type of resistance mechanism, including the expression of beta-lactamases (NDM-1, ES beta L, or AmpC) or the production of biofilm. We studied a series of thiosemicarbabazones derived from pyridoxal, their related Ga(III) complexes, and the speciation in solution of the Ga(III)/ligand systems as a function of the pH. Proton dissociation constants and conditional stability constants of Ga(III) complexes were evaluated by UV/Vis spectroscopy, and the most relevant species at physiological pH were identified. The compounds are active against resistant Gram-negative strain with minimal inhibitory concentration in the mu M range, while no cytotoxicity was detected in eukaryotic cells.
2022
Gallium(III)-pyridoxal thiosemicarbazone derivatives as nontoxic agents against Gram-negative bacteria / Scaccaglia, Mirco; Rega, Martina; Vescovi, Marianna; Pinelli, Silvana; Tegoni, Matteo; Bacci, Cristina; Pelosi, Giorgio; Bisceglie, Franco. - In: METALLOMICS. - ISSN 1756-5901. - 14:10(2022). [10.1093/mtomcs/mfac070]
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11381/2932552
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 4
  • ???jsp.display-item.citation.isi??? 6
social impact