Exploring the potential of highly charged Ru(II)- and heteronuclear Ru(II)/Cu(II)-polypyridyl complexes as antimicrobial agents.

Autor: Conti L; Department of Chemistry 'Ugo Schiff', University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy. Electronic address: luca.conti@unifi.it., Mengoni A; Department of Biology, University of Florence, via Madonna del Piano 6, 50019 Sesto Fiorentino (FI), Italy., Giacomazzo GE; Department of Chemistry 'Ugo Schiff', University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy., Mari L; Department of Chemistry 'Ugo Schiff', University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy., Perfetti M; Department of Chemistry 'Ugo Schiff', University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy., Fagorzi C; Department of Biology, University of Florence, via Madonna del Piano 6, 50019 Sesto Fiorentino (FI), Italy., Sorace L; Department of Chemistry 'Ugo Schiff', University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy., Valtancoli B; Department of Chemistry 'Ugo Schiff', University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy., Giorgi C; Department of Chemistry 'Ugo Schiff', University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy.
Jazyk: angličtina
Zdroj: Journal of inorganic biochemistry [J Inorg Biochem] 2021 Jul; Vol. 220, pp. 111467. Date of Electronic Publication: 2021 Apr 22.
DOI: 10.1016/j.jinorgbio.2021.111467
Abstrakt: The antimicrobial potential of two ruthenium(II) polypyridyl complexes, [Ru(phen) 2 L1] 2+ and [Ru(phen) 2 L2] 2+ (phen = 1,10-phenanthroline) containing the 4,4'-(2,5,8,11,14-pentaaza[15])-2,2'-bipyridilophane (L1) and the 4,4'-bis-[methylen-(1,4,7,10-tetraazacyclododecane)]-2,2' bipyridine (L2) units, is herein investigated. These peculiar polyamine frameworks afford the formation of highly charged species in solution, influence the DNA-binding and cleavage properties of compounds, but they do not undermine their singlet oxygen sensitizing capacities, thus making these complexes attractive 1 O 2 generators in aqueous solution. L1 and L2 also permit to stably host Fenton -active Cu 2+ ion/s, leading to the formation of mixed Ru 2+ /Cu 2+ forms capable to further strengthen the oxidative damages to biological targets. Herein, following a characterization of the Cu 2+ binding ability by [Ru(phen) 2 L2] 2+ , the water-octanol distribution coefficients, the DNA binding, cleavage and 1 O 2 sensitizing properties of [Ru(phen) 2 L2] 2+ and [Cu 2 Ru(phen) 2 L2] 6+ were analysed and compared with those of [Ru(phen) 2 L1] 2+ and [CuRu(phen) 2 L1] 4+ . The antimicrobial activity of all compounds was evaluated against B. subtilis, chosen as a model for gram-positive bacteria, both under dark and upon light-activation. Our results unveil a notable phototoxicity of [Ru(phen) 2 L2] 2+ and [Cu 2 Ru(phen) 2 L2] 6+ , with MIC (minimal inhibitory concentrations) values of 3.12 μM. This study highlights that the structural characteristics of polyamine ligands gathered on highly charged Ru(II)-polypyridyl complexes are versatile tools that can be exploited to achieve enhanced antibacterial strategies.
(Copyright © 2021 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
Externí odkaz: