title: Diastereomeric bactericidal effect of Ru(phenanthroline)2dipyridophenazine.
abstract: Metal susceptibility assays and spot plating were used to investigate the antimicrobial activity of enantiopure [Ru(phen)2dppz]2+(phen =1,10-phenanthroline and dppz = dipyrido[3,2-a:2´,3´-c]phenazine) and [μ-bidppz(phen)4Ru2]4+(bidppz =11,11´-bis(dipyrido[3,2-a:2´,3´-c]phenazinyl)), on Gram-negative Escherichia coli and Gram-positive Bacillus subtilis as bacterial models. The minimum inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC) were determined for both complexes: while [μ-bidppz(phen)4Ru2]4+only showed a bactericidal effect at the highest concentrations tested, the antimicrobial activity of [Ru(phen)2dppz]2+against B. subtilis was comparable to that of tetracyline. In addition, the Δ-enantiomer of [Ru(phen)2dppz]2+showed a 2-fold higher bacteriostatic and bactericidal effect compared to the Λ-enantiomer. This was in accordance with the enantiomers relative binding affinity for DNA, thus strongly indicating DNA binding as the mode of action.
authors: Department of Chemistry and Chemical Engineering, Chalmers University of Technology, Gothenburg, Sweden. marann@chalmers.se.
authors: Anna K F
authors: AK
authors: Mårtensson
authors: Wallenberg Laboratory and Sahlgrenska Center for Cardiovascular and Metabolic Research, Department of Molecular and Clinical Medicine, Institute of Medicine, University of Gothenburg, Gothenburg, Sweden.
authors: Mattias
authors: M
authors: Bergentall
authors: Wallenberg Laboratory and Sahlgrenska Center for Cardiovascular and Metabolic Research, Department of Molecular and Clinical Medicine, Institute of Medicine, University of Gothenburg, Gothenburg, Sweden.
authors: Valentina
authors: V
authors: Tremaroli
authors: Department of Chemistry and Chemical Engineering, Chalmers University of Technology, Gothenburg, Sweden.
authors: Per
authors: P
authors: Lincoln
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D009942:Organometallic Compounds / Q000737:chemistry; D010618:Phenanthrolines / Q000737:chemistry; D012428:Ruthenium / Q000737:chemistry* / Q000494:pharmacology; D013237:Stereoisomerism
chemical_list: D000900:Anti-Bacterial Agents; D009942:Organometallic Compounds; D010618:Phenanthrolines; D012428:Ruthenium
keywords: antimicrobial activity; chirality; confocal microscopy; emission; metal susceptibility assay; minimum bactericidal concentration; minimum inhibitory concentration; ruthenium complex