Mononuclear polypyridylruthenium(II) complexes with high membrane permeability in gram-negative bacteria—in particular Pseudomonas aeruginosa

Gorle, Anil K., Feterl, Marshall, Warner, Jeffrey M., Primrose, Sebastian, Constantinoiu, Constantin C., Keene, F. Richard, and Collins, J. Grant (2015) Mononuclear polypyridylruthenium(II) complexes with high membrane permeability in gram-negative bacteria—in particular Pseudomonas aeruginosa. Chemistry: a European journal, 21 (29). pp. 10472-10481.

[img] PDF (Published Version) - Published Version
Restricted to Repository staff only

View at Publisher Website: http://dx.doi.org/10.1002/chem.201500385
 
10
11


Abstract

Ruthenium(II) complexes containing the tetra dentate ligand bis[4(4'-methyl-2,2'-bipyridyl)]-1,n-alkane ("bb(n)"; n=10 and 12) have been synthesised and their geometric isomers separated. All [Ru(phen)(bb(n))]²⁺ (phen=1,10-phenanthroline) complexes exhibited excellent activity against Gram-positive bacteria, but only the cis-a-[Ru(phen)(bb₁₂)]²⁺ species showed good activity against Gram-negative species. In particular, the cis-a-[Ru(phen)(bb₁₂)]²⁺ complex was two to four times more active than the cis-b-[Ru(phen)(bb₁₂)]²⁺complex against the Gram-negative strains. The cis-a- and cis-b-[Ru(phen)(bb₁₂)]²⁺ complexes readily accumulated in the bacteria but, significantly, showed the highest level of uptake in Pseudomonas aeruginosa. Furthermore, the accumulation of the cis-a- and cis-b-[Ru(phen)(bb₁₂)]²⁺ complexes in P. aeruginosa was considerably greater than in Escherichia coli. The uptake of the cis-a-[Ru(phen)(bb₁₂)]²⁺ complex into live P. aeruginosa was confirmed by using fluorescence microscopy. The water/octanol partition coefficients (log P) were determined to gain understanding of the relative cellular uptake. The cis-a- and cis-b-[Ru(phen)(bb(n))]²⁺ complexes exhibited relatively strong binding to DNA (Kb≈10⁶M⁻¹ ), but no significant difference between the geometricisomers was observed.

Item ID: 39106
Item Type: Article (Refereed Research - C1)
Keywords: antibacterial; ruthenium; lipophilic; Gram negative bacteria; Pseudomonas aeruginosa
ISSN: 1521-3765
Date Deposited: 11 Jun 2015 04:36
FoR Codes: 03 CHEMICAL SCIENCES > 0302 Inorganic Chemistry > 030201 Bioinorganic Chemistry @ 70%
11 MEDICAL AND HEALTH SCIENCES > 1108 Medical Microbiology > 110899 Medical Microbiology not elsewhere classified @ 30%
SEO Codes: 97 EXPANDING KNOWLEDGE > 970103 Expanding Knowledge in the Chemical Sciences @ 70%
97 EXPANDING KNOWLEDGE > 970111 Expanding Knowledge in the Medical and Health Sciences @ 30%
Downloads: Total: 11
More Statistics

Actions (Repository Staff Only)

Item Control Page Item Control Page