The antimicrobial activity of mononuclear ruthenium(II) complexes containing the dppz ligand

Liu, Xuewen, Sun, Biyun, Kell, Ruby E.M., Southam, Hannah M., Butler, Jonathan A., Li, Xin, Poole, Robert K., Keene, F. Richard, and Collins, J. Grant (2018) The antimicrobial activity of mononuclear ruthenium(II) complexes containing the dppz ligand. ChemPlusChem, 83. pp. 643-650.

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Abstract

The cis-α isomer of [Ru(bb7)(dppz)]2+ {dppz = dipyrido[3,2-a:2′,3′-c]phenazine; bb7 = bis[4(4'-methyl-2,2'-bipyridyl)]-1,7-alkane} has been synthesised. The minimum inhibitory concentrations and the minimum bactericidal concentrations of [Ru(bb7)(dppz)]2+ and its parent complex [Ru(phen)2(dppz)]2+ (phen = 1,10-phenanthroline) were determined against a range of bacteria. The results showed that both ruthenium complexes exhibited good activity against Gram-positive bacteria, but [Ru(bb7)(dppz)]2+ showed at least eight-times better activity across the Gram-negative bacteria than [Ru(phen)2(dppz)]2+. Luminescence assays demonstrated that [Ru(bb7)(dppz)]2+ accumulated in a Gram-negative bacterium to the same degree as in a Gram-positive species, while assays with liposomes showed that [Ru(bb7)(dppz)]2+ interacted more strongly with membranes compared to the parent [Ru(phen)2(dppz)]2+ complex. The DNA binding affinity for [Ru(bb7)(dppz)]2+ was determined to be 6.7 × 106 M-1. Although more toxic to eukaryotic cells than [Ru(phen)2(dppz)]2+, [Ru(bb7)(dppz)]2+ exhibited greater activity against bacteria than eukaryotic cells.

Item ID: 53313
Item Type: Article (Research - C1)
ISSN: 2192-6506
Keywords: antimicrobial agents; bioinorganic chemistry; DNA binding; lipophilicity; ruthenium(II) complexes
Funders: China Scholarship Council (CSC), Science Foundation of Hunan Province Education Department (SFHPED), UNSW Canberra, Natural Science Foundation of Jiangsu Province of China (NSFJPC), UK Biotechnology and Biological Science Research Council (BBSRC)
Projects and Grants: SFHPED 16A145, NSFJPC Research Grant No. BK20170746, BBSCR grant BB/M022579/1
Date Deposited: 24 Apr 2018 03:10
FoR Codes: 03 CHEMICAL SCIENCES > 0302 Inorganic Chemistry > 030201 Bioinorganic Chemistry @ 50%
11 MEDICAL AND HEALTH SCIENCES > 1108 Medical Microbiology > 110801 Medical Bacteriology @ 50%
SEO Codes: 97 EXPANDING KNOWLEDGE > 970103 Expanding Knowledge in the Chemical Sciences @ 40%
97 EXPANDING KNOWLEDGE > 970106 Expanding Knowledge in the Biological Sciences @ 30%
97 EXPANDING KNOWLEDGE > 970111 Expanding Knowledge in the Medical and Health Sciences @ 30%
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