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Issue 9, 2016
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Dinuclear ruthenium(II) complexes containing one inert metal centre and one coordinatively-labile metal centre: syntheses and biological activities

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Abstract

A series of non-symmetric dinuclear polypyridylruthenium(II) complexes (Rubbn-Cl) that contain one inert metal centre and one coordinatively-labile metal centre, linked by the bis[4(4′-methyl-2,2′-bipyridyl)]-1,n-alkane ligand (“bbn” for n = 7, 12 and 16), have been synthesised and their potential as antimicrobial agents examined. The minimum inhibitory concentrations (MIC) of the ruthenium(II) complexes were determined against four strains of bacteria − Gram-positive Staphylococcus aureus (S. aureus) and methicillin-resistant S. aureus (MRSA), and Gram-negative Escherichia coli (E. coli) and Pseudomonas aeruginosa (P. aeruginosa). The Rubbn-Cl complexes displayed good antimicrobial activity, with Rubb12-Cl being the most active complex against both Gram-positive and Gram-negative strains. Interestingly, Rubb7-Cl was found to be eight- and sixteen-fold more active towards E. coli than against S. aureus and MRSA, respectively. The cytotoxicities of the Rubbn-Cl complexes against three eukaryotic cell lines – two kidney cell lines (BHK and HEK-293) and one liver cell line (HepG2) – were examined. The Rubbn-Cl complexes were found to be considerably less toxic towards eukaryotic cells than S. aureus, MRSA and E. coli, with Rubb12-Cl being thirty- to eighty-times more toxic to the bacteria than to BHK, HEK-293 or HepG2 cells. Unexpectedly, Rubb7-Cl was far more toxic to HepG2 cells (24 h-IC50 = 3.7 μM) and far less toxic to BHK cells (24 h-IC50 = 238 μM) than the Rubb12-Cl and Rubb16-Cl complexes. In order to understand the unexpected large differences in the cytotoxicities of the Rubbn-Cl complexes towards eukaryotic cells, a confocal microscopic study of their intracellular localisation was undertaken. The results suggest that the observed cytotoxicity might be related to the extent of DNA binding.

Graphical abstract: Dinuclear ruthenium(ii) complexes containing one inert metal centre and one coordinatively-labile metal centre: syntheses and biological activities

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Publication details

The article was received on 15 Dec 2015, accepted on 25 Jan 2016 and first published on 03 Feb 2016


Article type: Paper
DOI: 10.1039/C5DT04885K
Dalton Trans., 2016,45, 4017-4029
  • Open access: Creative Commons BY license
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    Dinuclear ruthenium(II) complexes containing one inert metal centre and one coordinatively-labile metal centre: syntheses and biological activities

    X. Li, K. Heimann, F. Li, J. M. Warner, F. Richard Keene and J. Grant Collins, Dalton Trans., 2016, 45, 4017
    DOI: 10.1039/C5DT04885K

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