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Issue 12, 2013
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Targeting the endoplasmic reticulum with a membrane-interactive luminescent ruthenium(II) polypyridyl complex

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Abstract

The characterization and bioactivity of the dinuclear ruthenium(II) complex [(Ru(DIP)2)2(tpphz)]4+ (DIP = 4,7-diphenyl-1,10-phenanthroline and tpphz = tetrapyrido[3,2-a:2′,3′-c:3′′,2′′-h:2′′′,3′′′-j]phenazine) is reported. This new complex is found to be luminescent in acetonitrile, where excitation into MLCT (metal-to-ligand charge-transfer) bands in the visible area of the spectrum (λex = 450 nm, ε = 45 000 M−1 cm−1) result in red emission (λem,max = 620 nm, ΦMLCT = 0.017). Aqueous in vitro binding studies indicate that this complex binds to duplex DNA with an affinity of 1.8 × 106 M−1 through a non-classical groove-binding interaction, however, unlike the parent complex [(Ru(phen)2)2(tpphz)]4+ (phen = 1,10-phenanthroline), it also displays an increase in MLCT luminescence on addition of liposomes. Confocal microscopy and TEM studies show that this lipophilic complex targets the endoplasmic reticulum of eukaryotic cells, where it functions as an imaging agent for this organelle, and cytotoxicity studies in human cancer cell lines indicate a comparable potency to the anti-cancer drug cisplatin.

Graphical abstract: Targeting the endoplasmic reticulum with a membrane-interactive luminescent ruthenium(ii) polypyridyl complex

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Publication details

The article was received on 20 Jun 2013, accepted on 02 Oct 2013 and first published on 03 Oct 2013


Article type: Edge Article
DOI: 10.1039/C3SC51725J
Citation: Chem. Sci., 2013,4, 4512-4519
  • Open access: Creative Commons BY license
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    Targeting the endoplasmic reticulum with a membrane-interactive luminescent ruthenium(II) polypyridyl complex

    M. R. Gill, D. Cecchin, M. G. Walker, R. S. Mulla, G. Battaglia, C. Smythe and J. A. Thomas, Chem. Sci., 2013, 4, 4512
    DOI: 10.1039/C3SC51725J

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