Cytotoxicity of cyclometallated ruthenium complexes: the role of ligand exchange on the activity
Alycia M. Palmer, Bruno Peña, R. Bryan Sears, Olivia Chen, Maya El Ojaimi, Randolph P. Thummel, Kim R. Dunbar, Claudia Turro
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Source: Crossref
Published: Jul 28, 2013
DOI: 10.1098/rsta.2012.0135
Open original source ↗Source abstract
The cyclometallated Ru(II) complexes cis -[Ru(phpy)(phen)(CH 3 CN) 2 ](PF 6 ) ( 1 ; phpy − =deprotonated 2-phenylpyridine, phen=1,10-phenanthroline) and cis -[Ru(phpy)(bpy)(CH 3 CN) 2 ](PF 6 ) ( 2 ; bpy=2,2′-bipyridine) were investigated as potential agents for photodynamic therapy. The presence of phpy − in the coordination sphere results in a red-shift of the Ru→phen and Ru→bpy metal-to-ligand charge transfer of 1 and 2 , respectively, thus improving the tissue penetration of light while maintaining the efficient photo-induced ligand exchange required for DNA binding. The 14-fold enhancement of OVCAR-5 cell death that occurs upon irradiation with 690 nm light can be attributed to photo-aquation. The role of glutathione (GSH) on the toxicity of the complex was also explored. Complexes 1 and 2 undergo ligand substitution in the presence of GSH in the dark, such that the metal may covalently bind to biomolecules. The combination of photo-induced ligand exchange and GSH-facilitated ligand exchange may explain the observed cytotoxicity.
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