NDLI: Green light-induced apoptosis in cancer cells by a tetrapyridyl ruthenium prodrug offering two <i>trans</i> coordination sites

Content Provider	Royal Society of Chemistry (RSC)
Author	Hopkins, S. L. Bonnet, Sylvestre Siegler, M. A. Askes, S. H. C. Siewert, B. Rixel, V. H. S. van Busemann, A.
Copyright Year	2016
Abstract	In this work, two new photopharmacological ruthenium prodrugs are described that can be activated by green light. They are based on the tetrapyridyl biqbpy ligand (6,6′-bis[N-(isoquinolyl)-1-amino]-2,2′-bipyridine), which coordinates to the basal plane of the metal centre and leaves two trans coordination sites for the binding of monodentate sulphur ligands. Due to the distortion of the coordination sphere these trans ligands are photosubstituted by water upon green light irradiation. In vitro cytotoxicity data on A431 and A549 cancer cell lines shows an up to 22-fold increase in cytotoxicity after green light irradiation (520 nm, 75 J cm−2), compared to the dark control. Optical microscopy cell imaging and flow cytometry indicate that the cancer cells die via apoptosis. Meanwhile, very low singlet oxygen quantum yields (∼1–2%) and cell-free DNA binding studies conclude that light-induced cell death is not caused by a photodynamic effect, but instead by the changes induced in the coordination sphere of the metal by light, which modifies how the metal complexes bind to biomolecules.
Starting Page	4922
Ending Page	4929
Page Count	8
File Format	HTM / HTML PDF
ISSN	20416520
Volume Number	7
Issue Number	8
Journal	Chemical Science
DOI	10.1039/c6sc00167j
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Subscribed
Subject Keyword	Flow cytometry Ruthenium Ligand Cytotoxicity Quantum Singlet oxygen Microscopy Bipyridine DNA Denticity Crystal structure Nucleophile Cancer Apoptosis
Content Type	Text
Resource Type	Article
Subject	Chemistry

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