3 years ago

Evaluation of the Medicinal Potential of Two Ruthenium(II) Polypyridine Complexes as One- and Two-Photon Photodynamic Therapy Photosensitizers

Evaluation of the Medicinal Potential of Two Ruthenium(II) Polypyridine Complexes as One- and Two-Photon Photodynamic Therapy Photosensitizers
Huaiyi Huang, Gilles Gasser, Adrian Kaiser, Hui Chao, Vanessa Pierroz, Olivier Blacque, Jeannine Hess
Two [Ru(phen)2dppz]2+ derivatives (phen=1,10-phenantroline, dppz=dipyrido[3,2-a:2′,3′-c]phenazine) with different functional groups on the dppz ligand [dppz-7,8-(OMe)2 (1), dppz-7,8-(OH)2 (2)] have been synthesized, characterized and investigated as photosensitizers (PSs) for photodynamic therapy (PDT) against cancer. Both complexes showed intense red phosphorescence and promising singlet oxygen (1O2) quantum yields of 75 % (1) and 54 % (2) in acetonitrile. Complex 1 (logPo/w=−0.52, 2.4 nmol Ru per mg protein) was found to be more lipophilic, having also a higher cellular uptake efficiency compared to 2 (logPo/w=−0.20, 0.9 nmol Ru per mg protein). Complex 1 localized evenly in HeLa cells whereas 2, was mainly visualized in the cell membrane by confocal microscopy. In the dark, complex 1 (IC50=36.5 μm) was found to be more toxic than complex 2 (IC50 >100 μm) on a HeLa cells monolayer. Importantly, in view of PDT applications, both complexes were found to be non-toxic in the dark towards multicellular HeLa spheroids (IC50>100 μm). Upon one-photon irradiation (420 nm, 9.27 J cm−2), 1 exhibited higher phototoxicity (IC50=3.1 μm) than 2 (IC50=16.7 μm) on HeLa cell monolayers. When two-photon irradiation (800 nm, 9.90 J cm−2) was applied, only 1 (IC50=9.5 μm) was found to be active toward HeLa spheroids. This study demonstrates that the functional group on the intercalative ligand has a strong influence on the cellular localization and anticancer activity of RuII polypyridyl complexes. The structure influences the activity! Two RuII polypyridyl complexes have been synthesized, characterized and investigated as photosensitizers (PSs) for photodynamic therapy (PDT) against cancer.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/chem.201701392

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