We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Evaluation of the Medicinal Potential of Two Ruthenium(II) Polypyridine Complexes as One- and Two-Photon Photodynamic Therapy Photosensitizers.
- Authors
Hess, Jeannine; Huang, Huaiyi; Kaiser, Adrian; Pierroz, Vanessa; Blacque, Olivier; Chao, Hui; Gasser, Gilles
- Abstract
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 (log Po/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 (log Po/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 μ m) was found to be more toxic than complex 2 (IC50 >100 μ m) 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 μ m). Upon one-photon irradiation (420 nm, 9.27 J cm−2), 1 exhibited higher phototoxicity (IC50=3.1 μ m) than 2 (IC50=16.7 μ m) on HeLa cell monolayers. When two-photon irradiation (800 nm, 9.90 J cm−2) was applied, only 1 (IC50=9.5 μ m) 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.
- Subjects
RUTHENIUM compound derivatives; POLYPYRIDINES; PHOTODYNAMIC therapy; PHOTOSENSITIZERS; COMPLEX compounds synthesis; REACTIVE oxygen species
- Publication
Chemistry - A European Journal, 2017, Vol 23, Issue 41, p9888
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201701392