Synthesis, Characterization, and Biological Evaluation of New Ru(II) Polypyridyl Photosensitizers for Photodynamic Therapy

Frei, Angelo and Rubbiani, Riccardo and Tubafard, Solmaz and Blacque, Olivier and Anstaett, Philipp and Felgentraeger, Ariane and Maisch, Tim and Spiccia, Leone and Gasser, Gilles (2014) Synthesis, Characterization, and Biological Evaluation of New Ru(II) Polypyridyl Photosensitizers for Photodynamic Therapy. JOURNAL OF MEDICINAL CHEMISTRY, 57 (17). pp. 7280-7292. ISSN 0022-2623, 1520-4804

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Abstract

Two Ru(II) polypyridyl complexes, Ru(DIP)(2)(bdt) (1) and [Ru(dqpCO(2)Me)(ptpy)](2+) (2) (DIP = 4,7-diphenyl-1,10-phenanthroline, bdt = 1,2-benzenedithiolate, dqpCO2Me = 4-methylcarboxy-2,6-di(quinolin-8-yl)pyridine), ptpy = 4'-phenyl-2,2':6',2 ''-terpyridine) have been investigated as photosensitizers (PSs) for photodynamic therapy (PDT). In our experimental settings, the phototoxicity and phototoxic index (PI) of 2 (IC50(light): 25.3 mu M, 420 nm, 6.95 J/cm(2); PI >4) and particularly of 1 (IC50(light): 0.62 mu M, 420 nm, 6.95 J/cm(2); PI: 80) are considerably superior compared to the two clinically approved PSs porfimer sodium and 5-aminolevulinic acid. Cellular uptake and distribution of these complexes was investigated by confocal microscopy (1) and by inductively coupled plasma mass spectrometry (1 and 2). Their phototoxicity was also determined against the Gram-(+) Staphylococcus aureus and Gram-(-) Escherichia coli for potential antimicrobial PDT (aPDT) applications. Both complexes showed significant aPDT activity (420 nm, 8 J/cm(2)) against Gram-(+) (S. aureus; >6 log(10) CFU reduction) and, for 2, also against Gram-(-) E. coli (>4 log10 CFU reduction).

Item Type: Article
Uncontrolled Keywords: RUTHENIUM COMPLEXES; CELLULAR UPTAKE; ANTIMICROBIAL AGENTS; TRIDENTATE LIGANDS; SINGLET OXYGEN; EXCITED-STATES; IN-VITRO; LIGHT; PORPHYRIN; DESIGN;
Subjects: 600 Technology > 610 Medical sciences Medicine
Divisions: Medicine > Lehrstuhl für Dermatologie und Venerologie
Depositing User: Dr. Gernot Deinzer
Date Deposited: 14 Aug 2019 08:42
Last Modified: 14 Aug 2019 08:42
URI: https://pred.uni-regensburg.de/id/eprint/9555

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