期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 57, 期 17, 页码 7280-7292出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm500566f
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资金
- Swiss National Science Foundation (SNSF Professorship) [PP00P2_133568]
- University of Zurich
- Stiftung fur Wissenschaftliche Forschung of the University of Zurich
- Novartis Jubilee Foundation
- Australian Research Council through the Australian Centre of Excellence for Electromaterials Science
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).
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