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EVALUATION OF PORPHYRIN CHARACTERISTICS REQUIRED FOR PHOTODYNAMIC THERAPY
Authors:K. W. Woooburn    N. J. Vardaxis    J. S. Hill    A. H. Kaye    J. A. Reiss   D. R. Phillips
Affiliation:Biochemistry Department, La Trobe University, Bundoora, Victoria, Australia.
Abstract:The cytotoxicity (in the dark), phototoxicity (red light) and subcellular localization (using confocal laser scanning microscopy) were determined for 15 porphyrins (1-15) in C6 glioma cells. The partition coefficient in 2-octanol was also determined for each porphyrin at pH 7.4. The cytotoxicity increased with pi (log of partition coefficient) up to pi values of +2. The 7 porphyrins with cationic side chains exhibited a classical parabolic correlation between phototoxicity and pi, with maximal activity at a pi value of approximately 1.0. There was also a significant correlation between subcellular localization and degree of phototoxicity, with the three most photosensitive porphyrins all possessing cationic side chains, and all three localizing in mitochondria.
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