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5,10,15,20-Tetrakis-(N-methyl-3'-pyridyl)-21H,23H-7,8,17,18-Tetrahydro-porphyrin tetratosylat (THPTs) and 5,10,15,20-Tetrakis-(N-methyl -3'-pyridyl)-21H,23H-7,8,17,18-Tetrahydroporphyrin tetraiodid (THPI)- new, Water-soluble, Positively-charged and Chemically-stable Photosen-sitizers with a Strong Absorption at 760 nm for Photodynamic Therapy (PDT) of Black Melanoma
1Schastak S., 2Shulga A., 1Wang Y.-S., 1Handzel R., 3Herrmann R.,
1Universität Leipzig, Klinik und Poliklinik für Augenheilkunde (Leipzig)
2Institut für Molekulare und Atomare Physik, Akademie der Wissenschaften (Minsk)
3Universität Leipzig, Fakultät für Chemie und Mineralogie (Leipzig)
Purpose: Investigation of the photophysical and photodynamic properties of the THPTs- and THPI compounds as the potential photosensitizer for the PDT of tumors.
Method: At first the absorption, fluorescence emission and NMR spectra of THPTs and THPI were measured. The photodynamic properties of the compounds were investigated using choroidal melanoma (CM) cells. Cells were incubated in the dark for 1 to 24 hours at 37 °C. Cellular uptake were investigated by a fluorometer and a confocal laser scanning microscope. The irradiation was performed at 760 nm using an Ar+ / Ti:Sa or a diode laser. Cell survival was measured using the MTT test. In each case, at least three independent experiments were performed.
Results: For the CM cell line, both photosensitizer showed low dark toxicity even after long term incubation (12-24h) and the concentrations of nearly 10 µM(LD10). The intracellular accumulation was completed after 12 h incubation of THPTs or THPI at non-cytotoxic concentrations (LD10). Significant cell inactivation of 95% was achieved after 24h incubation at non-cytotoxic concentrations and irradiation with 15.0 J/cm2 at 760nm. The cell inactivation increased considerably with increasing THPTs or THPI concentration in the incubation medium.
Conclusions: In accordance to the present results both compounds THPTs and THPI seem to be of interest for further in vivo investigations.