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BIOLOGICAL ACTIVITIES OF PHTHALOCYANINES. XIII. THE EFFECTS OF HUMAN SERUM COMPONENTS ON THE in vitro UPTAKE AND PHOTODYNAMIC ACTIVITY OF ZINC PHTHALOCYANINE

Abstract— The effect of human serum components on the photodynamic activity of zinc phthalocyanine (ZnPc) toward Chinese hamster fibroblasts (lineV–79) was studied. Photodynamic activities were correlated with cellular uptake of radiolabeled [65Zn]ZnPc, which allowed corrections to be made for the amount of sensitizer present in the cells at the time of irradiation and to express photodynamic efficiences on a cellular dye concentration basis. All serum components, with the exception of high‐density lipoproteins, inhibit uptake of ZnPc byV–79 cells, when compared to incubation of ZnPc with the same cells in serum‐free medium. High‐density lipoproteins increased ZnPc uptake by 23%, but the photodynamic efficiency corrected for the cellular ZnPc concentration was unaffected. Very low‐density lipoprotein and globulins decreased ZnPc cell uptake but likewise did not affect the cellular photodynamic efficiency of the dye. In contrast low‐density lipoprotein and albumin, while inhibiting ZnPc cell uptake, increased the cellular photodynamic efficiency of ZnPc, suggesting that these proteins facilitate localization of the dye at cellular targers sensitive to photodynamic damage and vital to cell survival. We conclude from these results that association of ZnPc with serum components can have important, and widely differing, effects on both degree of uptake and cellular distribution of the photosensitizer.