TUMOR-LOCALIZING AND PHOTOSENSITIZING PROPERTIES OF THE MAIN COMPONENTS OF HEMATOPORPHYRIN DERIVATIVE

Abstract

Both 3H-labeled and unlabeled hematoporphyrin derivative (HPD) were analyzed by high-pressure liquid chromatography (HPLC) and gel permeation chromatography. Four main components were isolated by HPLC, and 2 were isolated by gel permeation chromatography. The tumor-localizing ability of each component was tested and compared to that of 67Ga and 3H2O by injection in mice bearing Lewis lung carcinoma. The photosensitizing abilities of the HPLC-separated components in vitro were also tested. Finally, porphyrin extracts of tumors from mice given HPD were analyzed by HPLC. The tumor localizing ability of the components increased with decreasing polarity. While crude HPD localized in tumor tissue only to the same extent as did 3H2O, Component 7 was almost as effective as was 67Ga in localizing in the tumor. The cellular uptake of HPD components increased with decreasing polarity. In accordance with this, the low-polarity components were the most effective photosensitizer.