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Tumor-localizing and Photosensitizing Properties of the Main Components of Hematoporphyrin Derivative¹

Norwegian Radium Hospital, Oslo 3, Norway [J. F. E.], and Norsk Hydros Institute of Cancer Research [S. S., J. M., T. C.], Oslo, Norway

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 two 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 photosensitizers.

¹ This work was supported by the Norwegian Cancer Society (Landsforeningen mot kreft).

² To whom requests for reprints should be addressed.

Received 4/ 4/83. Accepted 10/15/83.