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Localization and Photosensitization of Murine Tumors in Vivo and in Vitro by a Chlorin-Porphyrin Ester¹

Departments of Pharmacology and Medicine, Wayne State University School of Medicine, and Harper-Grace Hospitals, Detroit, Michigan 48201

Preparation of the tumor-localizing preparation called hematoporphyrin derivative involves a two-step reaction wherein hematoporphyrin is acetylated and the reaction product subjected to alkaline hydrolysis. We have proposed that the tumor-localizing fraction of this product is composed of hematoporphyrin units joined by ester linkages. Using an analogous synthetic procedure, we prepared some new sensitizers in which hematoporphyrin is esterified to chlorins (reduced porphyrins). Because of the differences in absorption spectra, the porphyrin-chlorin esters are 5-fold more potent photosensitizers than are the porphyrinporphyrin esters, with light of wavelength > 600 nm.

¹ Supported in part by Grant CA 23378 from the National Cancer Institute, NIH, Department of Health and Human Services.

² To whom requests for reprints should be addressed, at the Department of Medicine, Harper-Grace Hospitals, Detroit, MI 48201.

Received 6/ 8/85. Revised 10/18/85. Revised 1/14/86. Accepted 1/20/86.