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Morphological Study of the Combined Effect of Purpurin Derivatives and Light on Transplantable Rat Bladder Tumors¹

Department of Chemistry [A. R. M.], The University of Toledo; Surgery/Urology [S. H. S., K. C., R. W. K., G. M. G.] and Biochemistry [M. K. B.], Medical College of Ohio; and Research Department and Porphyrin Laboratory [M. K. B., G. M. G.], St. Vincent Medical Center; Toledo, Ohio 43608

Purpurin derivatives, a group of synthetic photosensitizers, were tested for their photodynamic activity against transplantable N-[4-(5-nitro-2-furyl)-2-thiazolyl]formamide-induced urothelial tumors growing in male Fischer 344 rats. Histological examination of tumors in animals treated with the purpurin derivatives and red light (>590 nm, 360 joules/cm²) revealed tumor cell necrosis 24 h after completion of therapy. Control tumors showed no histological change.

Purpurins have a major absorption peak in the red region (>650 nm) of the visible spectrum, a region with good tissue penetration, and purpurins can be synthesized with a high degree of purity. This study demonstrates the potential of purpurin derivatives as photosensitizers for photodynamic cancer therapy.

¹ This work was supported in part by grants from the Geiger Foundation for Cancer Research and the F.M. Douglass Foundation and by the New Investigator Award (NIH R23-CA38754-01).

² To whom requests for reprints should be addressed, at Department of Chemistry, University of Toledo, Toledo, OH 43606.

Received 8/ 6/86. Accepted 10/ 9/86.