This paper is part of a special issue dedicated to Professor J. C. (Tito) Scaiano on the occasion of his 60th birthday.
Cellular and Antitumor Activity of a New Diethylene Glycol Benzoporphyrin Derivative (Lemuteporfin)†
Article first published online: 30 APR 2007
Photochemistry and Photobiology
Volume 82, Issue 1, pages 219–224, January 2006
How to Cite
Boch, R., Canaan, A. J., Cho, A., Dolphin, D. D., Hong, L., Jain, A. K., North, J. R., Richter, A. M., Smits, C. and Sternberg, E. D. (2006), Cellular and Antitumor Activity of a New Diethylene Glycol Benzoporphyrin Derivative (Lemuteporfin). Photochemistry and Photobiology, 82: 219–224. doi: 10.1562/2005-06-03-RA-564
- Issue published online: 30 APR 2007
- Article first published online: 30 APR 2007
- Received 3 June 2005; accepted 5 August 2005; published online 12 August 2005
A newly synthesized diethylene glycol functionalized chlorin-type photosensitizer, lemuteporfin, was characterized for use in photodynamic therapy (PDT) in a panel of in vitro and in vivo test systems. The photosensitizer was highly potent, killing cells at low nanomolar concentrations upon exposure to activating light. The cellular uptake of lemuteporfin was rapid, with maximum levels reached within 20 min. Mitogen-activated lymphoid cells accumulated more of the lemuteporfin than their quiescent equivalents, supporting selectivity. Photosensitizer fluorescence in the skin increased rapidly within the first few minutes following intravenous administration to mice, then decreased over the next 24 h. Skin photosensitivity reactions indicated rapid clearance of the photosensitizer. Intravenous doses as low as 1.4 μmol/kg combined with exposure to 50 J/cm2 red light suppressed tumor growth in a mouse model. In conclusion, this new benzoporphyrin was found to be an effective photosensitizer, showing rapid uptake and clearance both in vitro and in vivo. This rapid photosensitization of tumors could be useful in therapies requiring a potent, rapidly accumulating photosensitizer, while minimizing the potential for skin photosensitivity reactions to sunlight following treatment.