1.Cellular and antitumor activity of a new diethylene glycol benzoporphyrin derivative (lemuteporfin).
Boch R1, Canaan AJ, Cho A, Dolphin DD, Hong L, Jain AK, North JR, Richter AM, Smits C, Sternberg ED. Photochem Photobiol. 2006 Jan-Feb;82(1):219-24.
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 micromol/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.
2.Photobleaching kinetics of Verteporfin and Lemuteporfin in cells and optically trapped multilamellar vesicles using two-photon excitation.
Tekrony AD1, Kelly NM, Fage BA, Cramb DT. Photochem Photobiol. 2011 Jul-Aug;87(4):853-61. doi: 10.1111/j.1751-1097.2011.00933.x. Epub 2011 May 10.
Verteporfin and Lemuteporfin are compared to examine the effect of their functional groups and therefore the localization in two-photon excitation (TPE) photodynamic therapy (PDT). We used singlet oxygen-related photobleaching of the sensitizers to assess TPE-induced singlet oxygen generation in multilamellar vesicles (MLVs) and U343 glioma cells under a variety of conditions. It was found that Lemuteporfin photobleached at a faster rate than Verteporfin in the majority of environments. Also, Verteporfin and Lemuteporfin exhibited different behaviors when in hypoxic environments relative to those in oxygenated MLVs. These differences are attributed to the sensitizer location in the membrane and their relative mobilities throughout membranes and cells.