Abstract
Radioiodinated porphyrin derivatives and the corresponding nonradioactive iodine introduced compounds, [(125)I]I-TPP(OH) ([(125)I]3), [(125)I]I-l-tyrosine-TPP ([(125)I]9), I-TPP(OH) (3), and I-l-tyrosine-TPP (9) were designed, synthesized, and evaluated by in vitro and in vivo experiments. In cytotoxicity assays, 3 and 9 exhibited significant cytotoxicity under light conditions but did not show significant cytotoxicity without light irradiation. Biodistribution experiments with [(125)I]3 and [(125)I]9 showed similar distribution patterns with high retention in tumors. In photodynamic therapeutic (PDT) experiments, 3 and 9 at a dose of 13.6 μmol kg(-1) weight with 50 W single light irradiation onto the tumor area significantly inhibited tumor growth. These results indicate that the iodinated porphyrin derivatives [(123/nat)I]3 and [(123/nat)I]9 are promising cancer theranostic agents.