Development of glycoconjugated porphyrin metal complexes for X-ray dynamic therapy

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Radiotherapy is an excellent treatment for deep-seated cancer. However, repeated irradiation with nearly lethal dose is generally required to kill the tumor, which gives serious strains on patients. In this study, we propose a new radiotherapy which combines X-ray sensitizer with low-dose X-ray irradiation. We synthesized S-, O- and triazol-glucoconjugated porphyrin metal complexes (H2, Zn, Pd, Pt) with all five patterns of glucoconjugation as sensitizers. In addition, the cytotoxicity of porphyrins was evaluated without X-ray irradiation and under X-ray irradiation in normal rat gastric mucosal cells (RGM) and a rat murine RGM gastric carcinoma mucosal cells (RGK). Almost all of porphyrins afforded significantly higher cytotoxicity to RGK cells rather than to RGM cells upon X-ray irradiation. Furthermore, we succeeded in inhibiting the side effects of porphyrin ring, namely photocytotoxicity, by means of the coincubation of alpha-tocopherol with porphyrins.