An novel hematoporphyrin-anticancer drug conjugate for a therapy of lung metastasis of sarcoma.

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1.Implantation of rat osteosarcoma, S-SLM : A appropriate focus of lung metastasis was selected, and implanted into the subcutaneous layr of F344 rat (male). We divided the rats into 5 groups as described below, each group included 10 rats.2.Preparation of hematoporphyrin-mitomycin C conjugate : Hematoporphyrin and mitomycin c were conjugated by dehydrated reaction under the DCC and 4-dimethylaminopyridine.3.Experimental group : A single intravenous administration was performed ineach group1) Control : Only DMSO2) Low MMC group : 8.97 * 10 -8 mol MMC3) Low Hp-MMC group : 8.97 * 10 -8 mol Hp-MMC4) MMC group : 8.97 * 10 -7 mol MMC5) Hp-MMC group : 8.97 * 10 -7 mol Hp-MMC4. Results :1) Survival rate : Low MMC group showed best survival rate 90%). However, survival rate of Low Hp-MMC group, MMC group, Hp-MMC group, were 50%, 20%, and 70%, respectively (p<0.001).2) Number of metastatic lung nodule : Low MMC group showed lowest lung nodules (average : 35). However, number of nodules of Low Hp-MMC group, MMC group, Hp-MMC group, were 120,35, and 80, respectively.3) Necrosis ratio of metastatic foci : Low MMC group showed best necrosis ratio (55%). However, necrosis ratio of Low Hp-MMC group, MMC group, Hp-MMC group, were significantly lower, which were 12%, 12%, and 34%, respectively (p<0.001).5.Conclusion : Hematoporphyrin-mitomycin C conjugate showed a lower anti tumor effect than that of mitomucin C.Side effects of hematoporphyrin-mitomycin C conjugate, however, has been more acceptable. Therefore we believe that hematoporphyrin-mitomycin C conjugate should be a novel anti tumor chemotherapy agent, if a better protocol would be established.