Cobalt Chelate of Bleomycin. I. Physicochemical Properties and Distribution in Tumor Bearing Mice

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Cobalt chelate of bleomycin (Co-BLM) was inert to ligand exchange reaction and showed absorption at 450 nm and 580 nm, which indicated cobalt is trivalent. Co-BLM was accumulated in tumor tissue much more than BLM and other BLM metal chelates. In urine of ^<67>Ga-BLM or ^<111>In-BLM injected mice, most of radioactivity was not bound to BLM. On the other hand, all the radioactivity was attributable to BLM bound ^<57>Co in urine of ^<57>Co-BLM injected mice. In tumor tissue homogenate, most of Co-BLM was present in cell nuclei, while BLM, CoCl_2 and other BLM metal chelates distributed mainly in supernatant fractions. Co-BLM may bind to deoxyribonucleic acid (DNA) in tumor cell. From these results, we conclude Co-BLM to be superior as a tumor scanning agent than BLM and other BLM metal chelates.
公益社団法人日本薬学会の論文
1977-07-25