核酸関連化合物の抗腫瘍性の研究 (I)

6-Mercaptopurine-riboside (Thio-inosine) のRauscher Leukemia virus及びLeukemia 1210細胞に対する抑制効果

抄録

The inhibitory activity of 6-mercaptopurine and 6-mercaptopurine riboside against Rauscher Leukemia Virus and Leukemia 1210 cells was studied. LD₅₀ of 6-mercaptopurine riboside was 2.5g/kg in mice by intraperitoneal injection and that of 6-mercaptopurine was 380 mg/kg.
6-Mercaptopurine and 6-mercaptopurine-riboside were effective against Rauscher Leukemia Virus. The therapeutic index of 6-mercaptopurine-riboside was 8.3 and that of 6-mercaptopurine was 3. 8. These drugs were effective against Leukemia L-1210 cells too, and the therapeutic index of 6-mercaptopurine-riboside was 135, and that of 6-mercaptopurine was 51. From these results, it may be said that 6-mercaptopurine riboside was effective twice than 6-mercaptopurine.
The development of the resistance of L-1210 cells to 6-mercaptopurine riboside was slower and a little weaker than that of 6-mercaptopurine resistance.
The clear cross-resistance between 6-mercaptopurine resistant cells and 6-mercaptopurine-riboside resistant ones, was observed.