Arai T, Takahashi K, Ishiguro K, Mikami Y
Gan. 1980 Dec;71(6):790-6.
The antitumor activity of saframycin was examined against four different experimental tumor systems in mice. Saframycin A and C inhibited the growth of L1210 cells in suspension culture completely at concentrations of 0.02 microgram/ml and 1.0 microgram/ml, respectively. The LD50's of saframycin A for ddY mice were 4.9 mg/kg (ip) and 3.3 mg/kg (iv), respectively. In C3H/He mice, the LD50's were 10.5 mg/kg (ip) and 9.7 mg/kg (iv), respectively. Saframycin A was highly active against Ehrlich ascites carcinoma and P388 leukemia, and moderately active against L1210 leukemia and B16 melanoma. The antitumor activity of saframycin A was 50 to 100 times greater than that of saframycin C. The survivors cured of Ehrlich ascites carcinoma by treatment with saframycin A developed a resistance to rechallenge with the same tumor. On the other hand, when carbazilquinone and adriamycin were used as reference drugs, the cured mice in these cases did not resist rechallenge with the same tumor. When saframycin A (5 mg/kg) was administered intraperitoneally into mice, the blood concentration of saframycin A was 4.6 microgram/ml after 30 min, and 2.8 microgram/ml after 1 hr, and the total recovery within 3 hr from the urine was 30%. Saframycin A was found to be distributed widely, though to different extents, in various organs when injected intraperitoneally into mice.
研究了沙弗霉素对小鼠四种不同实验性肿瘤系统的抗肿瘤活性。沙弗霉素A和C分别在浓度为0.02微克/毫升和1.0微克/毫升时，完全抑制悬浮培养的L1210细胞生长。沙弗霉素A对ddY小鼠的半数致死量（LD50）腹腔注射为4.9毫克/千克，静脉注射为3.3毫克/千克。在C3H/He小鼠中，LD50腹腔注射为10.5毫克/千克，静脉注射为9.7毫克/千克。沙弗霉素A对艾氏腹水癌和P388白血病高度活跃，对L1210白血病和B16黑色素瘤中度活跃。沙弗霉素A的抗肿瘤活性比沙弗霉素C大50至100倍。用沙弗霉素A治疗治愈的艾氏腹水癌存活小鼠对同一肿瘤的再次攻击产生了抗性。另一方面，当卡巴醌和阿霉素用作参考药物时，这些病例中治愈的小鼠对同一肿瘤的再次攻击没有抗性。当将沙弗霉素A（5毫克/千克）腹腔注射到小鼠体内时，30分钟后沙弗霉素A的血药浓度为4.6微克/毫升，1小时后为2.8微克/毫升，3小时内从尿液中的总回收率为30%。当腹腔注射到小鼠体内时，发现沙弗霉素A在各种器官中广泛分布，尽管程度不同。
