SOME CHEMOTHERAPEUTIC PROPERTIES OF 2 NEW ANTI-TUMOR ANTIBIOTICS, SAFRAMYCIN-A AND SAFRAMYCIN-C

  • 1 January 1980
    • journal article
    • research article
    • Vol. 71  (6) , 790-796
Abstract
The antitumor activity of saframycin was examined against 4 different experimental tumor systems in mice. Saframycins A and C inhibited the growth of [mouse leukemia] L1210 cells in suspension culture completely at concentrations of 0.02 .mu.g/ml and 1.0 .mu.g/ml, respectively. The LD50 of saframycin A for ddY mice were 4.9 mg/kg (i.p.) and 3.3 mg/kg (i.v.), respectively. In C3H/He mice, the LD50 were 10.5 mg/kg (i.p.) and 9.7 mg/kg (i.v.), respectively. Saframycin A was highly active against [mouse] Ehrlich ascites carcinoma and [mouse] P388 leukemia cells, and moderately active against L1210 leukemia and [mouse] B16 melanoma cells. The antitumor activity of saframycin A was 50-100 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. 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 i.p. into mice, the blood concentration of saframycin A was 4.6 .mu.g/ml after 30 min, and 2.8 .mu.g/ml after 1 h; the total recovery within 3 h from the urine was 30%. Saframycin A was distributed widely, though to different extents, in various organs when injected i.p. into mice.