Mikami Y, Yokoyama K, Tabeta H, Nakagaki K, Arai T
J Pharmacobiodyn. 1981 Apr;4(4):282-6. doi: 10.1248/bpb1978.4.282.
Saframycin S, structurally the decyano-saframycin A and biosynthetically the precursor of saframycin A, is a new antibiotic and is assumed to be the active principle for the formation of the antibiotic-DNA complex to manifest its activity. In the present study on the biological activity of saframycin S, the antibiotic showed a marked activity against Ehrlich ascites tumor with the doses of 0.5 to 0.75 mg/kg/day for 10 days, and the rate of 40-day survivors was 80 to 90%. However, this antibiotic was less effective against P388 leukemia than saframycin A at the doses tested. Saframycin S also showed the highest antimicrobial activity, in particular against gram-positive bacteria, among the saframycin group antibiotics identified to date. the LD50 of saframycin S was 3.2 mg/kg (i.p.) for ddY mice. The biological activity and toxicity of saframycin S in relation to its structure were described.
沙弗霉素S在结构上是脱氰基沙弗霉素A，在生物合成上是沙弗霉素A的前体，它是一种新型抗生素，被认为是形成抗生素 - DNA复合物以发挥其活性的活性成分。在目前关于沙弗霉素S生物活性的研究中，该抗生素以0.5至0.75毫克/千克/天的剂量给药10天，对艾氏腹水瘤显示出显著活性，40天存活者的比例为80%至90%。然而，在测试剂量下，这种抗生素对P388白血病的疗效不如沙弗霉素A。在迄今为止鉴定的沙弗霉素类抗生素中，沙弗霉素S还表现出最高的抗菌活性，尤其是对革兰氏阳性菌。沙弗霉素S对ddY小鼠的腹腔注射半数致死量为3.2毫克/千克。描述了沙弗霉素S的生物活性和毒性与其结构的关系。
