丝裂霉素C：烷基化的化学与生物学研究

MITOMYCIN C: CHEMICAL AND BIOLOGICAL STUDIES ON ALKYLATION.

作者信息

SCHWARTZ H S, SODERGREN J E, PHILIPS F S

出版信息

Science. 1963 Nov 29;142(3596):1181-3. doi: 10.1126/science.142.3596.1181.

DOI:10.1126/science.142.3596.1181

Abstract

The presence of an aziridine ring in mitomycin C suggests that the mechanism of action of the antibiotic is like that of the antitumor alkylating agents. However the compound is unexpectedly stable during aerobic incubation with rat liver homogenates although rapidly metabolized anaerobically. Mitomycin is not reactive with gamma-(4-nitrobenzyl) pyridine and reacts only slowly at acid p(H) with thiosulfate. It is proposed that mitomycin is activated in vivo, possibly by a reduction which "unmasks" the potential activity of the fused aziridine ring.

摘要

丝裂霉素C中氮丙啶环的存在表明该抗生素的作用机制与抗肿瘤烷基化剂相似。然而，该化合物在与大鼠肝脏匀浆进行需氧孵育时出人意料地稳定，尽管在厌氧条件下会迅速代谢。丝裂霉素与γ-(4-硝基苄基)吡啶不发生反应，在酸性pH值下与硫代硫酸盐的反应也很缓慢。有人提出丝裂霉素在体内被激活，可能是通过一种还原反应，该反应“揭示”了稠合氮丙啶环的潜在活性。