关于某些抗癌药物作用模式中的还原激活机制。

On the mechanism of reductive activation in the mode of action of some anticancer drugs.

作者信息

Favaudon V

出版信息

Biochimie. 1982 Jul;64(7):457-75. doi: 10.1016/s0300-9084(82)80162-4.

Abstract

Bioactivation of a number of DNA-specific antitumor drugs depends on oxidoreduction. Bleomycin, neocarzinostatin and anthracycline glycosides are the best known among such drugs in terms of reductive activation processes. Their reduction results in short-lived radical or electrophilic intermediates attacking DNA stereospecifically. The physico-chemical properties of these drugs and the nature of DNA damage are reviewed. Models for DNA-intercalation, electron-donor systems involved in drug metabolisation, and the role of oxygen in radical reactions, are discussed in the light of recent reports.

摘要

多种DNA特异性抗肿瘤药物的生物活化依赖于氧化还原作用。就还原活化过程而言，博来霉素、新制癌菌素和蒽环糖苷是这类药物中最广为人知的。它们的还原会产生寿命短暂的自由基或亲电中间体，这些中间体对DNA进行立体特异性攻击。本文综述了这些药物的物理化学性质以及DNA损伤的性质。根据最近的报道，讨论了DNA嵌入模型、药物代谢中涉及的电子供体系统以及氧在自由基反应中的作用。