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博来霉素的化学性质及作用机制

Chemistry and mechanism of action of bleomycin.

作者信息

Mazzei T

出版信息

Chemioterapia. 1984 Oct;3(5):316-9.

PMID:6085286
Abstract

Bleomycin (BLM) is an antitumoral antibiotic active against various animal and human tumors. BLM causes a lot of biological effects characteristic of drugs which attack the DNA in cells. The nature of DNA damage consists of the release of bases and single and double-strand breaks. The Fe (II) is a necessary cofactor in the reaction of BLM with DNA. BLM is effective principally against non-dividing cells and against cells in mitotic phase, G2 and S. The various contents of BLM inactivating enzymes in tissues can explain the particular toxicity and therapeutic activity of this drug.

摘要

博来霉素(BLM)是一种对多种动物和人类肿瘤有效的抗肿瘤抗生素。博来霉素会引发许多攻击细胞中DNA的药物所特有的生物学效应。DNA损伤的本质包括碱基释放以及单链和双链断裂。亚铁离子(Fe (II))是博来霉素与DNA反应中必需的辅助因子。博来霉素主要对非分裂细胞以及处于有丝分裂期、G2期和S期的细胞有效。组织中博来霉素失活酶的不同含量可以解释该药物特殊的毒性和治疗活性。

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