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[蒽环类抗生素,博来霉素。与DNA形成复合物及抑制核酸生物合成]

[Anthracycline antibiotic, beromycin. The formation of complexes with DNA and the suppresion of nucleic acid biosynthesis].

作者信息

Ostanina L N, Dudnik Iu V, Koz'mian L I

出版信息

Antibiotiki. 1977 Jun;22(6):498-502.

PMID:407838
Abstract

Beromycin, an antitumor anthracycline antibiotic formed in vitro complexes with native and denaturated DNA and ribosomal RNA. Beromycin had a comparatively low constant of DNA binding and to a less extent increased the melting temperature and viscosity of DNA than the other anthracycline antibiotics. A peculiar property of beromycin was very slow binding with DNA, the complex formation was completed in 60 minutes. Beromycin had a selective inhibitory effect on synthesis of nucleic acids in bacterial and tumor cells. Beromycin inhibited synthesis of RNA in the DNA-dependent RNA-polymerase reaction when both the native and denaturated DNA were used as the template. A lower biological activity of beromycin as compared to the other anthracycline antibiotics, such as rubomycin or carminomycin may be explained by lower affinity of this antibiotic to DNA.

摘要

博来霉素是一种抗肿瘤蒽环类抗生素,能在体外与天然和变性的DNA及核糖体RNA形成复合物。博来霉素的DNA结合常数相对较低,与其他蒽环类抗生素相比,其提高DNA解链温度和黏度的程度较小。博来霉素的一个特殊性质是与DNA的结合非常缓慢,复合物形成过程在60分钟内完成。博来霉素对细菌和肿瘤细胞中的核酸合成具有选择性抑制作用。当使用天然和变性的DNA作为模板时,博来霉素在依赖DNA的RNA聚合酶反应中抑制RNA的合成。与其他蒽环类抗生素如柔红霉素或洋红霉素相比,博来霉素的生物活性较低,这可能是由于该抗生素对DNA的亲和力较低所致。

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