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蒽环类抗生素的抗癌活性与DNA凝聚作用

Anti-cancer activity of anthracycline antibiotics and DNA condensation.

作者信息

Cera C, Palumbo M

机构信息

Department of Organic Chemistry, University of Padova, Italy.

出版信息

Anticancer Drug Des. 1990 Aug;5(3):265-71.

PMID:2400539
Abstract

Light scattering techniques were used to investigate the ability of a number of anthracyclines to cause compaction in double-stranded DNA and nucleosomes at physiological ionic strength. The structurally organized polynucleotide was efficiently condensed by all of the drugs examined, while no appreciable aggregation of free double-stranded DNA is observed under the same experimental conditions. A model for the process is proposed. Our results suggest the lack of a direct relationship between the critical concentration of free drug at which condensation of DNA occurs and the cytotoxic and anti-cancer properties exhibited by the various anthracycline derivatives.

摘要

利用光散射技术研究了多种蒽环类药物在生理离子强度下使双链DNA和核小体压缩的能力。所有检测的药物均能有效地使结构有序的多核苷酸凝聚,而在相同实验条件下未观察到游离双链DNA有明显聚集。提出了该过程的一个模型。我们的结果表明,DNA发生凝聚时游离药物的临界浓度与各种蒽环类衍生物表现出的细胞毒性和抗癌特性之间缺乏直接关系。

相似文献

1
Anti-cancer activity of anthracycline antibiotics and DNA condensation.蒽环类抗生素的抗癌活性与DNA凝聚作用
Anticancer Drug Des. 1990 Aug;5(3):265-71.
2
[Structure and activity of anthracyclines].
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Single-strand DNA breaks induced by chromophore-modified anthracyclines in P388 leukemia cells.发色团修饰的蒽环类药物在P388白血病细胞中诱导产生的单链DNA断裂
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Effect of verapamil and other agents on the distribution of anthracyclines and on reversal of drug resistance.维拉帕米及其他药物对蒽环类药物分布和耐药逆转的影响。
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