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[椭圆玫瑰树碱衍生物对拓扑异构酶催化反应的抑制作用:对拓扑异构酶II的优先抑制]

[Inhibition by ellipticine derivatives of the reactions catalysed by the topoisomerases: preferential inhibition of topoisomerase II].

作者信息

Douc-Rasy S, Multon E, Kayser A, Riou G

出版信息

C R Seances Acad Sci III. 1983;296(19):899-904.

PMID:6311366
Abstract

We have studied inhibitory effects of ellipticine derivatives on the topoisomerisation reactions by Rat liver enzymes. We used the reactions of relaxation of supercoiled DNA, catalysed by topoisomerase I without ATP and by topoisomerase II with ATP, and also the reaction of decatenation of DNA networks by topoisomerase II. When studying intercalating agents--as elliptieine derivatives are--a problem arose. To distinguish relaxed DNA from native DNA we run our samples in electrophoretic gels containing an intercalating agent: chloroquine. Topoisomerase II, which was inhibited at concentrations about 10(-6) M, was more sensitive than topoisomerase I.

摘要

我们研究了玫瑰树碱衍生物对大鼠肝脏酶催化的拓扑异构化反应的抑制作用。我们利用了由无ATP的拓扑异构酶I和有ATP的拓扑异构酶II催化的超螺旋DNA松弛反应,以及拓扑异构酶II催化的DNA网络解连环反应。在研究作为嵌入剂的玫瑰树碱衍生物时出现了一个问题。为了区分松弛的DNA和天然DNA,我们在含有嵌入剂氯喹的电泳凝胶中对样品进行电泳。拓扑异构酶II在浓度约为10^(-6) M时受到抑制,比拓扑异构酶I更敏感。

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