Secalonic acid D as a novel DNA topoisomerase I inhibitor from marine lichen-derived fungus Gliocladium sp T31
Secalonic acid D as a novel DNA topoisomerase I inhibitor from marine lichen-derived fungus Gliocladium sp T31
复制标题
DOI：
10.3109/13880209.2010.548817
复制
发表时间：
2011-08-01
影响因子：
3.8
通讯作者：
Hong, Ren
中科院分区：
文献类型：
--
作者：
Hong, Ren
目的：材料与方法：以质粒pBR 322为底物，采用体外超螺旋松弛实验和电泳迁移率改变实验（EMSA），测定SAD对topo Ⅰ的抑制作用。结果：SAD对topo Ⅰ有明显的抑制作用，其最小抑制浓度（MIC）为0.4 μ A μ M，且呈剂量依赖性。与原型DNA拓扑异构酶I毒素喜树碱（CPT）不同，SAD抑制拓扑异构酶I与DNA的结合，但不诱导拓扑异构酶I-DNA共价复合物的形成。
Objective: The inhibitory activity of SAD on topo I was investigated for the first time.Materials and methods: The inhibitory effect of SAD on topo I was determined via in vitro supercoil relaxation assays and electrophoretic mobility shift assay (EMSA) using plasmid substrate, pBR322.Results: SAD displays a considerable inhibition on topo I in a dose-dependent manner with the minimum inhibitory concentration (MIC) of 0.4 mu A mu M. Unlike the prototypic DNA topo I poison camptothecin (CPT), SAD inhibits the binding of topo I to DNA but does not induce the formation of topo I-DNA covalent complexes.Discussion and conclusion: SAD is an excellent topo I inhibitor and thus a significantly potential anticancer candidate.