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- W2077676823 abstract "DNA topoisomerase I (topo I) is an essential enzyme which regulates the conformational changes in DNA topology by cleaving and rejoining DNA strands during normal cell growth. The inhibitors of topo I represent a major class of anticancer drugs. In our projects to isolate new anticancer agents from marine-derived fungi, secalonic acid D (SAD) with inhibitory activity on topo I was isolated from the fermentation broth of marine lichen-derived fungus Gliocladium sp. T31, which was collected from marine sediments in South Pole.The inhibitory activity of SAD on topo I was investigated for the first time.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.SAD displays a considerable inhibition on topo I in a dose-dependent manner with the minimum inhibitory concentration (MIC) of 0.4 µM. 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.SAD is an excellent topo I inhibitor and thus a significantly potential anticancer candidate." @default.
- W2077676823 created "2016-06-24" @default.
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- W2077676823 date "2011-04-15" @default.
- W2077676823 modified "2023-10-10" @default.
- W2077676823 title "Secalonic acid D as a novel DNA topoisomerase I inhibitor from marine lichen-derived fungus<i>Gliocladium</i>sp. T31" @default.
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- W2077676823 doi "https://doi.org/10.3109/13880209.2010.548817" @default.
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