Department of Pharmacology, University of Minnesota Medical School, Minneapolis, MN 55455, USA.
J Nat Prod. 2012 Aug 24;75(8):1485-9. doi: 10.1021/np300299y. Epub 2012 Aug 6.
Simocyclinone D8 is an antibiotic isolated from Streptomyces antibioticus Tü 6040 that inhibits the supercoiling activity of DNA gyrase. It also exhibits an inhibitory effect on human topoisomerase II and an antiproliferative activity against some cancer cell lines. Our biochemical studies have revealed that simocyclinone D8 can inhibit the catalytic activity of human topoisomerase I. Thus, simocyclinone D8 is a dual catalytic inhibitor of human topoisomerases I and II.
西罗莫司酮 D8 是从链霉菌属抗生素 Tü 6040 中分离得到的一种抗生素，它能抑制 DNA 拓扑异构酶的超螺旋活性。它还对人拓扑异构酶 II 具有抑制作用，并对一些癌细胞系具有抗增殖活性。我们的生化研究表明，西罗莫司酮 D8 可以抑制人拓扑异构酶 I 的催化活性。因此，西罗莫司酮 D8 是人拓扑异构酶 I 和 II 的双重催化抑制剂。
