拓扑异构酶（topoisomerase，topo）是解决DNA复制、转录等过程中出现拓扑问题的关键酶，是抗肿瘤药物作用的重要靶点之一。天然产物是topo抑制剂的重要来源，从天然产物中发现开发topo抑制剂是抗肿瘤药物研究的热点。以天然产物结构类型，分类综述了天然存在的具有topo抑制活性的天然产物及以它们为基础改造获得的衍生物，以期为抗肿瘤天然topo抑制剂的研发提供参考。

Topoisomerase (topo) plays the vital role in solving all of the topological problems of DNA in replication, transcription and other cellular transactions, which is one of the important targets of antitumor drugs. Natural products are an important source of development of topo inhibitors. Exploring topo inhibitors from natural products is one of the hot spots in the development of antitumor drugs. In this paper, the natural topo inhibitors and many derivatives based on natural products are reviewed, in order to provide reference for the development of antineoplastic topo inhibitors.

R282.71

安徽省教育厅自然科学研究重点项目（KJ2019A0873）