类黄酮是一组不同的植物来源的次级代谢产物，因其潜在的抗癌特性而受到广泛关注。这篇综述探讨了类黄酮作为 DNA 拓扑异构酶抑制剂的作用，DNA 拓扑异构酶是 DNA 复制、转录和细胞分裂所必需的关键酶。本文全面概述了类黄酮的分类、生物合成及其广泛的自然存在。它进一步深入研究了类黄酮发挥抗癌作用的分子机制，强调了它们与拓扑异构酶的相互作用。该综述对体外和体内研究进行了全面分析，强调了各种黄酮类化合物及其衍生物的拓扑异构酶抑制活性。主要发现表明，类黄酮可以作为催化抑制剂、毒物或 DNA 嵌入剂，影响 I 型和 II 型拓扑异构酶。还检查了黄酮类化合物与其拓扑异构酶抑制效力的结构-活性关系。该综述强调了黄酮类化合物作为开发新型拓扑异构酶抑制剂的有前途的先导化合物的潜力，这可能对癌症治疗产生重要影响。然而，它也承认需要进一步研究，以充分了解细胞环境中类黄酮和拓扑异构酶之间复杂的相互作用。版权所有 © 2024 作者。由爱思唯尔有限公司出版。保留所有权利。

Flavonoids, a diverse group of plant-derived secondary metabolites, have garnered significant attention for their potential anti-cancer properties. This review explores the role of flavonoids as inhibitors of DNA topoisomerases, key enzymes essential for DNA replication, transcription, and cell division. The article offers a comprehensive overview of flavonoid classification, biosynthesis, and their widespread natural occurrence. It further delves into the molecular mechanisms through which flavonoids exert their anti-cancer effects, emphasizing their interactions with topoisomerases. The review provides a thorough analysis of both in vitro and in vivo studies that highlight the topoisomerase inhibitory activities of various flavonoids and their derivatives. Key findings demonstrate that flavonoids can function as catalytic inhibitors, poisons, or DNA intercalators, affecting both type I and type II topoisomerases. The structure-activity relationships of flavonoids concerning their topoisomerase inhibitory potency are also examined. This review underscores the potential of flavonoids as promising lead compounds for the development of novel topoisomerase inhibitors, which could have important implications for cancer therapy. However, it also acknowledges the need for further research to fully understand the intricate interactions between flavonoids and topoisomerases within the cellular environment.Copyright © 2024 The Authors. Published by Elsevier Ltd.. All rights reserved.