Ren Qing, Chen Guoming, Wan Qi, Xiao Liangman, Zhang Zhitong, Feng Yibin
School of Chinese Medicine, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong SAR 999077, China.
Jiangxi University of Chinese Medicine, Nanchang 330006, China.
Bioorg Chem. 2024 Dec;153:107860. doi: 10.1016/j.bioorg.2024.107860. Epub 2024 Oct 15.
Topoisomerase is a ubiquitous enzyme in the control of DNA chain topology. There have been extensive research on topoisomerase inhibitors derived from natural sources, which act as partial inducers of tumor cell apoptosis. However, their specific efficacy in treating hepatocellular carcinoma is relatively unexplored. Hence, this comprehensive review focuses on the structural characteristics and anti-cancer properties of topoisomerase inhibitors in hepatocellular carcinoma. Furthermore, this review is also elucidating the mechanism of action, structure-activity relationships, therapeutic limitations, stage of clinical trials of described classes of natural bioactive compounds as well as their potential application in cancer chemotherapies. This broad understanding of topoisomerase medical biology will provide indispensable framework for enhancing the efficiency of rational anti-hepatocellular carcinoma drug discovery.
拓扑异构酶是一种在控制DNA链拓扑结构方面普遍存在的酶。人们对源自天然来源的拓扑异构酶抑制剂进行了广泛研究,这些抑制剂可作为肿瘤细胞凋亡的部分诱导剂。然而,它们在治疗肝细胞癌方面的具体疗效相对未被探索。因此,本综述聚焦于肝细胞癌中拓扑异构酶抑制剂的结构特征和抗癌特性。此外,本综述还阐述了所述各类天然生物活性化合物的作用机制、构效关系、治疗局限性、临床试验阶段以及它们在癌症化疗中的潜在应用。对拓扑异构酶医学生物学的这种广泛理解将为提高合理的抗肝细胞癌药物发现效率提供不可或缺的框架。