Zhang Yiyin, Li Zhengchun, Zhao Lili, Yang Yongming, Wang Jing, Yan Lei, Huang Ziyang, Yang Xihua, Chen Lixia
Laboratory Animal Center, Shanxi Province Cancer Hospital/Shanxi Hospital Affiliated to Cancer Hospital, Chinese Academy of Medical Sciences/Cancer Hospital Affiliated to Shanxi Medical University, Taiyuan, 030013, Shanxi, China.
School of Basic Medical Sciences, Shanxi Medical University, Taiyuan, 030013, Shanxi, China.
Naunyn Schmiedebergs Arch Pharmacol. 2025 Apr 14. doi: 10.1007/s00210-025-04097-9.
This study aims to investigate the therapeutic effects of brazilin in the treatment of bladder cancer through the inhibition of DNA topoisomerase I (Topo 1) and to explore its underlying mechanisms. In vitro experiments were conducted using bladder cancer T24 cell line and in vivo experiments were performed using a bladder cancer mouse model. The effects of brazilin on cell proliferation, apoptosis, and DNA damage were evaluated. RT-qPCR and Western Blot analyses were used to assess the expression of Topo 1 mRNA and protein after treatment with brazilin. Additionally, tumor growth inhibition and potential side effects were evaluated in the animal model. Brazilin significantly inhibited bladder cancer cell proliferation and induced apoptosis and DNA damage in vitro. The expression of Topo 1 was downregulated at both the mRNA and protein levels, suggesting that brazilin exerts its effects by inhibiting Topo 1 activity. In vivo, brazilin markedly suppressed tumor growth in the bladder cancer mouse model, with no significant toxic effects observed. Brazilin shows potential as a therapeutic agent for bladder cancer by inhibiting Topo 1 activity, leading to suppressed tumor growth and cellular damage. This study provides experimental evidence supporting the potential use of brazilin as a novel anticancer drug for bladder cancer treatment.
本研究旨在通过抑制DNA拓扑异构酶I（Topo 1）来探讨巴西苏木素对膀胱癌的治疗作用，并探索其潜在机制。使用膀胱癌T24细胞系进行体外实验，并使用膀胱癌小鼠模型进行体内实验。评估了巴西苏木素对细胞增殖、凋亡和DNA损伤的影响。采用RT-qPCR和蛋白质免疫印迹分析评估巴西苏木素处理后Topo 1 mRNA和蛋白质的表达。此外，在动物模型中评估了肿瘤生长抑制和潜在的副作用。巴西苏木素在体外显著抑制膀胱癌细胞增殖并诱导凋亡和DNA损伤。Topo 1的表达在mRNA和蛋白质水平均下调，表明巴西苏木素通过抑制Topo 1活性发挥其作用。在体内，巴西苏木素显著抑制膀胱癌小鼠模型中的肿瘤生长，未观察到明显的毒性作用。巴西苏木素通过抑制Topo 1活性显示出作为膀胱癌治疗药物的潜力，导致肿瘤生长受抑制和细胞损伤。本研究提供了实验证据，支持巴西苏木素作为一种新型抗癌药物用于膀胱癌治疗的潜在用途。
