State Key Laboratory of Bioreactor Engineering & Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, #268, 130 Meilong Road, Shanghai 200237, China.
Leuk Res. 2011 May;35(5):646-56. doi: 10.1016/j.leukres.2011.01.029. Epub 2011 Feb 18.
Previous studies have shown that 7-b (6-(dodecylamino)-2-(3-(4-methylpiperazin-1-yl)propyl)-1H-benzo-[de]isoquinoline-1,3(2H)-dione), a novel amonafide-based DNA intercalator, was generated as a new anticancer candidate. However, the effects induced by 7-b and the molecular mechanisms involved remain poorly understood in Burkitt's lymphoma. To shed light on these issues, we have investigated the effects of 7-b on proliferation, cell cycle progression, apoptosis activity and oxidative stress levels of lymphoma Raji cells in vitro. Our results showed that 7-b inhibited the proliferation of Raji cells and induced G1 cell cycle arrest in a dose-dependent manner. Moreover, 7-b treatment triggered programmed cell death, production of reactive oxygen species (ROS) and alteration of the mitochondrial membrane potential (Δψm). Altogether our results showed that 7-b mediated its growth inhibitory effects on Raji cells via the activation of a ROS-mediated mitochondrial pathway and cell cycle checkpoint signaling pathway which subsequently targeted p21.
先前的研究表明,7-b(6-(十二烷基氨基)-2-(3-(4-甲基哌嗪-1-基)丙基)-1H-苯并-[de]异喹啉-1,3(2H)-二酮),一种新型的基于阿莫萘非的 DNA 嵌入剂,被开发为一种新的抗癌候选药物。然而,7-b 诱导的作用及其涉及的分子机制在伯基特淋巴瘤中仍知之甚少。为了阐明这些问题,我们研究了 7-b 对体外淋巴瘤 Raji 细胞增殖、细胞周期进程、细胞凋亡活性和氧化应激水平的影响。我们的结果表明,7-b 抑制 Raji 细胞的增殖,并以剂量依赖的方式诱导 G1 细胞周期停滞。此外,7-b 处理触发程序性细胞死亡、活性氧(ROS)的产生和线粒体膜电位(Δψm)的改变。总之,我们的结果表明,7-b 通过激活 ROS 介导的线粒体途径和细胞周期检查点信号通路,从而靶向 p21,对 Raji 细胞发挥其生长抑制作用。