Department of Chemistry and Institute for Nano-Chemistry, Jinan University, Guangzhou 510632, China.
Bioorg Med Chem Lett. 2012 Feb 1;22(3):1459-63. doi: 10.1016/j.bmcl.2011.11.095. Epub 2011 Nov 30.
Cinobufacini is a traditional Chinese anti-tumor drug and widely used in clinic experiences. But little is known about its effect on the cells. In this study, the effects of cinobufacini on breast cancer MDA-MB-231 cell were evaluated by CCK-8 assay, and the data showed cinobufacini could inhibit the MDA-MB-231 cells growth effectively in dose-dependent and time-dependent manners. Cell apoptosis and cell cycle were detected by flow cytometry analysis. After the cells being treated with 50 μg/mL cinobufacini for 48 h, the early apoptosis percentage (20.45 ± 1.46%) is much higher than the normal group (7.73 ± 1.21%). The cell cycle data indicated that cinobufacini caused a cell cycle arrest at S phase. What's more, cinobufacini can affect the disruption of cytoskeleton, and these alterations changed the cell-surface ultrastructure and the cell morphology which were detected by atomic force microscopy (AFM) at nanoscale level. It indicated that the cell membrane structure and cytoskeleton networks were destroyed and the cell tails were narrowed after the cell being treated with cinobufacini. The present study is to provide valuable new insights to understand the mechanism of the drug in anti-tumor process. Furthermore, the knowledge concerning the signaling of cell cycle is potentially important to clinical utility.
华蟾素是一种传统的抗肿瘤中药,在临床应用中广泛使用。然而,其对细胞的作用机制却知之甚少。本研究采用 CCK-8 法评价华蟾素对乳腺癌 MDA-MB-231 细胞的作用,结果表明华蟾素能有效抑制 MDA-MB-231 细胞的生长,且呈剂量和时间依赖性。通过流式细胞术检测细胞凋亡和细胞周期。用 50μg/ml 华蟾素处理细胞 48h 后,早期凋亡率(20.45±1.46%)明显高于对照组(7.73±1.21%)。细胞周期数据表明,华蟾素导致 S 期细胞周期阻滞。此外,华蟾素能影响细胞骨架的破坏,这些变化通过原子力显微镜(AFM)在纳米尺度上检测到改变了细胞表面超微结构和细胞形态。结果表明,用华蟾素处理后,细胞膜结构和细胞骨架网络被破坏,细胞尾部变窄。本研究为深入了解该药物在抗肿瘤过程中的作用机制提供了有价值的新见解。此外,细胞周期信号通路的相关知识可能对临床应用具有重要意义。