Wei Jianghua, Zhu Yin, Xu Gang, Yang Fan, Guan Zhe, Wang Mao, Fang Yonghong
Orthopedic Department, Shanxi Tumor Hospital, Workers 3rd Street, Taiyuan, 030013, Shanxi Provence, People's Republic of China.
Cell Biochem Biophys. 2014 Nov;70(2):1439-44. doi: 10.1007/s12013-014-0078-2.
Oxymatrine, one of the most active components of the ethanol extracts from Sophora flavescens, is known for its potent antitumor activity both in vitro and in vivo. However, the mechanism of its action in mediating the cell apoptosis remains elusive. In this study, we investigated the proliferation inhibitory and apoptotic activities of oxymatrine against human osteosarcoma MG-63 cells. The compound was found to markedly and dose-dependently inhibit the cell proliferation determined by 5-bromo-2-deoxyuridine incorporation. Oxymatrine also induced the cell apoptosis in a dose- and time-dependent manner as showed by the annexin V-FITC/PI double staining and TUNEL assay. Furthermore, a disruption of mitochondrial membrane potential and an up-regulation of cleaved caspases-3, and-9 and downregulation of Bax/Bcl-2 was evidenced in the oxymatrine-treated cells. These proteins have been known to play a pivotal role in the regulation of apoptosis. In conclusion, these observations indicate of the oxymatrine potential as an effective antitumor agent against osteosarcoma. Moreover, the compound appears to exert its anti-tumor action by stimulating the caspase-triggered signaling pathway.
氧化苦参碱是苦参乙醇提取物中最具活性的成分之一，以其在体外和体内的强大抗肿瘤活性而闻名。然而，其介导细胞凋亡的作用机制仍不清楚。在本研究中，我们研究了氧化苦参碱对人骨肉瘤MG-63细胞的增殖抑制和凋亡活性。发现该化合物通过5-溴-2-脱氧尿苷掺入法显著且剂量依赖性地抑制细胞增殖。如膜联蛋白V-FITC/PI双染和TUNEL检测所示，氧化苦参碱还以剂量和时间依赖性方式诱导细胞凋亡。此外，在氧化苦参碱处理的细胞中，线粒体膜电位破坏，裂解的半胱天冬酶-3、-9上调，Bax/Bcl-2下调。已知这些蛋白质在细胞凋亡调节中起关键作用。总之，这些观察结果表明氧化苦参碱作为一种有效的骨肉瘤抗肿瘤药物具有潜力。此外，该化合物似乎通过刺激半胱天冬酶触发的信号通路发挥其抗肿瘤作用。
