Lu Na, Gao Ying, Ling Yun, Chen Yan, Yang Yong, Gu Hong-Yan, Qi Qi, Liu Wei, Wang Xiao-Tang, You Qi-Dong, Guo Qing-Long
Jiangsu Key Laboratory of Carcinogenesis and Intervention (China Pharmaceutical University), Nanjing 210009, People's Republic of China.
Life Sci. 2008 Apr 23;82(17-18):956-63. doi: 10.1016/j.lfs.2008.02.013. Epub 2008 Mar 4.
Previous studies revealed that wogonin, a naturally occurring monoflavonoid extracted from Scutellariae radix, possessed anticancer activity both in vitro and in vivo. However, the molecular mechanism of its potent anticancer activity remains poorly understood and warrants further investigations. In this study, we found for the first time that wogonin inhibited the growth and tumor angiogenesis of human gastric carcinoma in nude mice. We explored the inhibitory effect of wogonin on angiogenesis stimulated by vascular endothelial growth factor (VEGF) in vitro. Wogonin suppressed the VEGF-stimulated migration and tube formation of human umbilical vein endothelial cells (HUVECs). It also restrained VEGF-induced tyrosine phosphorylation of vascular endothelial growth factor receptor 2 (VEGFR2). This inhibition of receptor phosphorylation was correlated with a significant decrease in VEGF-triggered phosphorylated forms of ERK, AKT and p38. Taken together, these findings strongly suggest that wogonin might be a promising antitumor drug.
先前的研究表明，汉黄芩素是一种从黄芩中提取的天然单黄酮类化合物，在体外和体内均具有抗癌活性。然而，其强大抗癌活性的分子机制仍知之甚少，值得进一步研究。在本研究中，我们首次发现汉黄芩素可抑制裸鼠体内人胃癌的生长和肿瘤血管生成。我们在体外探究了汉黄芩素对血管内皮生长因子（VEGF）刺激的血管生成的抑制作用。汉黄芩素抑制了VEGF刺激的人脐静脉内皮细胞（HUVECs）的迁移和管腔形成。它还抑制了VEGF诱导的血管内皮生长因子受体2（VEGFR2）的酪氨酸磷酸化。这种对受体磷酸化的抑制与VEGF触发的ERK、AKT和p38磷酸化形式的显著减少相关。综上所述，这些发现强烈表明汉黄芩素可能是一种有前景的抗肿瘤药物。
