School of Pharmacy, South-Central University for Nationalities, Wuhan 430074, PR China.
Food Chem Toxicol. 2012 Sep;50(9):3166-73. doi: 10.1016/j.fct.2012.05.039. Epub 2012 Jun 8.
The fruit of Docynia delavayi (Franch.) Schneid is a kind of popular food in southwestern areas of China. Additionally, its rhizome has been long used as a folk medicine in the treatment of liver cancer by local people. Chrysin is a kind of flavonoid which induces cancer cell death in vitro. However, its anti-tumor activity in vivo and toxicological effects on the tumor-bearing animals still remain poorly understood. In this study, we obtained four flavonoids from this herb. Among them, chrysin showed the strongest cytotoxic effect on an array of cultured tumor cells. Further investigations revealed that it significantly repressed transplanted H22 ascitic hepatic tumor cell growth in vivo. Moreover, this compound displayed little toxic effects. Additionally, we demonstrated that in transplanted tumor tissues, chrysin not only activated caspase-3 and induced apoptosis, but also inhibited the production of vascular endothelial growth factor (VEGF) and suppressed angiogenesis. These data showed that chrysin exhibited prominent anti-tumor activities and low toxic effects in vivo.
滇刺枣的果实是中国西南地区的一种受欢迎的食物。此外,其根茎长期以来一直被当地人用作治疗肝癌的民间药物。白杨素是一种黄酮类化合物,能诱导体外癌细胞死亡。然而,其在体内的抗肿瘤活性及其对荷瘤动物的毒理学作用仍知之甚少。在本研究中,我们从这种植物中获得了四种黄酮类化合物。其中,白杨素对一系列培养的肿瘤细胞表现出最强的细胞毒性作用。进一步的研究表明,它能显著抑制体内移植的 H22 腹水肝癌细胞的生长。此外,该化合物表现出较小的毒性作用。此外,我们证明在移植的肿瘤组织中,白杨素不仅激活了 caspase-3 并诱导了细胞凋亡,而且还抑制了血管内皮生长因子(VEGF)的产生并抑制了血管生成。这些数据表明,白杨素在体内表现出显著的抗肿瘤活性和低毒性作用。