Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, PR China.
Eur J Med Chem. 2012 Oct;56:320-31. doi: 10.1016/j.ejmech.2012.07.051. Epub 2012 Aug 9.
Twenty-six emodin derivatives (17 novel) which attach quaternary ammonium salt were synthesized and evaluated for their anticancer activities in vitro and in vivo. Compounds 11g + 12g and 11h + 12h had more significant antiproliferative ability against three cancer cell lines and low cytotoxicity to HELF. 11g + 12g and 11h + 12h induced AGS cell apoptosis and arrested cell cycle at the G(0)/G(1) phase in a dose-dependent manner. Furthermore, the activities of the caspase-3, -9 enzymes were increased in the treated cells. In vivo studies revealed that compounds 11g + 12g and 11h + 12h showed significant anti-tumor activity compared with controlled group.
合成了 26 个大黄素衍生物（17 个新化合物），并对其进行了体外和体内的抗癌活性评价。化合物 11g+12g 和 11h+12h 对三种癌细胞系具有更显著的增殖抑制能力，对 HELF 的细胞毒性较低。11g+12g 和 11h+12h 以剂量依赖性方式诱导 AGS 细胞凋亡并将细胞周期阻滞在 G0/G1 期。此外，处理细胞中的 caspase-3、-9 酶的活性增加。体内研究表明，与对照组相比，化合物 11g+12g 和 11h+12h 表现出显著的抗肿瘤活性。
