Key Laboratory of Natural Medicinal Chemistry and Resources Evaluation of Hubei Province, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Cancer Lett. 2012 Nov 28;324(2):210-20. doi: 10.1016/j.canlet.2012.05.025. Epub 2012 May 28.
RY10-4, a novel protoapigenone analog, shows potent cytotoxicity against a broad spectrum of human cancer cells. Here we investigate its anti-tumor activity on breast cancer. The results indicated that RY10-4 suppressed proliferation, arrested cell cycle, induced apoptosis and inhibited invasion in MDA-MB-231, MCF-7 and SKBR3 breast cancer cells. Western blot analysis showed that RY10-4 down-regulated the PI3K/Akt signaling pathway and inhibited doxorubicin-induced p-Akt. Moreover, it effectively suppressed tumor growth in mice without major side effects. Therefore, RY10-4 had potential anti-tumor activity, and could be used as a lead to design more potent derivatives.
RY10-4 是一种新型原拟南芥素类似物，对多种人类癌细胞具有强大的细胞毒性。在这里，我们研究了它在乳腺癌中的抗肿瘤活性。结果表明，RY10-4 抑制了 MDA-MB-231、MCF-7 和 SKBR3 乳腺癌细胞的增殖，使细胞周期停滞，诱导细胞凋亡，并抑制细胞侵袭。Western blot 分析表明，RY10-4 下调了 PI3K/Akt 信号通路，并抑制了阿霉素诱导的 p-Akt。此外，它在没有明显副作用的情况下有效抑制了小鼠的肿瘤生长。因此，RY10-4 具有潜在的抗肿瘤活性，可以作为设计更有效的衍生物的先导化合物。
