Chemical modification and anticancer effect of prenylated flavanones from Taiwanese propolis
Chemical modification and anticancer effect of prenylated flavanones from Taiwanese propolis
复制标题
DOI：
10.1080/14786419.2010.535146
复制
发表时间：
2012-01-01
影响因子：
2.2
通讯作者：
Huang, Wei-Jan
中科院分区：
文献类型：
--
作者：
Chen, Chia-Nan;Hsiao, Che-Jen;Huang, Wei-Jan
我们先前的研究表明，从台湾蜂胶中分离出的8个烯丙基黄酮（1-8）具有广谱的生物活性。其中，台湾蜂胶中丰富的若虫酚A(3)、若虫酚B(4)和若虫酚C(7)表现出对癌细胞的细胞毒性。因此，通过半合成策略来改善它们的活动似乎很有趣。在本研究中，我们在实验室合成了12种新型的烯丙基黄酮，并评估了它们对两种人前列腺癌细胞系PC-3和DU-145以及一种人肝癌细胞系Hep-3B的活性。其中10c、11和12对PC-3细胞株的细胞毒性较5-Fu强。通过细胞分析和膜联蛋白V-FITC和碘化丙啶双染色，发现这些化合物也能诱导细胞凋亡。这表明丙烯化黄酮10c、11和12可能具有进一步开发的抗癌潜力。
Our previous studies demonstrated that eight prenylated flavanones (1-8), isolated from Taiwanese propolis, were capable of a broad spectrum of biological activities. Among them, nymphaeol A (3), nymphaeol B (4) and nymphaeol C (7), abundant in Taiwanese propolis, exhibited cytotoxicity against cancer cell lines. It therefore seemed interesting to improve their activity via a semi-synthetic strategy. In this study, 12 novel prenylated flavanones were synthesised in our laboratory and their activities were assessed for two human prostate cancer cell lines, PC-3 and DU-145, and a human hepatoma cell line, Hep-3B. Of these compounds, 10c, 11 and 12 showed more potent cytotoxicity against the PC-3 cell line than 5-Fu. Using cytometric analysis followed by double staining with annexin V-FITC and propidium iodide, it was observed that these compounds induced apoptosis as well. This suggests that prenylated flavanones 10c, 11 and 12 may have anticancer potential for further development.