NatureWise Biotech & Medicals Corporation, Taipei 115, Taiwan.
Nat Prod Res. 2012;26(2):116-24. doi: 10.1080/14786419.2010.535146. Epub 2011 Jul 27.
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.
我们之前的研究表明，从台湾蜂胶中分离出的八种类异戊二烯黄酮（1-8）具有广泛的生物活性。其中，大量存在于台湾蜂胶中的睡莲醇 A（3）、睡莲醇 B（4）和睡莲醇 C（7）对癌细胞系表现出细胞毒性。因此，通过半合成策略来提高它们的活性似乎很有趣。在这项研究中，我们实验室合成了 12 种新型的类异戊二烯黄酮，并评估了它们对两种人前列腺癌细胞系 PC-3 和 DU-145 以及人肝癌细胞系 Hep-3B 的活性。在这些化合物中，化合物 10c、11 和 12 对 PC-3 细胞系的细胞毒性比 5-Fu 更强。通过流式细胞术分析并用 Annexin V-FITC 和碘化丙啶双重染色观察到，这些化合物还诱导了细胞凋亡。这表明类异戊二烯黄酮 10c、11 和 12 可能具有进一步开发的抗癌潜力。
