College of Pharmaceutic Science, Yunnan University of Traditional Chinese Medicine, Kunming 650500, China.
Engineering Laboratory for National Healthcare Theories and Products of Yunnan Province, Yunnan University of Traditional Chinese Medicine, Kunming 650500, China.
Molecules. 2018 Feb 1;23(2):310. doi: 10.3390/molecules23020310.
Scutellarin is the major active flavonoid extracted from the traditional Chinese herbal medicine (Vant.) Hand-Mazz., which is widely used in China. Recently, accumulating evidence has highlighted the potential role of scutellarin and its main metabolite scutellarein in the treatment of cancer. To explore novel anticancer agents with high efficiency, a series of new scutellarein derivatives with a long aliphatic chain were synthesized, and the antiproliferative activities against Jurkat, HCT-116 and MDA-MB-231 cancer cell lines were assessed. Among them, compound exhibited the strongest antiproliferative effects on Jurkat (IC = 1.80 μM), HCT-116 (IC = 11.50 μM) and MDA-MB-231 (IC = 53.91 μM). In particular, even showed stronger antiproliferative effects than the positive control NaAsO₂ on Jurkat and HCT-116 cell lines. The results showed that a proper long aliphatic chain enhanced the antiproliferative activity of scutellarein.
野黄芩苷是从传统中药（Vant。）Hand-Mazz.中提取的主要活性黄酮类化合物，在中国被广泛应用。最近，越来越多的证据强调了野黄芩苷及其主要代谢物黄芩素在癌症治疗中的潜在作用。为了探索高效的新型抗癌药物，合成了一系列具有长脂肪链的新黄芩素衍生物，并评估了它们对 Jurkat、HCT-116 和 MDA-MB-231 癌细胞系的增殖抑制活性。其中，化合物 对 Jurkat（IC = 1.80 μM）、HCT-116（IC = 11.50 μM）和 MDA-MB-231（IC = 53.91 μM）的增殖抑制作用最强。特别是 对 Jurkat 和 HCT-116 细胞系的增殖抑制作用甚至强于阳性对照 NaAsO₂。结果表明，适当的长脂肪链增强了黄芩素的增殖抑制活性。
