Synthesis of Scutellarein Derivatives with a Long Aliphatic Chain and Their Biological Evaluation against Human Cancer Cells.
Synthesis of Scutellarein Derivatives with a Long Aliphatic Chain and Their Biological Evaluation against Human Cancer Cells.
复制标题
长脂肪链灯盏乙素衍生物的合成及其对人类癌细胞的生物学评价。
DOI：
10.3390/molecules23020310
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发表时间：
2018-02-01
期刊：
影响因子：
--
通讯作者：
Rao G
中科院分区：
文献类型：
--
作者：
Ni G;Tang Y;Li M;He Y;Rao G
灯盏乙素（Scutellarin）是从中药灯盏花（Erigeron breviscapus（Vant.）Hand-Mazz.在中国被广泛使用。近年来，越来越多的证据表明灯盏乙素及其主要代谢产物灯盏乙素在癌症治疗中的潜在作用。为探索新型高效抗癌药物，合成了一系列新的长链灯盏乙素衍生物，并对Jurkat、HCT-116和MDA-MB-231肿瘤细胞株进行了体外抗增殖活性测定。其中化合物6a对Jurkat（IC 50 = 1.80 μM）、HCT-116（IC 50 = 11.50 μM）和MDA-MB-231（IC 50 = 53.91 μM）的抗增殖作用最强。特别地，6a对Jurkat和HCT-116细胞系甚至显示出比阳性对照NaAsO 2更强的抗增殖作用。结果表明，合适的长脂肪链可增强黄芩素的抗增殖活性。
Scutellarin is the major active flavonoid extracted from the traditional Chinese herbal medicine Erigeron breviscapus (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 6a exhibited the strongest antiproliferative effects on Jurkat (IC50 = 1.80 μM), HCT-116 (IC50 = 11.50 μM) and MDA-MB-231 (IC50 = 53.91 μM). In particular, 6a 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.
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