入侵植物飞机草的化学成分及其抗肿瘤活性

Chemical constituents of Chromolaena odorata and their anticancer activities

目的分离、鉴定入侵植物飞机草叶片的化学成分,探讨其对肿瘤细胞的抑制活性。方法利用正相硅胶柱色谱、薄层色谱、羟丙基葡聚糖凝胶Sephadex LH-20和重结晶等方法对飞机草叶片乙醇提取物的乙酸乙酯萃取相进行分离纯化,根据核磁共振波谱数据鉴定化合物的结构,采用MTT法筛选具有抑制肿瘤细胞生长活性的化合物。结果共分离鉴定出11个化合物,分别为山柰酚-4'-甲基醚(1)、金合欢素(2)、异樱花素(3)、β-谷甾醇(4)、烟筒花素(5)、胡萝卜苷(6)、5,7-二羟基-6,4'-二甲氧基二氢黄酮(7)、4,2'-二羟基-4',5',6'-三甲氧基查尔酮(8)、飞机草素(9)、3,5-二羟基-7,4'-二甲氧基黄酮(10)和homohesperitin(11);化合物1、2、5、7和9～11对乳腺癌细胞(MCF-7)、人神经胶质瘤细胞(U251)、肝癌细胞(HepG2)、子宫颈癌细胞(HeLa)以及肺癌细胞(A549)有一定的抑制作用。结论化合物5、10、11为首次从飞机草中分离得到;化合物2和7对上述5种癌细胞的抑制活性强于阳性对照物顺铂。

AIM To study the chemical constituents from the leaves of Chromolaena odorata as an invasive plant and their anticancer activity.METHODS Methanol extract of Chromolaena odorata was isolated and purified from the acetic ether part of the alcohol extract of leaves of Chromolaena odorata by column chromatography on Silica gel and Sephadex LH-20,Silica gel thin layer chromatography and recrystallization.Nuclear magnetic resonance technique was used to identify structures of the chemicals isolated.The anticancer activity of the chemicals was evaluated by MTT method.RESULTS Eleven compounds were isolated as kaempferide-4′methoxy ether（1）,acacetin（2）,isosakurnaetni（3）,β-sitosterol（4）,hortensin（5）,daucosterol（6）,5,7-dihydroxy-6,4′-dimethoxy dihydroflavone（7）,4,2′-dihydroxy-4′,5′,6′-trimethoxychalcone（8）,odoratin（9）,3,5-dihydroxy-7,4′-dimethoxyflavone（10）,homohesperitin（11）.Compounds 1,2,5,7 and 9~11 showed the abilities to inhibit human cancer cells including breast cancer cell line MCF-7,human gliona cell U251,hepatoma cell line HepGa2,cervical cancer hela cells and lung cancer line A549 in vitro.CONCLUSION Compound 5,10 and 11 are isolated from Chromolaena odorata for the first time.Compound 2 and 7 perform more effective in anticancer than cisplatine as a positive control.