小蓟中氧化蒲公英赛酮和醇的分离鉴定和细胞毒活性测试

Isolation,Purification,Elucidation and Cytotoxicity Activity on Oxidotaraxerone and Oxidationtaraxerol of Cirsium Setosum(Willd.)MB

研究小蓟乙醇提取物中显示细胞毒活性的石油醚的化学成分,并对分离得到的化合物进行体外细胞毒活性的筛选。应用各种硅胶和凝胶色谱技术分离纯化,用MS和NMR等波谱学方法,结合文献对照确定化合物结构。从小蓟乙醇提取物的石油醚萃取部位分离得到3个氧化蒲公英赛烷型三萜类化合物,分别鉴定为11α,12α-氧化蒲公英赛酮、11α,12α-氧化蒲公英赛醇和11α,12α-氧化蒲公英赛醇棕榈酸酯。3个化合物均为首次从蓟属植物中发现,它们在人结肠癌细胞、肝癌细胞、胃癌细胞、肺癌细胞和卵巢癌细胞的体外细胞毒活性测试中均显示一定的抑制活性。

To investigate chemical constituents contained in cytotoxic petroleum ether-soluble portion from the ethanol extracts of Cirsium setosum（Willd.） MB,and evaluate their cytotoxic activity in vitro.The constituents were separated and purified by various chromatographic methods including silica gel and Sephadex LH-20,and their structures were elucidated by spectroscopic methods including NMR,MS methods and comparison with literature.Three oxidotaraxerane triterpenoids were isolated from the petroleum ether fraction of ethanolic extract of Cirsium setosum,and determined as 11α,12α-oxidotaraxerone,11α,12α-oxidotaraxerol and 11α,12α-oxidotaraxerol palmitate.To the best of our knowledge,this is the first report showing the presence of all the compounds in the genus Cirsium.In the in vitro assays,three compounds showed selective cytotoxicity against HCT-8,Bel-7402,BGC-823,A549 and A2780.