千年健的化学成分及抗肿瘤活性研究

Study on the chemical constituents and anti-tumor activity of Homalomena occulta

为探讨千年健的化学成分及抗肿瘤活性,应用正相硅胶、中压制备液相、Sephadex LH-20等多种色谱分离手段,从千年健乙醇提液中分离得到10个化合物,依据波谱分析方法,所得化合物分别为桦木酸(1)、3β-acetoxyolean-12-en-28-oic acid(2)、熊果酸(3)、antriptolactone(4)、黄花菜木脂素C(5)、bullatantriol(6)、菠萝香藤素(7)、mucrolidin(8)、pinocembrin(9)、3-(4-hydroxy-3-methoxyphenyl)-propenal(10)。除化合物7、8外,本实验所分离得到的其余化合物,均为首次从千年健中分离。通过对化合物2、4、9与抗肿瘤药物甲氨蝶呤的体外细胞毒性及单细胞凝胶电泳对比试验表明,化合物2、4、9的抗肿瘤细胞效果显著,同时,上述化合物对荷瘤小鼠体内抗肿瘤对比试验结果,亦显示出各化合物具有较强抑制肿瘤组织生长作用,且化合物2、4、9对人肺癌细胞(A549)等4种肿瘤细胞株的研究为首次报道。

In order to explore the chemical composition and anti-tumor activity of Homalomena occulta,10 compounds were separated from the ethanol extract of Homalomena occulta by using normal phase silica gel,medium-pressure liquid chromatography,Sephadex LH-20 and other chromatographic separation methods.According to spectral analysis method,the obtained compounds include betulinic acid(1),3β-acetoxyolean-12-en-28-oic acid(2),ursolic acid(3),antriptolactone(4),cleo-lignan C(5),bullatantriol(6),pineapple coriander(7),mucrolidin(8),pinocembrin(9),and 3-(4-hydroxy-3-methoxyphenyl)-propenal(10).Except for compounds 7 and 8,the remaining compounds isolated in this experiment were isolated from Homalomena occulta for the first time.The in vitro cytotoxicity and single-cell gel electrophoresis comparison tests of compounds 2,4,and 9 with the anti-tumor drug methotrexate showed that the anti-tumor cell effects of compounds 2,4,and 9 were significant.The anti-tumor comparative test in mice also showed that it has a strong inhibitory effect on tumor tissue growth.The study of compounds 2,4,and 9 against 4 kinds of tumor cell lines including human lung cancer cells(A549) is reported for the first time.