大戟脂中二萜类成分及细胞毒活性研究

Diterpenes from Euphorbium and their cytotoxicity

〔目的〕研究大戟脂中二萜类抗肿瘤活性成分。〔方法〕通过硅胶柱色谱、ODS柱色谱和RP-HPLC等方法,从大戟脂的甲醇提取物中共分离得到5个二萜类化合物,利用各种波谱学手段及理化性质确定化合物的结构。对分离得到的二萜类化合物的生合成途径进行了简单推测,并采用MTT法对分离得到的单体化合物进行细胞毒活性测试。〔结果〕分离得到的5个二萜类化合物包括3个Ingol烷型二萜、2个巴豆烷型二萜,分别鉴定为:ingol7,8,12-triacetate-3-(4-me-thoxy-phenyl)acetate(1)、ingol7,8,12-triacetate-3-phenylacetate(2)、ingol3,8,12-triacetate(3)、12-deoxyphorbol-13-isobu-tyrate-20-acetate(4)、12-deoxyphorbol-13-angelate-20-acetate(5)。〔结论〕化合物1~3是首次从该植物中分离得到,并对C6细胞株有较强的细胞毒活性。

Objective〕To study the antitumor active constituents of diterpenes from Euphorbium.〔Methods〕By means of various chromatographic methods such as silica gel, ODS and semi-preparative HPLC, five compounds were isolated from the methanol extraction of Euphorbium. Their structures were identified by spectroscopic methods and physicochemical properties. In addition, putative biogenetic relationships to these compounds were proposed and MTT assay was used to evaluate the compounds.〔Results〕The compounds include three ingol-type and two tigliane-type diterpenoids. These isolated compounds were identified as ingol 7,8,12-triacetate-3-(4-methoxy-phenyl) acetate (1), ingol 7,8,12-triacetate-3-phenylacetate (2), ingol 3,8,12-triacetate (3), 12-deoxyphorbol-13-isobutyrate-20-acetate (4), 12-deoxyphorbol-13-angelate-20-acetate (5).〔Conclusion〕Compounds 1 ~ 3 were firstly isolated from the plant and showed strong cytotoxic activity to C6 cell lines.