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目的以猫眼草Euphorbia lunulata全草为研究对象,对其有效成分进行分离纯化,并对分离得到的化合物进行活性测定。方法运用硅胶柱色谱、羟丙基葡聚糖凝胶柱色谱、ODS柱色谱以及制备高效液相色谱等方法进行分离,根据理化性质和谱学技术分析确定化合物的化学结构。采用细胞毒活性(MTT)法对提取物、各流分及分离得到的化合物进行抗肿瘤活性评价。结果从猫眼草60%乙醇提取物的醋酸乙酯萃取层中分离得到6个化合物,分别鉴定为大戟素M(1)、泽泻醇A(2)、大戟苷A(3)、甘遂大戟萜酯D(4)、18-羟基泽漆内酯A(5)和β-胡萝卜苷(6)。结论其中化合物1为新化合物,为假白榄烷型骨架二萜类化合物;化合物2～4为首次从该植物中分离得到。经MTT细胞毒活性测试后发现化合物1～4具有较强的肿瘤细胞抑制活性,尤其对人肝癌细胞HepG2有很强的抑制活性。
OBJECTIVE To isolate and purify the active ingredients of Euphorbia lunulata, and to determine the activity of the isolated compounds. Methods The compounds were isolated by silica gel column chromatography, hydroxypropyl dextran gel column chromatography, ODS column chromatography and preparative high performance liquid chromatography (HPLC). The chemical structures of the compounds were determined by physicochemical properties and spectroscopic techniques. The cytotoxic activity (MTT) method was used to evaluate the antitumor activity of extracts, fractions and isolated compounds. Results Six compounds were isolated from ethyl acetate extract of 60% ethanol extract of cat’s eye grass and identified as eugenol (1), alisol A (2), eugenol A (3) Ephthrionol ester D (4), 18-hydroxy lacquer lactone A (5) and beta-daucosterol (6) were then synthesized. Conclusions Among them, compound 1 is a new compound, which is a pseudo-aldane-type skeleton diterpenoid. Compounds 2 ~ 4 are isolated from this plant for the first time. After MTT cytotoxic activity test showed that compounds 1 to 4 have a strong tumor cell inhibitory activity, in particular, has a strong inhibitory activity on human hepatoma HepG2 cells.