伞房花耳草的化学成分及细胞毒活性研究

Chemical Constituents from Hedyotis Corymbosa and Their Cytotoxic Activity

伞房花耳草(Hedyotis corymbosa)为茜草科耳草属植物,本文利用硅胶柱色谱及葡聚糖凝胶色谱对其氯仿提取物进行分离纯化,从中分离及鉴定出4个化合物,分别为23-ethylcholesta-11(12),23(24)-dien-3β-ol(1),2-羟基-1-甲氧基蒽醌(2),齐墩果酸(3)和1-羟基-2-羟甲基蒽醌(4)。其中,化合物1和4为首次从伞房花耳草中分离得到,丰富了伞房花耳草的化学成分的结构多样性。进一步的细胞毒活性筛选发现,化合物3对人肺癌细胞株H460,人口腔癌细胞株KB及人肝癌细胞株HepG2的IC_(50)值分别为(40.82±3.82),(78.29±4.12)和(66.75±5.46)mg·L^(-1);化合物4对上述3种肿瘤细胞株的IC_(50)值分别为(13.20±1.49),(73.18±3.65)和(155.70±7.32)mg·L^(-1),而化合物1和2细胞毒活性较弱。化合物3和4可能是伞房花耳草抗肿瘤的活性成分。

Hedyotis corymbosa(L.)Lam.belongs to Rubiaceae Hedyotis Linn.Plants.In this paper,the chloroform extract of Hedyotis corymbosa was isolated and purified by silica gel and Sephadex LH-20 column chromatography.Four compounds were isolated and identified as follows:23-ethylcholesta-11(12),23(24)-dien-3β-ol(1),2-hydroxy-1-methoxy anthraquinone(2),olenolic acid(3)and 1-hydroxy-2-hydroxymethyl anthraquinone(4).Compounds 1 and 4 were isolated from Hedyotis corymbosa for the first time,which enriched the structural diversity of chemical constituents of Hedyotis corymbosa.Further cytotoxic activity screening found that the IC_(50)values of compound 3 on human lung cancer cell line H460,human oral cancer cell line KB and human liver cancer cell line HepG2 were(40.82±3.82),(78.29±4.12)and(66.75±5.46)mg/L,respectively.The IC_(50)values of compound 4 on H460,KB and HepG2 cells were(13.20±1.49),(73.18±3.65)and(155.70±7.32)mg/L,respectively.Compounds 1 and 2 showed weak cytotoxic activity against the above three tumor cell lines.Compounds 3 and 4 might be the antitumor active constituents of Hedyotis corymbosa.