皂角刺抗肿瘤活性成分的分离鉴定与活性测定

目的分离鉴定皂角刺中抗肿瘤活性成分。方法用四甲基偶氮唑盐(MTT)比色法,结合硅胶、葡聚糖凝胶等色谱方法追踪分离皂角刺抗肿瘤活性成分,根据理化性质和波谱数据鉴定化学结构,用半数抑制浓度(IC50)评价其抗肿瘤活性。结果从皂角刺中分离得到8个化合物,分别为黄颜木素(1)、槲皮素(2)、3-βacetoxyolean-12-en-28-oic acid(3)、木栓酮(4)、棕榈酸(5)、白桦醇(6)、β-谷甾醇(7),胡萝卜苷(8)。化合物1、3对7种体外培养的肿瘤细胞抑制作用较好,在测定浓度范围内剂量依赖关系良好;化合物3对Bel-7402、HeLa、HT1080、KB、A549、SGC-7901、Heps等7种肿瘤细胞株生长增殖均具有良好的抑制作用,IC50为11.61~18.73 mg.L-1;化合物1对除A549之外的6种肿瘤细胞株抑制作用良好,IC50为11.34~19.32 mg.L-1。结论化合物2~6和8为首次从皂角刺中分离;化合物1、3的抗肿瘤活性为皂角刺中首次发现。

Identification and anti-tumor activity determination about anti-tumor components of Gleditsia sinensis Lam. stings

Abstract：Objective To study the anti-tumor components of the Gleditsia sinensis Lam. stings Methods Bioassay-directed fractionation of the Gleditsia sinensis Lam.stings led to isolation of compounds with silica gel, Sephadex LH-20 etc. They were elucidated on the basis of physico-chemical properties and spectral methods and their anti-tumor activity were evaluated by MTT. Results Eight compounds were separated from the Gleditsia sinensis Lam. stings and identified as fisetin (1), quercetin (2), 3β-acetoxyolean-12-en-28-oic acid (3), friedelin (4), palmitic acid (5), betulin (6), β-sitosterol (7), daucosterol (8). Conclusions Among them, compounds 2-6 and 8 are isolated from the plant for the first time. The antiproliferative activities of 8 isolated compounds against seven tumor cell lines are evaluated by MTT. The results demonstrate that compounds 1 and 3 exhibit strong antiproliferative activity, and their anti-tumor activities are reported from the plant for the first time.