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综合运用硅胶、MCI、Sephadex LH-20柱色谱和制备薄层色谱、半制备高效液相色谱等方法,对巴豆Croton tiglium化学成分进行分离纯化,并采用波谱学手段鉴定化合物结构。从巴豆中分离并鉴定了7个化合物,分别为:壬二酸二甘油酯(1)、12-O-(α-甲基丁酰基)佛波醇-13-癸酸酯(2)、12-O-(α-甲基巴豆酰基)佛波醇-13-癸酸酯(3)、(9S,10R,11E,13R)-9,10,13-三羟基十八碳-11-烯酸(4)、(9S,10R,11E,13R)-9,10,13-三羟基十八碳-11-烯酸甲酯(5)、4(1H)-喹啉酮(6)、5-羟基-2-羟甲基吡啶(7)。其中化合物1为新化合物,化合物4~7均为首次从大戟科中分离得到,化合物2和3对人肺癌细胞A549和人肝癌细胞Hep G2有明显的细胞毒作用,抑制人肺癌细胞A549增值的IC50分别为47.8,7.0μmol·L-1,抑制人肝癌细胞Hep G2增值的IC50分别为71.4,44.0μmol·L-1。
The chemical constituents of Croton tiglium from Croton were separated and purified by silica gel, MCI, Sephadex LH-20 column chromatography, preparative thin-layer chromatography and semi-preparative high performance liquid chromatography. The structure of Croton tiglium was identified by spectroscopic methods. Seven compounds were isolated and identified from croton: diacetin azelate (1), 12-O- (α-methylbutyryl) phorbol-13-caprate (3), (9S, 10R, 11E, 13R) -9,10,13-trihydroxyoctadec-11-enoic acid (6), 5- (4), (9S, 10R, 11E, 13R) -9,10,13-trihydroxyoctadec-11-enoate Hydroxy-2-hydroxymethylpyridine (7). Compounds 1 and 2 were isolated from Euphorbiaceae for the first time. Compound 2 and 3 showed obvious cytotoxicity on human lung cancer cell line A549 and human hepatoma cell line Hep G2, and inhibited proliferation of human lung cancer cell line A549 The IC50 values were 47.8 and 7.0 μmol·L-1, respectively. The IC50 values of Hep G2 inhibition were 71.4 and 44.0 μmol·L-1, respectively.