论文部分内容阅读
目的分离牛角瓜(Calotropis gigantea L.)中的化学成分并评价其体外抗肿瘤活性,为确定牛角瓜中的抗肿瘤有效成分提供基础。方法牛角瓜全株用体积分数95%乙醇溶液加热回流提取,减压回收乙醇,浓缩液加水稀释后经石油醚、三氯甲烷萃取,三氯甲烷萃取物利用正相硅胶、反相Rp-18、微孔吸附树脂CHP 20P、Sephadex LH-20等柱色谱方法分离纯化,通过理化性质和光谱数据进行结构鉴定。结果从牛角瓜中分离鉴定了13个化合物,分别为:钉头果苷(1),乌沙苷元(2),阿江榄仁酸(3),3ξ-(1ξ-hydroxyethyl)-7-hydroxy-1-isobenzofuranone(4),胡萝卜苷(5),丁香脂素(6),12-O-benzoyl-deacylmetaplexigenin(7),3-羟基-4-甲氧基苯甲酸(8),齐墩果酸(9),β-谷甾醇(10),1-萘乙酸甲酯(11),对羟基苯甲酸丁酯(12),α-D-oleandropyranoside(13)。其中化合物2~4、6~9、11~13为首次从该植物中分离得到。体外活性检测显示,只有化合物1、2对肿瘤HLE、K562、RPMI8226、MCF7、MDA、WM9细胞的增殖具有明显的抑制活性,对肿瘤K562、RPMI8226细胞株的增殖抑制活性尤为显著。结论初步确定牛角瓜中的抗肿瘤有效成分为强心苷类化合物钉头果苷及乌沙苷元。
OBJECTIVE: To isolate the chemical constituents from Calotropis gigantea L. and evaluate the antitumor activity in vitro, and to provide a basis for the determination of antitumor active ingredients in the melon. Methods The whole plant was treated with 95% ethanol solution by heating and refluxing for extraction. The ethanol was recovered under reduced pressure. The concentrate was diluted with water and extracted with petroleum ether and chloroform. The chloroform extract was purified by normal phase silica gel, reverse phase Rp-18 , Microporous adsorption resin CHP 20P, Sephadex LH-20 and other column chromatography purification, physical and chemical properties and spectral data for structural identification. Results Thirteen compounds were isolated and identified from cantaloupe. They were: cedar (1), wrasser (2), acenaphthenic acid (3), 3ξ- 1-isobenzofuranone (4), daucosterol (5), melazein (6), 12-O-benzoyl-deacylmetaplexigenin (7), 3-hydroxy- (9), β-sitosterol (10), methyl 1-naphthaleneacetate (11), butylparaben (12) and α-D-oleandropyranoside (13). Compounds 2 ~ 4, 6 ~ 9 and 11 ~ 13 were isolated from this plant for the first time. In vitro activity assay showed that only compounds 1 and 2 had obvious inhibitory activity on the proliferation of HLE, K562, RPMI8226, MCF7, MDA and WM9 cells, especially on the proliferation of K562 and RPMI8226 cells. Conclusion The antitumor active ingredients in the horn melon are initially identified as cardiac glycosides,