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。
Abstract
OBJECTIVE To study the anti-cancer components of Calotropis gigantean L.METHODS The powdered whole plants of C. gigantea were extracted with 95% alcohol. After removal of the solvent, the residue was extracted with petroleum ether and chloroform, and the compounds in the chloroform extract were isolated and purified by different column chromatograghies carried out on silica gel, RP-18, MCI, and Sephadex LH-20 and their structures were elucidated by spectral data. RESULTS Thirteen compounds were isolated and their structures were characterized as gofruside(1), uzarigenin(2), arjunolic acid(3), 3ξ-(1ξ-hydroxyethyl)-7-hydroxy-1-isobenzofuranone(4), daucosterol(5), syringaresinol(6),12-O-benzoyl-deacylmetaplexigenin(7), 3-hydroxy-4-methoxybenzoic acid(8), oleanolic acid(9),β-sitosterol(10), methyl 1-naphthaleneacetate(11), butylparaben(12),α-D-oleandropyranoside(13), and compounds 2-4,6-9, and 11-13 were isolated from this plant for the first time. Compounds 1 and 2 showed cytotoxicity against HLE, K562, RPMI8226, MCF7, MDA, and WM9 cell lines, with K562 and RPMI8226 being the most sensitive cells.CONCLUSION Compounds 1 and 2 are premilinarily judged as the anti-cancer components in C. gigantean.
关键词
牛角瓜 /
抗肿瘤活性 /
萝藦科 /
钉头果苷 /
乌沙苷元
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Key words
Calotropis gigantea /
Antitumor activity /
Asclepiadaceae /
gofruside /
uzarigenin
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中图分类号：
R284
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参考文献
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脚注
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基金
科技部973计划前期研究专项资助项目(2012CB722601);国家重大科学仪器设备开发专项资助项目(2011YQ12003506)
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