漏芦抗肺癌活性部位的筛选  

Screening of active fractions from Rhaponticum uniflorum(L.) DC. for antilung cancer

作　　者：周婷[1,2] 王程成[1,2] 封亮[1] 谭晓斌[1] 贾晓斌[1] 

机构地区：[1]南京中医药大学附属中西医结合医院,江苏南京210028 [2]江苏省中医药研究院,江苏南京210028

出　　处：《中成药》2016年第10期2099-2105,共7页Chinese Traditional Patent Medicine

摘　　要：目的筛选漏芦Rhaponticum uniflorum(L.)DC.体内外抗肺腺癌的活性部位,并对其化学成分进行解析。方法漏芦经有机溶媒提取,其残渣再经水提,共5个活性部位与人肺腺癌细胞A549和H1299共孵育,从中筛选抗肺癌活性最强的部位;并观察它们对Lewis接种C57BL/6J荷瘤小鼠抑瘤率、胸腺指数、脾脏指数的影响,验证其体内抗肺癌作用。采用UPLC-Q-TOF-MS-MS对该活性部位进行解析。结果漏芦抑制A549细胞增殖作用的提取物依次为正丁醇(半数抑制浓度IC_(50)为205.43μg/m L)>乙酸乙酯(IC_(50)为244.22μg/m L)>二氯甲烷(IC_(50)为350.40μg/m L);漏芦抑制H1299细胞增殖作用的提取物依次为正丁醇(IC_(50)为315.87μg/m L)>乙酸乙酯(IC_(50)为356.13μg/m L)>二氯甲烷(IC_(50)为416.13μg/m L)。漏芦提取物抑制Lewis荷瘤小鼠肿瘤增长的作用排序为正丁醇高剂量组(37.43%)>正丁醇低剂量组(32.91%)>乙酸乙酯高剂量组(25.87%)>乙酸乙酯低剂量组(21.15%)。漏芦抗肺癌活性部位的主要成分为三萜类、甾醇类和植物激素类等。结论漏芦体内外抗肺癌作用最强的部位为正丁醇部位,该部位主要的成分为以齐墩果酸和熊果酸为代表的三萜类,以β-谷甾醇和豆甾醇为代表的甾醇类,以β-蜕皮甾酮、漏芦素甲为代表的植物激素类。AIM To screen the active fractions from Rhaponticum uniflorum（ L.） DC. for anti-lung cancer in vivo and to analyze its chemical composition. METHODS The five active fractions of organic extract of R. uniflorum plus aqueous extract of decoction dregs were incubated with human lung adenocarcinoma cells A549 and H1299 to screen the strongest active fraction. Tumor inhibition rate,thymus index,and spleen index were observed on Lewis transplanted C57 BL /6J-bearing mice. UPLC / Q-TOF-MS-MS was used to analyze the chemical composition of active fractions. RESULTS The fraction from R. uniflorum inhibited the proliferation of A549 and H1299 cells from the strongest to the least strong were n-butanol（ IC（50）205. 43 μg / m L）〉 ethyl acetate（ IC（50）244. 22 μg / m L）〉 dichloromethane（ IC（50）350. 40 μg / m L）,and n-butanol（ IC（50）315. 87 μg / m L） ethyl acetate（ IC（50）356. 13 μg / m L） dichloromethane（ IC（50）416. 13 μg /mL）,respectively. The fraction from R. uniflorum inhibited the Lewis tumor-bearing mice tumor growth in the order of n-butanol high dose group（ 37. 43%） 〉n-butanol low dose group（ 32. 91%） 〉ethyl acetate high dose group（ 25. 87%） 〉ethyl acetate low dose group（ 21. 15%）. The main chemical compositions of active fractions for anti-lung cancer are comprised terpenes,sterols and plant hormones. CONCLUSION The strongest active fraction from R. uniflorum for anti-lung cancer in vivois n-butanol fraction,which contains oleanolic acid and ursolic acid as triterpenes,beta-sitosterol and stigmasterol as sterols,and beta-ecdysterone and rhaponticum as plant hormones.

关 键 词：漏芦 活性部位 抗肺癌 成分 

分 类 号：R285.5[医药卫生—中药学]