全缘橐吾根部化学成分及生物活性研究  

Chemical constituents and biological activity of Ligularia mongolica root

作　　者：周慧超[1] 贺爽[1] 宋宇[1] 秦文平[1] 白素平[1] 

机构地区：[1]新乡医学院药学院,河南新乡453003

出　　处：《新乡医学院学报》2016年第12期1017-1021,1027,共6页Journal of Xinxiang Medical University

基　　金：国家自然科学基金资助项目(编号:81072552);河南省科技创新杰出青年基金资助项目(编号:104100510016)

摘　　要：目的研究全缘橐吾根部的化学成分及生物活性。方法采用柱层析对全缘橐吾根部的提取物进行分离提纯得到单体化合物,并用现代波谱方法(核磁共振氢谱、核磁共振碳谱、质谱)确定其化合物结构;用四甲基偶氮唑盐比色法对分离得到的化合物进行抗肿瘤活性评价。结果从全缘橐吾根部提取物中分离得到13种化合物,经结构鉴定分别为:蜂斗菜内酯A(1);8β-Hydroxyeremophil-7(11)-ene-12,8α(4β,6α)-diolide(2);8β-Hydroxyeremophil-7(11)-ene-12,8β(4β,6α-diolide(3);8β-Methoxyeremophil-7(11)-ene-12,8α(4β,6α)-diolide(4);8β-Hydroeremophil-7(11)-ene-12,8α(14β,6α)-diolide(5);异蜂斗菜素(6);蜂斗菜素(7);β-谷甾醇(8);豆甾醇(9);2α-羟基乌苏酸(10);齐墩果酸(11);正棕榈酸(12);对羟基苯甲醛(13)。其中倍半萜类化合物1、2、4、5、6对人肝癌Hep G2细胞、人食管癌Eca109细胞均表现出较强的体外抗肿瘤活性。结论 13种化合物均为首次从该植物中分离得到;体外抗肿瘤活性较强的化合物1、2、4、5、6有望成为天然抗肿瘤先导化合物。Objective To study the chemical constituents and biological activities of Ligularia mongolica roots. Methods The compounds were isolated and purified from the extracts of Ligularia mongolica roots by using the column chromatography and the structures of these compounds were identified by spectroscopic analysis including proton nuclear magnetic resonance( 1H-NMR),carbon nuclear magnetic resonance(13C-NMR) and mass spectrometry( MS). The antitumor activity of the compounds was evaluated by 3-( 4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide( MTT) method. Results Thirteen compounds were isolated from the roots of the Ligularia mongolica and their structures were identified as: bakkenolide A( 1); 8β-hydroxyeremophil-7( 11)-ene-12,8α( 4β,6α)-diolide( 2); 8β-hydroxy-eremophil- 7( 11)-ene-12,8( 4β,6α)-diolide( 3); 8β-methoxyeremophil-7( 11)-ene-12,8α( 4β,6α)-diolide( 4); 8β-hydroeremophil-7( 11)-ene-12,8α( 14β,6α)-diolide( 5); isopetasin( 6); petasin( 7); β-sitosterol( 8); stigmasterol( 9); 2α-hydroxyursoic acid( 10); oleanolic acid( 11); hexadecanoic acid( 12); p-hydroxybenzaldehyde( 13). Sesquiterpenoids compounds of 1,2,4,5 and 6 showed the potent antitumor activity on human tumor cell lines Hep G2 and Eca109. Conclusion Thirteen compounds are first isolated from this plants.Compounds 1,2,4,and 6 which with potent antitumor activity in vitro are promising natural antitumor leading compound.

关 键 词：全缘橐吾 倍半萜 化学成分 生物活性 细胞毒活性 

分 类 号：R284.1[医药卫生—中药学]