摘要
利用硅胶、Sephadex LH-20等多种柱色谱及制备液相色谱对白花蛇舌草氯仿部位和乙酸乙酯部位进行分离,依据核磁共振波谱法和质谱法作化合物结构鉴定,共分离得到13个化合物,分别为十五酸十七酯(1)、豆甾醇(2)、2-羟基-1-甲氧基-3-甲基蒽醌(3)、7-hydroxytectoquinone(4)、熊果酸(5)、齐墩果酸(6)、2-butyl-1-hydroxyanthra-9,10-quinone(7)、白桦脂酸(8)、芦丁(9)、槲皮素(10)、反式对羟基肉桂酸(11)、反式对甲氧基肉桂酸(12)、山奈酚(13)。化合物1、4、7首次从该植物中分离得到。采用CCK-8法检测白花蛇舌草不同极性部位及单体化合物对A549细胞体外增殖抑制作用,结果表明白花蛇舌草氯仿部位和乙酸乙酯部位均有很好抑制A549细胞增殖的作用,且有明显的剂量-效应关系。当药物浓度从25μmol/L到400μmol/L,氯仿部位和乙酸乙酯部位对A549的细胞增殖抑制率分别从12.9%、43.32%达到80.49%、63.74%。单体化合物熊果酸、齐墩果酸、白桦脂酸均能显著抑制A549细胞增殖,其IC值分别为13.85、12.81、8.38μmol/L。
The chemical constituents were separated from Hedyotis diffusa Willd by using silica gel,Sephadex LH-20,preparative liquid chromatography and other chromatographic separation methods.The obtained compounds were identified by NMR and MS.Thirteen compounds isolated from H.diffusa include pentadecanoic acid heptadecyl ester(1),stigmasterol(2),2-hydroxy-1-methoxy-3-methylanthraquinone(3),7-hydroxytectoquinone(4),ursolic acid(5),oleanolic acid(6),2-butyl-1-hydroxyanthra-9,10-quinone(7),betulinic acid(8),rutin(9),quercetin(10),trans-p-hydroxycinnamic acid(11),trans-p-methoxycinnamic acid(12)and kaempferol(13).Compounds 1,4 and 7 were isolated from H.diffusa for the first time.CCK-8 was used to detect the inhibitory effects of different polar sites and compounds on the proliferation of A549 cells in vitro.The chloroform extract and ethyl acetate extract from H.diffusa both inhibited the proliferation of A549 cells,also showed significant dose-effect relationship.When the concentrations of extract was from 25μmol/L to 400μmol/L,the inhibition rate of cell proliferation for the chloroform and ethyl acetate sites increased from 12.9%,43.32%to 80.49%,63.74%,respectively.Ursolic acid,oleanolic acid and betulinic acid can significantly inhibit the proliferation of A549 cells with ICvalues of 12.80,2.81 and 8.38μmol/L,respectively.
作者
王婷
梁艳妮
侯宝龙
吴柯楠
吴冬芝
裴刚
王征
WANG Ting;LIANG Yan-ni;HOU Bao-long;WU Ke-nan;WU Dong-zhi;PEI Gang;WANG Zheng(Shaanxi Innovation Drug Research Center,State Key Laboratory of Research&Development of Characteristic Qin Medicine Resources(Cultivation),Co-construction Collaborative Innovation Center for Chinese Medicine Resources Industrialization by Shaanxi&Education Ministry,Shaanxi University of Chinese Medicine,Xianyang 712083,China;Medicine School of Pharmacy,Hunan University of Chinese Medicine,Changsha 410208,China)
出处
《天然产物研究与开发》
CAS
CSCD
2022年第8期1281-1288,1300,共9页
Natural Product Research and Development
基金
国家自然科学基金(81703924)
陕西省重点产业创新链项目(2018ZDCXL-SF-01-02-02)
陕西省创新人才推进计划—青年科技新星项目(2019KJXX-025)
陕西高校青年科技创新团队(陕教[2019]90号)。
关键词
白花蛇舌草
化学成分
结构鉴定
抗肿瘤活性
Hedyotis diffusa Willd
chemical constituents
structural identification
anti-tumour activity
