摘要
采用溶剂提取、萃取粗分离和硅胶柱色谱纯化等天然药物化学研究手段,从罂粟科植物小果博落回的根中除得到部分已报道的苯菲啶型生物碱外,又进一步分离得到8个化合物。通过深入的波谱分析并参考文献数据鉴定其结构分别为1-氧代-2,22（30）-何帕二烯-29-羧酸（1）、3-氧代-12-齐墩果烯-30-羧酸（2）、3α-羟基-12-齐墩果烯-30-羧酸（3）、3β-羟基-12-齐墩果烯-30-羧酸（4）、阿魏酸（5）、阿魏酸-4-O-β-D-葡萄糖苷（6）、3-O-阿魏酰奎尼酸（7）和3-O-阿魏酰奎尼酸甲酯（8）。其中1为新的何帕烷型三萜类化合物,2~8为首次从该植物中分离得到的化合物。为寻找具有潜在抗溃疡性结肠炎活性的天然药物活性物质,本文采用特异的体外靶向xbp1高通量双荧光素酶报告基因药物筛选模型,对小果博落回所含主要成分进行了xbp1转录激活作用评价。实验结果首次阐明了二氢型苯菲啶生物碱类化合物,即二氢血根碱（9）和二氢白屈菜红碱（10）,具有一定的xbp1转录激活作用,其作用强度分别为空载体对照组的1.76倍和1.77倍。
Ongoing study on the chemical constituents of the roots of Macleaya microcarpa led to the isolation of eight compounds of derivatives of triterpenes and organic acids in addition to some previously identified benzophenanthridines. The eight compounds were identified by spectroscopic methods as well as comparison with literature values as 1-oxo-2, 22（30）-hopandien-29-oic acid（1）, 3-oxo-12-oleanen-30-oic acid（2）, 3α-hydroxy-12-oleanen-30-oic acid（3）, 3β-hydroxy-12-oleanen-30-oic acid（4）, ferulic acid（5）, ferulic acid 4-O-β-D-glucoside（6）, 3-O-feruloylquinic acid（7）, and methyl 3-O-feruloylquinate（8）. Of which, 1 is a new triterpenoid of hopanes and 2-8 are isolated from M. microcarpa for the first time. In order to discover natural active compounds as potential agents of anti-ulcerative colitis（UC）, an in vitro drug high-throughput screening model targeted x-box-binding protein 1（xbp1） was employed to evaluate the activity of the major chemical constituents of M. microcarpa. The result confirmed that two dihydrobenzophenanthridines, dihydrosanguinarine（9） and dihydrochelerythrine（10）, showed a certain activity on activating the transcription of xbp1, a transcription factor（TF） associated with the occurrence, development, and potential treatment of UC, with their relative activating ratios being 1.76 and 1.77 times, respectively, as compared with control group.
出处
《药学学报》
CAS
CSCD
北大核心
2015年第2期207-210,共4页
Acta Pharmaceutica Sinica
基金
国家自然科学基金资助项目(81202546)
中央高校直属单位基本科研业务费(2011CHX17)
重大新药创制科技重大专项(2012ZX09301002-002)
