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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。
The natural medicinal chemistry research methods such as solvent extraction, crude separation and silica gel column chromatography purification were used to get some reported phenanthroline alkaloids from the roots of Papaveraceae plants. Compound. The structure of 1-oxo-2,22 (30) -Hepatadiene-29-carboxylic acid (1), 3-oxo-12-oleanoporphyrin was identified by in-depth spectroscopic analysis and reference data -30-carboxylic acid (3), 3β-hydroxy-12-oleanophene-30-carboxylic acid (4), ferulic acid (5), ferulic acid -4-O-β-D-glucoside (6), 3-O-feruloylquinic acid (7) and 3-O-feruloylquinic acid methyl ester (8). Among them, 1 is a new Heparan type triterpenoid, and 2 to 8 are the compounds isolated from this plant for the first time. In order to find out the active drug substance with potential anti-ulcerative colitis activity, we used the specific xbp1 high-throughput dual luciferase reporter gene drug screening model in vitro to detect the main components contained in xBp1 Evaluation of transcriptional activation. The experimental results for the first time elucidated the dihydro-phenylenediamine alkaloids, ie dihydro salicylidene (9) and dihydroquercetin (10), has a certain xbp1 transcriptional activation, the intensity of action were Empty vector control group of 1.76 times and 1.77 times.