基于药效学指标筛选藏药湿生扁蕾抗溃疡性结肠炎的活性成分

Bioactive Constituents Studies on Gentianopsis paludosa against UC Fibrosis Based on the Pharmacodynamics Indexes

目的研究藏药湿生扁蕾抗溃疡性结肠炎(ulcerativecolitis,UC)肠纤维化的药效物质基础。方法将藏药湿生扁蕾用乙酸乙酯萃取的活性提取物以硅胶色谱分离、薄层定性得到的活性部位,分别灌胃用2,4,6-三硝基苯磺酸(trinitrobenzene sulphonic acid,TNBS)诱导的大鼠UC肠纤维化模型,采用荧光定量RT-PCR检测大鼠结肠组织胶原ⅠmRNA、胶原ⅢmRNA、α-SMAmRNA、E-cadmRNA的表达,筛选其活性成分。结果湿生扁蕾乙酸乙酯萃取物分离得到的活性部位经纯化得到4个单体化合物,用光谱分析等鉴定为1,8-二羟基-3,7-二甲氧基口山酮、1-羟基-3,7,8-三甲氧基口山酮、1,7-二羟基-3,8-二甲氧基口山酮和1-羟基-3,7-二甲氧基口山酮,4种单体化合物对UC肠纤维化大鼠模型均有明显的活性。结论湿生扁蕾抗UC肠纤维化的物质基础集中在乙酸乙酯部位,活性成分主要体现为4种口山酮类化合物。

Objective To study the bioactive constituents of Tibetan medicine Gentianopsis paludosa against UC fibrosis. Method Active fragment were obtained by silica gel and TLC from ethyl acetate active part which was extracted from Tibetan Gentianopsis paludosa. With the method of qRT-PCR,Collagen I,collagenⅢ,α-SMA,and E-cad were detected after treating model rats with active isolates to screen the active components. Result After Purified and identified from ethyl acetate part using spectroscopy,four monomer compounds（ 1,8-hydroxy-3,7-dimethoxy xanthones; 1-hydroxy-3,7,8-trimethoxysilane xanthones; 1,7-hydroxy-3,8-dimethoxy xanthones and 1-hydroxy-3,7-dimethoxy-xanthones）,had significant bioactive on UC fibrosis. Conclusion The material basis of Gentianopsis paludosa against fibrosis concentrated in parts of ethyl acetate,and the active ingredient mainly owed to four xanthones.