Lu Nian-Hua, Zhao Hui-Qiao, Jing Ming, Liu Xiong, Ren Chun-Zhen, Liu Xue-Feng, Liu Juan-Juan, Zhang Yan-Xia
Gansu University of Chinese Medicine, Lanzhou 730000, People's Republic of China.
Gansu University of Chinese Medicine, Lanzhou 730000, People's Republic of China.
Int Immunopharmacol. 2017 May;46:163-169. doi: 10.1016/j.intimp.2017.01.001. Epub 2017 Mar 11.
The current study focused on the pharmacodynamic activity components of Gentianopsis paludosa against ulcerative colitis (UC) fibrosis including symptoms of intestinal diarrhea and inflammatory. Trinitro-benzene-sulfonic acid induced UC model rats were gavaged with gradient polarity extracts respectively from ethanol-extract of Gentianopsis paludosa. Masson staining and qRT-PCR methods were respectively used to assess the degree of UC fibrosis and detect the mRNA expressions of collagen I, collagen III, a-smooth muscle actin (α-SMA) and E-cadherin in colon tissue. Separated by silica gel column chromatography, further screening was conducted until active components appeared. Infrared, nuclear magnetic resonance, mass spectroscopy and ultraviolet methods were applied to confirm active components' structures. The results indicated that the expression of collagen I, collagen III and α-SMA mRNA in the colon tissues of acetidin group rats was obviously depressed compared with control groups while E-cadherin displayed just opposite. Dyed in blue indicating UC fibrosis degree, the area of acetidin group was less than that other experimental groups. Four components: (1,8-Dihydroxy-3,7-Dimethoxyxanthones, 1-hydroxy-3,7,8-Trimethoxyxanthones, 1,7-Dihydroxy-3,8-Dimethoxyxanthones and 1-hydroxy-3,7-Dimethoxyxanthones), were obtained from acetidin group and all of which have a significant equivalence to Gentianopsis paludosa on the therapeutic effect of UC fibrosis. Our findings revealed the activity components for clinical application history of Gentianopsis paludosa and provided a preliminary foundation for further new drug research and exploitation.
本研究聚焦于湿生扁蕾抗溃疡性结肠炎（UC）纤维化的药效活性成分，包括肠道腹泻和炎症症状。采用三硝基苯磺酸诱导UC模型大鼠，分别灌胃给予湿生扁蕾乙醇提取物的不同极性梯度提取物。分别采用Masson染色和qRT-PCR方法评估UC纤维化程度，并检测结肠组织中I型胶原、III型胶原、α-平滑肌肌动蛋白（α-SMA）和E-钙黏蛋白的mRNA表达。通过硅胶柱色谱分离，进一步筛选直至出现活性成分。应用红外、核磁共振、质谱和紫外方法确证活性成分的结构。结果表明，与对照组相比，乙酸乙酯组大鼠结肠组织中I型胶原、III型胶原和α-SMA mRNA的表达明显降低，而E-钙黏蛋白则相反。乙酸乙酯组蓝色染色显示UC纤维化程度，其面积小于其他实验组。从乙酸乙酯组中获得了4种成分：（1,8-二羟基-3,7-二甲氧基呫吨酮、1-羟基-3,7,8-三甲氧基呫吨酮、1,7-二羟基-3,8-二甲氧基呫吨酮和1-羟基-3,7-二甲氧基呫吨酮），所有这些成分在UC纤维化治疗效果上与湿生扁蕾具有显著等效性。我们的研究结果揭示了湿生扁蕾临床应用历史中的活性成分，为进一步的新药研发提供了初步基础。
