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目的:探讨玄参化学成分和药理活性关系。方法:应用大孔树脂、葡聚糖凝胶和正、反相硅胶等层析方法,摸索多种溶剂系统对玄参中含量高的水溶性成分进行分离,应用化学和光谱方法鉴定结构。观察分离得到的主要单体成分对大鼠腹腔中性白细胞中花生四烯酸(AA)代谢产物白三烯B4(LTB4)的影响,及对阈剂量的二磷酸腺苷,AA和20nmol/LPAF诱导的血小板聚集的抑制作用。结果:共分得11种玄参水溶性成分,发现它们属于环烯醚萜甙和苯丙素甙类型。药理实验中苯丙素甙XS-8,XS-10在0.5mmol/L时对LTB4产生较强抑制作用;环烯醚萜甙XS-6,XS-7在相同条件下作用较弱。苯丙素甙和环烯醚萜甙在0.5mmol/L时,对体外诱导的血小板聚集都有不同程度的作用,但苯丙素甙的作用强于环烯醚萜甙。结论:玄参中的苯丙素甙和环烯醚萜甙成分与玄参的抗炎和抗血小板聚集作用有关。
Objective: To investigate the relationship between chemical composition and pharmacological activity of Radix Scrophulariae. METHODS: Macroporous resin, dextran gel, and positive and reversed-phase silica gel chromatography methods were used to explore a variety of solvent systems for the separation of water-soluble components with high content in Scrophulariae. Structures were identified by chemical and spectral methods. Observed the effects of the main monomer components isolated on leukotriene B4 (LTB4), a metabolite of arachidonic acid (AA) in rat peritoneal neutrophils, and a threshold dose of adenosine diphosphate, AA and 20 nmol/LPAF Inhibition of platelet aggregation induced. Results: A total of 11 water-soluble constituents of Scrophulariae were identified and they were found to be of the type iridoid and phenylpropanoid quinones. In the pharmacological experiments, the phenylpropanoid oxime XS-8 and XS-10 produced a strong inhibitory effect on LTB4 at 0.5 mmol/L. The iridoid oxime XS-6 and XS-7 showed weaker effects under the same conditions. When phenylpropanoid hydrazine and iridoid oxime were 0.5mmol/L, they had different effects on platelet aggregation induced in vitro, but the effect of phenylpropanoid quinone was stronger than that of iridoid hydrazine. CONCLUSION: The components of phenylpropanoid quinone and iridoid in Scrophulariae are related to the anti-inflammatory and anti-platelet aggregation effects of Scrophulariae.