中文摘要
中药材化学成分复杂,因传统研究模式周期长、难度大,导致多数中药材有效成分不清楚;中药有效部位的开发是中药材利用的重要途径,存在成分组成和比例不清、忽视非有效部位的协同作用等问题,以致质量控制水平不高,疗效难以充分发挥。探索一种快速、简便筛选优化中药材有效成分群及其比例的方法,具有很好的理论和实际意义。本项目首次将肠吸收谱-效相关法应用于中药材有效成分研究中,在前期对蜘蛛香深入研究基础上,采用液质联用技术,通过在体单向肠灌流、离体外翻肠囊吸收试验及抗焦虑药效学试验,获得药物谱、肠吸收谱与药效谱,采用偏最小二乘回归法及均匀设计-支持向量机非线性模型-进化多目标优化三联法,筛选优化有效成分群的量及比例并进行药效学验证,明确蜘蛛香抗焦虑有效成分群,验证一种在不进行化学系统分离,不过多涉及药物分布、代谢、排泄过程的情况下,快速筛选优化中药材有效成分群及比例的新方法,为其他中药材有效成分研究提供借鉴。
英文摘要
The chemical constituents of traditional Chinese medicinal materials are complex. The active ingredients of Chinese medicinal materials is not clear because of the traditional research modes are long and difficult. The development of effective components of traditional Chinese medicine is an important way to use Chinese medicinal materials, but the composition and proportion of components is not clear and the synergistic effect of non-effective parts is ignored, resulting in the quality control is not high and the effect is difficult to play. It has good theoretical and practical significance to explore a rapid and simple method for optimization and screening of effective ingredients group and the proportion of Chinese medicinal materials. It is the first time to apply the intestinal absorption spectrum effect relationship to the study of the active ingredients of Chinese medicinal materials in this project. In this study, we obtain the drug spectrum, intestinal absorption spectrum and drug effect spectrum by using the method of LC-MS, in vivo intestinal perfusion, in vitro everted sac absorption test and anti-anxiety pharmacodynamic test on the basis of early intensive research of Valeriana jatamansi Jones. Screen and optimize the amount and proportion of effective ingredients group and pharmacodynamics validation by using PLSR and UDM-SVM-EMO triplex-process optimization method. Clear the effective ingredients group and verify a new method for rapid screening effective ingredients group of Chinese medicinal materials without involving in chemical separation system, drug distribution, metabolism and excretion process. This will provide a reference for the effective component research of other Chinese medicinal materials.
