基于谱效关系表达的中药川芎药效物质筛选

Study of effective substances screening for Ligusticum Chuanxiong Hort.based on spectrumeffect relationship

目的:以犬心肌缺血模型为对象,研究中药川芎对犬心肌缺血保护作用谱效关系及药效物质基础。方法:在建立中药川芎液相特征指纹图谱分析方法的基础上,采用结扎犬冠状动脉致急性心肌缺血的模型,运用双变量相关分析和多元回归分析,将川芎提取物药效数据与特征指纹图谱的共有峰的相对峰面积相关联,研究药物治疗心肌缺血作用的物质基础及谱效关系。结果:研究证实川芎内酯,藁苯内酯,川芎嗪,阿魏酸均与药效呈显著正相关,其中川芎嗪、阿魏酸可显著降低血清中乳酸等浓度的升高,藁本内酯可显著降低血清FFA升高,是中药川芎治疗心肌缺血的主要有效成分。结论:通过谱效关系研究获得了药效活性物质,建立了川芎药材谱效关系评价的方法,客观反映了药物内在质量,为该类中药的创新研究提供了借鉴。

OBJECTIVE To study the protective effect of Ligusticum Chuanxiong Hort. on myocardial ischemia dog model, in order to reveal the spectrum-effect relationship and the effective substances. METHODS The HPLC fingerprint of Ligustic- um Chuanxiong Hort. was established, and then the myocardial ischemia dog model was induced by ligation of the canine coro- nary. After that, the spectrum-effect relationship and the effective substances of Ligusticum Chuanxiong Hort. were investiga- ted by bivariate correlations analysis and multiple regression analysis. RESULTS The main effective components of Ligusticum Chuxznxiong Hort. were tetramethylpyrazine,ferulic acid and ligustilide. The tetramethylpyrazine and ferulic acid decreased the plasma lactic acid concentration, while ligustilide increased FFA concentration significantly. CONCLUSION Through the re- search on spectrum-activity relationship, we directly obtained the active substances and established the new method to evaluate Ligusticum Chuanxiong Hort. Our research provided a new strategy for the further research of traditional Chinese medicine.