基于"味效相应"的江西道地药材枳实质量评价方法研究

Considering how to interpret the scientific connotation of traditional identification method and establish the modern quality standard of TCM, we put forward a hypothesis of "flavor-effect inter relation" based on the five flavors theory and the practice that TCM was identified and was used for treating illnesses according to its taste and flavor, 'flavor' indicated both taste and action in the treatment can be used as a kind of bridge to connect modern science to the theory of TCM. This project will provide a new way to solve the above two difficulties..Jiangxi Aurantii Fructus Immaturus constituents were looked as a set, this set will be divided into three taste subsets-fragrance (essential oils), acid (organic acid group) and bitter ( flavone, alkaloid, triterpene group) according to the level of "taste". The Fingerprints of three taste subsets will be studied, through profile-effect between chemical fingerprints information and pharmacodynamics of combination of above three subsets we can get three effective flavor subsets-pungent flavor which has an action of promoting circulation to treat thoracic fullness, acid flavor that has absorbing action and can used to treat uterus and bitter flavor which has the effects of promoting defecation to treat indigestion and fullness. The project will be of significance in inheriting the traditional identification method, establishing the modern quality standard of TCM，developing the theory of tradition Chinese medicine and the utilization of Jiangxi Aurantii Fructus Immaturus.

针对如何阐明经验鉴别的科学内涵、如何建立具有中医药特色的现代中药质量标准这两个难题；本课题根据五味理论和"依味辨药"、"依味用药"的实践特点，提出"味效相应"假说，以"味"这一标志药材特性和疗效双重内涵的概念作为架通现代科学和传统中医药理论的桥梁，探索解决这两个问题的新途径。.选取江枳实为例，将其成分集合从"味"的层面采用化学方法拆分为"清香"（挥发油组分）、"酸"（有机酸组分）、"苦"（黄酮、生物碱、三萜等组分）三种"性状味子集"并采用色谱技术获取相应化学指纹信息；组合还原后进行体内药效学研究，通过"谱效"关系分析，找出枳实在治疗胸痞、积食胀满、阴挺中发挥的"辛能行"、"苦能泄"和"酸能收敛"三种作用的"功效味子集", 并以"功效味子集"为质控指标，建立具有中医药特色的枳实"味-效图谱"鉴定方法。对继承传统经验、建立现代中药质量标准、发展中医药理论以及江枳实的开发利用具有重要意义。

本课题从枳实的主要来源酸橙Citrus aurantium L.中分离鉴定了52个化合物，其中新化合物5个，21个化合物为首次从该植物中发现；通过感官评价研究了化学成分的味感属性，除黄酮、柠檬苦素、生物碱外，香豆素类如水合橙皮内酯亦是枳实苦味物质之一；利用HPLC、UPLC以及GC-MS建立不同产地不同采收期枳实中苦味、芳香物质的含量测定方法及指纹图谱；“辛、苦、酸”三种“性状味”的提取部位、成分对小鼠在体肠胃运动均有调节作用，对小鼠离体子宫自主性收缩均有抑制作用，较高剂量均能增强大鼠离体血管的张力，表明枳实的“性状味”与“功效味”之间存在密切联系，但并非简单的一对一映射，而是复杂的多对多关系。