姜“炒炭存性”超分子客体“印迹模板”变化规律的研究

Traditional Chinese medicine(TCM) is a huge complex biological supramolecular, its active ingredients group is the guest molecule, also "imprinting template", the inactive component is herb residue, also the host molecule. In the early stage of the research project "The research of the relationship between the processing temperature and chemical composition of different processed products of ginger", found that, Supramolecular chemistry has a special role in explaining the processing mechanism of Chinese herbal pieces. So we deduced that, the processing technology of Chinese herbal pieces is a pharmaceutical technology essentially, which used to process the biological supramolecule, host molecule was destructed in the process of carbonizing, but guest molecule was retained, the change of the host-guest molecules was controlled by "imprinting template", which reflected the extent of change in potency and efficacy.In this project, ginger is the model drug, supramolecular chemistry as the breakthrough point.Through the study on the characteristics of "imprinting template", the change rule of host and guest molecule, and the influence of the supramolecular structure on the hemostatic effect before and after ginger processing, to clarify the supramolecular mechanism of TCM carbonizing process, in order to provide experimental basis for further clarify the hemostatic effect principle of TCM, lay the foundation for the carbonizing process and unified carbon medicine quality standard.

中药材为巨复生物超分子体，其有效成分群为客体小分子，亦“印迹模板”，无效成分为药渣，亦主体分子。在课题组前期项目“炮制火候与姜不同炮制品化学成分映对关系的研究”中，发现超分子化学对诠释中药饮片的炮制机理有特殊的作用。故推理出“中药饮片炮制本质上就是对生物超分子体的加工制药技术，中药“炒炭存性”炒的是主体分子，存的是客体分子，主客体分子的变化规律受控于“印迹模板”，反映到饮片药性与药效的变化程度上”假说。本项目以姜为模型药物，通过对姜炒炭前后超分子“印迹模板”特征、主客体变化规律及其止血作用影响的研究，阐明中药炮制“炒炭存性”的超分子原理，为进一步阐明中药炒炭后产生或增强止血作用的机理提供依据，为规范炮制炒炭工艺和统一炭药质量标准奠定基础。

本项目基于中医药超分子“气析”理论，对干姜炒炭前后超分子“印迹模板”变化特征进行研究。通过色差值测定结果确定了干姜炒制前后外观性状变化的量化标准为：干姜、炮姜、姜炭的E*ab依次为79.77、67.31、50.66；通过不同炮制温度、炮制时间与物质量变的热力学与动力学关系，以姜炭特征性“印迹模板”乙酸香叶酯为例成功地进行了验证；采用GC-MS对干姜、炮姜、姜炭挥发油客体成分进行检测分析，以大样本逼近法确定了三者的特征性“印迹模板”分别为30、37、7个，且发现了中药特征性“印迹模板”数量随批次增多而趋于稳定的规律；根据总量统计距原理计算得到干姜、炮姜、姜炭的一阶矩、二阶矩平均值依次为29.15、30.04、29.53min和38.87、30.08、 41.68min2，提示三者色谱印迹行为具有差异性；以总体平均MCIs相似度评价筛选出不同火候姜炭的客体成分，计算得干姜、轻炭、标准炭、重炭的客体成分数及平均MCIs依次为27、24、36、27和3.683、4.052、4.163、3.872，说明MCIs可量化表征炒炭程度；考察干姜炒制前后对虚寒性缺血证SD大鼠凝血五项及TXB2和6-keto-PGF1α的影响，与空白组、模型组相比较，干姜炒炭能显著缩短虚寒性出血证大鼠凝血时间。综上，本项目从干姜炒炭前后性状变化、印迹行为差异、“印迹模板”特征、药效关联等多角度阐述中药“炒炭存性”的科学内涵，为炭药炮制机理的研究提供了新的思路与方法。