清络通痹汤药效物质“组合筛选”库的制备

Establishment of "combinatorial screening" library of efficacy substances for Qingluo Tongbi Decoction

目的尝试建立具有"化学多样性"的中药复方药效物质组合库。方法依据中药复方药效物质"组合筛选"思路与方法,以目前报道对类风湿性关节炎具有确切疗效的清络通痹汤为研究体系,以该组方的药味重组合分组并运用膜分离法和大孔吸附树脂分离法等多种分离技术代替组合化学合成路线的多样性,以多种工业化分离技术的产物为"基本构造单元"形成"构件"以创建组合库。结果在制备组合库时,不同构件中的药效物质的量不同。AB-8树脂对青藤碱有较好的吸附和解吸作用,同时对皂苷也有很好的精制作用;各构件中奇任醇的量因组合不同而有一定的差异;各构件中都有较高量的总黄酮。结论配伍组合的不同和分离技术(制药工艺)的不同都能引起化学成分种类与数量的变化,因此需要借助一定的药效学实验对其制备进行评价,并筛选出相关的活性"构件"。

Objective Attempting to create a ＂chemical diversity＂ combinatorial library consisting of active components of Chinese materia medica compounds.Methods This paper was based on the theory of ＂thinking and method of ‘combinatorial screening’ of Chinese material medica compound＂,using the Qingluo Tongbi Decoction（QTD） which has exact effect against rheumatoid arthritis as system.Re-combination group of the formulation was used and various industrial separation techniques,such as resin and membrane,were used to replace the diversity of combinatorial chemistry synthetic route.Different products were used to establish combinatorial library using ＂Building Block＂.Results Different contents of active components in each ＂Building Block＂ were found during the establishment of combinatorial libraries.AB-8 resin had good adsorption and desorption functions on sinomenine,and good refined effects on saponin as well.The contents of kirenol were different in each ＂Building Block＂ of different combinations.Each ＂Building Block＂ had a relative high content of total flavonoids.Conclusion Different combinations and separation techniques lead the differences in types and contents of chemical constituents.So certain pharmacodynamic experiments are needed to evaluate the preparation and to filter out the relevant active ＂Building Blocks＂.