“配伍法则·拼合原理”在中药新药研发中的应用

Discovering leading compounds of new drugs in traditional Chinese medicine from classic formula via combination principle

中药配伍法则为中药复方理论的精华,复方配伍产生的中药多成分、多靶点、多途径的治疗作用为中药新药研发提供了理论指导和实践依据.中药复方的配伍原则和化药设计中的结构拼合原理均是将不同的药物单元按照一定的法则有机组合,以期达到增效、减毒的目的.受此启发,将配伍法则与拼合原理相结合,从经典药对中选择有效成分进行拼合,进而发现可开发为临床新药的先导化合物.本文介绍了相关研究中"配伍法则·拼合原理"成功结合的典型实例,本思路将在中药有效成分及新药先导化合物开发中得到更广泛的应用.

Compatibility theory is the essence of Traditional Chinese Medicine（TCM） formulations. It provides efficacy in clinic with multi-components, multi-targets, multi-approaches and inspires TCM research as a theoretical guidance and practical basis. While compatibility of TCM consists of various single Chinese herbal medicine, the structure combination principle unites different components via certain rules of chemical synthesis in order to achieve effect improvement and poison reduction as well. By combining the ＂compatibility theory＂ and ＂combination principles＂, active ingredients of TCM were chosen as chemical components and a series of synthetic products were obtained as leading compounds. In this paper, typical cases were mainly introduced, furthermore, results of relevant research showed that this method has further practical meaning and it will be widely used in new-drug discovering study of TCM.