中药水煎液自组装聚集体研究面临的问题初探

Challenges in the study of self-assembled aggregates in decoction of traditional Chinese medicine:A preliminary review

汤剂是中医临床用药的常用剂型。中药水煎液自组装聚集体(self-assembled aggregates in decoction,SADs)是指在煎煮过程中,中药活性成分受热运动剧烈,在氢键、π-π堆积、疏水相互作用、静电作用等分子作用力下自组装形成的颗粒、凝胶、纤维等聚集体。研究发现SADs普遍存在于中药水煎液中,并可发挥优于有效单体或其物理混合物的生物活性,从成分互作-相态结构角度为揭示中药药效物质基础提供新的思路,现已成为研究热点。本文总结归纳近年相关研究,发现水煎液体系的多分散性、煎煮过程中活性成分相互作用的不稳定性、聚集体自组装规律的未知性、产品物理化学稳定性、纯度与产率等问题在研究中值得关注,并提出解决思路和未来研究展望,以期为SADs的综合开发和临床应用提供参考。

Decoction is the most commonly used dosage form in the clinical treatment of traditional Chinese medicine(TCM).During boiling,the violent movement of various active ingredients in TCM creates molecular forces such as hydrogen bonding,π-πstacking,hydrophobic interactions and electrostatic interactions,which results in the formation of self-assembled aggregates in decoction(SADs),including particles,gels,fibers,etc.It was found that SADs widely existed in decoction with biological activities superior to both effective monomers and their physical mixtures,providing a new idea to reveal the pharmacodynamic material basis of Chinese herbal medicine from the perspective of component interactions-phase structure.Recently,SADs have become a novel focus of research in TCM.This paper reviewed their relevant studies in recent years and found some issues to be concerned in the research,such as the polydispersity of decoction system,instability of active ingredient interactions during boiling,uncertainty of the aggregates self-assembly rules,and stability,purity,yield of the products.In this regard,some solutions and new ideas were presented for the integrated development and clinical application of SADs.