基于中药超分子化学探究大黄-黄连配伍平和“苦-寒”之性物质基础

Material basis of Rhei Radix et Rhizoma-Coptidis Rhizoma combination in alleviating "bitter-cold" properties based on supramolecular chemistry of Chinese medicine

基于中药超分子化学探究均为苦寒之性的大黄-黄连配伍后,药性反而趋于平和的物质基础。采用动态光散射法、扫描/透射电镜表征大黄-黄连合煎液中超分子的形态学特征。通过超高效液相色谱-质谱联用技术测定超分子部位化学成分组成及该部位和黄连单煎液药效成分溶解释放过程,并利用感官评价、电子舌、小鼠腹泻模型和病理指标评价大黄-黄连单煎液与配伍合煎液的“苦-寒”药性差异。大黄-黄连共煎煮时蒽醌/鞣质类成分与生物碱类成分相互作用聚集形成尺度为400 nm左右的超分子,超分子的存在延缓以小檗碱为代表的有效成分溶解释放过程;与单味药(灌胃4 g·kg^(-1))苦寒之性峻猛相比,二者配伍(灌胃8 g·kg^(-1))“苦-寒”之性得到明显缓和。大黄-黄连配伍合煎中有效成分相互作用形成超分子,影响中药汤剂有效组分的溶解、释放过程进而缓和“苦寒”之性,这为揭示大黄-黄连配伍科学内涵提供新的思路。

The present study aimed to explore the material basis of Rhei Radix et Rhizoma-Coptidis Rhizoma combination in alleviating “bitter-cold” properties based on the supramolecular chemistry of Chinese medicine.Dynamic light scattering and scanning/transmission electron microscopy were used to characterize the morphological characteristics of supramolecules in the decoction of Rhei Radix et Rhizoma and Coptidis Rhizoma.The chemical composition of supramolecules, as well as the dissolution and release processes of supramolecules and the medicinal components of Coptidis Rhizoma decoction, was determined by the high-performance liquid chromatography-mass spectrometry.The differences in "bitter-cold" medicinal properties between Rhei Radix et Rhizoma decoction, Coptidis Rhizoma decoction, and co-decoction were analyzed by sensory evaluation, electronic tongue, mouse diarrhea model, and pathological indicators.The anthraquinones/tannins and alkaloids interacted to form supramolecules with a scale of about 400 nm when Rhei Radix et Rhizoma and Coptidis Rhizoma were decocted together, which delayed the dissolution and release of the active components represented by berberine. Compared with the consequence of single drug administration at 4 g·kg^(-1), the combination of the two drugs at 8 g·kg^(-1)significantly alleviated the "bitter-cold" properties.The effective components interacted to form supramolecules in the co-decoction of Rhei Radix et Rhizoma and Coptidis Rhizoma, which affected the dissolution and release of the effective components of Chinese medicinal decoction, thereby alleviating the "bitter-cold" properties.The findings of this study provide a new idea for revealing the scientific compatibility of Rhei Radix et Rhizoma and Coptidis Rhizoma.