A Kampo prescription usually consists of several crude drugs and contains many kinds of compounds. Physicochemical interactions between the compounds may occur in the process of decoction, by which Kampo prescriptions are usually prepared for ingestion, and the interactions may change the extraction yields of the constituents. Berberine and baicalin have been reported to form precipitates. Orengedokuto, which consist of Coptis Rhizome, Gardenia Fruit, Phellodendron Bark and Scutellaria Root, has been a representative Kampo prescription used to treat inflammatory diseases. In our previous papers, we revealed that the precipitates formed in the decoction of orengedokuto without Gardenia Fruit mainly consists of berberine–baicalin complex and that Gardenia Fruit reduced the amount of the precipitates in orengedokuto decoction. In this report, through solubility-enhancement assay based on HPLC, we identified crocins as the constituents of Gardenia Fruits, which enhanced the solubility of berberine–baicalin complex. All-trans crocin-1 (1) and 13-cis crocin-1 (5) showed high activities among the isolated crocins, and the number of glucosyl groups in the molecule seemed correlated with the activity. As berberine and baicalin were reported as the anti-inflammatory constituents of Coptis Rhizome and Phellodendron Bark, and Scutellaria Root, respectively, Gardenia Fruit contributes anti-inflammatory activity of orengedokuto by increasing solubilities of anti-inflammatory constituents of the other component crude drugs in the prescription. Our result will add a scientific basis to the understanding of the effectiveness of orengedokuto as a whole.

一份汉方方剂通常由几种生药组成，并含有多种化合物。化合物之间的物理化学相互作用可能发生在煎剂过程中，汉方方剂通常通过煎剂进行摄取，相互作用可能会改变成分的提取率。据报道，小檗碱和黄芩苷会形成沉淀。由黄连、栀子、黄柏和黄芩组成的五味子是治疗炎症性疾病的代表性汉方方剂。在我们之前的论文中，我们揭示了在没有栀子果实的煎药汤中形成的沉淀物主要由黄连素-黄芩苷复合物组成，并且栀子果实减少了煎药中沉淀物的量。在这份报告中，通过基于 HPLC 的溶解度增强测定，我们确定了藏红花素是栀子果实的成分，它增强了小檗碱-黄芩苷复合物的溶解度。全部-trans crocin-1 ( 1 ) 和 13 - cis crocin-1 ( 5 ) 在分离的 crocins 中表现出较高的活性，分子中的葡萄糖基数似乎与活性相关。据报道，黄连、黄柏和黄芩的抗炎成分分别为黄连素和黄芩苷，栀子果实通过增加其他成分生药的抗炎成分的溶解度来促进五棱芥的抗炎活性。处方。我们的结果将为理解整个 orengedokuto 的有效性提供科学依据。