Department of Pharmacognosy, Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto, 607-8412, Japan.
Department of Analytical Chemistry, Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto, 607-8414, Japan.
J Nat Med. 2020 Mar;74(2):421-433. doi: 10.1007/s11418-019-01382-9. Epub 2020 Jan 1.
It has been reported that Sanoshashinto (SanHuangXieXinTang, ), which is composed of Rhei Rhizoma, Scutellariae Radix, and Coptidis Rhizoma, exhibits vasorelaxant effects in vitro and lowers blood pressure of patients. Based on this discovery, in this study, a mixture containing those three materials and combinations of them were extracted with methanol, and the extracts were fractionated into different parts. Effects of all extracts and fractions on high concentration of potassium chloride (High K)- or noradrenaline (NA)-induced contractions of isolated rat aortic rings or helical strips were examined. Qualitative and quantitative HPLC analyses of the extracts and the fractions revealed that the contents of baicalin and berberine in Sanoshashinto methanol extract (SHXXTM) were higher than those of the other constituents. All pharmacological and HPLC data were analyzed by principal component analysis (PCA) software and the results indicated that baicalin, berberine, palmatine, baicalein, and wogonoside contributed significantly to the pharmacological activity. Furthermore, spontaneously hypertensive rats (SHRs) that were orally given SHXXTM or a baicalin-berberine combination showed significantly reduced increase in the rate of systolic blood pressure (SBP) compared to the control group. These findings suggested that Sanoshashinto has significant vasorelaxant effects in vitro and antihypertensive effects in vivo, and baicalin and berberine, which were the principal constituents of Scutellariae Radix and Coptidis Rhizoma, were the main antihypertensive constituents in Sanoshashinto. It was speculated that baicalin and berberine produced vasorelaxant effects by activating the NO/cGMP pathway and that the BK channel and the DAG/PKC/CPI-17 pathway were also involved.
据报道，由大黄、黄芩和黄连组成的三黄泻心汤在体外具有血管舒张作用，并降低高血压患者的血压。基于这一发现，本研究用甲醇提取了含有这三种材料的混合物以及它们的组合，并将提取物分为不同的部分。考察了所有提取物和馏分对分离的大鼠主动脉环或螺旋条高浓度氯化钾（高 K）或去甲肾上腺素（NA）诱导收缩的影响。提取物和馏分的定性和定量 HPLC 分析表明，三黄泻心汤甲醇提取物（SHXXTM）中黄芩苷和小檗碱的含量高于其他成分。所有药理和 HPLC 数据均由主成分分析（PCA）软件进行分析，结果表明黄芩苷、小檗碱、巴马汀、黄芩素和甘草苷对药理活性有重要贡献。此外，口服给予 SHXXTM 或黄芩苷-小檗碱混合物的自发性高血压大鼠（SHRs）的收缩压（SBP）升高率明显低于对照组。这些发现表明，三黄泻心汤在体外具有显著的血管舒张作用，在体内具有降压作用，黄芩苷和小檗碱是黄芩和黄连的主要成分，是三黄泻心汤的主要降压成分。据推测，黄芩苷和小檗碱通过激活 NO/cGMP 途径产生血管舒张作用，BK 通道和 DAG/PKC/CPI-17 途径也参与其中。
