Diabetic Complications Research Center, Division of Traditional Korean Medicine Integrated Research, Korea Institute of Oriental Medicine, Daejeon, Korea.
J Sep Sci. 2010 Mar;33(4-5):582-6. doi: 10.1002/jssc.200900693.
Two bioactive flavonol glucosides, hyperoside and quercitrin, were successfully isolated in one step from the phytochemically unknown medicinal plant Osteomeles schwerinae by high-speed counter-current chromatography using a two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water (0.5:5.5:1.5:4.5 v/v). From 160 mg of crude extract, 2.1 mg of hyperoside (98.6% purity, 83.3% recovery) and 4.5 mg of quercitrin (99.2% purity, 81.7% recovery) were separated and then their chemical structures were identified by (1)H and (13)C NMR analysis. In addition, the isolates were subjected to an in vitro bioassay to evaluate their inhibitory activity on rat lens aldose reductase. Both quercitrin and hyperoside showed excellent inhibitory activities toward rat lens aldose reductase with the IC(50) values of 0.16 and 4.33 microM, respectively, as compared with positive control, 3,3-tetramethyleneglutaric acid (28.7 microM). So far, chemical constituents and biological activities of O. schwerinae have never been reported. This is the first report on the chemical constituents and biological activity of this plant using semi-preparative high-speed counter-current chromatography separation technique.
两种具有生物活性的黄酮醇葡萄糖苷，根皮苷和槲皮素，成功地从植物化学未知的药用植物缬草中通过高速逆流色谱法一步分离出来，使用由正己烷-乙酸乙酯-甲醇-水（0.5：5.5：1.5：4.5 v/v）组成的两相溶剂系统。从 160mg 粗提物中，分离出 2.1mg 根皮苷（纯度 98.6%，回收率 83.3%）和 4.5mg 槲皮素（纯度 99.2%，回收率 81.7%），然后通过（1）H 和（13）C NMR 分析鉴定其化学结构。此外，对分离得到的化合物进行了体外生物测定，以评估其对大鼠晶状体醛糖还原酶的抑制活性。与阳性对照 3,3-四亚甲基戊二酸（28.7 microM）相比，槲皮素和根皮苷对大鼠晶状体醛糖还原酶均表现出优异的抑制活性，IC50 值分别为 0.16 和 4.33 microM。到目前为止，缬草的化学成分和生物活性从未被报道过。这是首次使用半制备高速逆流色谱分离技术对该植物的化学成分和生物活性进行报道。
