Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Republic of Korea.
Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5. doi: 10.1016/j.bmcl.2009.11.109. Epub 2009 Nov 26.
Five iridoid glycosides were isolated from the MeOH extract of Hedyotis diffusa, and their structures were elucidated as E-6-O-p-methoxycinnamoyl scandoside methyl ester (1), Z-6-O-p-methoxycinnamoyl scandoside methyl ester (2), E-6-O-p-feruloyl scandoside methyl ester (3), E-6-O-p-coumaroyl scandoside methyl ester (4), and Z-6-O-p-coumaroyl scandoside methyl ester (5) by interpretation of their spectroscopic data. All the isolated compounds were evaluated for human neutrophil elastase inhibitory effect, and compound 1 showed potent activity with an IC(50) value of 18.0muM. The molecular docking simulation suggested a structural model for the inhibition of human neutrophil elastase by compound 1.
从白花蛇舌草的甲醇提取物中分离得到 5 个环烯醚萜苷类化合物，并通过波谱数据分析鉴定它们的结构为 E-6-O-对甲氧基肉桂酰獐牙菜苷甲酯（1）、Z-6-O-对甲氧基肉桂酰獐牙菜苷甲酯（2）、E-6-O-对阿魏酰獐牙菜苷甲酯（3）、E-6-O-对香豆酰獐牙菜苷甲酯（4）和 Z-6-O-对香豆酰獐牙菜苷甲酯（5）。所有分离得到的化合物均进行了人中性粒细胞弹性蛋白酶抑制活性评价，化合物 1 表现出较强的活性，IC50 值为 18.0μM。分子对接模拟为化合物 1 抑制人中性粒细胞弹性蛋白酶的结构模型提供了依据。
