枸骨茎抗炎活性成分研究

Anti-inflammatory chemical constituents from the stem of Ilex cornuta Lindl.et Paxt

目的研究枸骨(Ilex cornuta Lindl.et Paxt)茎的抗炎活性成分。方法运用80%乙醇提取、大孔吸附树脂、正反相硅胶、Sephadex-LH20色谱柱等多种方法进行分离和纯化,根据理化性质和波谱数据进行结构鉴定。采用脂多糖(LPS)诱导的小鼠巨噬细胞RAW264.7的NO生成模型对部分化合物的抗炎活性进行测试。结果共分离得到10个化合物,经结构鉴定分别为α-香树脂醇(1)、齐墩果酸(2)、熊果酸(3)、羽扇豆醇(4)、menisdaurin(5)、lithospermoside(6)、槲皮素(7)、芦丁(8)、汉黄芩苷(9)、5,2′-二羟基-6,7,8,3′-四甲氧基黄酮(10)。测试了化合物2~8对LPS诱导的小鼠巨噬细胞RAW264.7的NO生成抑制活性。结论化合物5、6、9、10为首次从该植物中分离得到。化合物3和7能较明显地抑制LPS诱导的小鼠巨噬细胞RAW264.7的NO生成。

Objective To investigate the anti-inflammatory chemical constituents from the stem of Ilex cornuta Lindl.et Paxt.Methods The 80% EtOH extract of the stem of Ilex cornuta was purified by macro-porous adsorption resin chromatography,positive and negative silica gel chromatography,and Sephadex LH-20 chromatography.The structures of the purified compounds were determined by spectroscopic analysis and comparison with the reported data.Inhibitory effect of LPS induced mouse macrophage RAW264.7 on NO production was used to test the anti-inflammatory activity of compounds 2-8.ResultsTen compounds were isolated and their structures were determined asα-amyrin（1）,oleanolic acid（2）,ursolic acid（3）,lupeol（4）,menisdaurin（5）,lithospermoside（6）,quercetin（7）,rutin（8）,baicalin（9）,5,2′-dihydroxy-6,7,8,3′-tetra-methoxy flavone（10）.Conclusion Compounds 5,6,9,and10 were isolated from this plant for the first time.Compounds 3 and7 inhibited the NO production on LPS induced mouse macrophage RAW264.7 cell.