粗毛淫羊藿抗炎活性成分研究

Anti-inflammatory Constituents from Epimedium Acuminatum

目的:研究粗毛淫羊藿的抗炎活性组分。方法:用100 ng·mL^(-1) LPS诱导RAW264.7细胞建立炎症筛选模型,测定促炎细胞因子IL-1β、IL-6、iNOS的m RNA表达变化确定炎症的程度;采用多种色谱方法对粗毛淫羊藿抗炎活性部位进行分离纯化;采用~1H-NMR,13C-NMR,ESI-MS等方法,结合文献数据,鉴定化合物结构。结果:粗毛淫羊藿甲醇提取物经大孔吸附树脂吸附,80%甲醇洗脱得到总黄酮部位,抗炎活性筛选具有抗炎活性,从中分离得到6个黄酮类化合物(1-6),结构分别鉴定为大花淫羊藿苷B(1),4"-鼠李糖基淫羊藿次苷Ⅱ(2),淫羊藿次苷Ⅱ(3),脱水淫羊藿素(4),淫羊藿苷(5),4"-鼠李糖基淫羊藿次苷Ⅱ(6),其中化合物2,3,4为首次从粗毛淫羊藿中分离得到。这些化合物都具有一定的抗炎活性。结论:总黄酮和化合物(1-6)对LPS诱导升高的促炎因子表达均具有下调作用,说明黔产粗毛淫羊藿总黄酮具有一定的抗炎活性,其活性成分为其中的黄酮和黄酮苷。

Objective： To investigate the anti-inflammatory constituents from Epidemium acuminatum collected in Guiyang, Guizhou province. Method： the anti-inflammatory activity was screened on the LPS-stimulated RAW264.7 cells, and the active fraction of the methanol extracts was separated and purified by different chromatographic techniques. Structures of the yielded compounds were elucidated by 1H-NMR, 13C-NMR and ESI-MS methods, by comparison with the reported data. Results： The flavonoid traction of the methanol extracts was shown to be anti-inflammatory, and six flavonoids were isolated from it. The structures of the compounds（1-6）were identified as lkarisoside B（1 ）, 2＂-O-rhamnosyl icariside II（2）, lcarisid 11（3）, Anhydroicaritin（4）, Icariin（5）, Baohuoside 1 II （6）, compounds 3, 4, 6 were isolated from E. acuminatum for the first time, and all of the compounds showed anti-inflammatory activity. Conclusion： The expression of three pro-inflammation factors in the LPS-stimulated RAW264.7 cells was down-regulated by the total flavonoids of E. acuminatium and compounds I-6, showing that the anti-inflammatory activity of the plant were due to the flavonol and flavonol glycosides isolated from the extracts. K