1,6-<i>O</i>,<i>O</i>-二酰基大花旋覆花内酯衍生物的合成及其抑制NO生成活性

1,6-O,O-二酰基大花旋覆花内酯衍生物的合成及其抑制NO生成活性

摘要: 以从旋覆花中提取分离得到的1-O-乙酰基大花旋覆花内酯(ABL)为原料，经酯化反应或还原反应制备了8个1，6-O，O-二酰基大花旋覆花内酯(OABL)衍生物(化合物 1 ~ 8 )，并测定其对脂多糖(LPS)诱导的巨噬细胞一氧化氮(NO)生成的抑制作用，评价其抗炎活性。结果表明，化合物 5 ~ 8 具有良好的抑制NO生成活性(IC₅₀<；2 μmol/L)，其活性水平较先导化合物OABL显著提高。

Abstract: Eight 1, 6-O, O-diacetylbritannilactone(OABL)derivatives(compounds 1 - 8 )were synthesized by esterification or reduction of 1-O-diacetylbritannilactone(ABL)isolated from Inula japonica. All derivatives were evaluated for their anti-inflammation activities through the determination of inhibition of nitric oxide(NO)production in lipopolysaccharide(LPS)-induced macrophages. As results, compounds 5 - 8 (IC₅₀< 2 μmol/L)exhibited more potent inhibition of NO production activities than the lead compound OABL.