华蟹甲中的抗炎活性成分研究

Anti-inflammatory activity compounds from Sinacalia tangutica

目的研究华蟹甲中的抗炎活性成分。方法将活性追踪方法与现代分离技术相结合,从华蟹甲全草的乙醇粗提物中分离得到活性化合物。使用脂多糖诱导小鼠单核巨噬细胞RAW 264.7成炎症模型评价所分离化合物的抗炎活性。结果从华蟹甲全草的乙醇提取物中分离得到9个具有抗炎活性(P<0.05)的倍半萜类化合物,分别将其鉴定为3-isobutyroyloxy-7H-eremophila-9,11-dien-8-one、3-angeloyloxy-7H-eremophila-9,11-dien-8-one、isopetasin、isopetasol、6a-hydroxy-4(15)-eudesmen-1-one、4(15)-eudesmene-1β,6α-diol、(7R)-opposit-4(15)-ene-1β,7-diol、oplodiol、kobusone。其中化合物1、5、8的抗炎活性较好且表现出浓度依赖性(P<0.05),其抑制NO生成的IC50分别为(12.03±0.61)、(73.81±2.41)、(60.0±2.35)μmol/L。结论华蟹甲中的抗炎活性成分主要为倍半萜类化合物,特别是化合物1、5、8为主要的活性化合物。

Objective To explore the anti-inflammatory activity of compounds from Sinacalia tangutica.Methods The bioactive guiding method and modern separation techniques were used to isolate compounds with anti-inflammatory activity from the ethanol crude extract of Sinacalia tangutica.The anti-inflammatory activity of the isolated compounds was evaluated by using a lipopolysaccharide induced inflammation model in RAW 264.7 macrophages.Results Nine sesquiterpenoids with anti-inflammatory activity(P<0.05)were isolated from the ethanol crude extract of Sinacalia tangutica,and identified as 3-isobutyroyloxy-7H-eremophila-9,11-dien-8-one,3-angeloyloxy-7H-eremophila-9,11-dien-8-one,isopetasin,isopetasol,6a-hydroxy-4(15)-eudesmen-1-one,4(15)-eudesmene-1β,6α-diol,(7R)-opposit-4(15)-ene-1β,7-diol,oplodiol,and kobusone.Compound 1,5,and 8 showed considerable anti-inflammatory activities(P<0.05),with the IC50 of(12.03±0.61),(73.81±2.41),(60.0±2.35)μmol/L,respectively.Conclusion The anti-inflammatory active compounds in Sinacalia tangutica are mainly sesquiterpenoids,especially compound 1,5,and 8,which are the main active compounds.