小花异裂菊中的萜类成分及其活性

目的:研究异裂菊属Heteroplexis植物小花异裂菊的化学成分及其活性.方法:用乙醇提取后通过醋酸乙酯萃取、反复硅胶柱色谱、Pharmadex LH-20柱色谱以及反相HPLC柱色谱分离纯化;运用光谱数据解析鉴定化合物结构;采用人肿瘤细胞、MPP~+诱导PC12细胞损伤和多形核白细胞β葡萄糖苷酸酶释放药理模型筛选其活性.结果:从乙醇提取物的醋酸乙酯萃取部位中分离鉴定了17个萜类化合物,其中2个单萜类:(-)-龙脑阿魏酸酯(1)和黑麦交酯(2).7个倍半萜类:1β羟基-α-莎草酮(3),α-莎草醇(4),10α-hydroxycadin4-en-15-al(5),1-epi-10β-hydroxycadin-4-en-15-al(6),10α-hydroxyisodauc-3-en-15-al(7),大根香叶烯B(8)和mandassidione(9).5个二萜类:12-epi-bacchotricuneatin A(10),1-hydroxy-12-epi-bacchotricuneatinA(11),cleroinermin(12),desoxyarticulin(13)和anhydroolearin(14).3个三萜类:木栓酮(15),熊果酸(16)和obtusalin(17).化合物1对人胃癌细胞(BGC-823)显示一定的生长抑制作用,IC_(50)值为8.00×10~(-5)mol·L~(-1),活性强度与阳性对照喜树碱接近;在1×10~(-5)mol·L~(-1)浓度下,化合物12对MPP~+致PC12细胞损伤有保护作用,与模型组比较相对保护率为104.32%,有显著差异(P<0.001);在1×10~(-5)mol·L~(-1)浓度下,化合物2能抑制PAF刺激的多形核白细胞β葡萄糖苷酸酶释放,抑制率为52.7%(P<0.05).结论:化合物1～17均为首次从异裂菊属植物中分离鉴定;化合物1对人胃癌细胞具有选择性生长抑制活性,化合物12有神经细胞保护活性,化合物2具有潜在抗炎作用,其他化合物在测试浓度下在以上筛选模型中未显示明显活性.

Terpenoids of Heteroplexis micocephala and their bioactivities

Objective:To investigate the chemical constituents of Heteroplexis micocephala. Method:The constituents were isolated by using a combination of various chromatographic techniques including column chromatography over silica gel,Pharmadex LH-20,and C-18,as well as reversed-phase HPLC. Structures of the isolates were identified by spectroscopic data analysis. In vitro cytotoxic,neuroprotective,and anti-inflammatory activities were screened by using cell-based models. Result:Seventeen terpenoids were isolated. ...