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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、PharmadexLH-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-hydroxycadin-4-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-bacchotricuneatinA(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,IC50值为8.00×10-5mol·L-1,活性强度与阳性对照喜树碱接近;在1×10-5mol·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1×10-5mol·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。
Objective: To study the chemical constituents and activities of Heteroplexis genus Heteroplexis. Methods: After extracted with ethanol, the compounds were isolated and purified by ethyl acetate, repeated silica gel column chromatography, Pharmadex LH-20 column chromatography and reverse phase HPLC column chromatography. The structures of the compounds were identified by spectral data analysis. The injury of PC12 cells was induced by human tumor cells and MPP + Polymorphonuclear leukocyte β-glucuronidase release pharmacological model for screening of its activity. Results: Seventeen terpenoids were isolated and identified from the ethyl acetate extracts of ethanol extract. Among them, two monoterpenes: (-) - borneol ferulate (1) and rye lactide (2) . 7 sesquiterpenes: 1β-hydroxy-α-sesvlatan (3), α-sesamin (4), 10α-hydroxycadin-4-en- hydroxycadin-4-en-15-al (6), 10α-hydroxyisodauc-3-en-15-al (7), germacrene B (8) and mandassidione (9). Five diterpenoids: 12-epi-bacchotricuneatin A (10), 1-hydroxy-12-epi-bacchotricuneatin A (11), cleroinermin (12), desoxyarticulin (13) and anhydroolearin (14). Three triterpenes: Corydosterone (15), ursolic acid (16) and obtusalin (17). Compound 1 showed a certain growth inhibitory effect on human gastric cancer cells (BGC-823) with an IC50 value of 8.00 × 10-5 mol·L-1. The activity of compound 1 was similar to that of the positive control camptothecin. In the presence of 1 × 10-5 mol·L- 1, the protective effect of compound 12 on the injury of PC12 cells induced by MPP + was observed. Compared with the model group, the relative protection rate of compound 12 was 104.32% (P <0.001). At the concentration of 1 × 10-5mol·L-1, 2 inhibited PAF-stimulated polymorphonuclear leukocyte β-glucuronidase release with a rate of 52.7% (P <0.05). CONCLUSION: Compounds 1 to 17 are isolated and identified from the genus Heterodera for the first time. Compound 1 has selective growth inhibitory activity on human gastric cancer cells. Compound 12 has neuroprotective activity. Compound 2 has potential anti-inflammatory activity. Other compounds No significant activity was shown in the above screening model at the test concentration.