[关键词]
[摘要]
目的 研究黑紫獐牙菜Swertia atroviolacea叶片的化学成分。方法 采用硅胶柱色谱、Zorbax PrepHT GF反相柱色谱及Sephadex LH-20凝胶柱色谱等现代分离技术进行分离纯化,根据理化性质和波谱数据鉴定化合物结构,采用MTT法测定化合物1对5株人体癌细胞株NB4、A549、SHSY5Y、PC3和MCF-7的体外细胞毒活性。结果 从黑紫獐牙菜叶片95%乙醇提取物中分离得到5个化合物,分别鉴定为3-(3-甲基-2-氧代-丁-3-烯基)-6-乙酰基-1,5-二甲氧基 酮(1)、1,2,3,4-四氢-1,4,6,8-四羟基 酮(2)、1,3-二甲氧基-8-羟基 酮(3)、1,2,6,8-四羟基 酮(4)、熊果酸(5)。化合物1对NB4、A549、SHSY5Y、PC3、MCF-7细胞的IC50值均小于10 μmol/L,其中对A549和MCF-7细胞具有较高的细胞毒活性,其IC50值分别为5.2和3.8 μmol/L。结论 化合物1为新化合物,命名为黑紫獐牙菜素A,此化合物具有显著的细胞毒活性。
[Key word]
[Abstract]
Objective To study the chemical constituents from the leaves of Swertia atroviolacea and five compounds were obtained. In addition, the cytotoxic activity of compound 1 was tested. Methods Compounds 1—5 were isolated and purified by silica gel column chromatography, Zorbax PrepHT GF (250 mm × 21.2 mm) reversed phase and Sephadex LH-20 gel column chromatography, and other modern separation technology. Their structures were elucidated by physicochemical properties and spectroscopic methods. Compound 1 was evaluated for its in vitro cytotoxicity against human tumor NB4, A549, SHSY5Y, PC3, and MCF-7 cell line, using the MTT method. Results Five compounds were obtained from the 95% ethanol extract from the leaves of S. atroviolacea, and identified as 3-(3-methyl-2-oxobut-3-enyl)-6-acetyl-1,5-dimethoxy-xanthone (1), 1,2,3,4-tetrahydro-1,4,6,8-tetrahydroxyxanthone (2), 1,3-dimethoxy-8-hydroxy-xanthone (3), 1,2,6,8-tetrahydroxy-xanthone (4), and ursolic acid (5). The IC50 values of compound 1 on NB4, A549, SHSY5Y, PC3, and MCF-7 were all below 10 μmol/L. Compound 1 had higher cytotoxic activity on A549 and MCF-7, and the IC50 values were 5.2 and 3.8 μmol/L. Conclusion Compound 1, named atroviolacone A, is a new compound, and exhibits significant cytotoxic activity.
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[基金项目]
国家自然科学基金资助项目(21262048);云南省高校科技创新团队项目(IRTSTYN 2014-11)