[关键词]
[摘要]
目的 研究藏药高原天名精Carpesium lipskyi干燥根部的化学成分及抗炎活性。方法 利用硅胶柱色谱和Sephadex LH-20凝胶柱色谱等色谱分离技术进行分离纯化,根据理化性质、MS和NMR等波谱手段并结合文献鉴定化合物结构。采用脂多糖(lipopolysaccharide,LPS)诱导的小鼠巨噬细胞RAW264.7炎症模型,对化合物的体外抗炎活性进行评价。结果 从高原天名精根乙醇提取物中分离得到9个化合物,分别鉴定为 (1R,7R,10R,11S)-1-hydroxy-eudesma-3(4),5(6)-dien-11-oic acid methyl ester(1)、(1R,4S,5R,7R)-1-acetoxy-11-hydroxy-eremophil-9(10)-ene(2)、careudesmane D(3)、异土木香内酯(4)、11-hydroxy-eremophil-1(10)-en-2,9-dione(5)、carperemophilane A(6)、carperemophilane B(7)、原儿茶醛(8)和伞形酮(9)。抗炎活性结果表明,化合物2和7能够抑制LPS诱导的RAW264.7细胞中NO的生成量,半数抑制浓度(median inhibition concentration,IC50)值分别为(13.62±1.30)μmol/L和(19.47±2.67)μmol/L。结论 化合物1为新的桉烷型倍半萜化合物,命名为高原天名精甲素(carpesiol A)。化合物2为新的艾里莫芬烷型倍半萜化合物,命名为高原天名精乙素(carpesiol B)。化合物3~7为首次从该植物中分离得到。化合物2和7具有开发为抗炎活性药物的潜力。
[Key word]
[Abstract]
Objective To investigate the chemical constituents and anti-inflammatory activity of the dried roots of Tibetan medicine Carpesium lipskyi. Methods The ethanol extract of C. lipskyi was isolated and purified using chromatographic techniques including silica gel column chromatography and Sephadex LH-20 gel column chromatography. The structures of the compounds were identified based on their physicochemical properties, spectroscopic methods (MS, NMR), and literature data. The in vitro anti-inflammatory activity of the compounds was evaluated using a lipopolysaccharide (LPS)-induced inflammatory model in mouse macrophage RAW264.7 cells. Results Nine compounds were isolated from the roots of C. lipskyi and identified as (1R,7R,10R,11S)-1-hydroxy-eudesma-3(4),5(6)-dien-11-oic acid methyl ester (1), (1R,4S,5R,7R)-1-acetoxy-11-hydroxy-eremophil-9(10)-ene (2), careudesmane D (3), isoalantolactone (4), 11-hydroxy-eremophil-1(10)-en-2,9-dione (5), carperemophilane A (6), carperemophilane B (7), protocatechuyl aldehyde (8), and umbelliferone (9). Compounds 2 and 7 inhibited LPS-induced NO production in RAW264.7 cells with half maximal inhibitory concentration (IC50) values of (13.62 ± 1.30) μmol/L and (19.47 ± 2.67) μmol/L, respectively. Conclusion Compound 1 is a new eudesmane-type sesquiterpene and designated as carpesiol A, and compound 2 is a new eremophilane-type sesquiterpene and designated as carpesiol B. Compounds 3—7 were isolated from this plant for the first time. Compounds 2 and 7 show potential for development as anti-inflammatory drugs.
[中图分类号]
R284.1
[基金项目]
国家自然科学基金资助项目(32372638)