目的 研究丝叶蓍Achillea setacea全草的化学成分。方法 采用MCI、LH-20凝胶色谱柱、ODS、硅胶和pre-HPLC等方法将进行化合物分离和纯化，运用波谱技术和结合文献解析化合物结构。采用构建脂多糖（lipopolysaccharide，LPS）诱导的RAW264.7细胞体外炎症模型的方法，对分离得到的化合物进行体外抗炎活性评价。结果 从丝叶蓍二氯甲烷部位分离得到19个化合物，包括15个倍半萜、1个单萜、1个降倍半萜衍生物和2个黄酮类化合物，分别鉴定为(3S,3aS,6E,9S,10E,11aS)-cyclodeca[b] furan-2(3H)-one, 3a,4,5,8,9,11a-hexahydro-9-hydroxy-3,6,10-trimethyl（1）、desacetylherbohde A（2）、millefoliumon D（3）、sintenin（4）、millefoliumon C（5）、achigermalide D（6）、去乙酰氧母菊素（7）、蓍素（8）、8β-hydroxyachillin（9）、脱氢去乙酰氧母菊素（10）、母菊内酯酮（11）、achisecogunolide F（12）、1,10β-环氧蓍素（13）、lβ-hydroxy-acyperone（14）、millefoliumin A（15）、黑麦草内酯（16）、saniculamoid D（17）、泽兰黄素（18）、紫花牡荆素（19）。结论 化合物3、5、13、17为首次从该属植物中分离得到，化合物6～12、14～16为首次从丝叶蓍中分离得到。化合物1～19的体外抗炎活性筛选结果显示，化合物13和18能显著降低LPS诱导的RAW264.7小鼠巨噬细胞中NO的释放，其半数抑制浓度（median inhibition concentration，IC₅₀）值分别为19.93、13.91 μmol/L。

Objective To study the chemical constituents from the whole plant of Achillea setacea. Methods The extract from A. setacea was isolated and purified by MCI, Sephadex LH-20, ODS, silica gels and preparative HPLC. Their structures were identified by spectral analysis combined with literature. The model of LPS-induced RAW264.7 cells was applied to screen the anti-inflammatory activity of isolates. Results Nineteen compounds, including fifteen sesquiterpenes, a monoterpene, a norsesquiterpene, derivative and two flavonoids have been isolated from the dichloromethane extract of A. setacea, and they were identified as (3S,3aS,6E, 9S,10E, 11aS)-cyclodeca[b]furan-2(3H)-one, 3a,4,5,8,9,11a-hexahydro-9-hydroxy-3,6,10-trimethyl (1), desacetylherbohde A (2), millefoliumon D (3), sintenin (4), millefoliumon C (5), achigermalide D (6), leucodin (7), achillin (8), 8β-hydroxyachillin (9), desacetylmatricarin (10), matricarin (11), achisecogunolide F (12), 1,10β-epoxyachillin (13), l-hydroxy-acyperone (14), millefoliumin A (15), loliolide (16), saniculamoid D (17), eupatorin (18), and casticin (19). Conclusion Compounds 3, 5, 13 and 17 are isolated from Achillea genus for the first time. Compounds 6—12 and 14—16 were isolated from Achillea setacea for the first time. Compounds 1—19 were screened for anti-inflammatory activities in vitro. Compounds 13 and 18 significantly reduced the release of NO and inhibited the secretion of inflammatory mediators in LPS-stimulated RAW264.7 macrophages cells, Compounds 13 and 18 exhibited the inhibitory effects on LPS-stimulated RAW264.7 macrophages cells with median inhibition concentration (IC₅₀) values of 19.93, 13.91 μmol/L, respectively.

R284.1

河南省优秀青年科学基金项目（252300421137）；河南省科技研发计划联合基金（优势学科培育类）项目（242301420109）；河南省科技攻关项目（242102310520）；河南省高等学校重点科研项目（25A360024）；大学生创新训练计划项目（202410471008）