目的 研究巴山花椒Zanthoxylum pashanense根的醋酸乙酯部位的化学成分及其抗炎活性。方法 采用硅胶柱色谱、Sephadex LH-20凝胶柱色谱、MCI以及半制备高效液相色谱等多种分离手段进行分离纯化，并结合化合物的理化性质、质谱以及核磁数据进行结构鉴定。采用脂多糖（lipopolysaccharide，LPS）诱导的巨噬细胞RAW264.7炎症反应模型评价其抗炎活性。结果 从巴山花椒根的醋酸乙酯部位中分离出7个生物碱化合物，分别鉴定为15-羟基-柄果花椒酰胺（1）、柄果花椒酰胺（2）、beecheyamide（3）、(−)-N-acetylanonaine（4）、(−)-N-acetylxylopine（5）、白鲜碱（6）、γ-崖椒碱（7）。化合物1～5均具有不同程度的抗炎活性，其中化合物4的抗炎活性最强，其对LPS诱导的RAW264.7细胞所释放的炎症因子一氧化氮（NO）、肿瘤坏死因子-α（tumor necrosis factor-α，TNF-α）以及白细胞介素（interleukin-1β，IL-1β）的半数抑制浓度（median inhibition concentration，IC₅₀）分别为（13.64±0.32）、（27.27±2.86）、（29.54±0.20）μmol/L。结论 化合物1为新的酰胺类化合物，命名为15-羟基-柄果花椒酰胺，并首次对其氢谱和碳谱数据进行归属。其中，化合物5为首次从芸香科植物中分离得到，化合物2～4为首次从该植物中分离得到。化合物1～5均对LPS诱导RAW264.7巨噬细胞所释放的炎症因子NO、TNF-α、IL-1β具有不同程度的抑制作用。

Objective To study the chemical constituents of the ethyl acetate extract from the roots of Zanthoxylum pashanense and their anti-inflammatory effects. Methods The compounds were isolated and purified by silica, MCI and column chromatography (CC), and the structures of obtained compounds were identified by physicochemical properties, HRESIMS and spectral data. All of the compounds were evaluated for anti-inflammatory activity against the production of nitric oxide (NO) in lipopolysaccharide (LPS)-induced RAW264.7 cells. Results Seven compounds were isolated and identified as 15-hydroxy-podocarpamide (1), podocarpamide (2), beecheyamide (3), (−)-N-acetylanonaine (4), (−)-N-acetylxylopine (5), γ-fagarine (6), and dictamnine (7). The experiment of anti-inflammatory effects showed that compounds 1-5 had different inhibitory effects on the production of inflammatory factors. Conclusion Compound 1 was a new amide alkaloid named 15-hydroxy-podocarpamide. Its ¹H-NMR and ¹³C-NMR data was completely assigned on the basis of 1D and 2D NMR spectroscopic evidence for the first time. Activity assay showed that compounds 1-5 inhibited for NO, TNF-α and IL-1β at different levels. Among them, compound 4 presented strong inhibitory effect on NO, TNF-α, IL-1β production with IC₅₀ values of (13.64±0.32), (27.27±2.86), (29.54±0.20) μmol/L, respectively.

R284.1

国家自然科学基金资助项目（81774002）