目的 对东紫苏Elsholtzia bodinieri全株的化学成分及其抗炎活性进行研究。方法 采用正相硅胶色谱、Sephadex LH-20凝胶色谱、ODS柱色谱、高效液相色谱等技术进行分离纯化，根据核磁共振、质谱等波谱数据结合文献数据鉴定化合物结构。通过检测脂多糖（lipopolysaccharide，LPS）诱导的RAW 264.7巨噬细胞中炎症因子白细胞介素-6（interleukin-6，IL-6）、白细胞介素1β（interleukin-1β，IL-1β）、肿瘤坏死因子-α（tumor necrosis factor-α，TNF-α）的表达和一氧化氮（NO）的抑制能力，评价所分离化合物的抗炎活性。结果 从东紫苏全株的醋酸乙酯部位分离得到19个单体化合物，包括7个黄酮、5个倍半萜、3个三萜、3个甾体及1个苯丙素类化合物，结构分别鉴定为芹菜素（1）、木犀草素（2）、白杨素（3）、木犀草素-7-O-β-D-葡萄糖苷（4）、圣草酚（5）、乔松素（6）、semecarpanone（7）、咖啡酸乙烯酯（8）、oplodiol（9）、lβ,4β,6β-trihydroxyeudesmane（10）、1β,10α,4β,5α-diepoxy-7αH-germacran-6β-ol（11）、teucladiol（12）、caryolane-1,9β-diol（13）、齐墩果酸（14）、乌苏酸（15）、坡模酸（16）、5α,8α-环二氧-24(S)-甲基麦角甾-6,22-二烯-3β-醇（17）、β-谷甾醇（18）、豆甾醇（19）。结论 从东紫苏中分离获得19个单体化合物，其中化合物7、9～13、17首次从该属植物中分离得到。化合物1、4、9、12～14、17～19能显著降低LPS诱导的巨噬炎症细胞中NO的释放以及抑制炎症因子IL-6、IL-1β和TNF-α的分泌，具有较好的体外抗炎活性。

Objective The purpose was to analyze the chemical compositions and their anti-inflammatory activities from Elsholtzia bodinieri. Methods The separation and purification of compounds were performed by normal-phase silica gel chromatography column (CC), Sephadex LH-20 CC, ODS CC, and high-performance liquid chromatography (HPLC). The structures of the isolated compounds were identified based on the nuclear magnetic resonance spectroscopies (NMR) data and comparison with corresponding data of the reported literature. All the isolated compounds were assessed for their anti-inflammatory effects via detecting inflammatory mediator releases (IL-6, IL-1β, TNF-α) and NO medium level in RAW 264.7 macrophage cells induced by LPS. Results A total of 19 compounds were isolated from the ethyl acetate layer of E. bodinieri, including 7 flavonoids, 5 sesquiterpenoids, 3 triterpenoids, 3 steroids and 1 phenylpropanoids compound. The structures of these isolates were unambiguously identified as apigenin (1), luteolin (2), chrysin (3), luteolin-7-O-β-D-glucoside (4), eriodictyol (5), pinocembrin (6), semecarpanone (7), caffeic acid ethylene ester (8), oplodiol (9), lβ,4β,6β-trihydroxyeudesmane (10), 1β,10α,4β,5α-diepoxy-7αH-germacran-6β-ol (11), teucladiol (12), caryolane-1,9β-diol (13), oleanelic acid (14), ursolic acid (15), pomolic acid (16), 5α,8α-epidioxy-24(S)- methylergosta-6, 9(11), 22-trien-3β-ol (17), β-sitoster (18), stigmasterol (19). Conclusion Compounds 7, 9—13 and 17 are isolated from this genus Elsholtzia for the first time. Compounds 1, 4, 9, 12—14 and 17—19 significantly reduce the release of NO and inhibited the secretion of inflammatory mediators (IL-6、IL-1β、TNF-α) in LPS-stimulated RAW 264.7 macrophages cells at the concentration of 20μg·mL⁻¹, comparable to DXM used as the positive control, which suggested that E. bodinieri might be possess the anti-inflammatory activity.

R284.1

云南省基础研究面上项目（202101AT070436，202101BE070001-053）