Artemargyinolide E (AE), a new sesquiterpene lactone was isolated from the traditional Chinese medicine Artemisia argyi. Its structure was elucidated based on the extensive analysis of spectroscopic data. The absolute configuration of AE was assigned by X-ray crystallographic analysis. The effect of AE and its mechanism on lipopolysaccharide (LPS)-induced inflammatory responses in macrophages were investigated. AE displayed the inhibitory activity on the production of nitrogen oxide (NO) in LPS-induced RAW 264.7 macrophages with an IC₅₀ value of 17.20 ± 0.55 μM. Furthermore, AE intensively suppressed the secretion of key pro-inflammatory factors and chemokines, including tumor necrosis factor-α (TNF-α), prostaglandin E₂ (PGE₂) and interleukin-1β (IL-1β). It also significantly down-regulated the protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Further results revealed that AE inhibited LPS-induced phosphorylation of inhibitor of κBα (IκBα) and nuclear factor (NF)-κB p65, and suppressed the translocation of NF-κB p65 from the cytoplasm to the nucleus. These results suggest that AE could inhibit inflammatory responses in LPS-induced RAW 264.7 macrophages via down-regulating NF-κB signaling pathway.

从传统中草药艾蒿中分离出一种新的倍半萜内酯-蒿甲内酯E（AE）。基于对光谱数据的广泛分析，阐明了其结构。AE的绝对构型通过X射线晶体学分析确定。研究了AE及其对脂多糖（LPS）诱导的巨噬细胞炎症反应的影响。AE显示在生产氮氧化物的抑制活性（NO）中LPS诱导的RAW 264.7巨噬细胞中的IC ₅₀的17.20±0.55值μ M.此外，AE集中抑制关键促炎因子和趋化因子的分泌，包括肿瘤坏死因子-α（TNF- α），前列腺素E ₂（PGE ₂）和白细胞介素-1 β（IL-1 β）。它还显着下调了诱导型一氧化氮合酶（iNOS）和环氧合酶2（COX-2）的蛋白表达。进一步的结果表明，AE抑制LPS诱导的κBα（IκBα）和核因子（NF）-κBp65抑制剂的磷酸化，并抑制NF-κBp65从细胞质到核的转运。这些结果表明，AE可以通过下调NF-κB信号通路抑制LPS诱导的RAW 264.7巨噬细胞的炎症反应。