具有抗炎活性的葎草属半日花型倍半萜内酯。
ent-Abietane-type lactones with anti-inflammatory activity from Euphorbia helioscopia.
机构信息
State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, 222 South Tianshui Road, Lanzhou, 730000, People's Republic of China.
State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, 222 South Tianshui Road, Lanzhou, 730000, People's Republic of China.
出版信息
Phytochemistry. 2025 Jan;229:114313. doi: 10.1016/j.phytochem.2024.114313. Epub 2024 Oct 24.
Euphohelinodes D-I (1-6), six previously unreported ent-abietane lactones, along with two known analogues (7 and 8), were isolated from the anti-inflammatory fraction extracted from E. helioscopia by a bioactivity-guided isolation. Their structures were characterized using a combination of spectroscopic data interpretation, single-crystal X-ray diffraction and ECD analysis. The anti-inflammatory activity of these compounds was evaluated by measuring their inhibitory effects on NO production in LPS-stimulated RAW264.7 macrophages. The most active candidate, euphohelinode H (5), had better inhibitory activity against NO production with an IC value of 30.23 ± 2.33 μM. Further study revealed that 5 significantly suppressed the expressions of iNOS and COX-2 through the NF-κB signaling pathway.
Euphohelinodes D-I (1-6)，六种以前未报道的 ent-abietane 内酯，以及两种已知类似物（7 和 8），是从 Euphohelioscopia 的抗炎部分通过活性导向分离提取得到的。通过光谱数据分析、单晶 X 射线衍射和 ECD 分析，确定了它们的结构。通过测量它们对 LPS 刺激的 RAW264.7 巨噬细胞中 NO 产生的抑制作用，评估了这些化合物的抗炎活性。最具活性的候选化合物 euphohelinode H（5）对 NO 产生的抑制活性更好，IC 值为 30.23±2.33μM。进一步的研究表明，化合物 5 通过 NF-κB 信号通路显著抑制了 iNOS 和 COX-2 的表达。
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