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来自乳浆大戟的具有抗炎活性的麻风树烷型和瑞香烷型二萜类化合物。

Jatrophane and ingenane diterpenoids with anti-inflammatory activity from Euphorbia esula.

作者信息

Li Yu-Peng, Li Ying, Gao Wen-Jing, Fang Chu-Hong, Lv Ming-Jun, Yue Jian-Min, Yu Jin-Hai

机构信息

Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai, Shandong, 264117, China.

Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai, Shandong, 264117, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, China.

出版信息

Phytochemistry. 2025 Apr;232:114369. doi: 10.1016/j.phytochem.2024.114369. Epub 2024 Dec 18.

DOI:10.1016/j.phytochem.2024.114369
PMID:39706542
Abstract

A phytochemical investigation into the plants of Euphorbia esula L. has yielded 19 diterpenoids, comprising 17 jatrophane-type (1-7 and 9-18) and two ingenane-type (8 and 19). The structures of these compounds were elucidated by a combination of spectrum elucidations, quantum chemical calculations, and X-ray single crystal diffraction. Biological evaluations demonstrated that compounds 6, 8, 18, and 19 show significant anti-inflammatory activity with IC values within 10 μM, without displaying any morphological signs of cytotoxicity. Further biological analysis revealed that euphoresulin A (8) is involved in the suppression of inflammatory response by blocking the activation of NF-κB/MAPK and activating Nrf2/HO-1 singling pathways.

摘要

对乳浆大戟植物进行的植物化学研究已得到19种二萜类化合物,其中包括17种麻风树烷型(1 - 7和9 - 18)和两种瑞香烷型(8和19)。通过光谱解析、量子化学计算和X射线单晶衍射相结合的方法阐明了这些化合物的结构。生物学评价表明,化合物6、8、18和19显示出显著的抗炎活性,IC值在10 μM以内,且未表现出任何细胞毒性的形态学迹象。进一步的生物学分析表明,大戟素A(8)通过阻断NF-κB/MAPK的激活和激活Nrf2/HO-1信号通路来参与炎症反应的抑制。

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