Discovery of Ingenane Diterpenoids from Euphorbia hylonoma as Antiadipogenic Agents.
Discovery of Ingenane Diterpenoids from Euphorbia hylonoma as Antiadipogenic Agents.
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DOI：
10.1021/acs.jnatprod.3c00822
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发表时间：
2023-11
影响因子：
5.1
通讯作者：
Shuge Wu;Xinying Zhu;Tao Yuan;Fang-yu Yuan;Shiyou Zhou;Dong Huang;Ying Wang;Gui-Hua Tang;Zhishu Huang;Xin Chen;Sheng Yin
中科院分区：
文献类型：
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作者：
Shuge Wu;Xinying Zhu;Tao Yuan;Fang-yu Yuan;Shiyou Zhou;Dong Huang;Ying Wang;Gui-Hua Tang;Zhishu Huang;Xin Chen;Sheng Yin
本文报道了13个新的大戟属二萜类化合物（Euphylonanes A-M（1-13））和8个已知化合物。化合物1和2是两个重排的巨大二氢茚，具有罕见的6/6/7/3-稠环系统。化合物3代表9，10-环氧惕各烷的第一个实例，而4-21是随取代基变化的典型的巨大戟烷。使用光谱、计算和化学方法的组合来阐明结构。结果表明，大部分巨大戟烷类化合物对3 T3-L1脂肪细胞有明显的抑制成脂作用，其中4种化合物的抑制成脂作用最强，EC_（50）为0.60 ± 0.27 μM。机制研究表明，4通过激活AMPK信号通路抑制脂肪细胞的脂肪生成和脂肪生成。
Thirteen new Euphorbia diterpenoids, euphylonanes A-M (1-13), and eight known ones were isolated from the whole plants of Euphorbia hylonoma. Compounds 1 and 2 are two rearranged ingenanes bearing a rare 6/6/7/3-fused ring system. Compound 3 represents the first example of a 9,10-epoxy tigliane, while 4-21 are typical ingenanes varying with substituents. Structures were elucidated using a combination of spectroscopic, computational, and chemical methods. Most ingenanes exerted a significant antiadipogenic effect in 3T3-L1 adipocytes, among which 4 was the most active with an EC50 value of 0.60 ± 0.27 μM. Mechanistic study revealed that 4 inhibited the adipogenesis and lipogenesis in adipocytes via activation of the AMPK signaling pathway.