College of Pharmacy, Academy of Integrative Medicine, and National-Local Joint Engineering Research Center for Drug Research and Development of Neurodegenerative Disease , Dalian Medical University , Dalian 116044 , People's Republic of China.
The First Affiliated Hospital of Dalian Medical University , No. 222 Zhongshan Road , Dalian 116011 , People's Republic of China.
J Org Chem. 2019 Feb 1;84(3):1624-1629. doi: 10.1021/acs.joc.8b02800. Epub 2019 Jan 17.
Two unusual ring C- seco and ring D-aromatic nor-triterpenoids, ebracpenes A (1) and B (2), were obtained from Euphorbia ebracteolata roots and elucidated by widely spectroscopic data analyses, such as 1D, 2D NMR, HRESIMS, and X-ray crystallography analysis. Compound 2 showed a significant inhibitory activity on lipase (IC = 0.89 μM as well as the K determined to be 0.69 μM). Enzyme kinetics analysis and molecular docking experiments revealed that compound 2 was a competitive inhibitor, binding to the active site of lipase.
从大戟属植物 Ebracteolata 根部分离得到了两种不寻常的环 C-去甲和环 D-芳构化的 nor-三萜类化合物，ebracpenes A（1）和 B（2），并通过广泛的光谱数据分析，如 1D、2D NMR、HRESIMS 和 X 射线晶体学分析进行了阐明。化合物 2 对脂肪酶表现出显著的抑制活性（IC = 0.89 μM，K 值为 0.69 μM）。酶动力学分析和分子对接实验表明，化合物 2 是一种竞争性抑制剂，与脂肪酶的活性位点结合。
