College of Pharmacy, Academy of Integrative Medicine, and Liaoning Engineering Technology Centre of Target-based Nature Products for Prevention and Treatment of Ageing-related Neurodegeneration, Dalian Medical University , Dalian 116044, People's Republic of China.
School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University , Shenyang 110016, People's Republic of China.
J Nat Prod. 2017 Dec 22;80(12):3218-3223. doi: 10.1021/acs.jnatprod.7b00595. Epub 2017 Nov 17.
Two heterodimeric diterpenoids (1 and 2) comprising abietane lactone and nor-rosane constituent units were isolated from Euphorbia ebracteolata roots. Compound 1 exhibited a moderate inhibitory effect on α-glucosidase (IC = 7.94 μM), with a K value of 10.8 μM. In silico molecular docking has been performed to investigate the inhibition mechanism. Compound 2 inhibited the acetyl transfer activity of Mycobacterium tuberculosis GlmU (IC = 41.85 μM), which is a novel tuberculosis treatment target.
从大戟属植物 Ebracteolata 的根部分离得到两种包含贝壳杉烷内酯和降-贝壳杉烷组成单元的异二聚二萜(1 和 2)。化合物 1 对α-葡萄糖苷酶(IC = 7.94 μM)表现出中等抑制作用,K 值为 10.8 μM。通过计算机分子对接研究了抑制机制。化合物 2 抑制结核分枝杆菌 GlmU 的乙酰转移活性(IC = 41.85 μM),这是一个新的结核病治疗靶点。