Zhou Xu-Dong, Zhang Chen, He Shan, Zheng Bin, Zeng Ke-Wu, Zhao Ming-Bo, Jiang Yong, Tu Peng-Fei
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China; School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, Zhejiang 325035, China.
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China.
Bioorg Med Chem Lett. 2017 Dec 15;27(24):5441-5445. doi: 10.1016/j.bmcl.2017.10.077. Epub 2017 Nov 6.
One new highly oxygenated nortriterpene, named sieverlactone (1), one new sesquiterpene, 1β,10β-epoxy-8α-acetoxyachillin (2), one new natural product, 5-propinyl-thiophene-2-carboxylic acid (3), and one new thiophene, 3-hydroxy-5-propinyl-2-acetyl-thiophene (4), together with 10 other known compounds (5-14), were isolated from the dried aerial parts of Artemisia sieversiana. Their structures were elucidated by a combination of extensive spectroscopic analysis, including 1D, 2D NMR spectroscopic and mass spectrometric data. Meanwhile, the stereochemistry of 1 and 2 was confirmed by single-crystal X-ray diffraction technique using Cu radiation. All the isolates were evaluated for their anti-neuroinflammatory effects on the lipopolysaccharide-induced nitric oxide production in BV-2 murine microglial cells. Compounds 2, 5, and 6 exhibited the significant activities with IC values of 6.5 ± 0.5, 11.9 ± 0.7, and 10.1 ± 0.3 μM, respectively, comparable to the positive control, quercetin, with an IC value of 16.3 ± 0.4 μM.
从西伯利亚艾蒿干燥地上部分分离得到一个新的高度氧化的三萜类化合物，命名为西伯利亚内酯（1），一个新的倍半萜类化合物，1β,10β-环氧-8α-乙酰氧基紫菀素（2），一个新的天然产物，5-丙炔基噻吩-2-羧酸（3），以及一个新的噻吩类化合物，3-羟基-5-丙炔基-2-乙酰基噻吩（4），还有其他10个已知化合物（5 - 14）。通过综合运用广泛的光谱分析方法，包括一维、二维核磁共振光谱和质谱数据，阐明了它们的结构。同时，利用铜辐射的单晶X射线衍射技术确定了化合物1和2的立体化学结构。对所有分离得到的化合物进行了评估，考察它们对脂多糖诱导的BV - 2小鼠小胶质细胞产生一氧化氮的抗神经炎症作用。化合物2、5和6表现出显著的活性，IC值分别为6.5±0.5、11.9±0.7和10.1±0.3 μM，与阳性对照槲皮素（IC值为16.3±0.4 μM）相当。
