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New terpenoids and thiophene derivatives from the aerial parts of Artemisia sieversiana
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2017-11-01 , DOI: 10.1016/j.bmcl.2017.10.077
Xu-Dong Zhou , Chen Zhang , Shan He , Bin Zheng , Ke-Wu Zeng , Ming-Bo Zhao , Yong Jiang , Peng-Fei Tu

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 (514), 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 IC50 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 IC50 value of 16.3 ± 0.4 μM.



中文翻译:

蒿蒿地上部分的新萜类化合物和噻吩衍生物

一个新的高度氧化nortriterpene,命名sieverlactone(1),一个新的倍半萜烯,1个β,10 β -环氧-8 α -acetoxyachillin(2),一个新的天然产物,5-丙炔基-噻吩-2-羧酸(3)和一个新的噻吩,3-羟基-5-丙炔基-2-乙酰基噻吩(4),连同10种其它已知化合物(5 - 14),购自的干燥地上部分分离蒿碱地肤。通过广泛的光谱分析(包括1D,2D NMR光谱和质谱数据)的组合阐明了它们的结构。同时,1的立体化学2通过使用Cu辐射的单晶X射线衍射技术证实。评价所有分离物对BV-2鼠小神经胶质细胞中脂多糖诱导的一氧化氮产生的抗神经炎作用。化合物25,和6个表现出显著活动,IC 50倍为6.5±0.5的值,11.9±0.7,和10.1±0.3μM,分别与阳性对照,槲皮素,与IC 50 16.3±0.4μM的值。

更新日期:2017-11-01
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