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New terpenoids and thiophene derivatives from the aerial parts of Artemisia sieversiana

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 (5â??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 IC50 values of 6.5â?¯Â±â?¯0.5, 11.9â?¯Â±â?¯0.7, and 10.1â?¯Â±â?¯0.3â?¯Î¼M, respectively, comparable to the positive control, quercetin, with an IC50 value of 16.3â?¯Â±â?¯0.4â?¯Î¼M.

» Author: Xu-Dong Zhou, Chen Zhang, Shan He, Bin Zheng, Ke-Wu Zeng, Ming-Bo Zhao, Yong Jiang, Peng-Fei Tu

» Reference: Bioorganic & Medicinal Chemistry Letters, Volume 27, Issue 24

» Publication Date: 15/12/2017

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