New withanolides with anti-inflammatory activity from the leaves of Datura metel L.,Bioorganic Chemistry

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New withanolides with anti-inflammatory activity from the leaves of Datura metel L.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2019-12-28 , DOI: 10.1016/j.bioorg.2019.103541
Jinyan Tan ₁ , Yan Liu ₁ , Yangang Cheng ₁ , Yanping Sun ₁ , Juan Pan ₁ , Wei Guan ₁ , Xiaomao Li ₁ , Jin Huang ₁ , Peng Jiang ₁ , Shuang Guo ₁ , Haixue Kuang ₁ , Bingyou Yang ₁

Affiliation

Twenty three undescribed withanolides, daturmetelides A-W (1-23), were isolated from 70% EtOH extract of the leaves of Datura metel L. The structural characterizations and relative configurations of 1-23 were elucidated by extensive spectroscopic analysis as well as by comparison with literature values. The absolute configurations of 1 and 3 were determined by X-ray crystallography. Bioassay results showed that 1 and 7 exhibited moderate inhibitory effects against NO production in lipopolysaccharide-stimulated RAW 264.7 cells (IC50 values of 13.74 μM and 13.92 μM, respectively). In addition, 1 and 7 showed significant anti-inflammatory activities against the production of TNF-α, IL-1β, IL-6 and COX-2. Western blot analysis was further performed to reveal the mechanism of anti-inflammatory action via inhibition of the NF-κB activation.

中文翻译：

曼陀罗叶中具有抗炎活性的新型withanolides。

从70％曼陀罗（Datura metel L）叶片的乙醇提取液中分离出23种未述的醇化物，达特甲醚AW（1-23）。通过广泛的光谱分析以及与之比较，阐明了1-23的结构特征和相对构型。文献价值。1和3的绝对构型通过X射线晶体学确定。生物测定结果表明，1和7在脂多糖刺激的RAW 264.7细胞中表现出对NO产生的中度抑制作用（IC50值分别为13.74μM和13.92μM）。此外，1和7对TNF-α，IL-1β，IL-6和COX-2的产生具有显着的抗炎活性。进一步进行蛋白质印迹分析以揭示通过抑制NF-κB活化的抗炎作用的机制。

更新日期：2019-12-29

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