靶向小胶质细胞过度激活的新疆阿魏树脂中生物活性倍半萜香豆素。
Bioactive sesquiterpene coumarins from the resin of Ferula sinkiangensis targeted on over-activation of microglia.
机构信息
School of Traditional Chinese Materia Medica, Key Laboratory of Computational Chemistry-Based Natural Antitumor Drug Research & Development, Shenyang Pharmaceutical University, Shenyang 110016, Liaoning Province, China.
College of Life and Health Sciences, Northeastern University, Shenyang 110004, China; State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, Guilin, China.
出版信息
Bioorg Chem. 2020 Nov;104:104338. doi: 10.1016/j.bioorg.2020.104338. Epub 2020 Oct 8.
Nine undescribed (1-4, 6-10) sesquiterpene coumarins, together with a new natural one (5) and ten known ones (11-20), were isolated from the low polarity fraction of the 95% ethanol extract of the resin of Ferula sinkiangensis. Their structures were elucidated based on the comprehensive analysis of HRESIMS, 1D and 2D NMR data. The absolute configurations were determined by comparison of experimental and calculated ECD spectra. All the identified SCs were evaluated for their anti-neuroinflammatory activities in LPS-induced BV-2 cells. Ferusingensine G (8) displayed a significant inhibitory effect on nitric oxide (NO) production with an IC value of 1.2 μM. The results suggested that natural SCs might be served as potential neuroinflammatory inhibitors.
从新疆阿魏树脂的 95%乙醇提取物的低极性部分分离得到了九种未描述的（1-4、6-10）倍半萜香豆素，以及一种新的天然产物（5）和十种已知的产物（11-20）。基于 HRESIMS、1D 和 2D NMR 数据的综合分析，阐明了它们的结构。通过比较实验和计算的 ECD 光谱，确定了绝对构型。所有鉴定出的 SCs 都在 LPS 诱导的 BV-2 细胞中进行了抗神经炎症活性评估。Ferusingensine G（8）对一氧化氮（NO）的产生具有显著的抑制作用，IC 值为 1.2 μM。结果表明，天然 SCs 可能作为潜在的神经炎症抑制剂。
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