2. Academic Validation
  3. Bioactive sesquiterpene coumarins from the resin of Ferula sinkiangensis targeted on over-activation of microglia

Bioactive sesquiterpene coumarins from the resin of Ferula sinkiangensis targeted on over-activation of microglia

  • Bioorg Chem. 2020 Nov;104:104338. doi: 10.1016/j.bioorg.2020.104338.
Tingting Guo 1,  Di Zhou 1,  Yanqiu Yang 2,  Xueni Zhang 1,  Gang Chen 1,  Bin Lin 3,  Yu Sun 4,  Hui Ni 4,  Jingyu Liu 2,  Yue Hou 5,  Ning Li 6
Affiliations

Affiliations

  • 1 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.
  • 2 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.
  • 3 School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.
  • 4 XinJiang Institute of Chinese Materia Medica and Ethnodrug, Urumqi 830002, China.
  • 5 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. Electronic address: [email protected].
  • 6 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. Electronic address: [email protected].
PMID: 33142410 DOI: 10.1016/j.bioorg.2020.104338
Abstract

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 IC50 value of 1.2 μM. The results suggested that natural SCs might be served as potential neuroinflammatory inhibitors.

Keywords

BV2 microglial cell; Ferula sinkiangensis; Neuroinflammation; Sesquiterpene coumarins.

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