Molecular and Cellular Biochemistry

, Volume 428, Issue 1–2, pp 129–137 | Cite as

Anti-neuroinflammatory effects of grossamide from hemp seed via suppression of TLR-4-mediated NF-κB signaling pathways in lipopolysaccharide-stimulated BV2 microglia cells

  • Qian Luo
  • Xiaoli Yan
  • Larisa Bobrovskaya
  • Mei Ji
  • Huiqing Yuan
  • Hongxiang Lou
  • Peihong FanEmail author


Grossamide, a representative lignanamide in hemp seed, has been reported to possess potential anti-inflammatory effects. However, the potential anti-neuroinflammatory effects and underlying mechanisms of action of grossamide are still unclear. Therefore, the present study investigated the possible effects and underlying mechanisms of grossamide against lipopolysaccharide (LPS)-induced inflammatory response in BV2 microglia cells. BV2 microglia cells were pre-treated with various concentrations of grossamide before being stimulated with LPS to induce inflammation. The levels of pro-inflammatory cytokines were determined using the enzyme-linked immunoassay (ELISA) and mRNA expression levels were measured by real-time PCR. The translocation of nuclear factor-kappa B (NF-κB) and contribution of TLR4-mediated NF-κB activation on inflammatory effects were evaluated by immunostaining and Western blot analysis. This study demonstrated that grossamide significantly inhibited the secretion of pro-inflammatory mediators such as interleukin 6 (IL-6) and tumor necrosis factor α (TNF-α), and decreased the level of LPS-mediated IL-6 and TNF-α mRNA. In addition, it significantly reduced the phosphorylation levels of NF-κB subunit p65 in a concentration-dependent manner and suppressed translocation of NF-κB p65 into the nucleus. Furthermore, grossamide markedly attenuated the LPS-induced expression of Toll-like receptor 4 (TLR4) and myeloid differentiation factor 88 (MyD88). Taken together, these data suggest that grossamide could be a potential therapeutic candidate for inhibiting neuroinflammation in neurodegenerative diseases.


Hemp seed Lignanamide Grossamide Anti-neuroinflammatory BV2 microglia cells NF-κB 



This work was supported by the National Natural Science Foundation of China (Grant No. 81473323); Key R&D program in Shandong Province (No. 2015GSF119025) and the China-Australia Centre for Health Science Research (Grant No. 2015GJ04).

Compliance with ethical standards

Conflict of interest

The authors declare no competing financial interest.


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Copyright information

© Springer Science+Business Media New York 2017

Authors and Affiliations

  • Qian Luo
    • 1
  • Xiaoli Yan
    • 1
  • Larisa Bobrovskaya
    • 3
  • Mei Ji
    • 1
  • Huiqing Yuan
    • 2
  • Hongxiang Lou
    • 1
  • Peihong Fan
    • 1
    Email author
  1. 1.Department of Natural Product Chemistry, Key Lab of Chemical Biology of Ministry of Education, School of Pharmaceutical SciencesShandong UniversityJinanPeople’s Republic of China
  2. 2.Department of Biochemistry & Molecular Biology, School of MedicineShandong UniversityJinanPeople’s Republic of China
  3. 3.School of Pharmacy and Medical Sciences, Sansom Institute for Health ResearchUniversity of South AustraliaAdelaideAustralia

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