Antinociceptive Effects of Prim-O-Glucosylcimifugin in Inflammatory Nociception via Reducing Spinal COX-2

  • Wu, Liu-Qing (Department of Anesthesiology, Wenzhou Central Hospital) ;
  • Li, Yu (Department of Anesthesiology, Wenzhou Central Hospital) ;
  • Li, Yuan-Yan (Department of Anesthesiology, Wenzhou Central Hospital) ;
  • Xu, Shi-hao (Department of Anesthesiology, Wenzhou Central Hospital) ;
  • Yang, Zong-Yong (Department of Anesthesiology, Wenzhou Central Hospital) ;
  • Lin, Zheng (Department of Anesthesiology, Wenzhou Central Hospital) ;
  • Li, Jun (Department of Anesthesiology, Second Affiliated Hospital of Wenzhou Medical University)
  • Received : 2015.10.15
  • Accepted : 2016.03.24
  • Published : 2016.07.01


We measured anti-nociceptive activity of prim-o-glucosylcimifugin (POG), a molecule from Saposhnikovia divaricate (Turcz) Schischk. Anti-nociceptive or anti-inflammatory effects of POG on a formalin-induced tonic nociceptive response and a complete Freund's adjuvant (CFA) inoculation-induced rat arthritis pain model were studied. Single subcutaneous injections of POG produced potent anti-nociception in both models that was comparable to indomethacin analgesia. Anti-nociceptive activity of POG was dose-dependent, maximally reducing pain 56.6% with an $ED_{50}$ of 1.6 mg. Rats given POG over time did not develop tolerance. POG also time-dependently reduced serum TNF${\alpha}$, IL-$1{\beta}$ and IL-6 in arthritic rats and both POG and indomethacin reduced spinal prostaglandin E2 ($PGE_2$). Like indomethacin which inhibits cyclooxygenase-2 (COX-2) activity, POG dose-dependently decreased spinal COX-2 content in arthritic rats. Additionally, POG, and its metabolite cimifugin, downregulated COX-2 expression in vitro. Thus, POG produced potent anti-nociception by downregulating spinal COX-2 expression.


Supported by : Zhejiang Science Foundation


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