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

• Published in: Biomolecules & therapeutics Vol. 24; no. 4; pp. 418 - 425
• Main Authors: Wu, Liu-Qing, Li, Yu, Li, Yuan-Yan, Xu, Shi-hao, Yang, Zong-Yong, Lin, Zheng, Li, Jun
• Format: Journal Article
• Language: Korean
• Published: 한국응용약물학회 01.07.2016
• Subjects: Cyclooxygenase-2; Cytokine; Inflammation; Nociception; Prim-o-glucosylcimifugin; Prostaglandin E2; Nociception; Prostaglandin E2; Inflammation; Prim-o-glucosylcimifugin; Cyclooxygenase-2; Cytokine
• ISSN: 1976-9148; 2005-4483

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 ED50 of 1.6 mg. Rats given POG over time did not develop tolerance. POG also time-dependently reduced serum TNFα, IL-1β and IL-6 in arthritic rats and both POG and indomethacin reduced spinal prostaglandin E2 (PGE2). 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.