title: Antinociceptive Effects of Prim-O-Glucosylcimifugin in Inflammatory Nociception via Reducing Spinal COX-2.
abstract: 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.
authors.affiliation: Department of Anesthesiology, Wenzhou Central Hospital, Wenzhou, Zhejiang, China PR 325000.
authors.forename: Liu-Qing
authors.initials: LQ
authors.lastname: Wu
authors.affiliation: Department of Anesthesiology, Wenzhou Central Hospital, Wenzhou, Zhejiang, China PR 325000.
authors.forename: Yu
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Anesthesiology, Wenzhou Central Hospital, Wenzhou, Zhejiang, China PR 325000.
authors.forename: Yuan-Yan
authors.initials: YY
authors.lastname: Li
authors.affiliation: Department of Anesthesiology, Wenzhou Central Hospital, Wenzhou, Zhejiang, China PR 325000.
authors.forename: Shi-Hao
authors.initials: SH
authors.lastname: Xu
authors.affiliation: Department of Anesthesiology, Wenzhou Central Hospital, Wenzhou, Zhejiang, China PR 325000.
authors.forename: Zong-Yong
authors.initials: ZY
authors.lastname: Yang
authors.affiliation: Department of Anesthesiology, Wenzhou Central Hospital, Wenzhou, Zhejiang, China PR 325000.
authors.forename: Zheng
authors.initials: Z
authors.lastname: Lin
authors.affiliation: Department of Anesthesiology, Second Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang, China PR 325000.
authors.forename: Jun
authors.initials: J
authors.lastname: Li
keywords: Cyclooxygenase-2; Cytokine; Inflammation; Nociception; Prim-o-glucosylcimifugin; Prostaglandin E2