Antinociceptive Effects of Prim-O-Glucosylcimifugin in Inflammatory Nociception via Reducing Spinal COX-2.
10.4062/biomolther.2015.168
- Author:
Liu Qing WU
1
;
Yu LI
;
Yuan Yan LI
;
Shi hao XU
;
Zong Yong YANG
;
Zheng LIN
;
Jun LI
Author Information
1. Department of Anesthesiology, Wenzhou Central Hospital, Wenzhou, Zhejiang, China PR 325000. daiyueyue888@163.com
- Publication Type:Original Article
- Keywords:
Prim-o-glucosylcimifugin;
Nociception;
Inflammation;
Cytokine;
Prostaglandin E2;
Cyclooxygenase-2
- MeSH:
Analgesia;
Animals;
Apiaceae;
Arthritis;
Cyclooxygenase 2;
Dinoprostone;
Freund's Adjuvant;
In Vitro Techniques;
Indomethacin;
Inflammation;
Injections, Subcutaneous;
Interleukin-6;
Nociception*;
Rats
- From:Biomolecules & Therapeutics
2016;24(4):418-425
- CountryRepublic of Korea
- Language:English
-
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.
