Biomol Ther.  2016 Jul;24(4):418-425. 10.4062/biomolther.2015.168.

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

• Wu LQ
• Li Y
• Li YY
• Xu SH
• Yang ZY
• Lin Z
• Li J

• KMID: 2351691
• DOI: http://doi.org/10.4062/biomolther.2015.168

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.

Keyword

Prim-o-glucosylcimifugin; Nociception; Inflammation; Cytokine; Prostaglandin E2; Cyclooxygenase-2

MeSH Terms

Analgesia
Animals
Apiaceae
Arthritis
Cyclooxygenase 2
Dinoprostone
Freund's Adjuvant
In Vitro Techniques
Indomethacin
Inflammation
Injections, Subcutaneous
Interleukin-6
Nociception*
Rats
Cyclooxygenase 2
Dinoprostone
Freund's Adjuvant
Indomethacin
Interleukin-6