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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 - Biomol Ther (Seoul) (2016)

Bottom Line: 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.Anti-nociceptive activity of POG was dose-dependent, maximally reducing pain 56.6% with an ED50 of 1.6 mg.Thus, POG produced potent anti-nociception by downregulating spinal COX-2 expression.

View Article: PubMed Central - PubMed

Affiliation: Department of Anesthesiology, Wenzhou Central Hospital, Wenzhou, Zhejiang, China PR 325000.

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.

No MeSH data available.


Related in: MedlinePlus

Effects of POG on formalin-induced acute or tonic nociception. Flinch times in each 1-min epoch were quantified as nociceptive behavior. (A) Treatment with 1, 3, 10, or 30 mg/kg of POG (sc) once for formalin-induced nociception. (B) Dose-response analysis of anti-nociception of POG on formalin-induced tonic pain (AUC10–90 min). (C) Effects of POG after 7 days of administration. (D) Rotarod test of indomethacin (10 mg/kg) and POG (100 mg/kg). Falling latencies were normalized by latency at 0 min in each group. Data are presented as Means ± SEM, n=10 in each group.
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f2-bt-24-418: Effects of POG on formalin-induced acute or tonic nociception. Flinch times in each 1-min epoch were quantified as nociceptive behavior. (A) Treatment with 1, 3, 10, or 30 mg/kg of POG (sc) once for formalin-induced nociception. (B) Dose-response analysis of anti-nociception of POG on formalin-induced tonic pain (AUC10–90 min). (C) Effects of POG after 7 days of administration. (D) Rotarod test of indomethacin (10 mg/kg) and POG (100 mg/kg). Falling latencies were normalized by latency at 0 min in each group. Data are presented as Means ± SEM, n=10 in each group.

Mentions: After establishing pain models, POG and indomethacin were used to treat animals and POG dose-dependently inhibited tonic formalin-induced nociception (Fig. 2A) and the acute phase as well (Emax and ED50 in the tonic phase were 56.6% and 1.6 mg, respectively; Fig. 2B). Long-term anti-nociception of POG was also measured in the formalin pain model and (Fig. 2C) POG inhibited pain and no tolerance was observed A rotarod test to test drug effects on motor coordination revealed that saline, indomethacin, and POG at 0.5, 1, 2 and 4 h after injection (Fig. 2D) did not alter motor coordination.


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 - Biomol Ther (Seoul) (2016)

Effects of POG on formalin-induced acute or tonic nociception. Flinch times in each 1-min epoch were quantified as nociceptive behavior. (A) Treatment with 1, 3, 10, or 30 mg/kg of POG (sc) once for formalin-induced nociception. (B) Dose-response analysis of anti-nociception of POG on formalin-induced tonic pain (AUC10–90 min). (C) Effects of POG after 7 days of administration. (D) Rotarod test of indomethacin (10 mg/kg) and POG (100 mg/kg). Falling latencies were normalized by latency at 0 min in each group. Data are presented as Means ± SEM, n=10 in each group.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4930286&req=5

f2-bt-24-418: Effects of POG on formalin-induced acute or tonic nociception. Flinch times in each 1-min epoch were quantified as nociceptive behavior. (A) Treatment with 1, 3, 10, or 30 mg/kg of POG (sc) once for formalin-induced nociception. (B) Dose-response analysis of anti-nociception of POG on formalin-induced tonic pain (AUC10–90 min). (C) Effects of POG after 7 days of administration. (D) Rotarod test of indomethacin (10 mg/kg) and POG (100 mg/kg). Falling latencies were normalized by latency at 0 min in each group. Data are presented as Means ± SEM, n=10 in each group.
Mentions: After establishing pain models, POG and indomethacin were used to treat animals and POG dose-dependently inhibited tonic formalin-induced nociception (Fig. 2A) and the acute phase as well (Emax and ED50 in the tonic phase were 56.6% and 1.6 mg, respectively; Fig. 2B). Long-term anti-nociception of POG was also measured in the formalin pain model and (Fig. 2C) POG inhibited pain and no tolerance was observed A rotarod test to test drug effects on motor coordination revealed that saline, indomethacin, and POG at 0.5, 1, 2 and 4 h after injection (Fig. 2D) did not alter motor coordination.

Bottom Line: 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.Anti-nociceptive activity of POG was dose-dependent, maximally reducing pain 56.6% with an ED50 of 1.6 mg.Thus, POG produced potent anti-nociception by downregulating spinal COX-2 expression.

View Article: PubMed Central - PubMed

Affiliation: Department of Anesthesiology, Wenzhou Central Hospital, Wenzhou, Zhejiang, China PR 325000.

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.

No MeSH data available.


Related in: MedlinePlus