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Glycyrrhizin ameliorates inflammatory pain by inhibiting microglial activation-mediated inflammatory response via blockage of the HMGB1-TLR4-NF-kB pathway

Journal Article · · Experimental Cell Research
; ; ; ; ; ;  [1];  [2]
  1. Department of Anesthesiology, the Hospital of Chinese Traditional Medicine of Leshan, Leshan 614000, PR (China)
  2. Department of Hand Surgery, Xi'an Jiaotong University Health Science Center, Honghui Hospital, Xi'an 710054, PR (China)

Highlights: • Glycyrrhizin (Gly) represses LPS-induced microglial activation without cell toxicity. • Glycyrrhizin dose-dependently inhibits LPS-triggered inflammatory response. • Elevation of HMGB1 reverses glycyrrhizin-inhibited inflammatory response in microglia. • HMGB1-mediated TLR4-NF-κB activation account for gly-restrained inflammation. • Gly alleviates CFA-induced pain hypersensitivity, inflammation, microglia activation. Chronic inflammatory pain is a severe clinical problem that greatly affects patients’ quality of life and causes huge economic burden. Microglia-mediated neuroinflammation exerts critical roles in the pathogenic progression of inflammatory pain. Recent evidence corroborates the anti-inflammatory and neuroprotective efficacy of glycyrrhizin; however, its function in inflammatory pain remains poorly elucidated. In the present study, glycyrrhizin suppressed LPS-induced activation of microglial cell BV2 by inhibiting NO production and expression of microglial marker IBA-1. Intriguingly, LPS-induced high expression and generation of inflammatory cytokines (i.e., IL-6, TNF-α and IL-1β) was notably reversed by glycyrrhizin pre-treatment. Mechanistic analysis confirmed that high expression of high-mobility group box 1 (HMGB1) in LPS-activated microglia was inhibited following glycyrrhizin. More importantly, restoring HMGB1 expression by recombinant adenovirus vector of Ad-HMGB1 counteracted glycyrrhizin-restrained inflammatory response in microglia upon LPS stimulation. Furthermore, glycyrrhizin dampened the activation of subsequent TLR4-NF-κB pathway in LPS-stimulated microglia, which was abrogated by HMGB1 elevation. Furthermore, blocking this pathway by si-TLR4 transfection reversed the effects of HMGB1 overexpression on the inhibitor roles of glycyrrhizin in microglia-triggered inflammation. Additionally, glycyrrhizin administration also alleviated CFA-evoked mechanical allodynia and thermal hyperalgesia in inflammatory pain model of mice, concomitant with suppression in inflammatory response and microglial activation. Simultaneously, elevation of HMGB1, TLR4 and p65-NF-κB protein expression induced by CFA injection was also abrogated after glycyrrhizin. Accordingly, this study reveal that glycyrrhizin may act as a promising therapeutic avenue for the treatment of inflammatory pain.

OSTI ID:
23082707
Journal Information:
Experimental Cell Research, Journal Name: Experimental Cell Research Journal Issue: 1 Vol. 369; ISSN 0014-4827; ISSN ECREAL
Country of Publication:
United States
Language:
English

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