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Obacunone Alleviates Inflammatory Pain by Promoting M2 Microglial Polarization and by Activating Nrf2/HO-1 Signaling

Fubei Nan1, Qingxin Tian1, Shuangdong Chen1

  • 1Department of Anesthesiology, the First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang, People's Republic of China.

Drug Design, Development and Therapy
|April 23, 2024
PubMed
Abstract

Insights

Obacunone (OB) alleviates inflammatory pain by shifting microglia from M1 to M2 states, activating the Nrf2/HO-1 pathway. This compound shows potential as a novel therapeutic for inflammatory pain.

Area of Science:

  • Neuroscience
  • Immunology
  • Pharmacology

Background:

  • Inflammatory pain (IP) presents a significant clinical challenge due to limited effective treatments.
  • Microglial polarization is a key factor in the progression of inflammatory pain.
  • Obacunone (OB), known for its anti-inflammatory properties and activation of Nrf2, is investigated for its effects on IP.

Purpose of the Study:

  • To investigate whether Obacunone (OB) can alleviate inflammatory pain (IP).
  • To determine if OB facilitates microglial polarization from M1 to M2 phenotype.
  • To explore the role of the Nrf2/heme oxygenase-1 (HO-1) pathway in OB's effects on IP.

Main Methods:

  • An inflammatory pain (IP) model was induced in mice using Complete Freund's Adjuvant (CFA).
  • Pain behaviors were assessed using paw withdrawal latency (PWL) and paw withdrawal frequency (PWF).
  • Microglial polarization markers (M1/M2), Nrf2, and HO-1 levels were analyzed in spinal cord tissues via Western blot.

Main Results:

  • OB treatment significantly reduced pain behaviors (PWF, paw thickness) and M1 markers (iNOS, CD86) while increasing M2 markers (Arg-1, IL-10).
  • OB enhanced Nrf2 and HO-1 expression in spinal cord tissues.
  • OB treatment improved sciatic nerve morphology and modulated serum cytokine profiles, shifting from M1-related to M2-related markers.

Conclusions:

  • Obacunone (OB) effectively attenuates inflammatory pain by promoting M1 to M2 microglial polarization.
  • The analgesic effect of OB is mediated through the enhancement of the Nrf2/HO-1 signaling pathway.
  • Obacunone (OB) represents a promising therapeutic candidate for treating inflammatory pain.
Keywords:
HO-1Nrf2inflammatory painobacunone

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