A review on pain-relieving activity of berberine

Phytother Res. 2021 Jun;35(6):2846-2853. doi: 10.1002/ptr.6984. Epub 2020 Dec 19.

Abstract

As isoquinoline alkaloid naturally occurs in Coptis and Berberis species, berberine (BER) has shown anti-oxidant, anti-tumour, anti-bacterial and hepatoprotective activities and beneficial effects against digestive, cardiovascular and neurological conditions. Also, BER antiinflammatory, pain-relieving and anti-cholinesterase activities were widely studied. The present overview discusses the analgesic effects of BER. Based on the literature, BER exerted pain-relieving activity against diabetic and chemotherapy-induced neuropathy, and sciatic nerve injury-induced pain via down-regulation of transient receptor potential vanilloid 1, suppression of NF-κB and modulation of μ and δ opioid receptors. Besides, BER could repress inflammatory markers tumour necrosis factor-α, interleukin-6 and IL-1β, as well as prostaglandin E2, inducible nitric oxide synthase and cyclooxygenase-2. The modulatory effects of BER on dopamine and N-methyl d-aspartate systems were also noted. Moreover, BER could induce Nrf2 expression but inhibits p38-MAPK and STAT3 phosphorylation. Noteworthy, anti-cholinesterase activity, which may potentially contribute to BER analgesic properties, warrants particular attention.

Keywords: Berberis vulgaris; alkaloids; analgesia; herbal medicine; hyperalgesia; natural products.

Publication types

  • Review

MeSH terms

  • Analgesics / pharmacology*
  • Analgesics / therapeutic use
  • Animals
  • Berberine / pharmacology*
  • Berberine / therapeutic use
  • Berberis / chemistry
  • Coptis / chemistry
  • Cyclooxygenase 2 / metabolism
  • Dinoprostone / metabolism
  • Humans
  • Interleukin-1beta / metabolism
  • Interleukin-6 / metabolism
  • NF-E2-Related Factor 2 / metabolism
  • NF-kappa B / metabolism
  • Nitric Oxide Synthase Type II / metabolism
  • Pain* / drug therapy
  • Pain* / etiology
  • Phytotherapy
  • Plant Extracts / pharmacology*
  • Plant Extracts / therapeutic use
  • Receptors, Opioid, delta / metabolism
  • TRPV Cation Channels / metabolism
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Analgesics
  • IL1B protein, human
  • Interleukin-1beta
  • Interleukin-6
  • NF-E2-Related Factor 2
  • NF-kappa B
  • NFE2L2 protein, human
  • Plant Extracts
  • Receptors, Opioid, delta
  • TRPV Cation Channels
  • TRPV1 protein, human
  • Tumor Necrosis Factor-alpha
  • Berberine
  • NOS2 protein, human
  • Nitric Oxide Synthase Type II
  • Cyclooxygenase 2
  • Dinoprostone