A review on pain‐relieving activity of berberine

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.