A review on pain‐relieving activity of berberine

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.

Research progress of plant‐derived natural alkaloids in central nervous system diseases

“…Berberine ( 29 ) can also relieve pain in a variety of ways, such as downregulating TRPV1, suppression of NF‐κB pathway, regulating opioid receptors, anticholinesterase activity, etc. (Hashemzaei & Rezaee, 2021).…”

The mechanism of berberine alleviating metabolic disorder based on gut microbiome

“…Its chemical structure is represented in Figure 1 . In recent years, a large number of research confirmed that BBR has extensive pharmacological properties, such as anti-inflammatory ( Kuo et al., 2004 ), pain‐relieving ( Hashemzaei and Rezaee, 2021 ), anti-infective ( Aswathanarayan and Vittal, 2018 ), antitumor ( Liu et al., 2019 ),neuroprotective ( Luo et al., 2012 ) and modulate energy metabolism, which can be used to treat cancer ( Zhang et al., 2020 ), digestive ( Zou et al., 2017 ), metabolic ( Xu et al., 2021 ), cardiovascular ( Martini et al., 2020 ), and neurological diseases ( Kulkarni and Dhir, 2010 ). Formulas containing traditional herbal Coptis chinensis, has been used for thousands of years in traditional Chinese Medicine.…”

The Analgesic Properties of Corydalis yanhusuo

“…Berberine has been shown to display potent analgesic activity [32]. One study investigated berberine's role in visceral pain, observing that berberine antinociceptive activity was blocked by the administration of the opioid receptor antagonist naloxone or by selective mu and delta morphine receptor (MOR and DOR) antagonists [33], which suggests that berberine binding activities at MOR and DOR may be responsible for visceral pain analgesia [32]. Interestingly, berberine also has an effect on the endogenous opioid system due to its ability to easily cross the blood-brain barrier [34].…”