Coptisine fromCoptis chinensisexerts diverse beneficial properties: A concise review

Abstract

Coptisine is a natural small‐molecular compound extracted from Coptis chinensis (CC) with a history of using for thousands of years. This work aimed at summarizing coptisine's activity and providing advice for its clinical use. We analysed the online papers in the database of SciFinder, Web of Science, PubMed, Google scholar and CNKI by setting keywords as ‘coptisine’ in combination of ‘each pivotal pathway target’. Based on the existing literatures, we find (a) coptisine exerted potential to be an anti‐cancer, anti‐inflammatory, CAD ameliorating or anti‐bacterial drug through regulating the signalling transduction of pathways such as NF‐κB, MAPK, PI3K/Akt, NLRP3 inflammasome, RANKL/RANK and Beclin 1/Sirt1. However, we also (b) observe that the plasma concentration of coptisine demonstrates obvious non‐liner relationship with dosage, and even the highest dosage used in animal study actually cannot reach the minimum concentration level used in cell experiments owing to the poor absorption and low availability of coptisine. We conclude (a) further investigations can focus on coptisine's effect on caspase‐1‐involved inflammasome assembling and pyroptosis activation, as well as autophagy. (b) Under circumstance of promoting coptisine availability by pursuing nano‐ or microrods strategies or applying salt‐forming process to coptisine, can it be introduced to clinical trial.

Baitouweng Decoction Ameliorates Ulcerative Colitis in Mice Partially Attributed to Regulating Th17/Treg Balance and Restoring Intestinal Epithelial Barrier

“…Previous studies have indicated that the extract of Pulsatilla chinensis (Bunge) Regel acts as an anti-inflammatory and immunomodulator in a mouse model of lipopolysaccharide (LPS)-induced systemic inflammation (Kang et al, 2019). Coptidine and berberine, which are the main components in Coptis chinensis Franch, have been shown to exert antitumor, anti-inflammatory, and antibacterial effects in rats (Wu J. et al, 2019;Zhu et al, 2019). An increasing body of evidence has highlighted the therapeutic effect of BTW, although little is known about the precise mechanism of action of BTW against UC.…”

Gut Microbiota-Mediated Transformation of Coptisine Into a Novel Metabolite 8-Oxocoptisine: Insight Into Its Superior Anti-Colitis Effect

“…Rhizome Coptidis, a well-known herbal medicine with multiple applications including treatment for colitis in clinic, has attracted wide attention of scholars in China and elsewhere ( Lee et al, 2014 ; Wu et al, 2019 ). Unsurprisingly, as one of the characteristic active principles of Rhizome Coptidis, COP could also exhibit similar beneficial effects on those diseases.…”

“…Coptisine (COP), the characteristic active constituent of Rhizoma Coptidis with typical natural benzyltherahydroisoquinoline-type alkaloids skeleton as berberine, possesses a broad spectrum of prominent bioactivities including anti-inflammatory ( Zielinska et al, 2020 ), anti-diabetes ( Shi et al, 2019 ), anti-malaria ( Lang et al, 2018 ) and anti-cancer effects ( Ya et al, 2020 ), which is a promising active component to treat UC. Nevertheless, low oral bioavailability of COP is difficult to expound its various pharmacological activities ( Wu et al, 2019 ).…”

Crosstalks between inflammasome and autophagy in cancer

“…Given its multifaceted roles in the regulation of inflammasome activation [97,98], it would be interesting to assess whether the anti-cancer effects of curcumin are mediated by activation of autophagy or by modulation of inflammasomes and pyroptosis. Coptisine, a natural compound extracted from Coptis chinensis, exerted potent anti-cancer effects through activation of autophagy or NLRP3 inflammasomes [99][100][101]. Taken together, various small molecules and nanomaterials modulating autophagy and inflammasome activation are currently being tested as anti-cancer agents for numerous cancer types.…”