Coptisine from Coptis chinensis exerts 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.

Keywords: coptisine; crosstalk network; pharmacological mechanism; signalling pathways bioavailability.

Figure 1

Coptis chinensis Franch. Whole plant (A), dry root (B) and chemical structure of coptisine (C)

Figure 2

Non‐liner relationships between CC alkaloid dosages and plasma concentration (Cmax). There is an obvious process of limitation, and the bioavailability decreased along with the elevated dosage

Figure 3

Schematic summaries of coptisine's anti‐cancer targets. Coptisine regulates cell cycle and blocks the occurrence of apoptosis and metastasis initiation by modulating the marked targets. Red arrows represent for decreased expression and/or activity; blue arrows represent for increased expression and/or activity

Figure 4

Schematic summaries of coptisine's anti‐inflammatory and CVD protection targets. Coptisine blocks inflammatory response and ameliorates CADs through modulating the marked targets. Red arrows represent for decreased expression and/or activity; blue arrows represent for increased expression and/or activity

Figure 5

Isoquinoline parent nucleus of quaternary proberberine alkaloid

Figure 6

Recommendations for future investigations on coptisine. Once mitochondrion is damaged, PARK2 binds to PINK1 on the surface of mitochondrial and ubiquitinates mitochondrial outer membrane proteins, which then bind to SQSTM1, a receptor which can interact with LC3. The formation of autophagosome inhibits ROS, the overproduction of which causes NLRP3 inflammasome assembling and the downstream pyroptosis and inflammatory response