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Coptis chinensis  is commonly used in traditional Chinese medicine. The study investigated metabolic interaction of the active constituents (berberine, coptisine, palmatine, and jatrorrhizine) of  Coptis chinensis  in human liver microsomes. After incubation of the four constituents of  Coptis chinensis  in HLMs, the metabolism of the four constituents was observed by HPLC. The  in vitro  inhibition experiment between the active constituents was conducted, and IC 50  value was estimated. Coptisine exhibited inhibitions against the formation of the two metabolites of berberine with IC 50  values of 6.5 and 8.3  μ M, respectively. Palmatine and jatrorrhizine showed the weaker inhibitory effect on the formation of the metabolites of berberine. Berberine showed a weak inhibitory effect on the production of coptisine metabolite with an IC 50  value of 115  μ M, and palmatine and jatrorrhizine had little inhibitory effect on the formation of coptisine metabolite. Berberine, coptisine, and jatrorrhizine showed no inhibitory effect on the generation of palmatine metabolite (IC 50  > 200  μ M). The findings suggested that there are different degrees of metabolic interaction between the four components. Coptisine showed the strongest inhibition toward berberine metabolism.

Metabolic Interaction of the Active Constituents ofCoptis chinensisin Human Liver Microsomes