Liquid chromatography- mass spectrometry has been used to detect Berberine (BBR) metabolites and the effect that their bioactivities have on liver cells.
In the study, published by the Journal of Translational Medicine, the team of scientists aimed to discover which CYP450 (Cytochrome P450) isoenzymes execute the phase-I transformation for BBR, and what are the bioactivities of its metabolites on energy pathways.
During the experiments on rat liver cells, the team used liquid chromatography- mass spectrometry to identify four major metabolites of BBR, berberrubine (M1), thalifendine (M2), demethyleneberberine (M3) and jatrorrhizine (M4).
The hepatocyte culture showed that BBR was active in enhancing the expression of insulin
receptor (InsR) and low-density-lipoprotein receptor (LDLR) mRNA, as well as in activating AMP-activated protein kinase (AMPK).
Furthermore, BBR's metabolites, M1-M4, were active in up-regulating InsR expression with a potency reduced by 50-70 per cent, while LDLR mRNA was increased only by M1 or M2 (but not M3 and M4) with an activity level of 35 per cent or 26 per cent respectively of BBR.
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