BERBERNE is an isoquinoline alkaloid extracted from the dried rhizome of Coptis chinensis French. Berberine can treat hyperipidaemia, T2DM and fatty liver bymodulating various pathways and receptors, improve cardiovascular health, reduce body weight and prolong cellular life.
Berberine has poorsolubilityand low bioavailabil-ity in vivo. The metabolic form of berberine in the body is its interaction with the gutmicrobiota after oral administration. Nitroreductase (NR) in intestinal bacteria converts berberine in the intestine into the easily absorbed form - dihydroberberine, which is 5-10 times more absorbed than berberine in the intestine.
When dihydroberberine is absorbed into the intestinal wallby the epithelal cells ofthe small intestine, a non-enzymatic reaction occurs under the action of a largenumber of oxidising factors in the intestinal walltisues (e.g, monoamine oxidase, superoxide anion, metalions, etc,, causing dihydroberberine to auickly oxidize and convert back to berberine, and enter the bloodstream to exert its pharmacological efects. Dihydroberberine can significantly improve gastrointestinal discomfort, with lower doses and better absorption compared to berberine.
Increase serum berberine concentration
Subject: Five healthy males, using a randomised, double-blind, placebo-controlledtrial.Dosage:Placebo (resistant dextrin)(PLA), 500 mg berberine (B500), 100 mgdihydroberberine (D100)or200 mg dihydroberberine (D200).Assessment parameters: serum berberine concentration, glucose level and insulinlevel. Peak concentrations and areas under the curve are calculated for all variables
Results:DHB supplementation significantlyincreased serum berberine levels
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Figure 1 Individual and aggregated meanvalues for berberine AUC by condition
Promote GLP-1 release from STC-1 cells
STC-1 has many characteristics of natural intestinal endocrinecells and is commonly used as a screening platform to identify foods or compounds that regulate gastrointestinal hormonesecretion in vitro.STC-1 cells release GLP-l in response to berberine and PTC Berberine can increase the expression of pro-glucagon (GLP-1 precursor mRNA (1, 10, 100, and 200 uM) (A) and the secretion level ofGLP-1 (10,100,and 200 μM)(B)
Yue, X., Liang, 」., Gu, F, Du, D., & Chen, F. (2018). Berberine activates bitter taste responses ofenteroendocrine STC-1 cells. Molecular and Cellular Biochemistry. doi:10.1007/s11010-018-3290-3
Figure 2 Expression of pro-glucagon (GLP-1 precursor) mRNA(1, 10, 100, and 200 uM)(A) and secretion levels of GLP-1 (10, 100, and 200 uM) (B) in STc-1 cells in response to berberine.
Relieve insulin resistance and fat accumulation
Subiect: Male c57BL/6J mice (6 weeks old) fed with normal food for 2 weeks to acclimatise.Dosage: Six groups of 10 mice each. Normal food diet (NcD), NcD group supplemented with berberine (NcDBBR),high fat diet (HFD group), HFDsupplemented with berberine (HFDBBR, HFD supplemented with antibiotics (HFDABT and HFD supplemented with berberine and antibiotics(HFDBBRABT).
Assessment parameters: Insulin sensitivity test, pathological tissue sections.Results: Berberne sienificanty reduced blood glucose levels and aleviated insulin resistance in mice,Through liver tissue sice analysis it was foung that there were a arge number of red stained adipocvtes in the liver of HED group mice, but notin the iver of HED BBR grouo mice. reatment wit combination antilbiotics (HFD ABT and HFD ABT BBR groups significantly reduced the accumulation of red adipocytes in the livers of mic in the HFD group. These results indicate that the gut microbiota derived from a high-fat diet may promote fat accumulation in the liver, and both berberine andcompound antibiotics can aleviate fat accumulation
LiJ. LiJ,Niy,Zhangc,Jia J WuG, Sun Hand Wang Front Microbiol12-75251 doi: 10.3389/fmicb.2021.752512
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