Herbal Pharmacology – Berberine for cholesterol

Berberine has a strong yellow color, Berberis species were used to dye wool, leather, and wood.

Berberine, a natural alkaloid, is found in Goldenseal, a popular herb that has historically been used for its antimicrobial activity to improve symptoms associated with colds, cold sores, urinary tract infections, as well as other infections.

berberine for lowering cholesterol

Part of plant used

Berberine is naturally found in the root, rhizomes, stems, and bark of a variety of plants including

– Berberis (e.g. Berberis vulgaris (barberry)

– Berberis aristata (tree turmeric)

– Mahonia aquifolium (Oregon grape)

– Hydrastis canadensis (goldenseal)

– Xanthorhiza simplicissima (yellowroot)

– Phellodendron amurense (Amur cork tree)

– Coptis chinensis (Chinese goldthread)

– Tinospora cordifolia

– Argemone mexicana (prickly poppy),

– Eschscholzia californica (Californian poppy).

 

 

Chemical Constituents

Berberine is an alkaloid found in a variety of plants. It is considered a quaternary ammounium

 

MOA

Berberbine has been observed to increase the expression of LDL receptors on liver cells.  LDL receptors sit on the outer surface of many cells including liver cells where they can pick up LDL circulating in the bloodstream and transport them into the cell.  Once inside the cell, LDL is broken down and cholesterol is released.  The newly released cholesterol is then used by the cell, stored, or removed from the body.  After LDL receptors release LDL, they can be recycled back to the cell surface to pick up more LDL.  This mechanism of action appears to be unique compared to any of the current prescription drugs on the market.

 

Clinical Research

 

The first pivotal clinical trial that evaluated berberine for reducing total cholesterol and LDL in 32 human subjects was published in 2004.1  During the 12 week clinical trial berberine was observed to reduce serum cholesterol by 29%, triglycerides by 35% and LDL-cholesterol by 25%.  Interestingly, a mechanism of action was identified during this study that suggests berberine increases the amount of LDL receptor in liver cells.  Increased expression of LDL in liver cells will decrease the amount of circulating LDL.

 

Another clinical trial evaluated the efficacy of berberine in reducing total cholesterol and triglycerides over a 12 week period.2 Seven subjects received 500 mg three times daily representing a daily dose of 1,500 mg of berberine. Reductions in total cholesterol was 12.2% (197.6 before study; 173.4 after study) and triglycerides was reduced by 23% (134.9 before study; 103.9 after study) following 12 weeks of berberine.  During the study liver function and kidney function was evaluated with no evidence suggesting adverse effects of berberine during the study.

 

Dose

500 mg taken two times daily.  Doses up to 2,000 mg daily have been used in clinical trials.

*If used in combination with other ingredients the dose may be lowered.

 

 

References

  1. Kong et al.  Berberine is a novel cholesterol-lowering drug working through a unique mechanism distinct from statins.  Nature Medicine.2004 Dec; Volume 10 (Issue 12): Pages 1344-51.
  2. Hu et al.  Lipid-lowering effect of berberine in human subjects and rats. Phytomedicine.2012 Jul 15;19(10):861-7.

 

Jeremy Johnson, PharmD, PhD


Categories: Antioxidant, Cholesterol, Herbal Pharmacology