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Clinical pharmacology of bergamot for lowering cholesterol

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Bergamot (Citrus bergamia) is a citrus fruit about the size of an orange with a color similar to a lemon and is considered inedible, however extracts have been used to scent food and perfurmes.

One example would be Earl Grey Tea which is flavored with Bergamot. Historically, the juice has been used in Calabrian, a region in Italy (i.e. ‘toe’ of Italy) as a natural medicine to treat Malaria.

The name is derived from bergamotta in Italian and originates from Bergamo, a town in Southern Italy.

Two phytochemicals Melitidin and brutieridin, exist only in the citrus Bergamot and have been suggested to inhibit the cholesterol biosynthesis pathway, possibly through inhibition of HMG-coA-reductase.  It is important to point out that this mechanism of action would differ from the statin drugs that are widely prescribed.

Part of plant used

Fruit

 

Latin Name

Citrus bergamia

 

 

Chemical constituents

Two phytochemicals Melitidin and brutieridin,

 

Mechanism of action

Activates AMPK (AMP-activated protein kinase), a master switch that regulates cholesterol synthesis, lipogenesis, triglyceride synthesis.

 

Clinical Research

  1. In an open label clinical trial, Bergamot (1000 mg per day) was observed to reduce total cholesterol from 278 to 191, representing a 32% reduction.1 LDL cholesterol was reduced from 191 to 113 (31% reduction), reduce triglycerides from 238 to 165 (31% reduction).  HDL cholesterol, known for its cardio protective properties, was increased from 38 to 45 (18% increase).
  2. A second clinical trial evaluated the potential of bergamot at either 500 mg or 1,000 mg per day for three months to reduce total cholesterol, reduce LDL, and increase HDL.2  Total cholesterol was reduced by 20% (500 mg of berberine) and 30.9% (1,000 mg of berberine).  LDL was reduced by 23% (500 mg berberine) and by 38.6% (1,000 mg of berberine).  HDL was increased by 25.9% (500 mg of berberine) and by 39% (1,000 mg of berberine).

 

 

Dose

In Clinical trials doses typically are 500 or 1000 mg with a product that is standardized to polyphenols.  Analyzing the results of the clinical trials show that both doses will lower total and LDL cholesterol compared to placebo.

Statistically, there was not a benefit to increase the dose from 500 to 1000 mg with bergamot’s cholesterol lowering properties.

 

References

[1]M. Gliozzi, R. Walker, S. Muscoli, C. Vitale, S. Gratteri, C. Carresi, V. Musolino, V. Russo, E. Janda, S. Ragusa, A. Aloe, E. Palma, C. Muscoli, F. Romeo, V. Mollace, Bergamot polyphenolic fraction enhances rosuvastatin-induced effect on LDL-cholesterol, LOX-1 expression and protein kinase B phosphorylation in patients with hyperlipidemia. Int J Cardiol 170 (2013) 140-145.

[2]V. Mollace, I. Sacco, E. Janda, C. Malara, D. Ventrice, C. Colica, V. Visalli, S. Muscoli, S. Ragusa, C. Muscoli, D. Rotiroti, F. Romeo, Hypolipemic and hypoglycaemic activity of bergamot polyphenols: from animal models to human studies. Fitoterapia 82 (2011) 309-316.

 

 

 

 

Jeremy Johnson, PharmD, PhD
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Categories: Herbal Pharmacology