The Multiple Health Benefits of Citrus Bergamot

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Citrus Bergamot

Citrus bergamia Risso, also known as the bergamot orange or Citrus bergamot, is a fragrant citrus fruit the size of an orange, with a green color similar to a lime.  The word bergamot is etymologically derived from the Italian word “bergamotto”.

Image result for citrus bergamot

Figure 1.  Citrus bergamot on the vine  (Source)

Citrus bergamot is a citrus plant that grows almost exclusively in the narrow coastal Calabria region in Southern Italy, due to sensitivity to the weather and soil conditions.   It is cultivated in Italy for the production of bergamot oil, a component of many brands of perfume and tea, especially Earl Grey tea. 

While bergamot is native to Italy, it is now widely distributed throughout the subtropical regions of China, including Guangdong, Guangxi, Fujian and Yunnan.

Image result for citrus bergamot

Figure 2.  Citrus Bergamot  (Source)

Genetic researchers have found that the bergamot orange is probably a hybrid of Citrus limetta and Citrus aurantium.

Citrus bergamia is sometimes confused with (but is not the same as):

  • Citrus medica (citron, the yellow fruit of which is also known as etrog)
  • Citrus limetta, the “sweet lemon” or “sweet lime”

Citrus Bergamot differs from C. Aurantium as Citrus Bergamot does not contain Synepherine, N-methyltyramine, and octopamine, which have been shown in research to constrict arteries, increase blood pressure, increase heart rate, cause heart-rhythm disorders, heart attack, and stroke.

Bio-Active Ingredients of Citrus Bergamot

The bio-active ingredients in citrus bergamot includes a unique profile of flavonoid and glycosides, such as:  1  2

  • brutieridin
  • melitidine
  • naringin
  • neodesmin
  • neoeriocitrin
  • neohesperidin
  • ponceritin
  • poncirin
  • rhoifolin
  • rutin

Health Attributes of Citrus Bergamot

A number of studies have shown the positive and powerful health attributes of citrus bergamot.  Among these attributes include:

  • anti-inflammatory  3
  • anti-hypertensive  4
  • hepatic protective effects  5
  • promotes digestion  6 

A clinical study found reduced total low-density lipoprotein, cholesterol, triglyceride and blood glucose levels in 237 patients who had taken oral BPF for 30 days.  7 

Moreover, the expression levels of two autophagy markers (LC3 II/I and Beclin-1) were increased while SQSTM1/p62 expression was reduced, indicating that BPF could stimulate autophagy.  8 

Naringin has been shown to be beneficial in animal models of atherosclerosis, while neoeriocitrin and rutin have been found to exhibit a strong capacity to prevent LDL from oxidation.

Brutieridine and melitidine has been shown to have the ability to inhibit HMG-CoA reductase.

Bergamonte®

Bergamonte® is an exclusive product produced by HP Ingredients which contains bioactive compounds of extract of the juice and albedo of citrus bergamia risso. 

HP Ingredients is a fasty growing innovative herbal and nutraceutical extract health company focused on bringing effective remedies from Asia, Italy, and Chile to the North American Market. HP Ingredients is dedicated to innovating new products and providing accurate and timely information on benefits of these well-researched extracts. We work closely with several teams of scientists from University of Malaysia and Forest Research Institute of Malaysia, the Universidad Austral de Chile, and the University Magna Graecia.

Bergamonte®, an extract of the bergamot orange, was shown in a double-blind, placebo-controlled study to:

  • Support the healthy balance of HDL to LDL cholesterol
  • Support healthy triglycerides and total cholesterol levels
  • Promote healthy blood sugar levels already in the normal range

Melitidine and Brutieridine

A published research article in the Journal of Natural Products 2009 showed that bergamot juice contained novel compounds with statin like principles, having the 3-hydroxy3-methylglutaric acid (HMG) found to the naringin (melitidine) and neohesperidin (brutieridine).

These novel compounds interfere with the natural synthesis of the cholesterol pathway in the human body: The HMG-CoA substrate interferes with the synthesis of the mevalonate acid, blocking the cholesterol production.

Superior Full-Spectrum Antioxidant ORAC Potency

Mode of Action

  • Inhibiting HMG-CoA Reductase
  • Inhibiting Phosphodiesterases PDEs
  • ‘Activating’ AMPK

Efficacy Findings from Clinical Trials

In an unpublished human clinical trial involving 192 patients, the following are the result after patients consumed 100ml of Citrus Bergamot juice for 30 days.

Hypolipemic and Hypoglycemic Activity of Bergamot Polyphenolic Fraction

Fitoterapia 82 (Nov 2011) 309–316
237 patients with hyperlipemia, hypercholesterolemic (HC, cLDL, low cHDL), mixed dyslipidemic (HC and TG), or metabolic syndrome (HC, HT, and HG) were taking either placebo, 500mg, 1000mg.

The effect of Bergamot Polyphenolic Fraction (500 and 1000 mg/daily) on reactive vasodilatation in patients suffering from isolated (HC) or mixed hyperlipidemia (HC/HT) and associated hyperglycemia (HC/HT /HG).

Bergamot Polyphenolic Fraction reduces total and LDL cholesterol levels (an effect accompanied by elevation of cHDL), triglyceride levels and by a significant decrease in blood glucose. Moreover, it  inhibited HMG-CoA reductase activity and enhances reactive vasodilation.

Supports healthy cholesterol level, increase LOX-1 expression and Protein Kinase B phosphorylation

International Journal of Cardiology, 2013
In this open-label, parallel group, placebo-controlled study, 77 patients were randomly assigned either placebo, Rosuvastatin, Bergamot Polyphenolic Fraction or combination of Bergamot Polyphenolic Fraction with Rosuvastatin for 30 days.

Both doses of rosuvastatin and Bergamot Polyphenolic Fraction help support healthy cholesterol level and reduce urinary mevalonate compared to control group. The benefits are associated with significant reductions of biomarkers used for detecting oxidative vascular damage, including malondialdehyde, oxyLDL receptor LOX-1 and phosphoPKB.

Effects on LDL Small Dense Particles, Metabolic Biomarkers, and Liver Function

Advances in Biological Chemistry, 2014, 4, 129-137
107 patients with metabolic syndrome and non fatty liver disease were given either placebo or 650 mg of Bergamot Polyphenolic Fraction twice a day for 120 days. Bergamot Polyphenolic Fraction group showed significant reduction in fasting plasma glucose, rotal cholesterol, LDL cholesterol, triglycerides, and increase of HDL cholesterol. Bergamot Polyphenolic Fraction decrease IDL particles by 51%, increase large LDL by 38%, decrease small LDL by 35%, and 20% increase of total HDL particles. Hepatorenal index was significantly reduced by 46%, accompanied by reduction of hepatic ultrosonographic pattern of steatosis by 99%. This suggests Bergamot Polyphenolic Fraction improves both liver function and inflammation as confirmed by reduction of TNF-α and CRP.

Product Comparison

Already within the normal range  

References
References
  1. Ross Walker, Elzbieta Janda and Vincenzo Mollace. The Use of Bergamot-derived Polyphenol Fraction in Cardiometabolic Risk Prevention and its Possible Mechanisms of Action. Cardiac Health and Polyphenols. Chp 84, Pg 1085-1103, 2014
  2. Micaela Gliozzi, Ross Walker, Elzbjeta Janda, Vincenzo Mollace. Bergamot polyphenolic fraction enhances rosuvastatin-induced effect on LDLcholesterol, LOX-1 expression and Protein Kinase B phosphorylation in patients with hyperlipidemia. International Journal of Cardiology Dec 2013, 170(2):140-5
  3. Vincenzo Mollace, Iolanda Sacco, Elzbieta Janda, Claudio Malara, Domenica Ventrice, Carmen Colica, Valeria Visalli, Saverio Muscoli. Hypolipemic and hypoglycaemic activity of bergamot polyphenols: From animal models to human studies. Fitoterapia 82 (2011) 309–316
  4. Celia C, Trapasso E, Locatelli M, Navarra M, Ventura CA, Wolfram J, Carafa M, Morittu VM, Britti D, Di Marzio L.. Anticancer activity of liposomal bergamot essential oil (BEO) on human neuroblastoma cells. Colloids Surf B Biointerfaces. 2013 Dec 1;112:548-53
  5. Delle Monache S, Sanità P, Trapasso E, Ursino MR, Dugo P, Russo M, Ferlazzo N, Calapai G, Angelucci A, Navarra M. Mechanisms underlying the anti-tumoral effects of Citrus Bergamia juice. PLoS One. 2013 Apr 16;8(4)
  6. Kang P, Suh SH, Min SS, Seol GH. The essential oil of Citrus bergamia Risso induces vasorelaxation of the mouse aorta by activating K(+) channels and inhibiting Ca(2+) influx. J Pharm Pharmacol. 2013 May;65(5):745-9
  7. Leopoldini M, Malaj N, Toscano M, Sindona G, Russo N. On the inhibitor effects of bergamot juice flavonoids binding to the 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) enzyme. J Agric Food Chem. 2010 Oct 13;58(19):10768-73
  8. Di Donna L, De Luca G, Mazzotti F, Napoli A, Salerno R, Taverna D, Sindona G. Statin-like principles of bergamot fruit (Citrus bergamia): isolation of 3-hydroxymethylglutaryl flavonoid glycosides. J Nat Prod. 2009 Jul;72(7):1352-4
  9. Mollace V, Ragusa S, Sacco I, Muscoli C, Sculco F, Visalli V, Palma E. The protective effect of bergamot oil extract on lecitine-like oxyLDL receptor-1 expression in balloon injury-related neointima formation. J Cardiovasc Pharmacol Ther. 2008 Jun;13(2):120-9
  10. Natalizia Miceli, Maria Mondello, Maria Mondorte, Vasileios Sdrafkakis, Paola Dugo, Maria Crupi. Hypolipidemic effects of bergamot juice in rats Fed a Hypercholesterolemic Diet. J. Agric. Food Chem., Vol. 55, No. 26, 2007