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Bergenin is a c-glucoside of 4-O-methylgallic acid -referred to as an iso-coumarin derivative with the proper nomenclature: 4-methoxy-2-[(1S,2R,3S,4S,5R)-3,4,5,6-tetrahydro-3,4,5-trihydroxy-6-(hydroxymethyl)-2H-pyran-2-yl]-α-resorcylic acid δ-lactone monohydrate,

Its chemical formula is C14H16O9.H2O and molecular weight 346.3 grams per mole.

Bergenin's unique chemical structure involves 3 6-member rings: aromatic, glucopyranose, and annellated sigma-lactone. It has two analogues (norbergenin and acetylbergenin) with additional pharmacological effects.

Bergenin is most abundant in the genera of Euphorbeacea, Myrsinaceae, and Saxifragaceae plant families.

Bergenin is found in many plants of the genus Bergenia, as well as some plants of the genera Astilbe, Ardisia, Mallotus, and Flueggea. Bergenin containing plants have been used for thousands of years in India for many different purposes. Uses of bergenin in traditional medicine include to treat obesity, asthma, ulcers, as an anti-inflammatory, liver detoxifier, and an expectorant.

A limited amount of research has shown Bergenin to be useful for encouraging fat loss and preventing fat gain. Bergenin has been found oppose the insulin-induced storage of glucose as fat, so it may be useful for preventing fat gain when an individual is eating a surplus of carbohydrate calories. Bergenin has also been found to enhance the effects of norepinephrine on fat break down, leading to greater body fat breakdown and possibly more fat burned as opposed to glucose or protein when an individual is eating on a caloric deficit. Bergenin has some additional benefits as well. Bergenin has been shown to aid in liver detoxification, act as a anti-inflammatory and protect against arthritis, act as an expectorant, relieve asthma, stimulate the immune system, and may also have use in the treatment and prevention of ulcers.

Bergenin is often included in thermogenic fat burners along with ingredients that stimulate norepinephrine release for its ability to enhance the breakdown of fat by this hormone. Bergenin may also be purchased by itself as an extract of Bergenia root.

Some plant species with substantial levels of bergenin:

Bergenia species (B. cassifolia -leaves)

Corylopsis spicata (bark)

Fl ea virosa

Sacoglottis uchi

Bergenin-containing plant species have been used in traditional healing systems of India and China since at least the 7th century A.D. These herbs have been used to address wound healing, renal stone resolution, liver conditions, and cardiac arrhythmia. Bergenin appears to be a primary active ingredient, responsible for multiple actions.

Bergenin has evidence substantiating these properties:

antiarrhythmic

antioxidative

antimicrobial

hepatoprotective

protective against gastric ulcers

anti inflammatory

Insulin enhancing and lypolytic

Enhances Wound Healing

Influence on Cardiac Arrhythmias

Bergenin-containing herbs have traditionally been used to address cardiac arrhythmias. In several animal models arrhythmias have been countered effectively with varying dosages. While the mechanism for this is still being explored, it is hypothesized that bergenin augments the parasympathetic component of the autonomic nervous system.

Antioxidant Effects

Studies s est that bergenin has free-radical scavenging capability and decreases lipid peroxidation of cell membranes. It has a higher antioxidant activity than l-ascorbic acid (vitamin C) and protects against ascorbic acid depletion in several different body tissues.

Antimicrobial Characteristics

Bergenin has demonstrated antibacterial activity against species like E. coli and Pseudomonas aeruginosa. It is also effective against many types of fungus since it inhibits their energy metabolism. It does this by blocking a crucial enzyme called yeast alcohol-dehydrogenase which is required for fermentation reactions. This also makes it an effective preservative alternative in beverages.

Bergenin has demonstrated anti-hepatitis C virus (HCV) activity and weak anti-HIV activity in vitro. It is not effective at attacking HIV-I reverse transcriptase and HIV integrase.

Liver-Protective Properties

Bergenin appears to protect the liver against damaging environmental poisons. When animals are given bergenin and then challenged with toxins like carbon tetrachloride their livers experience less damage and secrete less of the indicators like aspartate aminotransferase (AST) and alanine aminotransferase (ALT). Part of the mechanism for this appears to be replenishment and protection of the crucial glutothione antioxidant system in liver cells burdened with the tasks of neutralizing or eliminating environmental toxins.

Inflammation

Bergenin effects inflammation by balancing secretion of cellular messengers (cytokines) from pro-inflammatory and inhibitory cells of the immune system.

It inhibits the release of inflammatory cytokines like Interleukin-2 (IL-2), gamma interferon (IFN-gamma), and Tumor Necrosis Factor-alpha (TNF-alpha). It also promotes the release of anti-inflammatory messengers like Interleukin-4 and Interleukin-5. It also stimulates the release of protective prostaglandins.

Obesity and Insulin

Bergenin also plays a role in the mobilization and breakdown of fat and is becoming a popular component of thermogenic fat-burning dietary supplements.

Bergenin does not directly stimulate lipolysis (fat breakdown from adipose tissue) but appears to enhance the activity of lipolytic adrenergic hormones like norepinephrine. It also opposes the lipogenic activities of insulin. The mechanism appears to be through the enhancement of norepinephrine to phospholipids of adipose cells.

Bergenin displays moderate activity against an enzyme called protein tyrosine phospatase 1B (PTP1B). This enzyme negatively regulates insulin and leptin signalling and some of the positive effects of insulin and leptin (blood sugar and appetite regulation) may be enhanced by its inhibition.

Toxicity

Bergenin is considered safe for long-term use.

In animal models no toxicity or adverse effects have been observed, even with very large dosages.