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.
Some plant species with substantial levels of bergenin:
- Bergenia species (B. cassifolia -leaves)
- Corylopsis spicata (bark)
- Fluggea 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 suggest 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.
Additional Resources
Han LK, Ninomiya H, Taniguchi M, Baba K, Kimura Y, Okuda H. Norepinephrine-augmenting lipolytic effectors from Astilbe thunbergii rhizomes. J Nat Prod 1998; 61:1006-11.
Nazir N, Koul S, Qurishi MA, taneja Sc, Ahmad SF, Bani S, Qazi GN. immunomodulatory effect of bergenin and norbergenin against adjuvant-induced arthritis. A flow cytometric study. J ethnopharmacol 2007;112:401-05
Zuo GY, li ZQ, chen lR, Xu XJ. in vitro anti-Hcv activities of Saxifraga melanocentra and its related polyphenolic compounds. Antivir chem chemother 2005; 16:393-8.
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