Hermetica Superfood Encyclopedia
The Short Answer
Bergenin is a C-glucoside of 4-O-methylgallic acid, a phenolic compound found in plants like Bergenia species. It modulates TRPA1/TRPV1 channels and NR2B receptors, showing promise for neuropathic pain relief and cognitive protection in animal studies.
CategoryNamed Bioactive Compounds
GroupCompound
Evidence LevelModerate
Primary Keywordbergenin benefits
Synergy Pairings3
Bergenin (C-Glucoside of 4-O-methylgallic acid) — botanical close-up
Health Benefits
Origin & History
Natural habitat
Bergenin is a C-glucoside of 4-O-methylgallic acid, a bioactive polyphenolic compound naturally sourced from plants including Mallotus japonicus, Bergenia ligulata, and Bergenia purpurascens. This compound can be obtained through both natural extraction from plant cortex and laboratory synthesis.
“Bergenin-containing plants have been used in Eastern traditional medicine for centuries, including applications in traditional cancer treatments. Specific traditional medicine systems and historical indications are not detailed in available research.”Traditional Medicine
Scientific Research
Current research consists entirely of preclinical studies in animal models and cell cultures, with no human clinical trials identified. Key studies include rat models of chemotherapy-induced neuropathic pain (PMID: 38149571), sodium azide-induced dementia (PMID: 36249784), and tuberculosis co-treatment (PMID: 30975902).
Preparation & Dosage
Traditional preparation
Animal studies have used 10 mg/kg body weight intraperitoneally for renal protection. No human dosage recommendations or standardized extracts have been established. Consult a healthcare provider before starting any new supplement.
Nutritional Profile
Bergenin is a pure isolated bioactive compound (C-glucoside of 4-O-methylgallic acid), not a whole food ingredient, and therefore has no conventional macronutrient or micronutrient profile. Molecular formula: C14H16O9; molecular weight: 328.26 g/mol. It is classified as an isocoumarin-related polyphenolic glycoside. As a compound, it contains no protein, fat, dietary fiber, or caloric value in pharmacological dosing contexts. Bioactive composition is 100% bergenin when in purified form. Natural source concentrations vary: found at approximately 0.5–2% dry weight in Bergenia crassifolia rhizomes, ~1–3% in Ardisia japonica aerial parts, and trace amounts (0.1–0.5%) in Saccharum officinarum (sugarcane) bark and Flueggea microcarpa. Solubility: moderately water-soluble (~1.8 mg/mL in water at 25°C), with improved solubility in polar organic solvents (DMSO, methanol). Bioavailability: oral bioavailability is limited due to poor gastrointestinal absorption and rapid hepatic metabolism; preclinical studies suggest peak plasma concentrations reached at 1–2 hours post-oral administration in rodent models, with a half-life of approximately 3–5 hours. Gut microbiota-mediated hydrolysis may partially convert bergenin to norbergenin (demethylated metabolite), which retains partial bioactivity. No clinically established human pharmacokinetic data is currently available. Relevant co-occurring phytochemicals in plant sources include gallic acid, catechins, and flavonoids, which may exhibit synergistic bioavailability enhancement.
How It Works
Mechanism of Action
Bergenin reduces neuropathic pain through dose-dependent modulation of TRPA1 and TRPV1 ion channels along with NR2B receptor inhibition. For cognitive protection, it appears to reduce amyloid-β accumulation, though the specific molecular pathways remain under investigation. The C-glucoside structure of 4-O-methylgallic acid contributes to its bioactivity and stability.
Clinical Evidence
Current evidence for bergenin comes exclusively from preclinical animal studies with no human clinical trials available. Animal research demonstrates dose-dependent reduction in chemotherapy-induced neuropathic pain and recovery from dementia-like symptoms. Studies show measurable decreases in amyloid-β accumulation in rodent models of cognitive decline. The lack of human data significantly limits the applicability of these findings to therapeutic use.
Safety & Interactions
Safety data for bergenin in humans is extremely limited due to the absence of clinical trials. No established side effect profile, drug interactions, or contraindications have been documented. Pregnant and breastfeeding women should avoid bergenin supplements due to insufficient safety data. Individuals taking medications for neurological conditions should consult healthcare providers before use given its effects on ion channels and neurotransmitter receptors.
Synergy Stack
Hermetica Formulation Heuristic
Frequently Asked Questions
What is bergenin and where does it come from?
Bergenin is a C-glucoside of 4-O-methylgallic acid, a phenolic compound naturally found in Bergenia species and other plants. It's classified as a polyphenolic compound with demonstrated bioactivity in preclinical research.
Does bergenin help with nerve pain?
Animal studies show bergenin reduces chemotherapy-induced neuropathic pain through modulation of TRPA1/TRPV1 channels and NR2B receptors. However, no human clinical trials have confirmed these pain-relieving effects in people.
Can bergenin improve memory and cognition?
Preclinical studies demonstrate bergenin helps recover dementia-like symptoms in animal models and reduces amyloid-β accumulation. These cognitive benefits have not been tested or confirmed in human studies.
What are the side effects of bergenin supplements?
No established side effects exist for bergenin due to lack of human clinical trials. Safety profile, drug interactions, and contraindications remain unknown without proper human testing.
How much bergenin should I take for benefits?
No established dosage recommendations exist for bergenin supplements since all research is limited to animal studies. Human dosing guidelines cannot be determined without clinical trials establishing safety and efficacy in people.
Is bergenin safe to take with common pain medications like ibuprofen or acetaminophen?
While bergenin and common over-the-counter pain relievers work through different mechanisms, combining them requires caution. Bergenin's effects on pain pathways (TRPA1/TRPV1/NR2B modulation) have only been demonstrated in animal studies, so human safety data on co-administration with NSAIDs or acetaminophen is limited. Consult a healthcare provider before combining bergenin with other pain medications to avoid potential interactions or additive effects.
What is the difference between bergenin and other herbal compounds studied for neuropathic pain?
Bergenin is a C-glucoside of 4-O-methylgallic acid with a specific mechanism targeting multiple pain receptors (TRPA1, TRPV1) and the NR2B pathway, whereas many traditional herbal pain compounds work through broader anti-inflammatory effects. Current evidence for bergenin is limited to preclinical animal models of chemotherapy-induced pain, whereas established compounds like curcumin or alpha-lipoic acid have more extensive human clinical trial data. The unique receptor-specific action of bergenin may offer targeted benefits, but direct comparative human studies are not yet available.
Who would be the best candidate for bergenin supplementation based on current research?
Based on preclinical evidence, bergenin may be of greatest interest to individuals experiencing chemotherapy-related neuropathic pain or cognitive concerns related to amyloid-β accumulation, though human clinical trials are needed to confirm efficacy. Elderly individuals or those with neuroinflammatory conditions may theoretically benefit from bergenin's effects on Th17 cell suppression and NF-κB inhibition, but this remains speculative. Anyone considering bergenin should recognize that current evidence is limited to animal studies and preliminary research, making it unsuitable as a replacement for established treatments without professional medical guidance.
Explore the Full Encyclopedia
7,400+ ingredients researched, verified, and formulated for optimal synergy.
Browse IngredientsThese statements have not been evaluated by the Food and Drug Administration. This content is for informational purposes only and is not intended to diagnose, treat, cure, or prevent any disease.
hermetica-encyclopedia-canary-zzqv9k4w bergenin curated by Hermetica Superfoods at ingredients.hermeticasuperfoods.com and licensed CC BY-NC-SA 4.0 (non-commercial share-alike, attribution required)
