Hermetica Superfood Encyclopedia
The Short Answer
Chelerythrine is a benzophenanthridine alkaloid derived primarily from Chelidonium majus (greater celandine) and Sanguinaria canadensis. It exerts cytotoxic and antimicrobial effects largely through protein kinase C (PKC) inhibition and direct DNA intercalation, with a reported IC50 of approximately 0.7 μM in cancer cell lines.
CategoryNamed Bioactive Compounds
GroupCompound
Evidence LevelModerate
Primary Keywordchelerythrine benefits
Synergy Pairings3
Chelerythrine — botanical close-up
Health Benefits
Origin & History
Natural habitat
Chelerythrine is a quaternary benzophenanthridine alkaloid (C₂₁H₁₈NO₄⁺) extracted from plants in the Papaveraceae family, including Chelidonium majus (greater celandine), Macleaya cordata, and Sanguinaria canadensis, as well as Rutaceae family plants like Zanthoxylum asiaticum. It exists in two pH-dependent forms: a charged iminium cation (active at acidic pH) and a neutral alkanolamine pseudo-base, typically extracted using ethanol or acid-base methods to yield chelerythrine chloride as the stable salt form.
“Chelerythrine-rich plants have been used for millennia across European, Chinese, and Native American traditional medicine. Chelidonium majus treated warts, jaundice, and gastrointestinal issues since Greek/Roman times, while in Traditional Chinese Medicine, Macleaya cordata and Zanthoxylum asiaticum addressed inflammation and tumors for over 1000 years.”Traditional Medicine
Scientific Research
No high-quality human clinical trials, randomized controlled trials (RCTs), or meta-analyses were identified for chelerythrine as a standalone therapeutic agent. Its evaluation is limited to preclinical in vitro and animal studies for anticancer effects, with PubMed searches yielding no human trials with PMIDs for chelerythrine monotherapy.
Preparation & Dosage
Traditional preparation
No clinically studied dosages exist due to absence of human trials. Preclinical studies use 1-50 μM concentrations in vitro and 5-20 mg/kg intraperitoneally in animal models. Traditional herbal preparations contain trace amounts (0.1-0.5% of dry weight) without standardization. Commercial supplements suggest 1-5 mg/day anecdotally, but this lacks clinical validation. Consult a healthcare provider before starting any new supplement.
Nutritional Profile
Chelerythrine is a benzophenanthridine alkaloid (not a nutrient or food ingredient), so classical macronutrient/micronutrient profiling is not applicable. Key chemical and bioactive data: Molecular formula C21H18NO4+ (quaternary ammonium salt, typically as chloride salt C21H18ClNO4, MW ~383.83 g/mol). Primary bioactive classification: isoquinoline alkaloid. Concentration in source plant Chelidonium majus (greater celandine): aerial parts ~0.01–0.1% dry weight; latex/sap: up to 0.4–1.0% dry weight (highest concentration). Co-occurring alkaloids in same plant matrix include sanguinarine (~0.01–0.05% dry weight), berberine, coptisine, and chelidonine, which influence combined bioactivity. Bioavailability notes: Chelerythrine is a planar aromatic cation with high lipophilicity (logP ~2.8–3.2), enabling membrane penetration and DNA intercalation. Oral bioavailability in humans is poorly characterized; preclinical data suggest rapid tissue distribution but significant first-pass hepatic metabolism. It binds strongly to plasma proteins and DNA. No dietary reference intake (DRI), recommended daily allowance (RDA), or tolerable upper intake level (UL) exists, as it is a pharmacologically active alkaloid, not a dietary nutrient. Protein content: not applicable (pure alkaloid compound). Fiber/carbohydrate/fat content: not applicable. Relevant physicochemical properties affecting bioavailability: water solubility ~0.5–2 mg/mL as chloride salt; pH-dependent ionization; stability reduced under alkaline conditions and UV light exposure.
How It Works
Mechanism of Action
Chelerythrine inhibits protein kinase C (PKC) by competing at the catalytic site, disrupting downstream phosphorylation cascades involved in cell proliferation and survival. It intercalates into double-stranded DNA, inducing strand breaks and apoptosis in rapidly dividing cells, with an IC50 near 0.7 μM in several tumor cell lines. Additionally, chelerythrine suppresses NF-κB signaling and inhibits COX-2 expression, contributing to its observed anti-inflammatory activity in preclinical models.
Clinical Evidence
Evidence for chelerythrine's benefits in humans is extremely limited; virtually all mechanistic data derive from in vitro cell-line studies and rodent models with no large-scale randomized controlled trials completed to date. Animal studies have demonstrated tumor growth inhibition and antimicrobial effects against Staphylococcus aureus and Candida species, but these have not been replicated in human trials. Traditional use in European herbal medicine for topical wart and skin lesion treatment via Chelidonium majus extracts provides historical context but no quantified clinical outcomes. The overall evidence level remains preliminary, and no established therapeutic dose for humans has been validated through controlled research.
Safety & Interactions
Chelerythrine is cytotoxic at relatively low concentrations and carries a narrow therapeutic index, making unsupervised supplementation potentially dangerous. Oral ingestion of Chelidonium majus extracts containing chelerythrine has been associated with hepatotoxicity, including cholestatic and cytolytic liver injury, and is contraindicated in individuals with pre-existing liver disease. Chelerythrine may potentiate the effects of anticoagulants and interact with CYP3A4-metabolized drugs due to enzyme inhibition observed in vitro. It is considered unsafe during pregnancy and breastfeeding given its demonstrated cytotoxic and mutagenic potential in preclinical models.
Synergy Stack
Hermetica Formulation Heuristic
Also Known As
Benzophenanthridine alkaloidQuaternary benzophenanthridineC₂₁H₁₈NO₄⁺Chelidonium alkaloidSanguinaria alkaloidMacleaya alkaloidPKC inhibitor alkaloidBenzylisoquinoline derivative
Frequently Asked Questions
What plant sources contain chelerythrine?
Chelerythrine is found in highest concentrations in Chelidonium majus (greater celandine) and Sanguinaria canadensis (bloodroot), where it can constitute up to 4% of the dried plant's alkaloid fraction. It is also present in Macleaya cordata, Bocconia frutescens, and several Papaver species. Chelidonium majus root and latex have historically been the primary extraction sources used in European herbal preparations.
Is chelerythrine safe to take as a supplement?
Chelerythrine is not considered safe for unsupervised oral supplementation due to its cytotoxic properties and documented association with hepatotoxicity in humans consuming Chelidonium majus products. Multiple case reports link oral celandine preparations to acute liver injury, and the European Medicines Agency has issued warnings regarding these products. No established safe oral dose for humans exists in the peer-reviewed literature.
Can chelerythrine kill cancer cells?
In vitro studies show chelerythrine induces apoptosis in cancer cell lines including HeLa, MCF-7, and HL-60 cells, primarily through PKC inhibition and DNA intercalation, with IC50 values as low as 0.7 μM. Rodent xenograft models have also demonstrated tumor growth suppression. However, no human clinical trials have evaluated chelerythrine as a standalone anticancer agent, so calling it an anticancer treatment in humans is not supported by current evidence.
How does chelerythrine inhibit protein kinase C?
Chelerythrine binds competitively to the catalytic domain of protein kinase C (PKC), blocking ATP binding and preventing phosphorylation of downstream substrates involved in cell growth, differentiation, and apoptosis signaling. This inhibition is selective for PKC over several other kinases tested in vitro, with a Ki reported in the nanomolar range. Disruption of PKC-mediated signaling is thought to be the primary mechanism underlying its observed cytotoxic and anti-inflammatory effects.
What is chelerythrine used for in traditional medicine?
Traditional European herbal medicine has used Chelidonium majus latex, which is rich in chelerythrine, topically for the treatment of warts, corns, and cutaneous papillomas for centuries. In Ayurvedic and Chinese traditional medicine, related benzophenanthridine alkaloids from Sanguinaria canadensis and Macleaya cordata were applied topically as antimicrobials and for oral hygiene. None of these traditional applications have been validated by modern randomized controlled trials, and topical use should also be approached cautiously given the compound's cytotoxic potential.
What does the current clinical evidence show about chelerythrine's effectiveness in humans?
Most evidence for chelerythrine comes from in vitro (laboratory cell culture) and animal model studies, with no published human clinical trials to date. While preliminary research demonstrates anticancer potential through protein kinase C inhibition and DNA intercalation at IC50 values around 0.7 μM, these results cannot be directly translated to human efficacy or safety. Any health claims about chelerythrine in humans remain scientifically unproven and should be considered highly speculative until rigorous clinical trials are completed.
Who should avoid chelerythrine supplementation due to safety concerns?
Chelerythrine should be avoided by pregnant and nursing women, as no safety data exists in these populations and alkaloid compounds carry potential reproductive risks. Individuals with liver disease, kidney dysfunction, or those taking immunosuppressive medications should consult a healthcare provider, as chelerythrine's metabolism and potential for toxicity in compromised systems is unknown. Children and the elderly should also avoid supplementation until human safety studies establish appropriate age-specific dosing and risk profiles.
How does chelerythrine's bioavailability differ between Chelidonium majus plant extracts and isolated alkaloid supplements?
Isolated chelerythrine alkaloid may have different absorption and metabolic pathways than the compound as it exists within whole Chelidonium majus extracts, which contain multiple synergistic alkaloids and plant compounds. Whole plant extracts may provide better bioavailability through cofactors and enhanced intestinal absorption, though no direct comparative studies in humans exist. The optimal form for supplement use remains undetermined, and isolated chelerythrine may be poorly absorbed orally compared to traditional topical or extract-based preparations.
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