Betulinic Acid (Lupane Triterpene · Anticancer Research · Anti-HIV · Anti-inflammatory)
| Compound | Betulinic Acid |
| Chemical class | Terpenoid — Pentacyclic Triterpene Acid (Lupane skeleton) |
| CAS | 472-15-1 |
| Primary source | Betula alba (white birch bark), Betula pendula; Platanus spp.; Diospyros spp. |
| Key applications | Anticancer (melanoma preclinical), anti-HIV, anti-inflammatory, hepatoprotective |
| Claim strength | Moderate |
| Typical form | Birch bark extract (betulinic acid-standardised); betulinic acid isolate |
| Buy from Herbuno |
Birch Bark Liquid Extract (Water Soluble) - Betula alba → Birch Bark Extract Powder - Betula alba → |
Name origin: From Betula (birch genus), the primary commercial source. Betulinic acid is a naturally occurring lupane-skeleton triterpene abundant in the bark of white birch trees. It is formed in the plant from betulin (birch bark’s major triterpene) via oxidation. Traditional use: Birch bark preparations have been used in Northern European, Siberian, and Native American traditions for wound healing, skin conditions, fever management, urinary tract complaints, and as a general anti-inflammatory tonic. Birch bark was historically used in traditional Finnish, Russian, and Scandinavian medicine for its antimicrobial and anti-inflammatory properties. Research trajectory: Betulinic acid gained significant pharmaceutical research attention in the 1990s when identified as a selective inducer of apoptosis in melanoma cells (with minimal effect on normal cells) — an unusual selectivity that made it a lead anticancer compound. It also has documented anti-HIV activity (entry inhibition). Multiple pharmaceutical derivatives are under clinical investigation. Commercial source: Birch Bark Extract (water-soluble, dry powder) from Herbuno provides betulinic acid alongside betulin and other birch bark triterpenoids. See sourcing options below.
Evidence for Betulinic Acid Applications
Anticancer — melanoma selectivity (preclinical): Betulinic acid selectively induces apoptosis in neuroectodermal tumour cells (melanoma, medulloblastoma, neuroblastoma) via direct mitochondrial membrane disruption and cytochrome c release, with minimal toxicity to normal cells. This selectivity has made it a leading natural compound in anticancer drug development. Phase I clinical trials have been conducted, though no approval exists. Claim strength: Moderate (compelling preclinical, Phase I data; no approved therapeutic claim for supplements).
Anti-HIV (entry inhibition): Betulinic acid and its derivatives inhibit HIV-1 entry by interfering with gp41-mediated viral membrane fusion. Several synthetic betulinic acid derivatives are under pharmaceutical development as HIV entry inhibitors. At supplement doses, anti-HIV activity is not clinically established. Claim strength: Moderate (mechanism well-characterised; no supplement-level clinical data).
Anti-inflammatory: Inhibits NF-κB, reduces TNF-α and IL-6 in macrophage models. In vivo anti-inflammatory efficacy in arthritis and colitis animal models is documented. The lupane skeleton provides a distinct interaction profile compared to oleanane and ursane triterpenoids. Claim strength: Moderate.
Hepatoprotective and antioxidant: Activates Nrf2/HO-1 pathway, protects against oxidative liver injury, and reduces hepatic lipid peroxidation in animal models. Relevant for liver health and antioxidant supplement formulations. Claim strength: Moderate.
Birch Bark Liquid Extract (Water Soluble) - Betula alba →
Birch Bark Extract Powder - Betula alba →
Browse Standardised Extract Powders →
Dosage & Formulator Specification
No established human supplement dose for betulinic acid. Phase I oncology trials used 20–50 mg/m² IV — not applicable to oral supplementation. For oral supplement formulations targeting anti-inflammatory and hepatoprotective applications, birch bark extract standardised to betulin + betulinic acid content at 200–500 mg/day is a working extrapolation from animal data. Birch bark extract typically contains 5–15% betulin (the dominant triterpene) and 0.5–3% betulinic acid.
Betulinic acid has poor aqueous solubility (logP ~5.8) — similar to ursolic and oleanolic acid. Same bioavailability enhancement strategies apply: nanoparticle, phytosome, or lipid-based delivery recommended. IMPORTANT for anticancer contexts: supplement-level positioning of betulinic acid for cancer must avoid therapeutic claims. Position as "traditionally used for skin health" or "studied for cellular health support" — not as an anticancer compound in supplement marketing.
Frequently Asked Questions — Betulinic Acid
Is betulinic acid the same as betulin?
Betulin (betulinol) and betulinic acid are related lupane-skeleton triterpenoids from white birch bark. Betulin is the dominant birch bark triterpenoid (10–30% of dry bark weight) — a diol (two hydroxyl groups). Betulinic acid is formed from betulin by oxidation of one of the hydroxyl groups to a carboxylic acid. Betulinic acid has significantly greater pharmacological activity than betulin, particularly for apoptosis induction and anti-HIV activity. Birch bark extracts contain both; for maximum betulinic acid content, specify the oxidation ratio or pure betulinic acid isolate.
Why does betulinic acid selectively kill melanoma cells?
Betulinic acid induces apoptosis by directly disrupting the outer mitochondrial membrane, releasing cytochrome c and activating caspase cascades. The selectivity for melanoma and neuroectodermal tumour cells appears to involve upregulation of reactive oxygen species production specifically in these cell types, alongside tumour-selective ceramide pathway activation. Normal cells have higher antioxidant capacity that protects them from the same mitochondrial stress. This mechanism is independent of p53 status, making it relevant to tumours with p53 mutations.
Can betulinic acid from birch bark be positioned for skin health?
Yes — and this is the most defensible supplement positioning for betulinic acid. Birch bark preparations have traditional and some modern evidence for skin conditions (eczema, psoriasis, wound healing). Topical betulinic acid/birch bark preparations are used in several European dermatological contexts. For oral supplement skin health positioning, the anti-inflammatory and antioxidant mechanisms are the appropriate claim basis rather than the anticancer research.
Are betulinic acid pharmaceutical derivatives available?
Multiple synthetic derivatives of betulinic acid are under pharmaceutical development — bevirimat (DSB), PA-457 (HIV inhibitor), and various triterpenoid acids derived from the betulinic acid scaffold. These are pharmaceutical candidates in clinical trials and are not the same as dietary betulinic acid from birch bark extract. The pharmaceutical research context provides scientific credibility for the betulinic acid class but does not translate to supplement-level clinical claims.
Related compounds: Ursolic Acid, Oleanolic Acid, Glycyrrhizin, Astragalosides
Claim-strength scale – High = multiple human RCTs; Moderate = limited trials or strong preclinical convergence; Emerging = early-stage lab or animal data.
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