Lupeol (Lupane Triterpene · Anti-inflammatory · Antiproliferative · Hepatoprotective · Birch)

Compound	Lupeol
Chemical class	Terpenoid — Triterpene (Lupane-type pentacyclic triterpene; β-amyrin analogue)
CAS	545-47-1
Primary source	Betula spp. (birch bark), Mangifera indica (mango fruit skin), Ficus spp., Aloe barbadensis
Key applications	Anti-inflammatory; antiproliferative; hepatoprotective; wound healing; anti-arthritic; product-live via Birch extract
Claim strength	Moderate
Typical form	Birch bark extract; mango skin extract; isolated lupeol (≥98%)
Buy from Herbuno	Birch Bark Liquid Extract (Water Soluble) - Betula alba → Birch Leaf Liquid Extract (Water Soluble) - Betula alba →

Name origin: From Lupinus (the lupin genus, from which lupeol was first characterised) — the lupane carbon skeleton takes its name from the same source. Lupeol is a lupane-type pentacyclic triterpene with a characteristic isopropenyl side chain at C-20 — the same carbon framework as betulin and betulinic acid (the more widely studied birch triterpenes) but with a different degree of oxidation at C-28 (lupeol has C-28 as the isopropenyl terminal CH2; betulin has C-28 as hydroxymethyl; betulinic acid has C-28 as carboxylic acid). Distribution: Lupeol is one of the most widely distributed triterpenes in the plant kingdom — found in the outer bark of birch (Betula) trees, mango fruit skin (Mangifera indica), aloe vera, fig (Ficus), olive (Olea europaea), and many traditional medicinal plants globally. This widespread distribution reflects its role as an upstream biosynthetic intermediate in the lupeol → betulin → betulinic acid biosynthetic pathway. Traditional use: Birch bark preparations have been used in European and North American traditional medicine for anti-inflammatory, diuretic, and skin conditions — applications consistent with lupeol’s documented anti-inflammatory pharmacology. Mango bark preparations in African traditional medicine use lupeol-containing extracts for antimicrobial and anti-inflammatory indications. Commercial source: Birch Bark and Birch Leaf liquid extracts, both delivering lupeol as a constituent triterpene is available from Herbuno.

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Evidence for Lupeol Applications

Anti-inflammatory — NF-κB and 5-LOX: Lupeol inhibits NF-κB nuclear translocation, COX-2, and 5-LOX in macrophage and chondrocyte models. In vivo anti-inflammatory activity in carrageenan-induced oedema and adjuvant-induced arthritis is well-documented. The dual COX + 5-LOX inhibition profile mirrors boswellic acid (5-LOX) + NSAID (COX) combination therapy in a single compound. Claim strength: Moderate (animal models; consistent mechanism).

Antiproliferative and pro-apoptotic: Lupeol induces apoptosis across multiple cancer cell lines (prostate, breast, colon, liver, bladder) via mitochondrial pathway activation and Sp1 transcription factor inhibition. An important selectivity claim: lupeol causes apoptosis in cancer cells while sparing normal cells in comparative studies. No clinical oncology trials have been conducted. Claim strength: Moderate (convergent preclinical).

Hepatoprotective: Lupeol reduces CCl4-induced hepatotoxicity and reduces hepatic inflammation and fibrosis markers in animal models. Traditional use of lupeol-containing plants for liver conditions aligns with this pharmacology. The hepatoprotective mechanism involves Nrf2 activation and NF-κB inhibition in hepatocytes. Claim strength: Moderate (animal; traditional).

Wound healing and skin applications: Lupeol promotes keratinocyte migration and proliferation, collagen synthesis, and reduces inflammatory mediator production in wound models. Topical lupeol or lupeol-containing birch extract shows accelerated wound closure in animal models. This makes lupeol a compound of interest for cosmeceutical wound healing and anti-inflammatory skin formulations. Claim strength: Moderate (topical animal; consistent with traditional birch bark wound use).

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Frequently Asked Questions — Lupeol

How does lupeol differ from betulinic acid?
Lupeol, betulin, and betulinic acid are all lupane triterpenes from the same biosynthetic pathway. Lupeol → betulin (C-28 oxidation to hydroxymethyl) → betulinic acid (C-28 oxidation to carboxylic acid). Betulinic acid has attracted specific anticancer research for its selective induction of apoptosis in melanoma, neuroblastoma, and glioma cells via the mitochondrial intrinsic apoptosis pathway — with selectivity for cancer cells. Lupeol has broader anti-inflammatory profile with complementary but less specific anticancer activity. Betulin is the most abundant birch bark triterpene and serves as a bulk raw material for betulinic acid semi-synthesis.

Is lupeol present in aloe vera?
Yes — lupeol is one of the triterpene constituents of the aloe vera gel alongside β-sitosterol, campesterol, and cycloartenol. The traditional wound-healing and anti-inflammatory properties of aloe vera are partially attributable to its triterpene fraction including lupeol. The primary bioactive contributors to aloe’s gel properties are acemannan (the polysaccharide fraction) and aloin (anthranoid, purgative — in the latex), but the triterpene fraction including lupeol contributes to topical anti-inflammatory and wound-healing properties.

Can lupeol be used in topical formulations?
Yes — lupeol is lipophilic (logP ~8) and penetrates skin well. Anti-inflammatory, wound-healing, and potential antiproliferative activities make it relevant for cosmeceutical formulations targeting: acne (antimicrobial + anti-inflammatory); anti-ageing (collagen synthesis promotion); wound healing (keratinocyte stimulation); and anti-inflammatory skin conditions. Typical inclusion at 0.1–0.5% lupeol equivalent in emulsion bases. Birch bark extract provides a natural lupeol-delivering ingredient for cosmetic formulations.

Is lupeol anti-arthritic at doses achievable from birch extract?
Animal arthritis studies use lupeol at 25–100 mg/kg doses. Human equivalent dose scaling (body surface area) suggests 150–600 mg/day lupeol for equivalent effects — achievable if birch bark extract is standardised and dosed at concentrations reflecting a meaningful lupeol fraction. Standard birch bark extracts are not typically standardised to lupeol content — request HPLC CoA quantification of lupeol alongside betulin/betulinic acid for anti-arthritic formulation contexts.

Related compounds: Boswellic Acid, Ursolic Acid, Betulin, Beta-Sitosterol

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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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