Arctigenin (Dibenzylbutyrolactone Lignan · Antiviral · Anti-inflammatory)

Compound	Arctigenin
Chemical class	Polyphenol — Dibenzylbutyrolactone Lignan
CAS	7770-78-7
Primary source	Arctium lappa (burdock root), Arctium minus, Trachelospermum jasminoides
Key applications	Anti-inflammatory, antiviral, antiproliferative, immunomodulatory
Claim strength	Moderate
Typical form	Burdock root extract; arctigenin isolate
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Name origin: From Arctium (burdock genus) — arctigenin is the aglycone of arctiin (the glucoside native form). It is a dibenzylbutyrolactone-type lignan — characterised by two benzyl groups flanking a butyrolactone ring, without the furofuran or cyclooctadiene ring systems of sesamin or schisandrin. Traditional use: Burdock root (Gobo in Japanese cuisine; Niu Bang in TCM) has been used as a food vegetable and medicinal herb across Japan, China, and Europe for centuries. TCM applications include fever, urinary tract health, and skin conditions (particularly for inflammatory skin disorders like eczema and psoriasis). European herbalism uses burdock as a “blood purifier” and lymphatic herb. Arctigenin is identified as a key immunomodulatory active. Research trajectory: Arctigenin has attracted research for antiviral activity (influenza, COVID-19 in silico studies), anti-inflammatory NF-κB inhibition, mTOR inhibition (anticancer research context), and immunomodulatory properties. Japanese research groups have been particularly active. Commercial source: Commercially available via burdock root extract. See sourcing options below.

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Evidence for Arctigenin Applications

Antiviral activity: Arctigenin inhibits influenza virus replication (H1N1, H3N2) in cell models by interfering with viral RNA polymerase and nucleoprotein functions. In vivo mouse influenza models show significantly improved survival with arctigenin treatment. Computational studies suggest potential activity against SARS-CoV-2 protease, though in vitro confirmation is limited. Claim strength: Moderate (preclinical antiviral; no human trials).

Anti-inflammatory via NF-κB and MAPK: Arctigenin inhibits NF-κB, JNK, and p38 MAPK inflammatory pathways in macrophage models, reducing TNF-α, IL-6, and COX-2. Uniquely, arctigenin has documented activation of PI3K/Akt pathway in ways that modulate macrophage polarisation toward anti-inflammatory M2 phenotype. Claim strength: Moderate.

mTOR inhibition and antiproliferative: Arctigenin inhibits mTOR (mechanistic target of rapamycin) signalling — a central growth and survival kinase — in cancer cell models, inducing autophagy and cell cycle arrest. This mechanism has pharmaceutical research interest for oncology. Claim strength: Moderate (preclinical; no human antiproliferative clinical data).

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Dosage & Formulator Specification

No established isolated human supplement dose for arctigenin. TCM burdock root dose: 6–12 g dried root/day as decoction. For standardised burdock root extract: 200–500 mg/day, with arctigenin content varying widely by extract standardisation — request HPLC quantification of arctigenin alongside arctiin (the glucoside) for complete characterisation.

Arctigenin is derived from gut microbial hydrolysis of arctiin (the native glucoside), paralleling the SDG–enterolignans conversion pathway. Burdock root preparations rich in arctiin are therefore the practical delivery vehicle for arctigenin in vivo. Isolated arctigenin is available from specialist suppliers for research-grade formulation work.

Arctigenin has moderate lipophilicity and moderate aqueous solubility. Standard capsule and tablet formats are appropriate. Stability in standard extract formats is good. No significant drug interaction data have been published for arctigenin at supplement doses.

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Frequently Asked Questions — Arctigenin

What is the relationship between arctiin and arctigenin?
Arctiin is the 4-O-β-D-glucoside of arctigenin — the native glycoside form in burdock root tissue. In the gut, lactobacillus and Clostridium species hydrolyse arctiin to release arctigenin aglycone and glucose. Arctigenin is the more membrane-permeable, pharmacologically active form. Burdock root extract “standardised to arctiin” therefore serves as a precursor for arctigenin generation in vivo.

Is burdock root appropriate for immune support formulations?
Yes. Arctigenin’s immunomodulatory properties (NF-κB inhibition, M2 macrophage polarisation) combined with burdock’s traditional immune and lymphatic use support positioning in immune support formulations. Unlike Echinacea (immunostimulatory), burdock/arctigenin is better characterised as immunomodulatory — balancing rather than stimulating immune response. This positioning may be appropriate for chronic inflammatory immune conditions where stimulation is not desired.

Can arctigenin be positioned for respiratory health and antiviral formulations?
The preclinical antiviral evidence (influenza models) provides a rationale for respiratory health positioning. Combined with burdock’s traditional use for respiratory and lymphatic applications, a respiratory immune support positioning is scientifically coherent. Position as “studied to support healthy respiratory immune response” consistent with the evidence base rather than making specific antiviral therapeutic claims.

Is there any concern about burdock root adulteration?
Yes — burdock root has been adulterated with belladonna (Atropa belladonna) root in historical records, leading to anticholinergic poisoning incidents in herbal tea preparations. Botanical identity verification (macroscopic and microscopic examination, or DNA barcoding) is strongly recommended for all burdock root raw materials before use in supplement manufacturing.

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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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