Wedelolactone (Coumestan · Hepatoprotective · NF-κB Inhibitor · Bhringraj)

Compound	Wedelolactone (1,8,9-Trihydroxy-3-methoxy-6H-[1]benzofuro[3,2-c]chromen-6-one; 3-Methoxycoumestrol)
Chemical class	Polyphenol — Coumestan (3-methoxycoumestrol; benzofuranone-fused chromene; primary Eclipta coumestan)
CAS	524-12-9
Primary source	Eclipta prostrata / Eclipta alba (Bhringraj), Wedelia calendulacea, Wedelia trilobata
Key applications	Hepatoprotective; NF-κB / IKK inhibition; 5-LOX inhibition; hair growth support; anti-inflammatory
Claim strength	Moderate
Typical form	Eclipta prostrata Extract Powder (Bhringraj); Bhringraj Liquid Extract; Organic Bhringraj Herb Powder
Buy from Herbuno	Eclipta prostrata (Bhringraj) Extract Powder | Kesharaj → Bhringraj Liquid Extract (Water Soluble) - Eclipta Alba →

Name origin: Wedelolactone is named after Wedelia — a genus of tropical Asteraceae plants (now reclassified, some species to Sphagneticola and others) from which it was first isolated. It is the 3-methoxy derivative of coumestrol — carrying a methoxy group at C-3 of the coumestrol scaffold — and is the characteristic coumestan of Eclipta alba/prostrata (Bhringraj), one of Ayurveda's most revered herbs. Traditional use: Eclipta alba (Bhringraj, Kesharaj — "king of hair" in Sanskrit) is a cornerstone of Ayurvedic hepatology and trichology. Classical Ayurvedic texts describe Bhringraj for liver conditions (Yakrit roga), jaundice, skin diseases, and notably as the primary herb for promoting hair growth and preventing hair loss — a traditional application validated by modern research. Bhringraj oil (Bhringaraj taila) is a classical preparation combining Eclipta leaf extract in sesame oil for scalp application, used continuously in South Asian hair care traditions for millennia. In TCM, Han Lian Cao (Eclipta prostrata) is prescribed for yin-deficiency conditions, hair loss, and liver protection. Research trajectory: Wedelolactone's pharmacological significance lies in its selective IKKβ (IκB kinase β) inhibition — a primary upstream regulator of NF-κB activation. This IKK inhibitory mechanism is shared with a small number of natural compounds and positions wedelolactone as a pharmacologically interesting NF-κB pathway modulator distinct from conventional IκB stabilisers. Hepatoprotective and hair growth activities are the most clinically relevant research domains. Commercial source: Wedelolactone is available from Herbuno via Eclipta prostrata Extract Powder (Bhringraj), Bhringraj Liquid Extract, and Organic Bhringraj Herb Powder — three complementary Eclipta preparations covering both extract-standardised and whole-herb applications.

---

Evidence for Wedelolactone Applications

Hepatoprotective activity: Wedelolactone demonstrates significant hepatoprotective activity in CCl₄, galactosamine, and alcohol-induced liver injury models — reducing ALT, AST, and histological damage at 10–50 mg/kg. In comparative studies, wedelolactone's hepatoprotection approaches silymarin at equivalent doses via mechanistically distinct pathways (IKK/NF-κB suppression vs. silymarin's Nrf2/membrane stabilisation). Eclipta alba preparations have clinical evidence for hepatitis supportive care in small Indian clinical studies. Claim strength: Moderate.

NF-κB / IKK inhibition: Wedelolactone directly inhibits IKKβ — the kinase responsible for phosphorylating IκBα, releasing NF-κB for nuclear translocation. IC₅₀ for IKKβ inhibition is approximately 25 μM — selective over other kinases in profiling studies. This IKK inhibitory mechanism suppresses downstream NF-κB target genes (COX-2, iNOS, TNF-α, IL-1β, IL-6) more broadly and potently than COX-2-selective inhibitors alone, explaining wedelolactone's multi-target anti-inflammatory profile. Claim strength: Moderate.

Hair growth support: Eclipta alba preparations applied topically to the scalp demonstrate hair growth promotion in rodent models — increasing follicle density, accelerating anagen phase initiation, and stimulating 5α-reductase inhibition (reducing DHT-mediated follicle miniaturisation). A small controlled study in alopecia areata patients using topical Bhringraj oil showed improvement comparable to minoxidil 2% in follicle count restoration. Wedelolactone's contribution to these effects is presumed but not isolated from other Eclipta constituents (coumestrol, ecliptine, phytosterols). Claim strength: Moderate (extract); Emerging (isolated wedelolactone).

5-LOX inhibition and antiallergic: Wedelolactone inhibits 5-lipoxygenase, reducing leukotriene B₄ and C₄ production in inflammatory models. This anti-leukotriene activity is relevant to allergic conditions (asthma, urticaria) where 5-LOX products are primary mediators. Claim strength: Moderate.

---

Dosage & Formulator Specification

No isolated wedelolactone human dosing data exist. Eclipta alba preparations used in hepatitis supportive studies: 1–3 g/day dried herb equivalent or 300–600 mg concentrated extract. Wedelolactone content in Eclipta extract is typically 0.1–1% dry weight depending on plant part and extraction method — delivering 0.3–6 mg wedelolactone per serving of 300–600 mg extract. For hair growth topical applications, Bhringraj preparations are formulated at 1–5% concentration in oil or water-soluble extract form.

For formulator specification: Eclipta prostrata Extract Powder from Herbuno (Bhringraj) is the most concentrated wedelolactone delivery form among the available Herbuno Eclipta preparations. Bhringraj Liquid Extract provides water-soluble wedelolactone for aqueous formulations. Organic Bhringraj Herb Powder provides the whole-herb matrix with all Eclipta constituents — suitable for traditional Ayurvedic formulations where full botanical authenticity is required.

Wedelolactone's coumestan scaffold gives it moderate lipophilicity — compatible with both oil-based (Bhringaraj taila preparation) and water-soluble extract delivery. Stability in alkaline pH environments is reduced due to lactone ring susceptibility to hydrolysis; pH 4–6 is optimal for aqueous formulations. The coumestan's ER-binding activity is less than coumestrol (the 3-methoxy group reduces ERβ affinity) but should still be noted in hormone-sensitive formulation contexts.

No significant drug interactions are documented for wedelolactone at botanical extract supplement doses. The IKK inhibitory mechanism theoretically potentiates anti-inflammatory drug effects — relevant for professional advice in patients on systemic corticosteroids or NSAIDs.

---

Frequently Asked Questions — Wedelolactone

What makes wedelolactone's IKK inhibition pharmacologically significant?
NF-κB is activated by the IKK complex phosphorylating IκBα, releasing NF-κB for nuclear translocation. Most natural anti-inflammatory compounds target downstream components (COX-2, individual cytokines); few inhibit the upstream IKK complex directly. Wedelolactone's IKKβ inhibition blocks NF-κB activation at the regulatory switch — theoretically suppressing all NF-κB target genes simultaneously. This upstream inhibition provides broader anti-inflammatory coverage than COX-2-selective inhibitors and positions wedelolactone as pharmacologically analogous to pharmaceutical IKK inhibitors under development for inflammatory and oncological applications.

Is Bhringraj (Eclipta alba) safe for long-term use?
Bhringraj has an excellent long-term safety record as a traditional Ayurvedic herb used continuously for millennia. No significant adverse events have been documented in traditional use or modern clinical studies at conventional doses. As a coumestan-containing plant, appropriate phytoestrogen cautions apply at high doses. The 5α-reductase inhibitory activity noted for Eclipta extracts is mild and has not been associated with sexual adverse effects at typical supplement doses.

How does wedelolactone differ from coumestrol?
Wedelolactone is coumestrol's 3-methyl ether — the 3-hydroxyl of coumestrol is methylated in wedelolactone. This single modification significantly reduces ERβ binding affinity (coumestrol's most potent pharmacological property) while preserving or enhancing IKK/NF-κB inhibitory activity. Wedelolactone's pharmacological profile therefore differs from coumestrol — emphasising anti-inflammatory/IKK and hepatoprotective activity over phytoestrogenic activity.

What is the traditional Bhringaraj oil preparation and how is it used?
Bhringaraj taila (Bhringaraj oil) is a classical Ayurvedic preparation — Eclipta leaf juice or extract infused in sesame oil at ratios specified in classical texts (typically 1:4 herb juice:oil), sometimes combined with other herbs (Brahmi, Amla, coconut milk). The preparation is applied to the scalp and hair, left for 30–60 minutes or overnight, then washed off. Traditional use recommends weekly to twice-weekly application for hair growth, prevention of premature greying, and scalp cooling effects. Commercial Bhringaraj oil products standardise this preparation for consistent actives delivery.

Related compounds: Coumestrol, Puerarin, Silybin, Liquiritin

---

Claim-strength scale – High = multiple human RCTs; Moderate = limited trials or strong preclinical convergence; Emerging = early-stage lab or animal data.

← HerbIQ Compound Index · HerbIQ P02: Extraction · HerbIQ P03: Delivery