Named Bioactive Compounds · Compound
Methoxyluteolin
Moderate Evidenceflavone
Hermetica Superfood Encyclopedia
Methoxyluteolin is a methylated flavone compound that demonstrates anti-inflammatory activity by inhibiting mast cell degranulation and mediator release. This bioactive flavonoid reduces pro-inflammatory cytokines including TNF-α, VEGF, and IL-8 while providing antioxidant protection through free radical scavenging.
Methoxyluteolin is a naturally occurring O-methylated flavone compound, with 6-methoxyluteolin (also called nepetin or eupafolin) being the most well-characterized variant. It is found in several plant species including Artemisia vulgaris (mugwort) and Eupatorium ballotaefolium, appearing as a yellow powder with molecular formula C₁₆H₁₂O₇.
The research dossier does not contain specific human clinical trials, randomized controlled trials (RCTs), or meta-analyses with PubMed PMIDs for methoxyluteolin. Current evidence appears limited to in vitro and mechanistic studies examining anti-inflammatory and antioxidant properties.
No clinically studied dosage ranges for methoxyluteolin in human subjects were found in the research dossier. Standardized extract concentrations and dosing protocols have not been established in clinical research. Consult a healthcare provider before starting any new supplement.
Methoxyluteolin (5,7,3'-trihydroxy-4'-methoxyflavone; also known as chrysoeriol) is a methylated flavone, not a macronutrient source. It is a bioactive polyphenolic compound with a molecular weight of approximately 300.26 g/mol and the molecular formula C16H12O6. Key characteristics: • It is a mono-O-methylated derivative of luteolin, where a methoxy group (-OCH3) replaces the 4'-hydroxyl group on the B-ring, which significantly enhances its lipophilicity and membrane permeability compared to luteolin. • Bioavailability: Methoxyluteolin demonstrates superior oral bioavailability relative to its parent compound luteolin due to increased metabolic stability conferred by the methyl ether group, which partially protects against rapid Phase II conjugation (glucuronidation and sulfation) in the gut and liver. Estimated oral bioavailability is modestly improved but still relatively low in absolute terms (typical of flavonoids), likely in the range of low single-digit percentages without formulation enhancement. • Natural dietary sources include certain herbs and plants, though concentrations are generally low (typically <0.1–0.5% dry weight in source plant material). It has been identified in Thai black ginger (Kaempferia parviflora), olive leaves, and certain Artemisia species. • It contains no appreciable macronutrients (protein, fat, carbohydrates, fiber) as it is consumed as an isolated bioactive compound or minor phytochemical constituent, not as a food. • No vitamins or minerals are intrinsic to the compound itself. • Key bioactive functional groups: Three free hydroxyl groups (positions 5, 7, and 3') responsible for antioxidant radical scavenging and metal chelation activity; the C2-C3 double bond conjugated with the 4-oxo group in the C-ring contributes to electron delocalization and potency; the 4'-methoxy group enhances blood-brain barrier penetration and metabolic resistance. • Lipophilicity (estimated LogP ~2.4–2.7) is higher than luteolin (~1.9–2.1), aiding cellular uptake and tissue distribution, particularly into lipid-rich compartments including neural tissue. • Formulation with lipid-based nanoparticles or liposomes may further enhance bioavailability and targeted delivery.
Methoxyluteolin inhibits mast cell degranulation by blocking calcium influx and preventing the release of inflammatory mediators like histamine and tryptase. The compound suppresses nuclear factor-kappa B (NF-κB) signaling pathway, leading to reduced production of pro-inflammatory cytokines TNF-α, VEGF, and IL-8/CXCL8. Its antioxidant activity involves direct free radical scavenging and upregulation of cellular antioxidant enzyme systems.
Current evidence for methoxyluteolin is primarily derived from in vitro mechanistic studies examining mast cell function and cytokine production. Laboratory studies demonstrate significant inhibition of mast cell mediator release at concentrations of 10-100 μM. No human clinical trials have been published to date evaluating methoxyluteolin's therapeutic efficacy or safety profile. The preliminary nature of existing research limits conclusions about real-world clinical applications.
Safety data for methoxyluteolin supplementation in humans is currently unavailable due to lack of clinical studies. As a flavone compound, it may theoretically interact with cytochrome P450 enzymes, potentially affecting drug metabolism. Individuals taking anticoagulant medications should exercise caution as flavonoids can influence bleeding risk. Pregnant and breastfeeding women should avoid methoxyluteolin supplements due to insufficient safety data.
