Diosmetin (Flavone · Venous Tone · Anti-inflammatory)

Compound	Diosmetin
Chemical class	Polyphenol — Flavone (Diosmin aglycone)
CAS	520-34-3
Primary source	Citrus aurantium, Vicia faba (pollen)
Key applications	Venous tone, anti-inflammatory, antioxidant
Claim strength	Moderate
Typical form	Diosmin aglycone; co-supplied with diosmin

Name origin: Diosmetin is the aglycone of diosmin — formed by enzymatic or acid hydrolysis of the diosmin glycoside. The "dios-" prefix relates to Diosma (buchu plant), where the parent compound was identified. Traditional use: Citrus peel preparations with venotonic properties have been used in European phytomedicine; diosmetin contributes alongside diosmin and hesperidin to the phlebotonic activity of flavonoid-rich citrus fractions. Research trajectory: Diosmetin has attracted recent research interest as a free aglycone with potentially superior cellular uptake over the glycoside diosmin. Anti-inflammatory, estrogenic, and antifibrotic activities are under investigation. Commercial source: Available as a minor co-component of diosmin preparations; Herbuno supplies high-purity diosmin (10% and 95% grades) from citrus sources.

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Evidence for Diosmetin Applications

Venous tone and chronic venous insufficiency: Diosmetin shares the venotonic mechanism of diosmin, reducing venous distensibility and capillary permeability. Most evidence is from MPFF (micronised purified flavonoid fraction) containing diosmin/diosmetin mixtures, which has multiple RCT support for chronic venous insufficiency and haemorrhoid symptom relief. Claim strength: Moderate (for diosmin/diosmetin mixtures; isolated diosmetin data limited).

Anti-inflammatory signalling: Diosmetin inhibits COX-2, NF-κB, and MAPK pathways in macrophage and epithelial cell models at 10–50 µM. More potent than diosmin in cell-based assays due to absence of the sugar moiety. Animal models support anti-inflammatory activity in colitis and lung injury models. Claim strength: Moderate.

Estrogen receptor modulation: Diosmetin demonstrates weak ERα/ERβ agonist activity, relevant to bone density and menopausal symptom research. Animal models show bone-protective effects. Human data are not available for diosmetin specifically. Claim strength: Emerging.

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Dosage & Formulator Specification

Diosmetin is not commercially formulated as a standalone ingredient. It is typically co-present in diosmin preparations (diosmetin constitutes 5–10% of commercial MPFF). For venous health applications, the standard clinical dose is 500 mg diosmin (as MPFF) twice daily, equivalent to approximately 450 mg diosmin + 50 mg diosmetin.

For formulations seeking the aglycone advantage, micronised diosmetin (particle size <2 µm) may offer improved GI absorption. Bioavailability enhancement via phospholipid complexation or nanoencapsulation is an area of current formulation research.

Stability: diosmetin is relatively stable at neutral to mildly acidic pH. Avoid alkaline processing conditions. Aqueous solubility is low (~0.1 mg/mL at pH 7); hydrophilic coatings or cyclodextrin complexation improves dissolution in functional food matrices.

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Frequently Asked Questions — Diosmetin

What is the difference between diosmin and diosmetin?
Diosmin is the glycoside (rutinose attached at C-7). Diosmetin is the aglycone formed by hydrolysis of that sugar. The aglycone has potentially superior direct cellular uptake but lower water solubility. Both are bioactive; in vivo, diosmin is partially converted to diosmetin by gut microbiota.

Can diosmetin be specified as the active in a venous health supplement?
Most regulatory and marketing precedent is built around diosmin or MPFF (diosmin + hesperidin fraction). Positioning diosmetin as the primary active is scientifically defensible but will require additional substantiation in markets that demand ingredient-level evidence.

Is diosmetin estrogenic — is there a safety concern for hormone-sensitive populations?
In vitro estrogenic activity is documented at concentrations well above typical dietary or supplement intakes. At doses present in standard diosmin formulations, estrogenic effects are not considered clinically significant based on current data. Formulator advisory language for hormone-sensitive individuals is a reasonable precaution.

Does Herbuno supply isolated diosmetin?
Herbuno supplies high-purity diosmin (10% and 95% grades) which will contain minor diosmetin fractions. For isolated diosmetin, contact Herbuno for custom availability and specification.

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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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