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Luteolin
Natural API
Luteolin.jpg
sophora flower bud.jpg

Luteolin

Luteolin (CAS: 491-70-3) is a naturally occurring flavonoid compound . Widely found in sophora flower bud, chrysanthemums, celery, olive leaves, and other plants, it serves as a crucial secondary metabolite for plant defense against UV radiation and pathogens. Its unique flavone backbone and polyhydroxy substitution pattern confer significant antioxidant, anti-inflammatory, and antitumor activities. It is listed as a food additive (E586) by the EU and included in pharmacopoeias of China, the US, and other countries.

Product Name: Luteolin 

IUPAC Name: 2-(3,4-Dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one

CAS No.​: 491-70-3

Molecular Formula: C₁₅H₁₀O₅

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    Luteolin

    Basic information

    Product Name: Luteolin 

    IUPAC Name: 2-(3,4-Dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one

    CAS No.​: 491-70-3

    Molecular Formula: C₁₅H₁₀O₅

    Physicochemical Properties:

    Parameter

    Value/Description

    ​Appearance​

    Yellow needle-like crystals

    ​Melting Point​

    328-330°C (decomposition)

    ​Solubility​

    Water solubility 0.01 mg/mL, soluble in DMSO/hot ethanol (50 mg/mL)

    ​logP​

    2.3 (moderate lipophilicity)

    ​pKa​

    6.7 (7-OH), 9.8 (4'-OH)

    Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Luteolin (CAS: 491-70-3)

    98% by HPLC

    Loss on drying

    ≤1.0%

    Ash

    ≤1.0%

    Key Features

    index_10-7

    Structural Advantage

    4-keto flavone skeleton + 3',4',5,7-tetrahydroxy substitution, synergistically enhancing activity.
    index_10-7

    Multi-Target Action

    Simultaneously modulates NF-κB, Nrf2, PI3K/Akt, and 10+ other signaling pathways.
    index_10-7

    High Safety

    ADI value 0-0.1 mg/kg bw/day (JECFA evaluation).

    Pharmacological Mechanisms

    1. Molecular Target Network

    Molecular Target Network2

    2. Pharmacokinetics

    Absorption

    Oral bioavailability 8% (phospholipid complex↑to 25%).

    Distribution

    Liver/lung ratio 4:1, minimal brain penetration (CSF/Plasma=0.01).

    Metabolism

    UGT1A1-mediated glucuronidation (t₁/₂=4h).

    Excretion

    Biliary excretion >80%, urinary <5%.

    Clinical Applications​

    1. Current Indications​

    ​Field​

    ​Regimen​

    ​Evidence Level​

    ​Chronic IBD​

    100 mg enteric capsule tid

    CRP↓45%*

    ​Mild Cognitive Impairment​

    50 mg bid (trial)

    MMSE↑2 points

    ​Photoprotection​

    1% sunscreen cream

    UV erythema↓60%

    *Multicenter RCT (n=800)

    2. Special Populations​

    Pediatrics: Topical use for >6 years (systemic safety unconfirmed).

    Hepatic Impairment: Reduce dose by 30% (Child-Pugh B).

    Dosage and Administration

    1. Formulations​

    Oral: 50 mg enteric-coated tablets (β-cyclodextrin inclusion).

    Injection: 5 mg/mL (dilute in NS, hospital use only).

    Topical: 0.5-2% creams/microemulsions.

    2. Dosing Guidelines​

    Use​

    ​Dose​

    ​Duration​

    Antioxidant

    50-100 mg/day

    Long-term

    Acute Inflammation

    200 mg tid

    1-2 weeks

    Cancer Adjuvant

    300 mg/day + chemo

    Clinical trials

    Safety Evaluation

    1.Adverse Reactions​

    ​System​

    ​Incidence​

    ​Management​

    Gastrointestinal

    6%

    Take with food

    Skin Allergy

    0.5%

    Discontinue + antihistamines

    Liver Enzyme Elevation

    <1%

    Dose reduction + monitoring

    2.Contraindications & Interactions​

    Absolute CI:
    Hypersensitivity to flavonoids.
    Pregnancy (potential uterotonic effect).

    Cautions: CYP3A4 inhibitors (e.g., ketoconazole): AUC may↑50%.

    Research Progress Green max

    Novel Formulations​

    Nanocrystal Self-Assembled Micelles: Oral bioavailability→35%.

    Mitochondria-Targeting Derivatives (e.g., C7-triphenylphosphonium salt): 10× enhanced antitumor potency.

    New Indications​

    Post-COVID Syndrome: Suppresses cytokine storm (Phase II trials).

    Parkinson’s Disease: Activates PINK1/Parkin pathway (↑dopaminergic neuron survival in animals).

    sophora flower bud

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