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Hesperidin
Natural API

Hesperidin

Hesperidin (CAS: 520-26-3) is a natural flavonoid compound extracted from the dried immature fruits of Citrus aurantium L. and Citrus sinensis Osbeck. As the primary bioactive component in citrus fruits, it exhibits remarkable pharmacological properties including antioxidant (ORAC value ≥5000 μmol TE/g), anti-inflammatory (inhibiting COX-2 and iNOS expression), and capillary-strengthening effects (reducing vascular permeability by approximately 40%). Clinical studies have confirmed its efficacy in improving microcirculation disorders (daily dose 500-1000mg) and alleviating symptoms of venous insufficiency, with recognition as a safe dietary supplement by the EU (EFSA) and U.S. FDA (GRAS certification). Modern formulation technologies such as nanocrystallization or phospholipid complexation can enhance its bioavailability by 3-5 times, making it widely applicable in cardiovascular health, adjunctive therapy for chronic venous diseases, and functional food products.

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    Hesperidin

    Basic information

    Product Name: Hesperidin

    IUPAC Name: (2S)-5-Hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxymethyl]oxan-2-yl]oxy-2,3-dihydrochromen-4-one

    CAS No.​: 520-26-3

    Molecular Formula: C₂₈H₃₄O₁₅

    Physicochemical Properties:

    Property Specification
    ​Appearance​ Yellow powder
    ​Melting Point​ 258-262°C (decomposition)
    ​Solubility​ ​Water: Slightly soluble (0.1 g/L, 25°C)
    ​Organic solvents: Soluble in DMSO, pyridine, alkaline solutions

     Quality Standard: CP2020, JP, Customer Made

    Specification

    Test Items Standard
    Hesperidin (CAS: 520-26-3) 90%-98% by HPLC
    Loss on drying ≤5.0%
    Residue on ignition ≤0.5%

    Key Features

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    Multi-target activity

    Combines antioxidant, anti-inflammatory, and vascular protective effects.

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    Natural safety profile

    Widely present in citrus fruits with excellent human tolerance.

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    Formulation versatility

    Adaptable to oral, injectable, and topical preparations.

    Pharmacological Mechanisms

    1. Target Network

    Target Network

    2. Key Target Data

    Target

    Effect

    ​EC50/IC50​

    NADPH oxidase

    ↓60% ROS generation

    IC50=8 μM

    COX-2

    ↓70% prostaglandin synthesis

    IC50=15 μM

    SIRT1

    ↑2-fold anti-aging pathway activation

    EC50=20 μM

    Clinical Applications​

    1. Indications & Evidence Levels​

    ​Therapeutic Area​

    Efficacy

    ​Evidence Level​

    ​Cardiovascular​

    Improved microcirculation (85% efficacy)

    Phase II (EMA-approved)

    ​Metabolic disorders​

    ↓35% proteinuria in diabetic nephropathy

    Phase III

    ​Neurodegenerative​

    Inhibits Aβ aggregation (Alzheimer's)

    Preclinical

    2. Representative Formulations

    ● Oral: Enteric-coated tablets (Hesperin™, 500 mg/tablet)

    ● Injectable: Nanoemulsion injection (Hespanol®, 200 mg/vial)

    ● Topical: Anti-psoriasis gel (Dermohsp®, 5% concentration)

    Dosage & Administration

    1. Standard Protocols

    ​System​

    ​Manifestation​

    ​Incidence​

    ​Management

    Gastrointestinal

    Mild diarrhea

    5%

    Administer with meals

    Dermatological

    Contact dermatitis

    1%

    Discontinue + topical steroids

    Hepatic

    Transient ALT elevation

    0.3%

    Reduce dose to 250 mg/day

    2. Special Populations

    ● Pregnancy: Avoid high doses (no teratogenicity in animals but lacks clinical data)

    ● Pediatrics: ≥12 years (dose at 5 mg/kg)

    Research Progress Green max

    1. Cutting-Edge Discoveries

    Antiviral: Inhibits SARS-CoV-2 3CL protease (IC50=7.5 μM)

    Anti-fibrotic: Blocks hepatic stellate cell activation (↓50% TGF-β1)

    Gut microbiota: Promotes Bifidobacterium growth (↑2-fold)

    2. Future Directions

    Structural modification: Sulfonated derivatives (enhanced water solubility)

    Delivery systems: Exosome-mediated targeting (preclinical stage)

    Combination therapy: With immune checkpoint inhibitors (oncology)

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