Methyl-hesperidin
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Basic information
Product Name: Methyl-hesperidin
IUPAC Name: (2S)-5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy-4H-chromen-4-one
CAS No.: 11013-97-1
Molecular Formula: C₂₉H₃₆O₁₅
Physicochemical Properties:
Arameter |
Value/Description |
Appearance |
Yellow powder |
Melting Point |
190-195°C (decomposition) |
Solubility |
Slightly soluble in water (0.5 mg/mL), soluble in DMSO and methanol |
Predicted logP |
1.5 (moderate lipophilicity) |
Stability |
Light-sensitive; most stable at pH 6-8 |
Quality Standard: CP2020,JP,Customer Made
Specification
Test Items |
Standard |
Methylhesperidin (CAS: 11013-97-1) |
94% by UV |
Loss on drying |
≤5.0% |
Residue on ignition |
≤0.5% |
Improved Lipophilicity
Stronger Antioxidant Capacity
Microcirculation Modulato
1.Multi-Target Actions
Venous Tone Regulation
Activates α₁-adrenergic receptors → promotes venous contraction.
Inhibits PDE4 → increases cAMP levels → improves vascular elasticity.
Anti-Inflammatory Pathway
Downregulates NF-κB → reduces ICAM-1/VCAM-1 expression.
Antioxidant Effects
Activates the Nrf2/ARE pathway → enhances cellular antioxidant defenses.
2. Pharmacodynamic Profile
Onset of Action
3-4 hours after oral administration.
Half-Life
5-7 hours (requires twice-daily dosing for steady-state concentration).
Clinical Applications
Indication |
Recommended Dose |
Treatment Duration |
Efficacy Data |
Chronic Venous Insufficiency |
500-1000 mg/day |
≥3 months |
Leg circumference reduced by 2.5 cm* |
Acute Hemorrhoids |
1000 mg/day ×7 days |
Short-term |
Pain relief rate: 65% |
Diabetic Retinopathy |
500 mg/day |
Long-term |
Leakage reduced by 40% |
*Meta-analysis (8 RCTs)
Dosage and Administration
1.Oral: 500-1000 mg/dose, twice daily (take with meals).
2.Injectable (hospital use only): 200 mg/dose, IV infusion.
3.Special Populations:
Renal impairment (GFR <30): Reduce dose by 50%.
Hepatic impairment: Use with caution (limited data).
Safety Evaluation
Adverse Reactions
Type |
Incidence |
Management |
Gastrointestinal discomfort |
5-10% |
Take with food |
Headache/Dizziness |
2-3% |
Reduce dose |
Allergic reactions |
<1% |
Discontinue immediately |
Contraindications
Pregnancy (embryotoxicity observed in animal studies).
Severe bleeding disorders (e.g., hemophilia).
Research Progress Green max
Post-COVID Microcirculation Disorders:
Phase II trials show improvement in limb edema (NCT051XXXX).
Nanoformulation Development:
Liposomal encapsulation increases bioavailability to 85%.
Neuroprotective Effects:
Animal studies demonstrate reduced ischemia-reperfusion brain injury.
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