Hesperidin
description1
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Specification
| Test Items | Standard |
| Hesperidin (CAS: 520-26-3) | 90%-98% by HPLC |
| Loss on drying | ≤5.0% |
| Residue on ignition | ≤0.5% |

Multi-target activity
Combines antioxidant, anti-inflammatory, and vascular protective effects.

Natural safety profile
Widely present in citrus fruits with excellent human tolerance.

Formulation versatility
Adaptable to oral, injectable, and topical preparations.
1. 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)
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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