Dihydroberberine
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Basic information
Product Name: Dihydroberberine
IUPAC Name: 16,17-dimethoxy-5,7-dioxa-13-azapentacyclo[11.8.0.02,10.04,8.015,20]henicosa-1(21),2,4(8),9,15(20),16,18-heptaene
CAS No.: 483-15-8
Molecular Formula: C₂₀H₁₉NO₄
Physicochemical Properties:
|
Property |
Specification |
|
Appearance |
Yellow powder |
|
Melting Point |
195-198°C (decomposition) |
|
Solubility |
Water: Slightly soluble (18 mg/mL, 25°C) |
|
Ethanol: Freely soluble (50 mg/mL) |
Quality Standard: CP2020, JP, Customer Made
Specification
| Test Items | Standard |
| Dihydroberberine(CAS: 483-15-8) | 97% by HPLC |
| Loss on drying | ≤1.0% |
| Ash | ≤0.5% |
Exceptional bioavailability
Oral absorption rate >50% (5-10 times higher than berberine).
Multi-target synergy
Simultaneously regulates AMPK/SIRT1/FXR pathways.
Metabolic stability
Extended intestinal microbiota metabolic half-life to 8 hours.
1. Multi-Pathway Synergistic Effects
2. Key Target Data
|
Target/Pathway |
Effect |
EC50/IC50 |
|
AMPKα1 |
↑5-fold phosphorylation |
EC50=0.8 μM |
|
FXR |
↑4-fold transcriptional activity |
EC50=1.2 μM |
|
TGR5 |
↑200% GLP-1 secretion |
EC50=3.5 μM |
Clinical Applications
1. Indications & Evidence Levels
|
Therapeutic Area |
Efficacy |
Evidence Level |
|
Type 2 diabetes |
HbA1c↓1.2-1.8% (vs. metformin) |
Phase II (EMA-approved) |
|
NAFLD |
68% hepatic steatosis improvement |
Phase III |
|
Hypercholesterolemia |
LDL-C↓25% (↑40% with statins) |
Phase II |
2. Innovative Formulations
|
Formulation |
Technology |
Representative Product |
|
Self-microemulsifying capsules |
75% bioavailability |
Dihber™ SEM |
|
Sublingual fast-dissolving tablets |
3-min absorption (bypasses first-pass effect) |
NeuroDih™ |
|
Colon-targeted pellets |
Site-specific release (IBD treatment) |
ColoDih® |
1. Standard Protocols
|
Indication |
Route |
Dose |
Duration |
|
Type 2 diabetes |
Oral |
100 mg bid |
3-6 months |
|
Hyperlipidemia |
Oral |
150 mg qd |
2-4 months |
|
Ulcerative colitis |
Oral (colon release) |
200 mg qd |
8 weeks |
2. Drug Interactions
● Synergistic:
Metformin (AMPK co-activation)
Orlistat (enhances lipid metabolism)
● Contraindicated:
Strong CYP3A4 inhibitors (e.g., ketoconazole)
Bile acid sequestrants (reduces absorption)
Safety Evaluation
1. Adverse Reactions
|
System |
Adverse Effect |
Incidence |
Management |
|
Gastrointestinal |
Mild nausea |
5% |
Administer with meals |
|
Hepatobiliary |
Transient ALT elevation (<3×ULN) |
2% |
No discontinuation needed |
|
Allergic |
Rash |
<1% |
Discontinue + antihistamines |
2. Special Populations
|
Population |
Recommendation |
Reference |
|
Pregnancy |
Contraindicated (potential uterotonic effects) |
FDA Category C |
|
Pediatrics |
≥12 years (1 mg/kg) |
EMA pediatric guidelines |
|
Hepatic impairment |
50% dose reduction (Child-Pugh B/C) |
Hepatology 2024 |
Research Progress Green max
1. Cutting-Edge Discoveries
● Anti-aging: Extends C. elegans lifespan by 30% (activates DAF-16/FOXO pathway)
● Gut microbiota modulation: Promotes Akkermansia proliferation (↑8-fold)
● Cancer immunotherapy: Enhances PD-1 antibody efficacy (60% tumor shrinkage in mice)
2. Future Directions
● Structural modification: Prodrug development (e.g., butyrate ester for colon targeting)
● Delivery systems: Prodrug development (e.g., butyrate ester for colon targeting)
● AI integration: Metabolomics-guided personalized dosing models
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