Berberine Sulfate
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Basic information
Product Name: Berberine Sulfate
IUPAC Name: 16,17-dimethoxy-5,7-dioxa-13-azoniapentacyclo[11.8.0.02,10.04,8.015,20]henicosa-1(13),2,4(8),9,14,16,18,20-octaene;hydrogen sulfate
CAS No.: 316-41-6
Molecular Formula: C₂₀H₁₉NO₈S
Physicochemical Properties:
|
Property |
Specification |
|
Appearance |
Yellow crystalline powder |
|
Melting Point |
208-210°C (decomposition) |
|
Solubility |
Water: Freely soluble (58 mg/mL, 25°C) |
|
Ethanol: Slightly soluble (5 mg/mL) |
Quality Standard: CP2020, JP, Customer Made
Specification
| Test Items | Standard |
| Berberine Sulfate(CAS: 316-41-6) | 98% by titration |
| Loss on drying | ≤15.0% |
| Residue on ignition | ≤0.2% |
Broad-spectrum antimicrobial activity
Effective against bacteria, fungi, and parasites.
Multi-target modulation
Simultaneously regulates AMPK/mTOR/SIRT1 metabolic pathways.
Clinically validated
Supported by 20+ global Phase III clinical trials for its glucose- and lipid-lowering efficacy.
1. Multi-Target Network
2. Key Target Data
|
Target/Pathway |
Effect |
EC50/IC50 |
|
Bacterial DNA gyrase |
Inhibits DNA replication (MIC=10 μg/mL) |
IC50=2.5 μM |
|
AMPK |
↑3-fold phosphorylation |
EC50=5 μM |
|
PCSK9 |
↓60% expression |
IC50=8 μM |
Clinical Applications
1. Indications & Efficacy
● Metabolic disorders:
Type 2 diabetes: Reduces HbA1c by 1.0-1.5% (comparable to metformin)
Hyperlipidemia: Lowers LDL-C by 20-25%
● Infectious diseases:
Bacterial diarrhea (85% efficacy)
Candida albicans vaginitis (75% cure rate)
● Other applications:
NAFLD (↓30% ALT levels)
PCOS (↑2-fold ovulation rate)
2. Innovative Formulations
|
Formulation |
Technology |
Representative Product |
|
Enteric-coated capsules |
Prevents gastric acid degradation (↑50% bioavailability) |
BerbElite® |
|
Nanosuspension |
<200 nm particles (↑3x intestinal absorption) |
NanoBerb® |
|
Extended-release tablets |
8-h sustained blood concentration |
GlucoBalance® |
1. Standard Protocols
|
Indication |
Route |
Dose |
Duration |
|
Type 2 diabetes |
Oral |
500 mg tid |
≥3 months |
|
Hypercholesterolemia |
Oral |
300 mg bid |
2-6 months |
|
Bacillary dysentery |
Oral |
100 mg qid |
5-7 days |
2. Drug Interactions
● Synergistic:
Metformin (AMPK co-activation)
Statins (further LDL-C reduction)
● Contraindicated:
Cyclosporine (CYP3A4 competition)
Digoxin (↑cardiotoxicity risk)
Safety Evaluation
1. Adverse Reactions
|
System |
Adverse Effect |
Incidence |
Management |
|
Gastrointestinal |
Diarrhea/abdominal pain |
15-20% |
Dose reduction + post-meal intake |
|
Hepatic |
Transient ALT elevation |
3% |
Discontinue for 2 weeks |
|
Allergic |
Rash |
<1% |
Discontinue + antihistamines |
2. Special Populations
|
Population |
Recommendation |
Reference |
|
Pregnancy |
Contraindicated (embryotoxic in animals) |
FDA Category D |
|
Lactation |
Suspend nursing (detected in milk) |
LactMed database |
|
Hepatic impairment |
50% dose reduction (Child-Pugh B/C) |
Hepatology 2023 |
Research Progress Green max
1. Cutting-Edge Discoveries
● Anticancer:
↓PD-L1 expression (enhances immunotherapy)
Blocks Wnt/β-catenin (colorectal cancer models)
● Neuroprotection:
Reduces α-synuclein aggregation (Parkinson's models)
Improves Aβ clearance (Alzheimer's models)
● Gut microbiota: ↑5-fold Akkermansia muciniphila proliferation
2. Future Directions
● Structural modification: Prodrug development (e.g., palmitate ester for ↑oral absorption)
● Delivery systems: Exosome-based targeted delivery (preclinical)
● AI integration: Machine learning for personalized dosing
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