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| 25mg |
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| Targets |
Epiberberine targets multiple enzymes. It is a potent AChE and BChE inhibitor, making it a potential candidate for Alzheimer's disease research. It is also a non-competitive BACE1 inhibitor, targeting a key enzyme in amyloid-beta production. Additionally, it is a potent inhibitor against both ureases. Its antioxidant activity is attributed to its ability to scavenge peroxynitrite (ONOO⁻).
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| ln Vitro |
Epiberberine (0, 12.5, 25 or 50 μM) dose-dependently reduces cellular triglyceride formation in 3T3-L1 adipocytes with an IC50 of 52.8 μM [2]. Epiberberine (12.5-50 μM) suppresses the Raf/MEK1/ERK1/2 and AMPKα/Akt pathways during the early stages of 3T3-L1 adipocyte development [2]. Epiberberine (0.2, 1, 5 μg/mL) reduces glucose absorption in HepG2 cells in a concentration-dependent manner [3].
In vitro, Epiberberine exhibits potent inhibition of AChE (IC₅₀ = 1.07 µM), BChE (IC₅₀ = 6.03 µM), and BACE1 (IC₅₀ = 8.55 µM). It also shows significant urease inhibitory activity and antioxidant activity by scavenging ONOO⁻ (IC₅₀ = 16.83 µM). Its multi-targeted activity makes it a promising compound for the study of Alzheimer's disease and diabetes. |
| ln Vivo |
In KK-Ay mice, oral administration of epiberberine (225 mg/kg) for 40 days results in decreased body weight, food consumption, water intake, and urine output [3].
In vivo, Epiberberine's ability to inhibit AChE and BACE1 suggests potential for treating Alzheimer's disease, while its urease inhibitory activity could be relevant for treating Helicobacter pylori infections. It has been shown to have effects in 3T3-L1 cell differentiation. However, specific in vivo efficacy data are not detailed in the provided search results. |
| Enzyme Assay |
In vitro non-cell enzyme assays for Epiberberine typically involve measuring the inhibition of AChE, BChE, and BACE1 activities. For AChE and BChE, the compound is incubated with the enzyme and a chromogenic substrate (e.g., Ellman's reagent), and the inhibition of activity is measured. For BACE1, a fluorogenic substrate is used. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for Epiberberine use various cell lines, such as neuronal cells, to study its neuroprotective effects. Cells are treated with the compound, and its ability to protect against amyloid-beta-induced toxicity or to modulate cholinergic signaling is assessed. Its effects on urease activity can be studied in bacterial cultures.
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| Animal Protocol |
In vivo animal studies for Epiberberine would likely employ models of Alzheimer's disease (e.g., transgenic mice) to study its effects on cognitive function and amyloid plaque burden. Its effects on urease activity could be studied in animal models of H. pylori infection.
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| ADME/Pharmacokinetics |
Epiberberine has a molecular weight of 336.36 g/mol and a molecular formula of C₂₀H₁₈NO₄. It is an alkaloid. It is soluble in organic solvents. Detailed pharmacokinetic data are not widely published.
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| Toxicity/Toxicokinetics |
The toxicity profile of Epiberberine is not extensively detailed in the provided search results. As a natural alkaloid, it may have significant biological activity and potential toxicity. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
According to reports, epiberberine is found in corydalis, Coptis triangularis, and other organisms with available data.
Epiberberine is a protoberberine alkaloid from Coptis chinensis with potent AChE, BChE, and BACE1 inhibitory activities. It also has urease inhibitory and antioxidant activities. It is being studied for its potential in Alzheimer's disease and diabetes. It is not approved for clinical use and is intended for research purposes only. |
| Molecular Formula |
C₂₀H₁₈NO₄+
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|---|---|
| Molecular Weight |
336.36
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| Exact Mass |
336.123
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| CAS # |
6873-09-2
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| Related CAS # |
Epiberberine chloride;889665-86-5
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| PubChem CID |
160876
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| Appearance |
Orange red solid powder
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| Melting Point |
260ºC
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| LogP |
-0.99
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
488
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FPJQGFLUORYYPE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H18NO4/c1-22-18-8-13-5-6-21-10-15-12(3-4-17-20(15)25-11-24-17)7-16(21)14(13)9-19(18)23-2/h3-4,7-10H,5-6,11H2,1-2H3/q+1
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| Chemical Name |
16,17-dimethoxy-5,7-dioxa-1-azoniapentacyclo[11.8.0.03,11.04,8.014,19]henicosa-1(13),2,4(8),9,11,14,16,18-octaene
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~3.33 mg/mL (~9.90 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9730 mL | 14.8650 mL | 29.7301 mL | |
| 5 mM | 0.5946 mL | 2.9730 mL | 5.9460 mL | |
| 10 mM | 0.2973 mL | 1.4865 mL | 2.9730 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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