| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
| ln Vivo |
In a dextran sodium sulfate (DSS)-induced colitis mouse model, oral administration of Berberrubine (20 mg/kg) significantly ameliorated clinical symptoms, as evidenced by reduced disease activity index (DAI) scores, prevention of body weight loss, and attenuation of colon shortening compared to the DSS model group. [1]
Berberrubine treatment (20 mg/kg) markedly improved histopathological damage in colon tissues, reducing inflammation, epithelial destruction, and crypt loss. It also significantly decreased myeloperoxidase (MPO) activity, a marker of neutrophil infiltration. [1] Berberrubine (20 mg/kg) significantly suppressed the colonic production of pro-inflammatory cytokines, including TNF-α, IFN-γ, IL-6, IL-1β, and IL-4, in DSS-treated mice. It also reduced the level of IL-10. [1] Berberrubine treatment (20 mg/kg) upregulated the mRNA expression of colonic mucins (Mucin-1 and Mucin-2) and increased the protein expression of tight junction proteins (ZO-1, ZO-2, Occludin, and Claudin-1), which were downregulated in DSS-induced colitis. [1] Berberrubine (20 mg/kg) modulated apoptosis-related proteins in colonic tissue by upregulating Bcl-2 expression and downregulating Bax expression, leading to a decreased Bax/Bcl-2 ratio. [1] |
|---|---|
| Animal Protocol |
Six-week-old male Balb/c mice were used. Colitis was induced by administering 3% (w/v) dextran sodium sulfate (DSS) in drinking water ad libitum for 7 days. [1]
Berberrubine was synthesized from berberine hydrochloride via microwave-assisted pyrolysis and purification. It was dissolved in 0.5% sodium carboxymethyl cellulose (CMC-Na) solution. [1] Mice were divided into groups (n=12): Control (water), DSS model (0.5% CMC-Na), Berberrubine low dose (10 mg/kg), Berberrubine high dose (20 mg/kg), Berberine (50 mg/kg), and Sulfasalazine (200 mg/kg). [1] Drugs or vehicle were administered once daily by oral gavage (0.1 mL/10 g body weight) for 7 consecutive days, concurrent with DSS exposure. [1] On day 8, mice were euthanized. Colons were collected, measured for length, and processed for histology (fixed in 4% paraformaldehyde), MPO/cytokine assays (tissue homogenization), Western blotting, and RT-PCR analysis (snap-frozen at -80°C). [1] |
| ADME/Pharmacokinetics |
Berberrubine is considered to be the main active metabolite of Berberrubine (BBR) in the body. [1] It is noteworthy that Berberrubine is more lipophilic than Berberrubine, and its plasma concentration is higher after oral administration due to its higher intestinal absorption efficiency. [1]
|
| References | |
| Additional Infomation |
Berberrubine is an alkaloid. Berberrubine is a naturally occurring isoquinoline alkaloid, a demethylated metabolite of Berberrubine. Its chemical structure differs from that of Berberrubine in that the hydroxyl group at the C-9 position is replaced by a methoxy group. [1] Studies have shown that the anti-ulcerative colitis effect of Berberrubine is achieved by reducing intestinal inflammation, upregulating tight junction proteins and mucins to maintain mucosal barrier integrity, and regulating apoptosis. [1] In a DSS-induced colitis model, the therapeutic effect of Berberrubine (20 mg/kg) was comparable to that of Berberrubine (50 mg/kg) and the positive control drug sulfasalazine (200 mg/kg), indicating that it can exert potential therapeutic effects at low doses. [1] The authors believe that Berberrubine may be a promising candidate drug worthy of further development for the treatment of ulcerative colitis. [1]
|
| Molecular Formula |
C19H16CLNO4
|
|---|---|
| Molecular Weight |
357.7876
|
| Exact Mass |
357.076
|
| CAS # |
15401-69-1
|
| PubChem CID |
72703
|
| Appearance |
Yellow to reddish brown solid powder
|
| Melting Point |
245℃ (DEC.)
|
| Vapour Pressure |
4.28E-15mmHg at 25°C
|
| Index of Refraction |
1.724
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
25
|
| Complexity |
474
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
GYFSYEVKFOOLFZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H15NO4.ClH/c1-22-16-3-2-11-6-15-13-8-18-17(23-10-24-18)7-12(13)4-5-20(15)9-14(11)19(16)21;/h2-3,6-9H,4-5,10H2,1H3;1H
|
| Chemical Name |
17-methoxy-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-octaen-16-ol;chloride
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
Ethanol : ~2 mg/mL (~5.59 mM)
|
|---|---|
| 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 | 2.7949 mL | 13.9747 mL | 27.9494 mL | |
| 5 mM | 0.5590 mL | 2.7949 mL | 5.5899 mL | |
| 10 mM | 0.2795 mL | 1.3975 mL | 2.7949 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
