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Berbamine is a naturally occuring isoquinoline alkaloid found in traditional Chinese medicine Barberry with anti-tumor, immunomodulatory and cardiovascular effects. Calcium channel blockers include berbamine. It can be used to treat or prevent cardiac arrhythmias, and it may have an impact on the action potential's polarization-repolarization phase, excitability or refractoriness, impulse conduction, or membrane responsiveness within cardiac fibers.
| Targets |
Bcr-Abl; NF-κB; CaMKII
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|---|---|
| ln Vitro |
KM3 cell growth is inhibited by beribamine (8.17 μg/mL, 24 h) at a 50% rate [1]. Normal cell growth is induced by beribamine (185.20 μg/mL, 48 h), and the cell inhibition rate reaches 50% [1]. The growth of KM3 cells is inhibited by berabamine (8 μg/mL, 24 h), and 14.32% of the cells are stained[1]. IKKα expression and p65 nuclear translocation are inhibited by berabamine (8 μg/mL, 24 hours) [1].
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| ln Vivo |
Berbamine (100 mg/kg, barrier) causes a 70% weight loss and time-dependently suppresses the formation of Huh7 xenograft tumors [2].
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| Cell Assay |
Cell viability assay [1]
Cell Types: KM3 cells Tested Concentrations: 1−32 μg/mL Incubation Duration: 24, 48 or 72 h Experimental Results: Inhibited the growth of KM3 cells in a dose- and time-dependent manner. Apoptosis analysis[1] Cell Types: KM3 Cell Tested Concentrations: 4 μg/mL Incubation Duration: 6, 12 or 24 hrs (hours) Experimental Results: Treatment with 8 μg/mL induces apoptosis in a time-dependent manner. Western Blot Analysis[1] Cell Types: KM3 Cell Tested Concentrations: 8 μg/mL Incubation Duration: 0, 6, 12 or 24 h Experimental Results: Inhibition of p65 nuclear translocation and IKKα expression. |
| Animal Protocol |
Animal/Disease Models: Huh7 xenograft NOD/SCID mouse model [2]
Doses: 100mg/kg Route of Administration: po (oral gavage), twice a day for 5 days. Experimental Results: Inhibited tumor growth and diminished tumor weight by 70%. |
| References |
[1]. Liang Y, et al. Berbamine, a novel nuclear factor kappaB inhibitor, inhibits growth and induces apoptosis in human myeloma cells. Acta Pharmacol Sin. 2009 Dec;30(12):1659-65.
[2]. Meng Z, et al. Berbamine inhibits the growth of liver cancer cells and cancer-initiating cells by targeting Ca2+/calmodulin-dependent protein kinase II. Mol Cancer Ther. 2013 Oct;12(10):2067-77. |
| Molecular Formula |
C₃₇H₄₀N₂O₆
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|---|---|
| Molecular Weight |
608.72
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| Exact Mass |
608.28863700
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| CAS # |
478-61-5
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| Related CAS # |
Berbamine dihydrochloride;6078-17-7
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| Appearance |
Solid
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| SMILES |
CN1CCC2=CC(=C3C=C2[C@@H]1CC4=CC=C(C=C4)OC5=C(C=CC(=C5)C[C@@H]6C7=C(O3)C(=C(C=C7CCN6C)OC)OC)O)OC
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| InChi Key |
DFOCUWZXJBAUSQ-URLMMPGGSA-N
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| InChi Code |
InChI=1S/C37H40N2O6/c1-38-14-12-24-19-32(41-3)33-21-27(24)28(38)16-22-6-9-26(10-7-22)44-31-18-23(8-11-30(31)40)17-29-35-25(13-15-39(29)2)20-34(42-4)36(43-5)37(35)45-33/h6-11,18-21,28-29,40H,12-17H2,1-5H3/t28-,29+/m0/s1
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| Chemical Name |
(1S,14R)-20,21,25-trimethoxy-15,30-dimethyl-7,23-dioxa-15,30-diazaheptacyclo[22.6.2.23,6.18,12.114,18.027,31.022,33]hexatriaconta-3(36),4,6(35),8,10,12(34),18,20,22(33),24,26,31-dodecaen-9-ol
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| Synonyms |
Berbamine HCl; Berbamine hydrochloride
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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: ~100 mg/mL (~164.3 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6428 mL | 8.2140 mL | 16.4279 mL | |
| 5 mM | 0.3286 mL | 1.6428 mL | 3.2856 mL | |
| 10 mM | 0.1643 mL | 0.8214 mL | 1.6428 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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