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Berberine is a naturally occurring isoqinoline alkaloid found in Chinese herbal medicine Huanglian with a variety of biological activities. It is a quaternary ammonium salt from the group of isoquinoline alkaloids with varoius biological activities. Berberine has been reported to have a chemopreventive property against colon tumor formation by inhibiting the enzyme Cox-2 (cyclooxygenase-2) which is abundantly expressed in colon cancer cells. Also inhibits c-Jun (Activator Protein 1), a transcription factor that plays a critical role in inflammation and carcinogenesis.
Targets |
ROS; DNA topoisomerase
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ln Vitro |
Four colorectal cancer cell lines—LoVo, HCT116, SW480, and HT-29—may be inhibited from proliferating by berberine (1.25–160 μM; 72 hours)[1]. A dose- and time-dependent suppression of LoVo cell proliferation is induced by berberine (1.25-160 μM; 24-72 hours)[1]. Berberine (10–80 μM) is applied to LoVo cells for a full day. When LoVo cells are treated with 40 μM Berberine, flow cytometry analysis of their cell cycle reveals an accumulation of cells in the G2/M phase[1]. After a day, berberine (10-80 μM), particularly at a level of 80.0 μM, inhibits the expression of cyclin B1, cdc2, and cdc25c proteins[1].
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ln Vivo |
For ten consecutive days, gastric gavage with berberine at 10, 30, or 50 mg/kg/day suppresses the growth of human colorectal adenocarcinoma in vivo. Results: Displayed inhibitory rates of 33.1% and 45.3% at dosages of 30 and 50 mg/kg/day administered by gastrointestinal gavage; for 10 consecutive days. Dosage: 10, 30, or 50 mg/kg/day; Administration: Gastrointestinal gavage.
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Enzyme Assay |
Western blotting and OPTDI analysis for detecting cell cycle proteins[1]
LoVo cells were harvested, lysed in lysis buffer [50 mmol/L TrisCl (pH 6.8), 100 mmol/L DTT, 2 % SDS, 0.1 % bromophenol blue, 10 % glycerin] at 100 °C for 10 min and stored at −20 °C. Protein concentrations were determined by BCA assay. Equal protein amounts were loaded onto SDS-polyacrylamide gels, and the proteins were transferred electrophoretically to a PVDF membrane. Immunoblots were analyzed using specific primary antibodies to cyclin B1, cdc2 and cdc25c (1:200 dilution) and incubated with horseradish peroxidase-conjugated secondary antibodies (1:1,000 dilution), and the proteins were visualized using an enhanced chemiluminescence detection kit. The optical density integral (OPTDI) was analyzed by an automatic image analysis system. The expression of cyclin B1, cdc2 and cdc25c was normalized to internal controls (GAPDH). The results were presented as percentages of treatments compared to the control. Measurement of DNA and protein synthesis[1] DNA and protein synthesis was assessed by the cellular incorporation of 3H-thymidine and L-[4,5-3H]-leucine (60 Ci/mg molecular and 0.5 μCi/well respectively). Isolated cells (1 × 105 cells per well) were incubated with medium containing a series of concentrations of berberine. Four hours before the 24-h berberine exposure, radioactive precursors were added to the culture. At the end of the incubation period, the medium was removed to a piece of filter membrane; the cells were washed three times with distilled water. 3H-thymidine and L-[4,5-3H]-leucine incorporation was determined by liquid scintillation spectrometry. |
Cell Assay |
Cell Proliferation Assay[1]
Cell Types: Four colorectal carcinoma cell lines LoVo, HCT116, SW480, and HT-29 Tested Concentrations: 1.25, 2.5, 5, 10, 20, 40, 80, and 160 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited the proliferation of four cell lines. The IC50 ranged from 40.8±4.1 μM (LoVo) to 98.6±2.9 μM (HCT116). Cell Proliferation Assay[1] Cell Types: Colorectal carcinoma cell lines LoVo Tested Concentrations: 1.25, 2.5, 5, 10, 20, 40, 80, and 160 μM Incubation Duration: 24, 48, 72 hrs (hours) Experimental Results: Induced a time- and dose-dependent inhibition of cell growth. By 72 h, 160.0 μM induced 71.1±1.9 % growth inhibitions in LoVo cells. Cell Cycle Analysis[1] Cell Types: LoVo cells Tested Concentrations: 0, 10, 20, 40, or 80 μM Incubation Duration: 24 hrs (hours) Experimental Results: Exposure to 40.0 μM induced G2/M-phase cell cycle arrest, an increase in the G2/M-phase population and a progressive decline in the G1 population. Western Blot Analysis[1] Cell Types: LoVo cells Tested Concentrations: 10, 20, 40, or 80 μM Incubation Duration: 24 hrs (hours) Experimental Results: Berberine suppressed cyclin B1, cdc2 and cdc25c protein expression after 24 h, especially at the dose of 80.0 μM. |
Animal Protocol |
In vivo anti-tumor effect of berberine in human colorectal adenocarcinoma (LoVo)[1]
The in vivo antitumor efficacy of berberine was examined using human colorectal adenocarcinoma LoVo xenografts in a nude mouse model; 1 × 107 cells were implanted subcutaneous injection (s.c.) in the flanks of 5-week-old BALB/c nu/nu mice. After the tumors were grown up to about 1,000–1,500 mm3, the mice were sacrificed and the tumors were divided into equal fragments. Fragments (6–8 mm3) of colorectal adenocarcinoma were implanted s.c. in the flanks of 5-week-old BALB/c nu/nu mice. Tumors were allowed to develop for 2 weeks. Once tumors were established, the mice were divided randomly into five groups. The berberine-treated groups (ten mice each group) received 10, 30, or 50 mg kg−1 day−1 berberine by gastrointestinal gavage for 10 consecutive days. The 5-FU-treated group (10 mice) was given 30 mg kg−1 day−1 by intraperitoneal injection for 10 consecutive days. The control group (11 mice) was given sterile water. Measurements of body weights and tumor volumes were recorded every 1–3 days until the experimental endpoint, at which the tumors were debilitating to the mice. The long axis (L) and the short axis (S) were measured, and the tumor volume (V) was calculated using the following equation: V = S × S × L/2. Once the final measurement was taken, the mice were sacrificed by cervical dislocation. The inhibitory rates were determined by comparing the volume of the control group and the treatment group: (1 − V treatment/Vcontrol). Effect of the combination of berberine and 5-FU on the growth of human colorectal adenocarcinoma (HT-29) xenografts in nude mice[1] The in vivo antitumor efficacy of the combination of berberine and 5-FU was examined using human colorectal adenocarcinoma HT-29 xenografts in a nude mouse model; 1 × 107 cells were implanted subcutaneous injection (s.c.) in the flanks of 5-week-old BALB/c nu/nu mice. After the tumors were grown up to about 1,000–1,500 mm3, the mice were sacrificed and the tumors were divided into equal fragments. Fragments (6–8 mm3) of colorectal adenocarcinoma were implanted s.c. in the flanks of 5-week-old BALB/c nu/nu mice. Tumors were allowed to develop for 3 weeks. Once tumors were established, the mice were divided randomly into four groups. The berberine-treated group (ten mice) received 50 mg kg−1 day−1 berberine by gastrointestinal gavage for 10 consecutive days. The 5-FU-treated group (10 mice) was given 30 mg kg−1 day−1 by intraperitoneal injection for 10 consecutive days. The combination group (10 mice) was given berberine and 5-FU. The control group (10 mice) was given sterile water. Measurements of body weights and tumor volumes were recorded every 3–4 days until the experimental endpoint, at which the tumors were debilitating to the mice. The long axis (L) and the short axis (S) were measured, and the tumor volume (V) was calculated using the following equation: V = S × S × L/2. Once the final measurement was taken, the mice were sacrificed by cervical dislocation. The inhibitory rates were determined by comparing the volume of the control group and the treatment group: (1 − V treatment/V control). |
References |
[1]. Cai Y, et al. Berberine inhibits the growth of human colorectal adenocarcinoma in vitro and in vivo. J Nat Med. 2014 Jan;68(1):53-62.
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Molecular Formula |
C20H18NO4
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Molecular Weight |
336.3612
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Exact Mass |
336.12304
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CAS # |
2086-83-1
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Related CAS # |
Berberine chloride hydrate;68030-18-2;Berberine chloride;633-65-8;Berberine sulfate;633-66-9
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Appearance |
Solid
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Source |
Chinese herb Huanglian
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LogP |
-0.99
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tPSA |
40.8
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SMILES |
O1C([H])([H])OC2=C1C([H])=C1C(=C2[H])C2C([H])=C3C([H])=C([H])C(=C(C3=C([H])[N+]=2C([H])([H])C1([H])[H])OC([H])([H])[H])OC([H])([H])[H]
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InChi Key |
YBHILYKTIRIUTE-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H18NO4/c1-22-17-4-3-12-7-16-14-9-19-18(24-11-25-19)8-13(14)5-6-21(16)10-15(12)20(17)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-13-azoniapentacyclo[11.8.0.02,10.04,8.015,20]henicosa-1(13),2,4(8),9,14,16,18,20-octaene
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Synonyms |
Natural Yellow 18; Umbellatine; Berberin; Berbericine; Majarine; Thalsine; Umbellatin;
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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: > 10 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.