Berberine hydrochloride (Synonyms: BBR, Umbellatine, NSC 163088, NSC 646666) |
| Catalog No.GN10208 |
Berberine hydrochloride is a bioactive alkaloid of the isoquinoline class derived from the medicinal plant Coptis chinensis of the Ranunculaceae family, possessing a wide range of pharmacological functions with applications in cancer, inflammation, diabetes, depression, hypertension, and various infections.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 633-65-8
Sample solution is provided at 25 µL, 10mM.
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Berberine hydrochloride is a bioactive alkaloid of the isoquinoline class derived from the medicinal plant Coptis chinensis of the Ranunculaceae family, possessing a wide range of pharmacological functions with applications in cancer, inflammation, diabetes, depression, hypertension, and various infections. Berberine hydrochloride can induce oxidative DNA damage in cancer cells[1]. It is a dual inhibitor of topoisomerase I and II and a potential autophagy modulator [2]. Due to its activating effect on AMPK, it can improve insulin sensitivity and reduce blood sugar levels [3].
In vitro, berberine hydrochloride (1.25-160μM; 72 hours) exhibits potential inhibitory effects on the proliferation of four colorectal cancer cell lines, LoVo, HCT116, SW480, and HT-29, with IC50 values ranging from 40.8±4.1 μM (LoVo) to 98.6±2.9μM (HCT116) [1]. Berberine hydrochloride (40.0μM) can induce G2/M phase cell cycle arrest, with an increase in the G2/M cell population and a progressive decrease in the G1 cell population [1]. It induces a significant increase in apoptosis in MG63 cells in a concentration- and time-dependent manner [4].
In vivo, oral doses of berberine hydrochloride at 30 and 50 mg/kg/day inhibited the growth of human colorectal adenocarcinoma xenografts in nude mice by 33.1% and 45.3%,respectively[1].Berberine hydrochloride alleviates lipopolysaccharide-induced mouse enteritis by inhibiting the activation of the NF-κB signaling pathway [5].
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.
[2] Md. Reyad-ul F, et al. Berberine chloride (dual topoisomerase I and II inhibitor) modulate mitochondrial uncoupling protein (UCP1) in molecular docking and dynamic with in-vitro cytotoxic and mitochondrial ATP production.Journal of Biomolecular Structure and Dynamics. 2022 May;41: 1704-1714.
[3] J Yin, J Ye, W Jia, et al. Effects and mechanisms of berberine in diabetes treatment[J]. Acta Pharmaceutica Sinica B, 2012.
[4] Zhu Y , Ma N , Li H X ,et al.Berberine induces apoptosis and DNA damage in MG-63 human osteosarcoma cells[J].Molecular Medicine Reports, 2014, 10(4).
[5] Fu K , Lv X , Li W ,et al.Berberine hydrochloride attenuates lipopolysaccharide-induced endometritis in mice by suppressing activation of NF-kB signal pathway[J].INTERNATIONAL IMMUNOPHARMACOLOGY, 2015.
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Cell experiment [1]: |
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Cell lines |
Four colorectal carcinoma cell lines LoVo, HCT116, SW480, and HT-29 |
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Preparation method |
Cells were treated with 0-160 μM berberine for 72 hours or for different time periods (24-72 hours). Add water-soluble tetrazolium salt (WST-1) and continue incubation for another 4 hours. Then use a microplate reader to read the OD value at a test wavelength of 440 nm and a reference wavelength of 620 nm. |
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Reaction Conditions |
0-160 μM; 24-72 hours |
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Applications |
Inhibited the proliferation of four cell lines. The IC50 ranged from 40.8±4.1 μM (LoVo) to 98.6±2.9 μM (HCT116). |
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Cell experiment [2]: |
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Cell lines |
MG-63 human osteosarcoma cell line (wild type) |
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Preparation method |
MG-63 cells were seeded at a density of 1x104cells//well in 100 μl of cell culture medium and then placed in a 96-well plate. Followi ng 12 h of incubation, the cells were treated with 0, 20, 40, 80 μM berberi ine for 12 and 24 h. |
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Reaction Conditions |
0, 20, 40, 80 μM; 12 and 24 h |
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Applications |
Berberine induced a significant increase in apoptosis in MG63 cells in a concentration and timedependent manner. |
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Animal experiment [1]: |
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Animal models |
BALB/c nu/nu mice |
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Preparation method |
Fragments (6-8 mm) of colorectal adenocarcinoma were implanted subcutaneously. in the flank of 5-week-old BALB/c nu/nu mice. Tumors were allowed to develop for 2 weeks. Once tumors were established, mice were randomly divided into five groups. The berberine treatment group (10 animals in each group) was given 10, 30 or 50 mg/kg berberine by gastrointestinal gavage for 10 consecutive days. |
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Dosage form |
10, 30, or 50 mg/kg/day; Gastrointestinal gavage; for 10 consecutive days |
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Applications |
Showed inhibitory rates of 33.1 % and 45.3 % at doses of 30 and 50 mg/kg/day. |
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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. [2]Zhu Y , Ma N , Li H X ,et al.Berberine induces apoptosis and DNA damage in MG-63 human osteosarcoma cells[J].Molecular Medicine Reports, 2014, 10(4). |
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| Cas No. | 633-65-8 | SDF | |
| Synonyms | BBR, Umbellatine, NSC 163088, NSC 646666 | ||
| Chemical Name | 9,10-dimethoxy-5,6-dihydro-[1,3]dioxolo[4,5-g]isoquinolino[3,2-a]isoquinolin-7-ium chloride | ||
| Canonical SMILES | [H]C(C([H])([H])C1=C2[H])([H])[N+](C([H])=C(C(OC([H])([H])[H])=C3OC([H])([H])[H])C(C([H])=C3[H])=C4[H])=C4C1=C([H])C5=C2OC([H])([H])O5.[Cl-] | ||
| Formula | C20H18ClNO4 | M.Wt | 371.81 |
| Solubility | ≥ 18.6mg/mL in DMSO with gentle warming | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6895 mL | 13.4477 mL | 26.8955 mL |
| 5 mM | 0.5379 mL | 2.6895 mL | 5.3791 mL |
| 10 mM | 0.269 mL | 1.3448 mL | 2.6895 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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