Berberine chloride

Synonyms: NSC 646666, Natural Yellow 18 chloride

Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

Berberine chloride Chemical Structure

Berberine chloride Chemical Structure

CAS No. 633-65-8

Purity & Quality Control

Berberine chloride Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MRC5 cells Function assay Antiviral activity against HCMV in MRC5 cells by plaque reduction assay, IC50=0.68 μM 17239594
MRC5 cells Proliferation assay 10 μM 54 hrs Inhibition of HCMV proliferation in MRC5 cells after 54 hrs post-infection at 10 uM by plaque assay 17239594
MRC5 cells Proliferation assay 10 μM 24 h Inhibition of HCMV proliferation in MRC5 cells after 24 hrs post-infection at 10 uM by plaque assay 17239594
Bel7402 cells Function assay 12 h Induction of LDLR protein in human Bel7402 cells after 12 hrs by RT-PCR assay relative to control 19090767
HepG2 cells Function assay 10 ug/mL 12 h Induction of LDLR protein expression in human HepG2 cells at 10 ug/mL after 12 hrs by flow cytometry 19090767
KB cells Cytotoxicity assay 72 h Cytotoxicity against human KB cells after 72 hrs, IC50=7.32 μM 11141105
HL60 cells Apoptosis assay 48 hrs Induction of apoptosis in human HL60 cells after 48 hrs using annexin V-propidium iodide staining by FACS analysis 20227144
A549 cells Cytotoxicity assay Cytotoxicity against human A549 cells by SRB assay, IC50=6.27 μM 20594848
SKOV3 cells Cytotoxicity assay Cytotoxicity against human SKOV3 cells by SRB assay, IC50=16.44 μM 20594848
SK-MEL-2 cells Cytotoxicity assay Cytotoxicity against human SK-MEL-2 cells by SRB assay, IC50=13.76 μM 20594848
HCT15 cells Cytotoxicity assay Cytotoxicity against human HCT15 cells by SRB assay, IC50=16.59 μM 20594848
CEM cells Cytotoxicity assay 48 hrs Cytotoxicity against human CEM cells expressing green fluorescent protein after 48 hrs by MTT assay, CC50=2.09 μM 21295891
human CEM cells Function assay 7 days Antiviral activity against 0.05 MOI Human immunodeficiency virus 1 NL4.3 infected in human CEM cells expressing green fluorescent protein assessed as p24 antigen production measured 7 days post infection by ELISA, EC50=0.13 μM 21295891
SKN cells Growth inhibition assay 72 h Growth inhibition against human SKN cells after 72 hrs by MTT assay, GI50=15.88 μM 21401114
RKN cells Growth inhibition assay 48 hrs Growth inhibition against human RKN cells after 48 hrs by MTT assay, GI50=49.6 μM 21401114
G402 cells Growth inhibition assay 48 hrs Growth inhibition against human G402 cells after 48 hrs by MTT assay, GI50=11.87 μM 21401114
A10 cells Function assay 30 μM 24 hrs Downregulation of Scd2 mRNA expression in rat A10 cells at 30 uM after 24 hrs by quantitative RT-PCR analysis 21401114
A10 cells Function assay 30 μM 24 hrs Down regulation of Prim2 mRNA expression in rat A10 cells at 30 uM after 24 hrs by quantitative RT-PCR analysis 21401114
A10 cells Function assay 30 μM 24 hrs Downregulation of Impk mRNA expression in rat A10 cells at 30 uM after 24 hrs by quantitative RT-PCR analysis 21401114
HepG2-A16-CD81 cells Function assay 10 μM NOVARTIS: Antimalarial liver stage activity measured as a greater than 50% reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells at 10uM compound concentration, determined by immuno-fluorescence. 22096101
HepG2-A16-CD81 cells Function assay 10 μM NOVARTIS: Antimalarial liver stage activity measured as reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells by immuno-fluorescence, and median schizont size at 10uM compound concentration, IC50=0.548 μM 22096101
HepG2 cells Function assay 10 μM 4 h Increase in AMPKalpha phosphorylation in human HepG2 cells at 10 uM after 4 hrs by Western blot analysis relative to untreated control 23058107
HepG2 cells Function assay 10 μM 4 h Increase in total AMPKalpha level in human HepG2 cells at 10 uM after 4 hrs by Western blot analysis relative to untreated control 23058107
HepG2 cells Function assay 20 μM 24 hrs Induction of apoptosis in human HepG2 cells assessed as morphological changes at 20 uM after 24 hrs using Hoechst 33258 staining by fluorescence microscopic analysis 23182088
HT-29 cells Cytotoxicity assay 48 hrs Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay, IC50=8.45 μM 23182088
HepG2 cells Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay, IC50=11.22 μM 23182088
HepG2 cells Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50=8.32 μM 23182088
Click to View More Cell Line Experimental Data

Biological Activity

Description Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Targets
Caspase-3 [1] Caspase-8 [1] PARP [1] cytochrome c [1] cIAP1 [1] Click to View More Targets
In vitro
In vitro

Compared with regorafenib alone, the combined treatment of Berberine (BBR) and regorafenib significantly inhibits the proliferation of hepatocellular carcinoma (HCC) cells and induces cellular apoptosis.[3]

Cell Research Cell lines hepatocellular carcinoma (HCC) cells
Concentrations 5, 10, 20, 40, 80, 160, 320, 640 and 1280 μM
Incubation Time 48 h
Method

HCC cells are seeded into a 96-well plate with 5,000 cells per well. After overnight incubation, HCC cells are treated with the indicated concentrations of regorafenib, Berberine (BBR) or their combination for 24h or 48h. The viability of HCC is examined by MTS Assay and Synergy H1/Epoch microplate reader.The interaction between regorafenib and BBR is quantified by Com-puSyn software. The Cell-LightTM EdU ApolloR567 In Vitro Imaging Kit is used to detect the level of cell proliferation. The Annexin V-FITC/PI Apoptosis Detection Kit and DeadEndTM Fluorometric Tunel System assay are used to measure cellular apoptotic level.

In Vivo
In vivo

The combined treatment group with Berberine (BBR) and regorafenib has a dramatic inhibitory effect on the growth of hepatocellular carcinoma (HCC) xenograft tumors in nude mice. The increased apoptosis of xenograft tumors is seen in the combined treatment group.[3]

Animal Research Animal Models Male BALB/c nude mice
Dosages 10mg/kg/day
Administration i.p.

(Data sourced from selleck products)
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06273241 Not yet recruiting
Pharmacokinetic Study in Healthy Volunteers
University Medicine Greifswald
March 4 2024 Not Applicable
NCT05845931 Recruiting
Pharmacokinetic Study in Healthy Volunteers
University Medicine Greifswald
May 5 2023 Not Applicable
NCT05480670 Completed
Polycystic Ovary Syndrome
Ayub Teaching Hospital
November 1 2022 Not Applicable
NCT05463003 Completed
Pharmacokinetic Study in Healthy Volunteers
University Medicine Greifswald
July 19 2022 Not Applicable

Chemical Information & Solubility

Molecular Weight 371.81 Formula

C20H18NO4.Cl

CAS No. 633-65-8 SDF Download Berberine chloride SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 40 mg/mL ( (107.58 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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