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Berberine chloride Anti-infection chemical

Name: Berberine chloride
Brand: Selleck Chemicals
SKU: S2271
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S2271

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

Chemical Structure

Molecular Weight: 371.81

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Quality Control

Batch: Purity: 99.75%

99.75

Related Targets	Integrase Bacterial Antibiotics Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease
Other Anti-infection Inhibitors	Clorsulon Sodium Tauroursodeoxycholate (TUDC) Cystamine dihydrochloride p-Coumaric Acid Ascomycin (FK520) LL37 (Human cathelicidin) Cinchonidine Berberine chloride hydrate Cetylpyridinium Chloride Chlorquinaldol

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
MRC5 cells	Function assay			Antiviral activity against HCMV in MRC5 cells by plaque reduction assay, IC50=0.68 μM
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
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
Bel7402 cells	Function assay		12 h	Induction of LDLR protein in human Bel7402 cells after 12 hrs by RT-PCR assay relative to control
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
KB cells	Cytotoxicity assay		72 h	Cytotoxicity against human KB cells after 72 hrs, IC50=7.32 μM
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
A549 cells	Cytotoxicity assay			Cytotoxicity against human A549 cells by SRB assay, IC50=6.27 μM
SKOV3 cells	Cytotoxicity assay			Cytotoxicity against human SKOV3 cells by SRB assay, IC50=16.44 μM
SK-MEL-2 cells	Cytotoxicity assay			Cytotoxicity against human SK-MEL-2 cells by SRB assay, IC50=13.76 μM
HCT15 cells	Cytotoxicity assay			Cytotoxicity against human HCT15 cells by SRB assay, IC50=16.59 μM
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
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
SKN cells	Growth inhibition assay		72 h	Growth inhibition against human SKN cells after 72 hrs by MTT assay, GI50=15.88 μM
RKN cells	Growth inhibition assay		48 hrs	Growth inhibition against human RKN cells after 48 hrs by MTT assay, GI50=49.6 μM
G402 cells	Growth inhibition assay		48 hrs	Growth inhibition against human G402 cells after 48 hrs by MTT assay, GI50=11.87 μM
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
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
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
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.
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
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
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
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
HT-29 cells	Cytotoxicity assay		48 hrs	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay, IC50=8.45 μM
HepG2 cells	Cytotoxicity assay		24 hrs	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay, IC50=11.22 μM
HepG2 cells	Cytotoxicity assay		48 hrs	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50=8.32 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (67.23 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	4%DMSO 1 30%PEG300 2 66%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (8.07mM)	Taking the 1 mL working solution as an example, add 40 μL of 75 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.69mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight	371.81	Formula	C₂₀H₁₈NO₄.Cl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	633-65-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	Caspase-3 Caspase-8 PARP cytochrome c cIAP1 Bcl-2 Bcl-xL JNK p38 MAPK ROS Topo I Topo II
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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17673978/ [2] https://pubmed.ncbi.nlm.nih.gov/11943071/ [3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8248669/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Handling Instructions

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