Berberine 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.

CAS No. 633-65-8

サイズ	価格(税別)	在庫状況
10mg	JPY 22000	国内在庫あり
50mg	JPY 37000	国内在庫あり
200mg	JPY 52000	国内在庫あり
1g	JPY 130500	国内在庫なし(納期7~10日)

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関連化合物ライブラリー	Anti-infection Compound Library Antibiotics compound Library Antiviral Compound Library Anti-parasitic Compound Library Gut Microbial Metabolite Library	もっと見る

Anti-infection阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
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
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 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
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
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
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
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
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
MRC5 cells	Function assay			Antiviral activity against HCMV in MRC5 cells by plaque reduction assay, IC50=0.68 μM	17239594
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
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生物活性

製品説明

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]

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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]
細胞実験	細胞株	hepatocellular carcinoma (HCC) cells
	濃度	5, 10, 20, 40, 80, 160, 320, 640 and 1280 μM
	反応時間	48 h
	実験の流れ	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-Light^TM EdU ApolloR567 In Vitro Imaging Kit is used to detect the level of cell proliferation. The Annexin V-FITC/PI Apoptosis Detection Kit and DeadEnd^TM 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]
動物実験	動物モデル	Male BALB/c nude mice
	投与量	10mg/kg/day
	投与経路	i.p. (Data sourced from selleck products)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

参考
[1] Wen-Hsiu Hsu, et al. Arch Toxicol. 2007 Oct;81(10):719-28. [2] Marta Cernáková, et al. BMC Complement Altern Med. 2002 Feb 19;2:2. [3] Wang K, et al. Front Pharmacol. 2021;12:632201.

参考

化学情報

分子量	371.81	化学式	C₂₀H₁₈NO₄.Cl
CAS No.	633-65-8	SDF	Download Berberine chloride SDFをダウンロードする
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 40 mg/mL ( (107.58 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):