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Butein

Butein, a plant polyphenol isolated from Rhus verniciflua, is able to inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, also inhibits EGFR.

Butein化学構造

CAS No. 487-52-5

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代表番号: 045-509-1970|電子メール：[email protected]
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製品安全説明書

現在のバッチを見る： S803601 DMSO] 55 mg/mL] false] Ethanol] 55 mg/mL] false] Water] Insoluble] false 純度： 99.98%
99.98

Butein関連製品

シグナル伝達経路

EGFR Signaling Pathways

EGFRシグナル伝達経路

EGFR阻害剤の選択性比較

生物活性

製品説明 Butein, a plant polyphenol isolated from Rhus verniciflua, is able to inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, also inhibits EGFR.
Targets
EGFR [1]
In Vitro
In vitro Butein inhibits the epidermal growth factor (EGF)-stimulated auto-phosphotyrosine level of EGF receptor in HepG2 cells, and also inhibits tyrosine-specific protein kinase activities of EGF receptor and p60c-src with IC50 of 65 μM in vitro. The inhibition is competitive to ATP and non-competitive to the phosphate acceptor, poly (Glu, Ala, Tyr) 6:3:1 for EGF receptor tyrosine kinase. In contrast, Butein non-significantly inhibits the activities of serine- and threonine-specific protein kinases such as PKC or PKA. [1] Butein inhibits Nuclear Factor(NF)-κB and NF-κB-regulated gene expression through direct inhibition of IκBα Kinase β on Cysteine 179 Residue. [2] Butein (10 μM) inhibits over 90% iNOS and COX-2 expression, as well as nitrite and TNF-α production in LPS-stimulated RAW 264.7 cells. Butein (10 μM) inhibits LPS-induced DNA binding activity of NF-κB, which is mediated through inhibition of the degradation of inhibitory factor-κB and phosphorylation of Erk1/2 MAP kinase, as well as increases binding of the osteopontin a vb3 integrin receptor. [3] Butein (20 μM) treatment induces morphologic changes of bladder cancer cells BLS(M) from elongated morphology to rounded epithelial-like cells, accompanied by downregulation of vimentin, and gaining of E-cadherin compared to untreated control cells, indicating the reversal of mesenchymal-like phenotype. Butein (20 μM) suppresses motility and invasion capacity of BLS(M) cells, and reverts EMT-like phenotype induced by TNF-α, through the ERK1/2 and NF-κB signaling pathways. [4] Butein inhibits the constitutive activation of STAT3 in HepG2 cells in a dose-dependent manner, with maximum inhibition occurring at 50 μM, mediated through the inhibition of activation of upstream kinases c-Src and Janus-activated kinase2. Butein (50 μM) also could completely inhibit IL-6-induced STAT3 phosphorylation in SNU-387 cells. Butein downregulates the expression of cyclin D1, Bcl-2, Bcl-xL, survivin, and VEGF, markers of STAT3 activation. Butein (50 μM) significantly enhance the apoptotic effects of doxorubicin from 18% to 55% and of paclitaxel from 15% to 42%. [5] Butein is as a powerful antioxidant against lipid and LDL peroxidation. Butein inhibits iron-induced lipid peroxidation in rat brain homogenate with an IC50 of 3.3 μM. Butein is as potent α-tocopherol in reducing the stable free radical diphenyl-2-picrylhydrazyl (DPPH) with IC0.2 of 9.2 μM. Butein also inhibits the activity of xanthine oxidase with an IC50 of 5.9 μM. Butein scavenges the peroxyl radical derived from 2,2-azobis(2-amidinopropane) dihydrochloride (AAPH) in aqueous phase. Furthermore, Butein inhibits copper-catalyzed oxidation of human low-density lipoprotein (LDL) in a concentration-dependent manner. Butein is a chelator of ferrous and copper ions. [6]
細胞実験 細胞株 Human hepatoma cells HepG2
濃度 ~50 μM
反応時間 1 days
実験の流れ The cells (5× 103/mL) are incubated in triplicate in a 96-well plate in the presence or absence of indicated concentration of Butein in a final volume of 0.2 mL for different time intervals at 37 ℃. Thereafter, 20 μL MTT solution (5 mg/mL in PBS) is added to each well. After a 2-hour incubation at 37 ℃, 0.1 mL lysis buffer (20% SDS, 50% dimethylformamide) is added, incubation is continued overnight at 37 ℃, and then the optical density at 570 nm is measured by plate reader.
In Vivo
In Vivo Butein at 2 mg/kg induces significant inhibition of hepatocellular tumor growth compared with the corn oil-treated controls. At necropsy on day 22 after initial treatment, there is more than 2-fold decrease in tumor growth in the Butein-treated group (mean relativetumor burden, 3.90) compared with the control group (8.46), associated with reduced constitutive p-STAT3 (9% vs 81% of vehicle group), Bcl-2 levels (26% vs 96% of vehicle group), and increased caspase-3 level (98% vs 21% of vehicle group) in HCC tumor tissues. [5] Butein shows antifibrogenic activity. Butein (25 mg/kg/day) reduces serum AST and ALT activation to 35% and 69%, respectively, of control CCl4-induced rat levels. Butein (25 mg/kg/day) reduces liver hydroxyproline contents and TBAR4 concentration to 54% and 54%, respectively. α1(I) collagen and TIMP-1 expression in Butein-treated rats is 28% and 20.3% compared with the values for the respective CCl4-treated control. [7]
動物実験 動物モデル Human hepatocellular carcinoma xenografts HepG2
投与量 2 mg/kg
投与経路 intraperitoneal injection, 5 doses per week for 3 consecutive weeks

化学情報

分子量 272.25 化学式

C15H12O5
CAS No. 487-52-5 SDF Download Butein SDFをダウンロードする
Smiles C1=CC(=C(C=C1C=CC(=O)C2=C(C=C(C=C2)O)O)O)O
保管

In vitro
Batch:

DMSO : 55 mg/mL ( (202.02 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。)

Ethanol : 55 mg/mL

Water : 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

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）

mg/kg g μL 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。

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