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Cardamonin

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Catalog No.
B7085
NF-κB抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 840.00
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50mg
¥ 2,640.00
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Background

IC50: 1.2 μM (NF-κB activation) [1]

Cardamonin (2′,4′-dihydroxy-6′-methoxychalcone), a chalcone isolated from the fruits of Alpinia rafflesiana, shows anti-inflammatory activity by targeting the nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway. NF-κB is a protein complex that controls cytokine production, transcription of DNA and cell survival.

In vitro: Cardamonin is a potential anti-inflammatory drug that targets the NF-κB pathway, which leads to suppress both NO and PGE2 synthesis, iNOS and COX-2 expression and enzymatic activity. The inhibition activation was due to a dose-dependent inhibition of phosphorylation and degradation of I-κBα, which resulted in a reduction of p65 NF-κB nuclear translocation [2]. Cardamonin also appears to inhibit prostaglandin E2, thromboxane B2 production, tumor necrosis factor a (TNF-a) release, and intracellular reactive oxygen species generation, all in a dose-dependent manner [3]

In vivo: Cardamonin shows protective effects on acute lung injury in sepsis. In mice, the results showed that cardamonin decreases systemic inflammatory responses, during sepsis, by downregulating TNF-a and interleukins [3].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Lee JH, Jung HS, Giang PM, Jin X, Lee S, Son PT, Lee D, Hong YS, Lee K, Lee JJ.  Blockade of nuclear factor-kappaB signaling pathway and anti-inflammatory activity of cardamomin, a chalcone analog from Alpinia conchigera. J Pharmacol Exp Ther. 2006 Jan;316(1):271-8. Epub 2005 Sep 23.
[2] Israf DA, Khaizurin TA, Syahida A, Lajis NH, Khozirah S.  Cardamonin inhibits COX and iNOS expression via inhibition of p65NF-kappaB nuclear translocation and Ikappa-B phosphorylation in RAW 264.7 macrophage cells. Mol Immunol. 2007 Feb;44(5):673-9. Epub 2006 Jun 13.
[3] Gonalves LM, Valente IM, Rodrigues JA.  An overview on cardamonin. J Med Food. 2014 Jun;17(6):633-40.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt270.28
Cas No.19309-14-9; 18956-16-6
FormulaC16H14O4
SolubilitySoluble in DMSO
Chemical Name(E)-1-(2,4-dihydroxy-6-methoxyphenyl)-3-phenylprop-2-en-1-one
SDFDownload SDF
Canonical SMILESOC1=C(C(/C=C/C2=CC=CC=C2)=O)C(OC)=CC(O)=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1, 2]:

细胞系

活化RAW 264.7细胞和全血,血管平滑肌细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

17–20 h

应用

Cardamonin抑制脂多糖和IFN-γ诱导的RAW细胞和全血的NO和PGE2产生,IC50值分别为11.4 μM和26.8 μM。在全血中,Cardamonin抑制了TxB2的产生。Cardamonin以剂量依赖性方式抑制RAW 264.7细胞内活性氧的产生和TNF-α的分泌,IC50值分别为12.8 μM和4.6 μM。Cardamonin(37、74或111 μM)抑制Ang II诱导的大鼠血管平滑肌细胞的增殖。Cardamonin抑制大鼠血管平滑肌细胞中Ang II刺激的细胞迁移。

动物实验 [3,4]:

动物模型

雌性ICR小鼠,雄性Sprague-Dawley大鼠

给药剂量

腹腔注射,0.02-20 mg/kg,连续4天;口服给药,3-30 mg/kg

应用

在雌性ICR小鼠中,腹腔注射0.02-20 mg/kg剂量的cardamonin抑制NO产生。在雄性Sprague-Dawley大鼠中,口服给药3-30 mg/kg剂量cardamonin显著抑制PBQ引起的扭动。Cardamonin以剂量依赖的方式增加carrageenan诱导的痛觉过敏的戒断反应延迟。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Ahmad S, Israf D A, Lajis N H, et al. Cardamonin, inhibits pro-inflammatory mediators in activated RAW 264.7 cells and whole blood[J]. European journal of pharmacology, 2006, 538(1): 188-194.

[2]. Shen Y J, Zhu X X, Yang X, et al. Cardamonin inhibits angiotensin II-induced vascular smooth muscle cell proliferation and migration by downregulating p38 MAPK, Akt, and ERK phosphorylation[J]. Journal of natural medicines, 2014, 68(3): 623-629.

[3]. Takahashi A, Yamamoto N, Murakami A. Cardamonin suppresses nitric oxide production via blocking the IFN-γ/STAT pathway in endotoxin-challenged peritoneal macrophages of ICR mice[J]. Life sciences, 2011, 89(9): 337-342.

[4]. Park MK, et al. Novel anti-nociceptive effects of cardamonin via blocking expression of cyclooxygenase-2 andtransglutaminase-2. Pharmacol Biochem Behav. 2014 Mar;118:10-5.

质量控制

化学结构

Cardamonin