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Cardamonin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cardamonin图片
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Cardamonin ((E)-Cardamomin) 是一种新型的 hTRPA1 阳离子通道拮抗剂,IC50 为 454 nM。

Cell lines

Activated RAW 264.7 cells and whole blood, vascular smooth muscle cell

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

17–20 h

Applications

Cardamonin inhibited NO and PGE2 production from lipopolysaccharide- and IFNγ-induced RAW cells and whole blood with IC50 values of 11.4 μM and 26.8 μM, respectively. In whole blood, cardamonin inhibited the generation of TxB2. Cardamonin dose-dependently inhibited the generation of intracellular reactive oxygen species and secretion of TNF-α from RAW 264.7 cells with IC50 values of 12.8 μM and 4.6 μM, respectively. Treatment with Cardamonin (37, 74, or 111 μM) inhibited Ang II-induced proliferation of rat VSMCs. Cardamonin suppressed Ang II-stimulated migration of rat VSMCs.

Animal models

Female ICR mice, Male Sprague-Dawley rats

Dosage form

Intraperitoneal injection, 0.02-20 mg/kg, daily for 4 consecutive days; oral administration, 3-30 mg/kg

Application

In female ICR mice, Cardamonin (0.02–2 mg/kg, i.p.) inhibited NO production. In male Sprague-Dawley rats, Cardamonin (3-30 mg/kg, oral administration) significantly inhibited PBQ-induced writhing. Cardamonin dose-dependently increased the withdrawal response latencies in carrageenan-induced hyperalgesia.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

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.