Cardamonin (Synonyms: Alpinetin chalcone, Cardamomin) |
| Catalog No.GC18069 |
Cardamonin ((E)-Cardamomin) is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 19309-14-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1, 2]: | |
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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 experiment [3, 4]: | |
|
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. |
|
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. |
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| Cas No. | 19309-14-9 | SDF | |
| Synonyms | Alpinetin chalcone, Cardamomin | ||
| Chemical Name | (E)-1-(2,4-dihydroxy-6-methoxyphenyl)-3-phenylprop-2-en-1-one | ||
| Canonical SMILES | OC1=C(C(/C=C/C2=CC=CC=C2)=O)C(OC)=CC(O)=C1 | ||
| Formula | C16H14O4 | M.Wt | 270.28 |
| Solubility | DMF: 25 mg/ml,DMSO: 25 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml,Ethanol: 1 mg/ml | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6999 mL | 18.4993 mL | 36.9987 mL |
| 5 mM | 0.74 mL | 3.6999 mL | 7.3997 mL |
| 10 mM | 0.37 mL | 1.8499 mL | 3.6999 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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