Home Transmembrane Transporters TRP Channel antagonist Cardamonin For research use only.

Cardamonin

Synonyms: Alpinetin chalcone

Cardamonin (Alpinetin chalcone), isolated from the fruits of Alpinia species, is a chalconoid with anti-inflammatory and anti-tumor activity. It has been shown to be a novel antagonist of hTRPA1 cation channel with IC50 of 454 nM while does not interact with TRPV1 nor TRPV4 channel.

Cardamonin Chemical Structure

Cardamonin Chemical Structure

CAS No. 18956-16-6

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Cardamonin Related Products

Biological Activity

Description Cardamonin (Alpinetin chalcone), isolated from the fruits of Alpinia species, is a chalconoid with anti-inflammatory and anti-tumor activity. It has been shown to be a novel antagonist of hTRPA1 cation channel with IC50 of 454 nM while does not interact with TRPV1 nor TRPV4 channel.
Targets
hTRPA1 [1]
454 nM
In vitro
In vitro Cardamonin selectively blocks TRPA1 activation while does not interact with TRPV1 nor TRPV4 channel. A concentration-dependent inhibitory effect is observed with IC50 of 454 nM. Cardamonin does not significantly reduce HEK293 cell viability, nor does it impair cardiomyocyte constriction[1]. In vitro, cardamonin (25 and 50 μM) concentration dependently inhibits endothelium permeability and down-regulates phosphorylation of P38 in rat lung microvascular endothelial cells induced by lipopolysaccharide (LPS). In RAW 264.7 macrophage cells, cardamonin also shows selective inhibition of P38 phosphorylation induced by LPS[2]. Cardamonin inhibits the growth of several cancer cell types including breast cancer, glioblastoma, ovarian, prostate, and lung. Treatment of cardamonin in CRC cell lines induces cell cycle arrest mostly in the S phase of cell cycle. It activates both apoptosis and induces cell cycle arrest to inhibit the cell proliferation. Cardamonin is known to inhibit various signaling pathways which play a major role in the process of inflammation and cancer. This natural product inhibits the phosphorylation and translocation of both STAT3 and NF-κB. Cardamonin also inhibits angiogenesis through downregulation of miR-21 expression[3].
Cell Research Cell lines rat lung microvascular endothelial cells (isolated form Sprague-Dawley rats)
Concentrations 12.5, 25, and 50 μM
Incubation Time 12 h
Method

Endothelial cells are preincubated with different concentrations of cardamonin for 12 h. Then, Trypan blue-labeled BSA is added into the upper compartments of Transwell membranes. Thirty minutes later, cells are stimulated by  LPS  (1 μg/mL) for 1 h. Trypan blue dye content in the lower compartment is assayed by spectrophotometry at 590 nm and expressed as a percentage of the maximum concentration that would have been achieved at equilibrium.
In Vivo
In vivo Cardamonin (30 and 100 mg/kg) significantly elevates the survival rate of septic mice, alleviates ALI and lung microvascular leak, and lowers the serum levels of proinflammatory cytokines TNF-α, IL-1β,and IL-6[2]. Cardamonin inhibits Azoxymethane-induced colorectal cancer (CRC). Its treatment inhibits the tumor incidence, tumor multiplicity, Ki-67 and β-catenin positive cells. The preclinical pharmacokinetics and ADME characterization of cardamonin in mice reports that cardamonin is highly permeable with an effective permeability value in ileum is (Peff) 3 × 10−4 which is highly significant. Within 30 minutes of oral dosing, cardamonin is distributed to various tissues[3].
Animal Research Animal Models Male ICR mice
Dosages 0, 30, and 100 mg/kg
Administration oral

Chemical Information & Solubility

Molecular Weight 270.28 Formula

C16H14O4
CAS No. 18956-16-6 SDF Download Cardamonin SDF
Smiles COC1=CC(=CC(=C1C(=O)C=CC2=CC=CC=C2)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 54 mg/mL ( (199.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 54 mg/mL

Water : Insoluble


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In vivo
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