Cardamonin

Catalog No.S3942 Batch:S394202

Technical Data

Formula	C₁₆H₁₄O₄
Molecular Weight	270.28	CAS No.	18956-16-6
Solubility (25°C)*	In vitro	DMSO	54 mg/mL (199.79 mM)
		Ethanol	7 mg/mL (25.89 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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].

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 (P_eff) 3 × 10⁻⁴ which is highly significant. Within 30 minutes of oral dosing, cardamonin is distributed to various tissues^[3].

Protocol (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[2]}	Animal Models Male ICR mice Dosages 0, 30, and 100 mg/kg Administration oral

Cell Assay:^{^[2]}

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.

Animal Study:^{^[2]}

Animal Models
Male ICR mice
Dosages
0, 30, and 100 mg/kg
Administration
oral

References

Selleck's Cardamonin has been cited by 2 publications

Distinct longevity mechanisms across and within species and their association with aging [ Cell, 2023, 186(13):2929-2949.e20]	PubMed: 37269831
Cardamonin inhibits osteogenic differentiation of human valve interstitial cells and ameliorates aortic valve calcification via interfering in the NF-κB/NLRP3 inflammasome pathway [ Food Funct, 2021, 12(23):11808-11818]	PubMed: 34766179

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SHIPPING AND STORAGE
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