Scoparone

Catalog No.S3613 Batch:S361301

Technical Data

Formula	C₁₁H₁₀O₄
Molecular Weight	206.19	CAS No.	120-08-1
Solubility (25°C)*	In vitro	DMSO	41 mg/mL (198.84 mM)
		Ethanol	41 mg/mL (198.84 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.)

Preparing Stock Solutions

Biological Activity

Description	Scoparone (6,7-dimethoxycoumarin, Aesculetin dimethyl ether, 6,7-Dimethylesculetin, Escoparone) is a natural organic compound discovered from Chinese herb Artemisia scoparia with anticoagulant, hypolipidemic, vasorelaxant, antioxidant, and anti-inflammatory actions.
In vitro	The proliferation of VSMCs is significantly attenuated by scoparone in a dose-dependent manner. Scoparone markedly reduces the serum-stimulated accumulation of cells in the S phase and concomitantly increases the proportion of cells in the G0/G1 phase, which is consistent with the reduced expression of cyclin D1, phosphorylated Rb and survivin in the VSMCs. Cell adhesion markers, such as MCP-1 and ICAM-1, are significantly reduced by scoparone. It attenuates the increase in cyclin D promoter activity by inhibiting the activities of both the WT and active forms of STAT3. scoparone blocks the accumulation of STAT3 transported from the cytosol to the nucleus, leading to the suppression of VSMC proliferation through G1 phase arrest and the inhibition of Rb phosphorylation. This activity occurs independent of the form of STAT3 and upstream of kinases, such as Jak and Src, which are correlated with abnormal vascular remodeling due to the presence of an excess of growth factors following vascular injury. The protective effect of scoparone involves anti-inflammatory functions that occur via the inhibition of NF-κB activity, leading to the downregulation of pro-inflammatory cytokines and chemokines, such as tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-8 and monocyte chemoattractant protein (MCP)-1^[1].
In vivo	The free radical scavenging property of scoparone leads to the attenuation of intima thickening and improves hemodynamics in cholesterol-fed alloxan-diabetic rabbits concurrent with decreases in plasma lipid and lipoprotein cholesterol concentrations^[1]. Scoparone exhibited therapeutic efficacies on liver damage in vivo^[2].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines rat VSMCs Concentrations 500 μM Incubation Time 24 h Method The rat VSMCs are seeded in six-well plates at 90% confluence and are starved in serum-free media for 24 h followed by incubation in 1% FBS for an additional 24 h. The cells in the wells are detached by razor scraping, rinsed with PBS, stimulated in media containing 20% FBS, co-treated with 0.2% DMSO or 500 μM scoparone for 24 h and then stained with hematoxylin. Cell images are obtained via microscopy.
Animal Study:^{^[2]}	Animal Models Male Wistar rats Dosages 0.7 mg/kg Administration oral

Cell Assay:^{^[1]}

Cell lines
rat VSMCs
Concentrations
500 μM
Incubation Time
24 h
Method
The rat VSMCs are seeded in six-well plates at 90% confluence and are starved in serum-free media for 24 h followed by incubation in 1% FBS for an additional 24 h. The cells in the wells are detached by razor scraping, rinsed with PBS, stimulated in media containing 20% FBS, co-treated with 0.2% DMSO or 500 μM scoparone for 24 h and then stained with hematoxylin. Cell images are obtained via microscopy.

Animal Study:^{^[2]}

Animal Models
Male Wistar rats
Dosages
0.7 mg/kg
Administration
oral

References

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