Psoralidin

Catalog No.S5464

Psoralidin Chemical Structure

Molecular Weight(MW): 336.34

Psoralidin, a naturally occurring coumestan isolated from the fractions of organic solvents such as ethylacetate, hexane, or n-butanol of the seed extract of Psoralea corylifolia L., has a variety of biological activities such as anticancer, antioxidant, antibacterial, antidepressant, anti-inflammatory activities, and regulation of insulin signaling. It is an agonist for both estrogen receptor (ER)α and ERβ with binding affinities (IC50s) of 1.03 and 24.6 μM, respectively.

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Biological Activity

Description Psoralidin, a naturally occurring coumestan isolated from the fractions of organic solvents such as ethylacetate, hexane, or n-butanol of the seed extract of Psoralea corylifolia L., has a variety of biological activities such as anticancer, antioxidant, antibacterial, antidepressant, anti-inflammatory activities, and regulation of insulin signaling. It is an agonist for both estrogen receptor (ER)α and ERβ with binding affinities (IC50s) of 1.03 and 24.6 μM, respectively.
Targets
ERα [1]
(Cell-free)
ERβ [1]
(Cell-free)
1.03 μM 24.6 μM
In vitro

Psoralidin has been characterized as a full ER agonist, which activates the classical ER-signaling pathway in both ER-positive human breast and endometrial cell lines as well as non-human cultured cells transiently expressing either ERα or ERβ. Psoralidin was also able to induce the endogenous estrogen-responsive gene, pS2, in human breast cancer cells MCF-7. The IC50 values for psoralidin to replace the binding of E2 to both receptors were 1.03 and 24.6 μM, respectively. Psoralidin is able to bind to both receptors within the micromolar range and has preferential affinity for ERα over ERβ[1].

In vivo Acute and subchronic administrations of psoralidin produced a significant reduction in immobility time in the mouse forced swimming test. Psoralidin dose-dependently increased swimming and failed to affect climbing[2].

Protocol

Cell Research:

[1]

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  • Cell lines: MCF-7 cells
  • Concentrations: 10 μM
  • Incubation Time: 24 h
  • Method:

    MCF-7 cells were cultured in estrogen-free RPMI 1640 media for 4 days before transfection, and plated (4 × 105 cells/well) in triplicate onto a 12-well plate. Cells were transiently transfected with pERE-luciferase plasmid (0.5 μg/well) and with an internal control plasmid pRL-Tk (0.1 μg/well) using Lipofectamine 2000 Reagent. ERE-luciferase plasmid contains three copies of the Xenopus laevis vitellogenin A2 ERE upstream of fire fly luciferase. The pRL-Tk plasmid contains a cDNA encoding Renilla luciferase. At 24 h post-transfection, cells were treated DMSO, various concentrations of E2, psoralidin, ICI, or appropriate combination of two compounds and incubated for another 24 h. The cells were harvested with Passive Lysis buffer. Luciferase activity present in the cell lysates was measured.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Male ICR strain of mice
  • Formulation: water
  • Dosages: 20, 40 and 60 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 67 mg/mL (199.2 mM)
Ethanol 1 mg/mL (2.97 mM)
Water 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.

Chemical Information

Molecular Weight 336.34
Formula

C20H16O5

CAS No. 18642-23-4
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID