Glabridin

Catalog No.S3786 Synonyms: Q-100692, KB-289522, LS-176045

For research use only.

Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.

Glabridin Chemical Structure

CAS No. 59870-68-7

Selleck's Glabridin has been cited by 1 Publication

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Biological Activity

Description Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
Targets
PPARγ [1]
(Cell-free assay)
α1β2γ2 (GABAA receptor) [3] α1β3γ2 (GABAA receptor) [3] α1β2 (GABAA receptor) [3] α1β1γ2 (GABAA receptor) [3]
6.3 μM(EC50) 6.83 μM(EC50) 9.63 μM(EC50) 17.23 μM(EC50)
In vitro

Glabridin induces dose-dependent increase in estrogenic activity and cell proliferation in Ishikawa cells. Glabridin exerts estrogenic activity via the ER-α-SRC-1-co-activator complex[1]. Glabridin has substantial neuroprotective effects, as indicated by the reduced cell death, apoptosis, DNA fragmentation, probably through the regulation of bcl-2, Bax and caspase-3 which are all closely related to cell apoptotic process[2].

In vivo Glabridin at 25mg/kg by intraperitoneal injection, but not at 5mg/kg, significantly decreases the focal infarct volume, cerebral histological damage and apoptosis in MCAO rats compared to sham-operated rats. Glabridin significantly attenuates the level of brain malonyldialdehyde (MDA) in MCAO rats, while it elevates the level of two endogenous antioxidants in the brain, i.e. superoxide dismutase (SOD) and reduced glutathione (GSH). Co-treatment with glabridin significantly inhibits the staurosporine-induced cytotoxicity and apoptosis of cultured rat cortical neurons in a concentration-dependent manner. Consistently, glabridin significantly reduces the DNA laddering caused by staurosporine in a concentration-dependent manner. Glabridin has a neuroprotective effect via modulation of multiple pathways associated with apoptosis. Glabridin appears to achieve steady state concentrations slowly in humans. The limited penetration of glabridin into the brain due to the activity of P-glycoprotein in the blood-brain barrier may also lessen the activity of glabridin at low doses[2].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: Ishikawa cells
  • Concentrations: 1nM to 10μM
  • Incubation Time: 72 h
  • Method: The effect of the extracts on cell proliferation are estimated using MTT assay. Briefly, 10μL of 5 mg/ml MTT is added to each well after incubation with test compounds for 72 h. DMSO is then added to dissolve the formazan and the plate read at 595 nm. The cell proliferation of control cells is 100.00% and any increase or decrease in cell proliferation of treated cells is compared to the control cells. All experimental conditions are assayed in triplicate.
Animal Research:[2]
  • Animal Models: Male healthy Sprague-Dawley rats
  • Dosages: 5 mg/kg and 25 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 324.37
Formula

C20H20O4

CAS No. 59870-68-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1(C=CC2=C(O1)C=CC3=C2OCC(C3)C4=C(C=C(C=C4)O)O)C

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