Drug intelligence / Profile preview

isoliquiritigenin

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Isoliquiritigenin is a naturally occurring chalcone-type flavonoid found in the roots of several Glycyrrhiza species (licorice). It is studied for its diverse pharmacological activities including anti-inflammatory, antioxidant, antineoplastic (anticancer), antimicrobial, immunoregulatory, hepatoprotective and cardioprotective effects. Mechanistically, isoliquiritigenin acts as an inhibitor of aldose reductase and tyrosinase; it modulates multiple molecular pathways such as inhibition of the nuclear factor kappa B (NF-kB) pathway and activation of the nuclear factor erythroid related factor 2 (Nrf2) pathway. It also inhibits NOD-like receptor protein 3 (NLRP3) inflammasome activation and restrains mitogen activated protein kinase (MAPK) signaling. Additional reported mechanisms include antagonism at NMDA receptors and modulation of GABAergic activity. Isoliquiritigenin has shown potential in preclinical models for cancer therapy and inflammation-associated diseases but is not approved for clinical use[1][2][3][7][8][10].

Other names
(E)-1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)-propenone(E)-1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)-2-propene-1-one2',4,4'-trihydroxychalcone4,2',4'-trihydroxychalconetrans-2',4,4'-trihydroxychalcone6'-deoxychalcone
02

Targets

NOS3 (eNOS)GABRR (GABA-A receptor subunit rho)GABA-B (Gamma-aminobutyric acid receptor type B)PDE5 (Phosphodiesterase 5A)AR (Adrenergic receptors)NMDAR (Glutamate receptor ionotropic, NMDA)TYR (Tyrosinase)

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