Isoliquiritigenin (ISL) is a chalcone compound with valuable pharmacological properties such as antioxidant, anti-inflammatory, anticancer and anti-allergic activities.Isoliquiritigenin, a chalcone compound, is a positive allosteric modulator of GABA receptors and shows hypnotic effects.
Targets
IC50
N/A
In vitro
Isoliquiritigenin (ISL) is a chalcone compound with valuable pharmacological properties such as antioxidant, anti-inflammatory, anticancer and anti-allergic activities.Isoliquiritigenin, a chalcone compound, is a positive allosteric modulator of GABA A receptors and shows hypnotic effects. ISL also can suppress HIF-1alpha level, VEGF expression and secretion, cell migration and to decrease the expression and secretion of MMP-9/-2. ISL inhibited the proliferation of U87 cells in a time-dependent and dose-dependent manner.ISL induced the apoptosis of the U87 cells and blocked cell cycle progression at the S and G2/M phases. ISL induced the apoptosis of the U87 cells in a caspase-dependent manner. ISL upregulated p21/WAF1 and p27. Cell cycle arrest and the caspase-mediated apoptosis pathway may participate in the antiproliferative activity of ISL in U87 cells by regulating the expression of ISL. There is a strong dose-response relationship between ISL exposure and the characteristics of B16F0 differentiation in terms of morphology changes and melanogenesis. Isoliquiritigenin also can inhibit one of the most drug-metabolizing enzymes (DMEs) UDP-glucuronosyltransferase (UGT). 100uM of isoliquiritigenin inhibited the activity of UGT1A1, UGT1A3, UGT1A6, UGT1A7, UGT1A8, UGT1A9, and UGT1A10 by 95.2%, 76.1%, 78.9%, 87.2%, 67.2%, 94.8%, and 91.7%. Low concentration of ISL may have therapeutic potential in the treatment of aggressive breast carcinoma and other neoplasms.
In vivo
The tumorigenicity of ISL-treated cells was limited significantly in an animal model assay in vivo respectively.