Inhibits tyrosinase. Has pleiotropic effects. Inhibitor of CES2A.High specificity over CES1A (>500-fold) and other serine hydrolases. Glabridin is cell permeable and low cytotoxicity. IC50 0.52 muM in cells
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Title: Flavonoids as human carboxylesterase 2 inhibitors: Inhibition potentials and molecular docking simulations Song SS, Sun CP, Zhou JJ, Chu L Ref: Int J Biol Macromol, 131:201, 2019 : PubMed
In our search for natural human carboxylesterase 2 (hCE 2) inhibitors from natural products, we investigated inhibitory effects and mechanisms of flavonoids (1-16) against hCE 2. The results demonstrated that kurarinone (1), baicalein (2), 2-[(2'-(1-hydroxy-1-methylethyl)-7'-(3-methyl-2-butenyl)-2',3'-dihydrobenzofuran) -5-yl]-7-hydroxy-8-(3-methyl-2-butenyl)chroman-4-one (5), luteolin (6), kushenol X (9), and kushenol C (11) displayed significantly inhibitory effects against hCE 2 with IC50 values of 1.46+/-0.43, 5.22+/-0.89, 1.13+/-0.19, 9.78+/-0.98, 3.05+/-0.46, and 2.61+/-0.52muM, respectively. Compounds 1, 5, 6, 9, and 11 were all uncompetitive inhibitors with Ki values of 1.73, 1.59, 16.89, 1.72, and 0.79muM, respectively, and their Km values ranged from 2.08muM to 5.41muM. Furthermore, molecular docking was conducted for investigating mechanisms of compounds 1, 5, 6, 9, and 11 with hCE 2. These results suggested that compounds 1, 5, 6, 9, and 11 could be served as lead compounds for the development of novel hCE 2 inhibitors.