Phenolics from Glycyrrhiza glabra roots and their PPAR-gamma ligand-binding activity.
Bioassay-guided fractionation of the EtOH extract of licorice (Glycyrrhiza glabra roots), using a GAL-4-PPAR-gamma chimera assay method, resulted in the isolation of 39 phenolics, including 10 new compounds (1-10). The structures of the new compounds were determined by analysis of their spectroscopic data. Among the isolated compounds, 5'-formylglabridin (5), (2R,3R)-3,4',7-trihydroxy-3'-prenylflavane (7), echinatin, (3R)-2',3',7-trihydroxy-4'-methoxyisoflavan, kanzonol X, kanzonol W, shinpterocarpin, licoflavanone A, glabrol, shinflavanone, gancaonin L, and glabrone all exhibited significant PPAR-gamma ligand-binding activity. The activity of these compounds at a sample concentration of 10microg/mL was three times more potent than that of 0.5microM troglitazone.
Kuroda
Minpei
M
School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1, Horinouchi, Hachioji, Tokyo 192 0392, Japan. kurodam@toyaku.ac.jp
Mimaki
Yoshihiro
Y
Honda
Shinichi
S
Tanaka
Hozumi
H
Yokota
Shinichi
S
Mae
Tatsumasa
T
D000818:Animals; D001665:Binding Sites; D002460:Cell Line; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D006035:Glycyrrhiza / Q000737:chemistry*; D008024:Ligands; D015394:Molecular Structure; D047495:PPAR gamma / Q000187:drug effects*; D010636:Phenols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D008024:Ligands; D047495:PPAR gamma; D010636:Phenols