Abstract
The EtOAc extract of licorice (Glycyrrhiza uralensis roots) exhibited considerable PPAR-gamma ligand-binding activity. Bioassay-guided fractionation of the extract using a GAL-4-PPAR-gamma chimera assay method resulted in the isolation of two isoflavenes, one of which is a new compound named dehydroglyasperin D, an isoflavan, two 3-arylcoumarins, and an isoflavanone as the PPAR-gamma ligand-binding active ingredients of licorice. The isoprenyl group at C-6 and the C-2' hydroxyl group in the aromatic ring-C part in the isoflavan, isoflavene, or arylcoumarin skeleton were found to be the structural requirements for PPAR-gamma ligand-binding activity. Glycyrin, one of the main PPAR-gamma ligands of licorice, significantly decreased the blood glucose levels of genetically diabetic KK-A(y) mice.
MeSH terms
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Animals
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Binding Sites
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Cell Line
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Chlorocebus aethiops
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Coumarins / therapeutic use*
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Diabetes Mellitus, Type 2 / drug therapy*
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Diabetes Mellitus, Type 2 / genetics*
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Glycyrrhiza*
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Hypoglycemic Agents / therapeutic use*
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Ligands
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Mice
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Mice, Mutant Strains
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Phenols / pharmacokinetics
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Phenols / pharmacology*
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Phenols / therapeutic use
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Phytotherapy*
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Pioglitazone
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Plant Extracts / pharmacokinetics
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Plant Extracts / pharmacology*
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Plant Extracts / therapeutic use
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Receptors, Cytoplasmic and Nuclear / genetics
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Receptors, Cytoplasmic and Nuclear / metabolism*
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Recombinant Fusion Proteins / metabolism
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Structure-Activity Relationship
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Thiazolidinediones / therapeutic use
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Transcription Factors / genetics
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Transcription Factors / metabolism*
Substances
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Coumarins
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Hypoglycemic Agents
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Ligands
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Phenols
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Plant Extracts
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Receptors, Cytoplasmic and Nuclear
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Recombinant Fusion Proteins
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Thiazolidinediones
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Transcription Factors
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Pioglitazone