Phenolics with PPAR-gamma ligand-binding activity obtained from licorice (Glycyrrhiza uralensis roots) and ameliorative effects of glycyrin on genetically diabetic KK-A(y) mice.
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.
Kuroda
Minpei
M
Laboratory of Medicinal Plant Science, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Hachioji, Tokyo 192-0392, Japan.
Mimaki
Yoshihiro
Y
Sashida
Yutaka
Y
Mae
Tatsumasa
T
Kishida
Hideyuki
H
Nishiyama
Tozo
T
Tsukagawa
Misuzu
M
Konishi
Eisaku
E
Takahashi
Kazuma
K
Kawada
Teruo
T
Nakagawa
Kaku
K
Kitahara
Mikio
M
D000818:Animals; D001665:Binding Sites; D002460:Cell Line; D002522:Chlorocebus aethiops; D003374:Coumarins / Q000627:therapeutic use*; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy* / Q000235:genetics*; D006035:Glycyrrhiza; D007004:Hypoglycemic Agents / Q000627:therapeutic use*; D008024:Ligands; D051379:Mice; D008817:Mice, Mutant Strains; D010636:Phenols / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D008517:Phytotherapy; D000077205:Pioglitazone; D010936:Plant Extracts / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D018160:Receptors, Cytoplasmic and Nuclear / Q000235:genetics / Q000378:metabolism*; D011993:Recombinant Fusion Proteins / Q000378:metabolism; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000627:therapeutic use; D014157:Transcription Factors / Q000235:genetics / Q000378:metabolism*
D003374:Coumarins; D007004:Hypoglycemic Agents; D008024:Ligands; D010636:Phenols; D010936:Plant Extracts; D018160:Receptors, Cytoplasmic and Nuclear; D011993:Recombinant Fusion Proteins; D045162:Thiazolidinediones; D014157:Transcription Factors; D000077205:Pioglitazone