Effects of coumestrol on lipid and glucose metabolism as a farnesoid X receptor ligand.
In the course of an effort to identify novel agonists of the farnesoid X receptor (FXR), coumestrol was determined to be one such ligand. Reporter and in vitro coactivator interaction assays revealed that coumestrol bound and activated FXR. Treatment of Hep G2 cells with coumestrol stimulated the expression of FXR target genes, thereby regulating the expression of target genes of the liver X receptor and hepatocyte nuclear factor-4alpha. Through these actions, coumestrol is expected to exert beneficial effects on lipid and glucose metabolism.
Takahashi
Miki
M
Biological Science Laboratories, Kao Corporation, 2606 Akabane, Ichikai-machi, Haga-gun, Tochigi 321-3497, Japan.
Kanayama
Tomohiko
T
Yashiro
Takuya
T
Kondo
Hidehiko
H
Murase
Takatoshi
T
Hase
Tadashi
T
Tokimitsu
Ichiro
I
Nishikawa
Jun-Ichi
J
Sato
Ryuichiro
R
D001055:Apolipoproteins B / Q000378:metabolism; D002460:Cell Line; D003375:Coumestrol / Q000494:pharmacology*; D004268:DNA-Binding Proteins / Q000819:agonists* / Q000378:metabolism; D005947:Glucose / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D050356:Lipid Metabolism / Q000187:drug effects* / Q000235:genetics; D048789:Phytoestrogens / Q000494:pharmacology*; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000378:metabolism; D014157:Transcription Factors / Q000819:agonists* / Q000378:metabolism; D014158:Transcription, Genetic / Q000187:drug effects*; D000099150:Receptor, Farnesoid X-Activated
D001055:Apolipoproteins B; D003375:Coumestrol; D004268:DNA-Binding Proteins; D005947:Glucose; D008024:Ligands; D048789:Phytoestrogens; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors; D000099150:Receptor, Farnesoid X-Activated