[Effects of farnesoid X receptor agonist on adiponectin and its receptors].
OBJECTIVE
To investigate the effects of GW4064, a farnesoid X receptor (FXR) agonist, on adiponectin and its receptors during the differentiation of 3T3-L1 preadipocytes and on adiponectin receptors in HepG2 cells.


METHODS
The mRNA expressions of FXR, PPARγ2, adiponectin, AdipoR1, and AdipoR2 and the protein levels of adiponectin on days 0, 2, 4, 6, and 8 during the differentiation of 3T3-L1 preadipocytes treated with GW4064 were detected by fluorescent real-time PCR and ELISA, respectively. The mRNA expressions of AdipoR1 and AdipoR2 in HepG2 cells were also examined at 0, 12, 24, and 48 h after GW4064 treatment.


RESULTS
The mRNA expressions of FXR, PPARγ2, adiponectin, and AdipoR2 in 3T3-L1 preadipocytes and AdipoR2 in HepG2 cells treated with GW4064 was significantly increased compared with the control group (all P<0.05). The protein level of adiponectin was also significantly increased after GW4064 treatment. The expression of AdipoR1 in either 3T3-L1 preadipocytes or HepG2 cells showed no significant changes after GW4064 treatment.


CONCLUSIONS
GW4064 can up-regulate the expressions of FXR, PPARγ2, adiponectin, AdipoR2 in 3T3-L1 preadipocytes and AdipoR2 in HepG2 cells. As adiponectin and its receptors are two important factors in the treatment of non-alcoholic fatty liver disease, FXR agonist may potentially produce therapeutic effect on non-alcoholic fatty liver disease and can regulate adipocytes via up-regulating PPARγ during adipocyte differentiation.
Institute of Digestive Diseases, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China. E-mail: 27216571@qq.com.
Xiaomin
X
Xin
Muxiao
M
Zhong
Shanshan
S
Zhang
Yao
Y
Peng
Wei
W
Zhu
Yali
Y
Zhang
D041721:3T3-L1 Cells; D052242:Adiponectin / Q000378:metabolism*; D000818:Animals; D002454:Cell Differentiation / Q000187:drug effects*; D056945:Hep G2 Cells; D006801:Humans; D007555:Isoxazoles / Q000494:pharmacology*; D051379:Mice; D047495:PPAR gamma / Q000378:metabolism; D054419:Receptors, Adiponectin / Q000378:metabolism*; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists*; D000099150:Receptor, Farnesoid X-Activated
D052242:Adiponectin; D007555:Isoxazoles; D047495:PPAR gamma; D054419:Receptors, Adiponectin; D018160:Receptors, Cytoplasmic and Nuclear; D000099150:Receptor, Farnesoid X-Activated; C475418:ADIPOR1 protein, human; C475420:ADIPOR2 protein, human; C412815:GW 4064