Abstract: 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. Conculsion
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.