Figure 1.

ER-β-selective ligand inhibits obesity. A) Structure of β-LGND2. B) β-LGND2 inhibits HFD-induced body weight and fat mass better than commercial drugs. Male C57BL6/J mice (6–8 wk old; n = 6–7 per group) were fed with ND or HFD. Animals fed with HFD were treated with vehicle, 30 mg/kg/d s.c. β-LGND2, lorcaserin (18 mg/kg/twice daily/s.c.), or orlistat (10 mg/kg/d s.c.). Body weight (left panel) was recorded weekly, and body fat mass (center panel) was measured using MRI once every 3 wk. Animals were humanely killed after 9 wk, and epididymal WAT weight was recorded (right panel). C) β-LGND2 inhibits body weight and fat in ob/ob mice. Male ob/ob mice (6–8 wk; n = 5) were treated with vehicle or 30 mg/kg/d s.c. β-LGND2. Weekly body weight and fat mass were recorded. Values are represented as percentage change from initiation of experiment. D) β-LGND2 inhibits body fat in WT, but not in ER-βKO, male mice. Male WT or ER-βKO mice (6–8 wk old; n = 6 per group) were maintained on ND or HFD and treated with vehicle or 30 mg/kg/d s.c. β-LGND2. Body fat was measured once every 3 wk using MRI. Animals were humanely killed, and epididymal WAT weight was recorded. Values are expressed as averages ± se. Lorc, lorcaserin; Orli, orlistat. *P < 0.05 vs. ND; ^#P < 0.05 vs. HFD.