Paper
International Journal of Obesity (2005) 29, 1236–1244. doi:10.1038/sj.ijo.0803014; published online 31 May 2005
Estrogen receptor 
-mediated adiposity-lowering and hypocholesterolemic actions of the selective estrogen receptor modulator acolbifene
C Lemieux1, D Phaneuf2, F Labrie2, V Giguère3, D Richard1 and Y Deshaies1
- 1Department of Anatomy and Physiology, Faculty of Medicine, Laval Hospital Research Center, Laval University, Quebec City, Quebec, Canada
- 2Department of Anatomy and Physiology, Faculty of Medicine, Molecular Endocrinology and Oncology Research Center of Laval University Hospital Research Center, Laval University, Quebec City, Quebec, Canada
- 3Molecular Oncology Group, Royal Victoria Hospital, Montreal, Quebec City, Quebec, Canada
Correspondence: Dr Y Deshaies, Department of Anatomy and Physiology, School of Medicine, Laval University, Quebec City, Quebec, Canada G1K 7P4. E-mail: yves.deshaies@phs.ulaval.ca
Received 30 November 2004; Revised 21 April 2005; Accepted 27 April 2005; Published online 31 May 2005.
Abstract
OBJECTIVE:
The selective estrogen receptor (ER) modulator (SERM) acolbifene (ACOL), a potent and pure antiestrogen in the mammary gland and uterus, exerts beneficial pro-estrogenic actions on energy balance, insulin sensitivity and lipid metabolism. ACOL binds ERs 
and 
, both of which have been involved in the metabolic actions of estrogen. This study aimed at determining the identity of the ER involved in the beneficial metabolic actions of ACOL.
DESIGN AND MEASUREMENTS:
ACOL was administered for 4 weeks to male and female wild-type and ER knockout (KO) mice, and indices of energy balance as well as plasma and liver lipid concentrations were determined.
RESULTS:
ER KO mice were heavier, gained more fat mass and had larger adipose depots than their wild-type counterparts. In both genders, ACOL decreased fat gain (50%) and white adipose tissue mass in male and female wild-type, but not in ER KO mice. ACOL reduced plasma cholesterol in female wild-type mice (-27%), whereas the compound remained ineffective in their ER KO counterparts. Plasma triglycerides were unaffected by ACOL. Finally, ACOL decreased liver cholesterol and triglyceride concentrations only in wild-type female animals.
CONCLUSION:
The beneficial metabolic actions of the SERM ACOL on adiposity and on plasma and liver lipids are entirely due to its interaction with the ER.
Keywords:
estrogen antagonist, estrogen receptor, EM-652, adiposity, blood cholesterol
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