title: Effects of raloxifene treatment on the phenotype of blood monocytes.
abstract: Raloxifene (RLX), a selective oestrogen receptor modulator, has oestrogen-agonist effects on bone, lipoproteins, and homocysteine and oestrogen-antagonist activity in the breast and uterus, positioning it as a potential drug for long-term prevention of coronary heart disease in postmenopausal women. To further evaluate its influence on cardiovascular risk factors, we studied the effects of 60 mg/day RLX on serum lipid levels, inflammatory (high-sensitivity C-reactive protein, and coagulation (fibrinogen) markers, monocytes, and fibrinolysis in 15 healthy postmenopausal women. Markers were measured at baseline, after 1 month without treatment, and after 3 months of treatment. Fibrinolysis was evaluated using the euglobulin clot lysis time (ECLT) determined with a new semiautomatic optical method. Monocyte phenotype was determined by measurement of the expression of the antigens CD14, HLA-DR, and CD62-L using flow cytometry. After 3 months of RLX treatment, we observed a decrease in total cholesterol (p = 0.002), in low-density lipoprotein cholesterol (p <0.001), and in lipoprotein A (p = 0.01). Fibrinogen (p = 0.002) decreased significantly, and high-sensitivity C-reactive protein had a tendency to decrease, but this did not reach statistical significance (p = 0.06). RLX treatment had no effect on ECLT (p = 0.223) or on white blood cell, lymphocyte, and total monocyte counts (p = 0.313). Monocyte expression of HLA-DR, CD14, and CD62-L was not modified by the treatment. In conclusion, we confirm that RLX has beneficial short-term effects on levels of lipids and inflammatory markers, with no effect on fibrinolysis or monocyte phenotype.
authors.affiliation: Experimental Medicine Laboratory, ULB 222 Unit, Université Libre de Bruxelles, Intercommunale de santé publique du pays de Charleroi, CHU de Charleroi, Hôpital André Vésale, 6110 Montigny-Le-Tilleul, Belgium. karim.zouaoui@chu-charleroi.be
authors.forename: Karim Zouaoui
authors.initials: KZ
authors.lastname: Boudjeltia
authors.forename: Patrick
authors.initials: P
authors.lastname: Durez
authors.forename: Didier
authors.initials: D
authors.lastname: Oberweis
authors.forename: Michel
authors.initials: M
authors.lastname: Guillaume
authors.forename: Claude
authors.initials: C
authors.lastname: Remacle
authors.forename: Philippe
authors.initials: P
authors.lastname: Cauchie
authors.forename: Michel
authors.initials: M
authors.lastname: Vanhaeverbeek
authors.forename: Dany
authors.initials: D
authors.lastname: Brohée
authors.forename: Jean
authors.initials: J
authors.lastname: Ducobu
authors.forename: Catherine
authors.initials: C
authors.lastname: Gregoir
mesh_terms: D000368:Aged; D002784:Cholesterol / Q000097:blood; D008076:Cholesterol, HDL / Q000097:blood; D003327:Coronary Disease / Q000097:blood / Q000517:prevention & control*; D016207:Cytokines / Q000096:biosynthesis / Q000097:blood; D005260:Female; D005342:Fibrinolysis / Q000187:drug effects*; D005434:Flow Cytometry; D006801:Humans; D019041:L-Selectin / Q000096:biosynthesis / Q000097:blood; D007958:Leukocyte Count; D018950:Lipopolysaccharide Receptors / Q000096:biosynthesis / Q000097:blood; D017270:Lipoprotein(a) / Q000097:blood; D008875:Middle Aged; D009000:Monocytes / Q000187:drug effects* / Q000276:immunology / Q000378:metabolism; D017698:Postmenopause / Q000097:blood / Q000187:drug effects*; D020849:Raloxifene Hydrochloride / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D020845:Selective Estrogen Receptor Modulators / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D008076:Cholesterol, HDL; D016207:Cytokines; D018950:Lipopolysaccharide Receptors; D017270:Lipoprotein(a); D020845:Selective Estrogen Receptor Modulators; D019041:L-Selectin; D020849:Raloxifene Hydrochloride; D002784:Cholesterol