In vitro study of the effect of raloxifene on lipid metabolism compared with tamoxifen.
OBJECTIVE
Tamoxifen and raloxifene, selective estrogen receptor modulators, decrease serum concentrations of total cholesterol; however, the effect of these drugs on triglyceride metabolism is unclear. In the present study, we investigated the in vitro effect of raloxifene on lipid metabolism and compared it with that of tamoxifen.


METHODS
Intracellular concentrations of total cholesterol and triglyceride in HepG2 cells were measured by an enzymatic method after tamoxifen or raloxifene treatment with or without oleic acid and with or without very low density lipoprotein.


RESULTS
Intracellular concentrations of total cholesterol and triglyceride without oleic acid or very low density lipoprotein were not significantly different after treatment with tamoxifen or raloxifene. In contrast, although raloxifene with oleic acid did not increase the intracellular concentrations of triglyceride, tamoxifen treatment in the presence of oleic acid or very low density lipoprotein significantly increased (P<0.05) the triglyceride concentrations.


CONCLUSIONS
The present study suggests that raloxifene does not increase intracellular triglyceride in the presence of oleic acid or very low density lipoprotein, in contrast to tamoxifen. Therefore, raloxifene might be safer than tamoxifen for treating patients with unstable triglyceride levels or a history of hypertriglyceridemia.
Hozumi
Y
Y
Robert H Lurie Comprehensive Cancer Center, Northwestern University Medical School, 303 E Chicago Avenue, Olson Pavilion 8258, Chicago, Illinois 60611, USA. y-hozumi@jichi.ac.jp
Kawano
M
M
Jordan
V C
VC
D018931:Antineoplastic Agents, Hormonal / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular; D002784:Cholesterol / Q000097:blood; D006801:Humans; D050356:Lipid Metabolism; D008079:Lipoproteins, VLDL / Q000097:blood; D020849:Raloxifene Hydrochloride / Q000494:pharmacology*; D013629:Tamoxifen / Q000494:pharmacology*; D014280:Triglycerides / Q000097:blood; D014407:Tumor Cells, Cultured
D018931:Antineoplastic Agents, Hormonal; D008079:Lipoproteins, VLDL; D014280:Triglycerides; D013629:Tamoxifen; D020849:Raloxifene Hydrochloride; D002784:Cholesterol