Effects of bezafibrate on biosynthesis of cholesterol and on degradation of native and acetylated low-density lipoproteins in incubated human monocytes.
The effects of bezafibrate on 14C-acetate incorporation into non-saponifiable lipids and on degradation of native and acetylated [125I] low-density lipoproteins (LDL) in cultured human monocytes has been evaluated. The presence of bezafibrate in the incubation medium resulted in a decrease of labelled acetate incorporation into non-saponifiable lipids. In parallel with the decrease in sterol synthesis, bezafibrate produced an increase in total and specific degradation of native low-density lipoproteins, whereas the degradation of acetylated low-density lipoproteins was not affected by the drug. These data, though obtained with concentrations of bezafibrate in the incubation medium greater than those encountered in ordinary therapeutic conditions, support the hypothesis that bezafibrate inhibits cholesterol biosynthesis and increases removal of low-density lipoproteins by activating the specific receptor pathway.
Cosentini
R
R
Institute of Internal Medicine and Medical Physiopathology, University of Milan, Italy.
Blasi
F
F
Sommariva
D
D
Tosi
C
C
Fasoli
A
A
D001629:Bezafibrate / Q000494:pharmacology*; D002478:Cells, Cultured; D002784:Cholesterol / Q000096:biosynthesis*; D006801:Humans; D008077:Lipoproteins, LDL / Q000378:metabolism*; D009000:Monocytes / Q000187:drug effects* / Q000378:metabolism
D008077:Lipoproteins, LDL; D002784:Cholesterol; D001629:Bezafibrate