Effects of phenothiazines on low density lipoprotein metabolism in cultured human fibroblasts.

J. C. Maziere , C. Maziere , J. Gardette , J. D. Routier , C. Wolf (1) , D. Rainteau (1) , J. Polonovski

1 UPMC - Université Pierre et Marie Curie - Paris 6

Treatment of cultured human fibroblasts with trifluoperazine or chlorpromazine resulted in a biphasic effect on low density lipoprotein (LDL) catabolism, depending upon the dose. At up to 10(-5) M, a marked increase in LDL binding, internalization and degradation was observed. This phenomenon took place within the first hours of incubation with the drugs, suggesting a direct effect on cell membrane physical characteristics, probably related to the lipophilic properties of phenothiazines. Concentrations above 2 X 10(-5) M resulted in a relative decrease in LDL binding and internalization, and in a dramatic decrease in LDL degradation, which may be related to an inhibition of calmodulin-dependent processes.

Domaines: Chimie organique

J. C. Maziere, C. Maziere, J. Gardette, J. D. Routier, C. Wolf, et al.. Effects of phenothiazines on low density lipoprotein metabolism in cultured human fibroblasts.. FEBS Letters, 1983, 162 ((2)), pp.396-9. ⟨hal-00813726⟩