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

FEBS Letters

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

[1] Service de Biochimie, C.H.U. Saint-Antoine et ERA 481 du CNRS, 27 rue Chaligny, 75012, Paris, France

关键词: Trifluoperazine;    Chlorpromazine;    Low density lipoprotein catabolism;    Human fibroblast;   

DOI  :  10.1016/0014-5793(83)80794-7

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 × 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.

【 授权许可】

Unknown