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Effects of phenothiazines on low density lipoprotein metabolism in cultured human fibroblasts
Author(s) -
Maziere J.C.,
Maziere C.,
Gardette J.,
Routier J.D.,
Wolf C.,
Rainteau D.,
Polonovski J.
Publication year - 1983
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(83)80794-7
Subject(s) - trifluoperazine , internalization , catabolism , incubation , chemistry , metabolism , low density lipoprotein , lipoprotein , chlorpromazine , calmodulin , biochemistry , cell , endocrinology , cholesterol , biology , enzyme
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.