Lipophilic beta-adrenoceptor antagonists stimulate low density lipoprotein receptor activity in human skin fibroblasts

F. Bernini, A. Corsini, R. Musanti, Remo Fumagalli

Research output: Contribution to journalArticlepeer-review

Abstract

The effect of (β-adrenoccptor antagonists on the rcccptor-mediated low density lipoprotein (LDL) binding and internalization w'as studied in vitro in human skin fibro-blasts. The cellular uptake of l25I-labeIcd human LDL was dose depcndcntly elevated by some, but not all, of the drugs used. This effect of (β-adrenoccptor antagonists was positively related to their lipophilicity, and was prevented by cycloheximide and by α-amanitin.Scatchard analysis of the saturable LDL binding indicates an increased number of LDL binding sites. Our studies show that the stimulating effect of (β-adrenoccptor antagonists on the high affinity LDL binding and internalization in human skin fibroblasts involves DNA transcription and new protein synthesis, and identify drug lipophilicity as a major determi-nant of this action. This effect could be relevant in vivo in adipose tissue which accumulates lipophilic drugs and derives its cholesterol mainly from circulating LDL.

Original languageEnglish
Pages (from-to)225-232
Number of pages8
JournalPharmacology
Volume34
Issue number4
DOIs
Publication statusPublished - 1987

Keywords

  • Human fibroblasts
  • Low density lipoprotein receptor
  • Low density lipoproteins
  • β-Adrenoceptor antagonists

ASJC Scopus subject areas

  • Pharmacology

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