Effect of trapidil derivative AR 12456 on intracellular cholesterol homeostasis in human hepatoma cell line Hep G2

A. Corsini, P. Grignaffini, J. Beitz, H. J. Mest, S. Bellosta, R. Fumagalli, R. Paoletti

Research output: Contribution to journalArticlepeer-review

Abstract

The effect of trapidil derivative AR12456 on intracellular cholesterol metabolism was investigated in human hepatoma cell line HepG2. AR12456 enhanced the uptake and degradation of125I-LDL in a dose-dependent manner. The drug inhibited cholesterol synthesis and esterification without affecting cellular cholesterol content and bile acid synthesis; cholesterol efflux was slightly increased. These results show that the inhibition of cholesterol synthesis together with the enhanced expression of LDL receptors may partially explain the hypocholesterolemic activity of compound AR12456.

Original languageEnglish
JournalCytotechnology
Volume11
Issue number1 Supplement
DOIs
Publication statusPublished - Jan 1993

ASJC Scopus subject areas

  • Clinical Biochemistry
  • Cell Biology
  • Biotechnology

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