Literature DB >> 22358683

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

A Corsini1, P Grignaffini, J Beitz, H Mest, S Bellosta, R Fumagalli, R Paoletti.   

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 of(125)I-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.

Entities:  

Year:  1993        PMID： 22358683     DOI： 10.1007/BF00746043

Source DB:  PubMed          Journal:  Cytotechnology        ISSN： 0920-9069            Impact factor:   2.058


  6 in total

1.  The trapidil derivative AR 12456 protects against serum hyperlipidemia in guinea pigs.

Authors:  J Beitz; A Riedel; A Beitz; C Giessler; A Kittel; H J Mest
Journal:  J Lipid Mediat       Date:  1991 Mar-Apr

2.  Binding and degradation of human high-density lipoproteins by human hepatoma cell line HepG2.

Authors:  N Dashti; G Wolfbauer; P Alaupovic
Journal:  Biochim Biophys Acta       Date:  1985-01-09

Review 3.  A receptor-mediated pathway for cholesterol homeostasis.

Authors:  M S Brown; J L Goldstein
Journal:  Science       Date:  1986-04-04       Impact factor: 47.728

4.  Consensus conference. Lowering blood cholesterol to prevent heart disease.

Authors: 
Journal:  JAMA       Date:  1985-04-12       Impact factor: 56.272

5.  Trapidil derivatives as potential antiatherosclerotic drugs.

Authors:  C Giessler; A Fahr; V V Tertov; S A Kudryashov; A N Orekhov; V N Smirnov; H J Mest
Journal:  Arzneimittelforschung       Date:  1987-05

6.  Trapidil derivatives and low density lipoprotein metabolism by human skin fibroblasts and by human hepatoma cell line Hep G2.

Authors:  A Corsini; J Beitz; A Granata; R Fumagalli; H J Mest; R Paoletti
Journal:  Pharmacol Res       Date:  1989 Sep-Oct       Impact factor: 7.658
  6 in total

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