A. Corsini et al., EFFECT OF TRAPIDIL DERIVATIVE AR-12456 ON INTRACELLULAR CHOLESTEROL HOMEOSTASIS IN HUMAN HEPATOMA-CELL LINE HEP-G2, Cytotechnology, 11, 1993, pp. 15-17
The effect of trapidil derivative AR12456 on intracellular cholesterol
metabolism was investigated in human hepatoma cell line HepG2. AR1245
6 enhanced the uptake and degradation of I-125-LDL in a dose-dependent
manner. The drug inhibited cholesterol synthesis and esterification w
ithout affecting cellular cholesterol content and bile acid synthesis;
cholesterol efflux was slightly increased. These results show that th
e inhibition of cholesterol synthesis together with the enhanced expre
ssion of LDL receptors may partially explain the hypocholesterolemic a
ctivity of compound AR12456.