Probucol enhances cholesterol transport in cultured rat hepatocytes

Probucol has been investigated extensively in vivo and ex vivo. However, little information is available on direct treatment of cultured cells. Treatment of cultured hepatocytes by 1 to 10 μ M probucol for 16 to 20 hours had no apparent deleterious effect on the cell, and in fact decreased lactic dehydrogenase leakage. Also, total cellular cholesterol was increased, cholesterol synthesis was decreased, and cholesterol esterification was increased. The increase in cellular cholesterol was not the result of increased lipoprotein uptake but appeared to be the result of an interaction between cell and lipoprotein in which the cell became enriched and the lipoprotein depleted in cholesterol. This type of change in lipoprotein composition after treatment is also observed clinically.