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Human foetal lung fibroblasts were pretreated for 24 h with the antithrombotic drug, suloctidil (1 to 10 mumol/l), which induced a dose-dependent increase in LDL binding, uptake and degradation. At 10 mumol/l suloctidil, the respective increases in these parameters were 40%, 80% and 50%. The same treatment also resulted in increases of 1.5 to 2-fold in the synthesis of sterols, fatty acids and triacylglycerols from sodium acetate. In contrast, the esterification of cholesterol with oleic acid was specifically decreased by 35% by 24 h pretreatment of fibroblasts with 10 mumol/l suloctidil. A similar decrease of cholesterol esterification was observed in cholesterol-laden fibroblasts. It is suggested that these effects of suloctidil on LDL processing and cholesterol metabolism are related to the amphiphilic characteristics of the drug and to its calcium-blocking properties.

Effects of the Antithrombotic Drug Suloctidil on Low Density Lipoprotein Processing and Cholesterol Metabolism in Cultured Human Fibroblasts