Antiatherogenic activity of cetaben sodium, sodium p-(hexadecylamino) benzoate, in the aortae of hypercholesteremic rabbits subjected to aortic endothelial cell desquamation.

The effects of sodium p-(hexadecylamino)benzoate [cetaben sodium] on plasma sterol concentrations, aortic sterol deposition and the incidence of atherosclerotic lesions in cholesterol-fed rabbits subjected to aortic deendothelialization with a balloon catheter have been studied. At a dose of 113 mg/kg/day, cetaben sodium decreased plasma cholesterol and the accumulation of aortic sterol and appeared to decrease the incidence of gross atherosclerotic lesions. At a dose of 27 mg/kg/day, no hypocholesteremic activity was observed, but cetaben sodium decreased both aortic sterol deposition and lesion development in the abdominal segment of the aorta. The decreases in total aortic sterol content observed in the drug-treated rabbits were shown to have resulted from a reduction in esterified rather than free sterol. When tested in vitro, cetaben sodium effectively inhibited (KI = 7.4 x 10(-5) M) the esterification of cholesterol catalyzed by a crude preparation of fatty acyl CoA:cholesterol acyl transferase isolated from cholesterol-fed rabbit aortae. These observations suggest that cetaben sodium possesses antiatherosclerotic activity and that this activity may result from direct actions on the aortic wall, in addition to vascular effects secondary to hypocholesteremic activity.