Probucol is a hypolipidemic agent with a unique pharm ac odynamic and clinical profile. It has a significant antiatherosclerogenic role a lthough it causes a marked decrease in serum high-density lipoprotein (HDL)-ch olesterol levels. The metabolism of HDL in vivois unclear. Some preliminary investigations suggest a beneficial effect in enhancing reverse cholesterol tra nsport which contributes to antiatherosclerosis of probucol. This paper reviews the mechanism of HDL-lowering effects of probucol.

Aim To investigate the effect of probucol on reverse cholesterol transport from macrophage to feces in vivo,serum lipid profiles of mice were tested before and after probucol administration for 4 weeks,and the 3H-contents in serum,liver and feces in mice were quantitated after 24 hours intraperitoneally injected macrophages which were labeled with 3H cholesterol.Methods 32 C57BL/6 mice were treated with different probucol(0,0.1%,0.5%,1% W/W)in chow diet for 4 weeks,then these mice were injected intraperitoneally with RAW264.7 macrophages(0.5 ml?mice,cells 5.0?106 with 6.2?106 cpm)which were loaded with cholesterol by incubation with acetylated LDL,labeled with 3H-cholesterol.Serum profiles were quantitated by enzymatic method;serum and liver tissues were harvested at 24th hour,feces were collected(0~24 hs),and all were analyzed for tracer counts(all were expressed as the percentage of the total injected counts per minute).Results After 4 weeks 0.1% probucol administration,the levels of total cholesterol(TC),high-density lipoprotein cholesterol(HDL-C)decreased markedly by 34.3%,52.8%,(P