Chronic feeding of guggulsterone to rats showed hypolipidaemic activity in blood serum and liver membrane lipids. The decrease in serum cholesterol is associated with enhanced uptake of LDL by the liver through receptor mediated endocytosis, located on the surface of the cell membrane. In the present communication it has been shown that membranes prepared from liver of guggulsterone treated rats exhibit up to 87% increase in binding sites for human 125I-LDL. Significant decrease in lipid levels of serum as well as of membrane were observed. Lipid lowering activity of the drug in relation to LDL catabolism and other possible mechanisms have been explained.