Guggulsterone: an old approach to a new problem

The hepatic conversion of cholesterol to bile acids is an important mechanism for the elimination of excess dietary cholesterol. Bile acid biosynthesis and transport are regulated by the farnesoid X receptor (FXR), a member of the of nuclear hormone receptor gene superfamily. Thus, therapeutic strategies that target FXR represent a promising new approach for the treatment of hypercholesterolemia. Recent studies have provided new evidence in support of the potential for FXR ligands as antihypercholesterolemic agents.