This study was conducted to compare the hypocholesterolemic and antioxidant effects of naringenin (0.02%), and its metabolites, rho-hyproxyphenylpropionic acid (PHPP, 0.012%) and rho-hydroxybenzoic acid (PHB, 0.012%), in 1% cholesterol diet-fed rats. All supplements significantly lowered the plasma total-cholesterol (total-C), triglyceride (TG) and atherogenic index, and hepatic cholesterol levels compared with the control group. The plasma high-density lipoprotein-cholesterol (HDL-C) concentration was significantly higher in these supplemented groups. However, PHB group only affected the reduction of hepatic TG content. The hydroxyl-3-methylglutaryl-coenzyme A reductase (HMGR) activity was significantly lower in all supplemented groups, whereas only the naringenin group reduced the acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity compared with the control group. The fecal acidic sterol excretion and hepatic superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities were significantly higher in all supplemented groups. All supplements also significantly decreased the contents of plasma and hepatic thiobarbituric acid reactive substances (TBARS). Accordingly, it was considered that naringenin and its metabolites were effective on improving the cholesterol and antioxidant metabolism.