Cholesterol is always an issue because blood total cholesterol (TC) and low-density lipoprotein (LDL) correlate strongly with coronary heart disease. Cholesterol homeostasis is maintained by a complex mechanism of sterol absorption, anabolism, catabolism and excretion. Nutraceuticals and functional foods which lower TC must affect the genes which regulate cholesterol homeostasis. In general, cholesterol-lowering functional foods and nutraceuticals can be classified into seven types namely intestinal Niemann-Pick Cl like 1 (NPC1L1) competitors, intestinal acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors, 3-hydroxy-3-methylglutaryl (HMG-CoA) reductase inhibitors, LDL receptor up-regulators, bile acid reabsorption inhibitors, cholesterol-7 alpha-hydroxylase (CYP7A1) activators, and plasma cholesteryl ester transporting protein (CETP) inhibitors. This mini-review classifies the popular cholesterol-lowering nutraceuticals and functional foods, and explores their underlying mechanisms. (C) 2011 Elsevier Ltd. All rights reserved.