Cholesterol oxidation products (COP), also called oxysterols, enter th
e organism by intake of COP-containing foodstuff or are generated in v
ivo by enzymatic or non-enzymatic oxidation (peroxidation) of choleste
rol. COP are transported in lymph and blood with lipoproteins (mainly
fatty acyl monoesters at the 3 beta-position) or bound to albumin. As
being substrates for acyl CoA:choresterol acyltransferase (ACAT), leci
thin:cholesterol acyltransferase (LCAT), and cholesteryl ester transfe
r protein (CETP), COP are esterified and exchanged between lipoprotein
s and are distributed in the whole organism. Kupffer cells and hepatoc
ytes are the target cells for COP transformation and excretion via bil
e secretion. Regarding biological activities, COP reveal widespread ef
fects on cholesterol metabolism as well as on structure and function o
f cellular membranes. Throughout their actions, COP were shown to be c
ytotoxic but they were also suggested to be regulatory agents. Their d
etrimental part in atherogenesis seems to be still underestimated, whi
le valid data on the role of COP in carcinogenesis are still missing.