A close structure-activity relationship exists between the transport o
f bile acids (BA) in the liver and intestine; hepatic and intestinal B
A transport can be evaluated and compared by using perfused liver and
perfused intestine in the rabbit, The passive intestinal absorption is
limited to the unconjugated BA, which occurs throughout the small bow
el and colon, and is conditioned by the apical membrane lipid composit
ion, A higher diffusion component is found in the terminal ileum compa
red to the jejunum, and seems to be related to the higher cholesterol-
to-phospholipid ratio of the ileal brush border membranes, The active
transport system is well characterized and the brush border membrane r
eceptor, cytosolic BA binding proteins and basolateral anion exchange
protein have been identified, Recently, the ileal BA transporter has b
een cloned from the hamster and human ileum and the main cytosolic BA
binding protein was cloned from the rat ileum, In the liver, the activ
e transport predominates on the passive diffusion both for conjugated
and unconjugated BA, The maximal transport capacity in the liver is te
nfold higher than in the intestine, while the Km values are of the sam
e order of magnitude, i.e. in the millimolar range, Neither system ope
rates at its maximum transport rate with prevalent concentrations of B
A in portal blood or luminal content.