Bile is produced by the liver and stored in the gallbladder during fasting. With eating, bile is
discharged into the small intestine. As a digestive secretion, bile acts as a detergent by forming mixed
micelles with lipid nutrients, thereby enhancing their absorption. As an excretory secretion, it delivers
lipid waste products to the intestine from which they are poorly absorbed. The main component of bile
is conjugated bile acids, which are amphipathic steroids formed in the liver as the end-products of
cholesterol metabolism. Bile acids are recycled between liver and small intestine (i.e. the enterohepatic
circulation) with low plasma concentrations. In addition to providing the detergent property of bile and
being a major driving force of bile flow, bile acids are signalling molecules that carry signals from the
intestine to the liver. Homeostasis of bile acid synthesis and ileal conservation is essential not only to
achieve the physiological functions of bile acids, but also to avoid pathological effects caused by their
amphipathic property. Bile acid retention in the hepatocyte due to bile duct disease (e.g. PBC, PSC)
leads to cell death. In terms of functional molecular imaging, dynamic planar cholescintigraphy is
currently the modality of choice for the evaluation of the biliary system often with Tc-99m-mebrofenin
as the radiotracer. Hepatic bile acid synthesis and handling, as well as intestinal malabsorption of bile
acids, have been assessed by dynamic planar cholescintigraphy using the labelled bile acid analogue
75SeHCAT. Positron emission tomography (PET) using radiolabelled bile acid analogues has, to date,
only been applied in preliminary studies regarding biliary secretion.
Keywords: Bile; Bile acids; Micelles; Metabolism; Enterohepatic circulation; Transporter proteins;
Hepatobiliary disease; Scintigraphy; 99mTc-HIDA agents; 75SeHCAT; PET.