It has been proposed that the hepatocellular Na+-dependent bile salt uptake system exhibits a broad substrate specificity in intact hepatocytes. In contrast, recent expression studies in mammalian cell lines have suggested that the cloned rat liver Na+-taurocholate cotransporting polypeptide (Ntcp) may transport only taurocholate. To characterize its substrate specificity Ntcp was stably transf...

BACKGROUND The clinical application of nimodipine (NIM) is limited by several unfavorable properties, which are induced by its low aqueous solubility. In the present study, nimodipine-loaded egg phosphatidylcholine-sodium glycocholate mixed micelles (NIM-EPC-SGC-MMs) were prepared to improve the water solubility of NIM, thus allowing it to be more applicable for clinical use. METHODS NIM-EPC-...

The neuromuscular blocking effects of Org 6368 and Org NC 45 were studied in rats with experimental cholestasis and in controls. The effect of Org NC 45 during infusion of taurocholate was investigated. In cholestatic rats we observed a three-fold increase of the duration of action of Org 6368 and Org NC 45. The same was observed for Org NC 45 with taurocholate. In the rat phrenic nerve-hemidia...

Cholestyramine is the most widely used bile acid sequestrant in the treatment of hypercholesterolemia. However, cholestyramine has unpleasant side effects as a consequence of its hydrophobic backbone. Therefore, high-capacity bile acid sequestering biopolymers with cationic chitosan derivatives were developed, because electrostatic interactions are important for binding with bile acid anions. D...

In a recent communication by Arthur Edmunds, t it is stated that the fall of blood pressure produced by intravenous injection of bile salts is insignificant. The statement is supported by the reproduction of tracings obtained from such experiments. The one obtained after an injection of 5 cubic centimeters of a i per cent. solution of sodium glycocholate shows hardly any depression. The depress...

In a previous study from our laboratory (Drug Metab Dispos 34: 660-666, 2006), we found several limitations with published methods (cholate gel filtration and cholate dialysis) for the incorporation of cytochromes P450 and P450 reductase into phospholipid vesicles. We found that a significant proportion of reductase was not incorporated in the vesicles when the amount of reductase was equal to ...

The presence of a cholesterol esterase in blood serum was demonstrated by the finding (1) that a marked esterification of free cholesterol occurs on incubation of untreated serum, but does not occur on incubation of serum which has previously been heated for 1 hour at 55-60’.1’ In studying this reaction further it was of interest to ascertain the effect of bile salts, first, because it is known...

Barrett's oesophagus is an acquired precancerous condition that develops from mucosal injury incurred due to chronic gastro-oesophageal reflux. The aim of this study was to determine if bile and/or acid components of the refluxate can induce DNA damage in vitro. The oesophageal cell lines FLO-1 and HET1-A were exposed to primary bile salts, individually or as a mixture, and the secondary bile s...

Bile salts are predominantly taken up by hepatocytes via the basolateral Na(+)-taurocholate cotransporting polypeptide (NTCP/SLC10A1) and secreted into the bile by the bile salt export pump (BSEP/ABCB11). In the present study, we transfected rat Ntcp and rat Bsep into polarized Madin-Darby canine kidney cells and characterized the transport properties of these cells for eight bile salts. Immuno...

Enterotoxigenic Escherichia coli (ETEC) is an important cause of acute watery diarrhoea in developing countries. Colonization factors (CFs) on the bacterial surface mediate adhesion to the small intestinal epithelium. Two of the most common CFs worldwide are coli surface antigens 5 and 6 (CS5, CS6). In this study we investigated the expression of CS5 and CS6 in vivo, and the effects of bile and...