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Physicochemical properties of bile acids and their relationship to biological properties: an overview of the problem.
TLDR
The structure of the bile acid molecule is described and correlated with physiochemical properties of bile acids such as solubility, ionization, and micelle formation, and recent measurements of the critical micellar concentration indicate that the CMC is influenced by both side chain and nuclear structure. Expand
Bile acid structure-activity relationship: evaluation of bile acid lipophilicity using 1-octanol/water partition coefficient and reverse phase HPLC.
TLDR
The experimental data show that both the protonated (HA) and ionized (A-) forms of BA can distribute in 1-octanol, and consequently a partition coefficient for HA (logP' HA) and for A- ( logP' A-) must be defined. Expand
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.
TLDR
Lead optimization efforts that have led to the discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a novel potent and selective TGR5 agonist with remarkable in vivo activity are reported. Expand
The influence of bile salt structure on self-association in aqueous solutions.
TLDR
The results indicate that the concentration at which bile salt aggregation occurs varies widely and is determined not only by the number, type, and orientation of nuclear substituents, but also by side chain structure. Expand
Tear proteomics in evaporative dry eye disease
TLDR
Analysis of tear protein variations in patients suffering from dry eye symptoms in the presence of tear film instability but without epithelial defects shows that tear protein changes anticipate the onset of more extensive clinical signs in early stage dry eye disease. Expand
Berberine and its metabolites: relationship between physicochemical properties and plasma levels after administration to human subjects.
TLDR
Results indicate that the higher plasma concentration of 2 was a consequence of a more efficient intestinal absorption, suggesting that berberrubine is potentially more pharmacologically active than berberine. Expand
Enzymatic determination of cholesterol in bile.
TLDR
The results obtained with this method are compared with those obtained by the standard Liebermann-Burchard reaction on the same samples and are found to be in close agreement. Expand
Brain Glucose Sensors Play a Significant Role in the Regulation of Pancreatic Glucose-Stimulated Insulin Secretion
TLDR
A role for brain glucose sensors in the regulation of GSIS is suggested, particularly during the early phase, and pharmacological agents targeting hypothalamic glucose-sensing pathways may represent novel therapeutic strategies for enhancing early phase insulin secretion in type 2 diabetes. Expand
Effect of simvastatin, ursodeoxycholic acid and simvastatin plus ursodeoxycholic acid on biliary lipid secretion and cholic acid kinetics in nonfamilial hypercholesterolemia
TLDR
To determine the mechanism by which simvastatin decreases the biliary cholesterol saturation index, hepatic secretion rates of cholesterol, bile acids and phospholipids, and cholic acid pool size, turnover and synthesis in eight hyperlipidemic patients are evaluated. Expand
Bioavailability study of a new, sinking, enteric-coated ursodeoxycholic acid formulation.
TLDR
A new enteric-coated ursodeoxycholic acid (UDCA) formulation which sinks in the stomach and releases the drug only at a pH > or = 6.5 was developed, and the maximum UDCA serum concentration was significantly higher with the enteric coated sinking UDCA formulation when compared to the other two formulations. Expand
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