scholarly journals Structural modifications that increase gut restriction of bile acid derivatives

2021 ◽  
Author(s):  
Ali Nakhi ◽  
Henry L. Wong ◽  
Melissa Weldy ◽  
Alexander Khoruts ◽  
Michael J. Sadowsky ◽  
...  
Keyword(s):  
Bile Acid ◽  
Bile Acids ◽  
Structural Modifications ◽  
Bile Acid Derivatives

Modifications can be made to bile acids that decrease their absorption from the gut by active and passive mechanisms.

scholarly journals Microwave-assisted green synthesis of bile acid derivatives and evaluation of glucocorticoid receptor binding

2020 ◽  
Author(s):  
Bojana R. Vasiljević ◽  
Edward T. Petri ◽  
Sofija S. Bekić ◽  
Andjelka S. Ćelić ◽  
Ljubica M. Grbović ◽  
...  
Keyword(s):  
Bile Acid ◽  
Microwave Irradiation ◽  
Glucocorticoid Receptor ◽  
Ligand Binding ◽  
Green Synthesis ◽  
Bile Acids ◽  
Receptor Binding ◽  
Microwave Assisted ◽  
Bile Acid Derivatives ◽  
Cholanic Acid

Green synthesis of bile acids derivatives and 5β-cholanic acid was achieved under microwave irradiation, and the binding affinity for the ligand binding domain of the glucocorticoid receptor was measured.

Interaction between bile acids and staphylococcal polysaccharide: inhibition of capsule formation in encapsulated mutant strains (taurine+, taurine−) of Staphylococcus aureus

1983 ◽  
Vol 29 (12) ◽  
pp. 1653-1660 ◽  
Author(s):  
Toshichika Ohtomo
Keyword(s):  
Staphylococcus Aureus ◽  
Bile Acid ◽  
Bile Acids ◽  
Cholic Acid ◽  
Taurocholic Acid ◽  
Polysaccharide Antigen ◽  
Capsule Formation ◽  
Mutant Strains ◽  
Bile Acid Derivatives ◽  
Capsular Material

In a previous paper, we showed that bile acid derivatives inhibit capsule formation as well as taurine biosynthesis in a taurine+ (Tau+) encapsulated strain of Staphylococcus aureus. In the present study, binding of [14C]cholic acid ([14C]CA) and [14C]taurocholic acid ([14C]TA) to the staphylococcal polysaccharide antigen (SPA) of the capsular fraction was examined. The bile acids were found to bind with SPA via taurine of the Tau+ cells. [14C]CA bound with the SPA fraction of the Tau+ strain within 10–30 min, whereas 60–120 min was required in the binding of [14C]TA. Various bile acids competed with cholic acid binding to Tau+ cells which was shown by the inhibition of binding with cholic acid or taurocholic acid but not with glycholic acid. Binding of bile acid derivatives to a Tau− encapsulated mutant or to capsular material from this mutant was not observed.

Precipitation and 13C-NMR relaxation enhancement measurements of the interactions of bile acids with synthetic cationic bile acid derivatives, and with spin labelled fatty acids

1991 ◽  
Vol 60 (2) ◽  
pp. 143-151 ◽  
Author(s):  
David G. Reid ◽  
Kaushika Gajjar ◽  
Simon P. Robinson ◽  
Deirdre M.B. Hickey ◽  
G.Martin Benson ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Bile Acid ◽  
Bile Acids ◽  
13C Nmr ◽  
Nmr Relaxation ◽  
Bile Acid Derivatives

Influence of side-chain charge on hepatic transport of bile acids and bile acid analogues

1985 ◽  
Vol 249 (4) ◽  
pp. G479-G488 ◽  
Author(s):  
M. S. Anwer ◽  
E. R. O'Maille ◽  
A. F. Hofmann ◽  
R. A. DiPietro ◽  
E. Michelotti
Keyword(s):  
Bile Acid ◽  
Bile Acids ◽  
Liver Cell ◽  
Hepatic Uptake ◽  
Biliary Secretion ◽  
Side Chain ◽  
Bile Fistula ◽  
Bile Acid Derivatives ◽  
Derivatives Of ◽  
Secretion Rates

The importance of side-chain charge on hepatic uptake and biliary secretion of bile acids and analogues was studied using the isolated, perfused rat liver and the anesthetized rat with a bile fistula. Derivatives of cholic acid with negative, neutral, zwitterionic, or positive charges on the side chain were synthesized and studied. Hepatic uptake by the isolated perfused liver, determined by measuring the rate of disappearance of a single 20-mumol bolus added to the perfusate, was strongly influenced by side-chain charge. A fully positively charged bile acid derivative (cholylcholamine) and two fully zwitterionic bile acid derivatives (CHAPS and cholyllysine) showed no appreciable uptake (less than 1% of the uptake rate of cholyltaurine). Bile acid derivatives existing mostly in cationic form (cholylamine) at pH 7.4, in neutral form (cholylglycylhistamine), or in divalent anion form (cholylaspartate and cholylcysteate) had an uptake rate that was greater but only 7-19% that of cholyltaurine. Side-chain charge also appeared to influence the rate of secretion into bile. Bile acids existing in mono- or dianionic form were well secreted (greater than 95% of dose in 2 h) into the bile, but all other derivatives had much lower secretion rates (less than 20% of dose in 2 h). When the biliary secretion of each bile acid derivative was expressed in relation to the amount that had entered the liver, relative secretion rates (presumably from liver cell) into bile decreased in the following order: cholyltaurine greater than cholylaspartate and cholylcysteate greater than CHAPS greater than cholyllysine greater than cholylglycylhistamine approximately equal to cholylamine. In bile fistula rats, cholylaspartate was quantitatively secreted into bile when infused at rates below its secretory maximum, whereas only very low biliary secretion rates of CHAPS were observed even during relatively high infusion rates; cholylamine was cholestatic. The above data show that, although uncharged and anionic derivatives of cholic acid may be taken up by the liver at a moderate rate, only anionic derivatives (both monovalent and divalent) are well secreted from within the liver cell into bile. A single negative charge on the side chain appears to be required for optimal transport of a bile acid from sinusoidal blood to bile.

Bile acids and bile acid derivatives: use in drug delivery systems and as therapeutic agents

2016 ◽  
Vol 13 (8) ◽  
pp. 1133-1148 ◽  
Author(s):  
Célia Faustino ◽  
Cláudia Serafim ◽  
Patrícia Rijo ◽  
Catarina Pinto Reis
Keyword(s):  
Drug Delivery ◽  
Bile Acid ◽  
Bile Acids ◽  
Drug Delivery Systems ◽  
Therapeutic Agents ◽  
Delivery Systems ◽  
Bile Acid Derivatives

Pharmacological effects of secondary bile acid microparticles in diabetic murine model

2020 ◽  
Vol 16 ◽  
Author(s):  
Armin Mooranian ◽  
Nassim Zamani ◽  
Bozica Kovacevic ◽  
Corina Mihaela Ionescu ◽  
Giuseppe Luna ◽  
...  
Keyword(s):  
Bile Acid ◽  
Blood Glucose ◽  
Bile Acids ◽  
Lithocholic Acid ◽  
Diabetes Treatment ◽  
Secondary Bile Acid ◽  
Glucose Levels ◽  
Anti Inflammatory ◽  
Antidiabetic Effects

Aim: Examine bile acids effects in Type 2 diabetes. Background: In recent studies, the bile acid ursodeoxycholic acid (UDCA) has shown potent anti-inflammatory effects in obese patients while in type 2 diabetics (T2D) levels of the pro-inflammatory bile acid lithocholic acid were increased, and levels of the anti-inflammatory bile acid chenodeoxycholic acid were decreased, in plasma. Objective: Hence, this study aimed to examine applications of novel UDCA nanoparticles in diabetes. Methods: Diabetic balb/c adult mice were divided into three equal groups and gavaged daily with either empty microcapsules, free UDCA, or microencapsulated UDCA over two weeks. Their blood, tissues, urine, and faeces were collected for blood glucose, inflammation, and bile acid analyses. UDCA resulted in modulatory effects on bile acids profile without antidiabetic effects suggesting that bile acid modulation was not directly linked to diabetes treatment. Results: UDCA resulted in modulatory effects on bile acids profile without antidiabetic effects suggesting that bile acid modulation was not directly linked to diabetes treatment. Conclusion: Bile acids modulated the bile profile without affecting blood glucose levels.

Sign in / Sign up

Export Citation Format

Share Document