Polymeric bile acid sequestrants: Review of design, in vitro binding activities, and hypocholesterolemic effects
| Autor: | Eva Heřmánková, A. Žák, Jakub Sirc, Radka Hobzova, Róbert Hromádka, Lenka Poláková |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
medicine.drug_class
Polymers education Hypercholesterolemia 02 engineering and technology 010402 general chemistry 01 natural sciences Bile Acids and Salts chemistry.chemical_compound Bile acid sequestrant Drug Discovery medicine Animals Humans Enterohepatic circulation Pharmacology chemistry.chemical_classification Cholestyramine Binding Sites Bile acid Cyclodextrin Molecular Structure Chemistry Anticholesteremic Agents Organic Chemistry General Medicine Meth 021001 nanoscience & nanotechnology Combinatorial chemistry 0104 chemical sciences Sequestrant Drug Design 0210 nano-technology Molecular imprinting medicine.drug |
| Zdroj: | European journal of medicinal chemistry. 144 |
| ISSN: | 1768-3254 |
| Popis: | Polymeric bile acid sequestrants (BAS) have recently attracted much attention as lipid-lowering agents. These non-absorbable materials specifically bind bile acids (BAs) in the intestine, preventing bile acid (BA) reabsorption into the blood through enterohepatic circulation. Therefore, it is important to understand the structure-property relationships between the polymer sequestrant and its ability to bind specific BAs molecules. In this review, we describe pleiotropic effects of bile acids, and we focus on BAS with various molecular architectures that result in different mechanisms of BA sequestration. Here, we present 1) amphiphilic polymers based on poly(meth)acrylates, poly(meth)acrylamides, polyalkylamines and polyallylamines containing quaternary ammonium groups, 2) cyclodextrins, and 3) BAS prepared via molecular imprinting methods. The synthetic approaches leading to individual BAS preparation, as well as results of their in vitro BA binding activities and in vivo lipid-lowering activities, are discussed. |
| Databáze: | OpenAIRE |
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