Polymeric bile acid sequestrants: Review of design, in vitro binding activities, and hypocholesterolemic effects.
Eur J Med Chem
; 144: 300-317, 2018 Jan 20.
Article
in En
| MEDLINE
| ID: mdl-29275230
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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Polymers
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Bile Acids and Salts
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Drug Design
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Hypercholesterolemia
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Anticholesteremic Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Eur J Med Chem
Year:
2018
Document type:
Article
Country of publication: