期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 144, 期 -, 页码 300-317出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.12.015
关键词
Review; Bile acid sequestrant; Pleiotropic effect; Cholestyramine; Cyclodextrin; Molecular imprinting
资金
- Ministry of Industry and Trade [FV10380]
- Ministry of Education, Youth and Sports of the Czech Republic within National Sustainability Program II [BIOCEV-FAR LQ1604]
- project BIOCEV [CZ.1.05/1.1.00/02.0109]
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. (C) 2017 Elsevier Masson SAS. All rights reserved.
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