Abstract:
: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.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Heřmánková E,Žák A,Poláková L,Hobzová R,Hromádka R,Širc Jdoi
10.1016/j.ejmech.2017.12.015subject
Has Abstractpub_date
2018-01-20 00:00:00pages
300-317eissn
0223-5234issn
1768-3254pii
S0223-5234(17)31021-8journal_volume
144pub_type
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