Polymeric bile acid sequestrants: Review of design, in vitro binding activities, and hypocholesterolemic effects.

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 Chem

authors

Heřmánková E,Žák A,Poláková L,Hobzová R,Hromádka R,Širc J

doi

10.1016/j.ejmech.2017.12.015

subject

Has Abstract

pub_date

2018-01-20 00:00:00

pages

300-317

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)31021-8

journal_volume

144

pub_type

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