0483932 - ÚMCH 2019 RIV FR eng J - Journal Article
Heřmánková, Eva - Žák, A. - Poláková, Lenka - Hobzová, Radka - Hromádka, R. - Širc, Jakub
Polymeric bile acid sequestrants: review of design, in vitro binding activities, and hypocholesterolemic effects.
European Journal of Medicinal Chemistry. Roč. 144, 20 January (2018), s. 300-317. ISSN 0223-5234. E-ISSN 1768-3254
R&D Projects: GA MPO(CZ) FV10380; GA MŠMT(CZ) LQ1604; GA MŠMT(CZ) ED1.1.00/02.0109
Institutional support: RVO:61389013
Keywords : review * bile acid sequestrant * pleiotropic effect
OECD category: Medicinal chemistry
Impact factor: 4.833, year: 2018
DOI: https://doi.org/10.1016/j.ejmech.2017.12.015

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.
Permanent Link: http://hdl.handle.net/11104/0279315