Design, Synthesis, and Therapeutic Evaluation of Poly(acrylic acid)-tetraDOCA Conjugate as a Bile Acid Transporter Inhibitor

Title
Design, Synthesis, and Therapeutic Evaluation of Poly(acrylic acid)-tetraDOCA Conjugate as a Bile Acid Transporter Inhibitor
Author(s)
박주호[박주호]Taslim A. Al-Hilal[Taslim A. Al-Hilal]정지헌최정욱[최정욱]변영로[변영로]
Keywords
FARNESOID-X-RECEPTOR; MOLECULAR-WEIGHT HEPARIN; ENTEROHEPATIC CIRCULATION; DEOXYCHOLIC-ACID; OBETICHOLIC ACID; DRUG-DELIVERY; ORAL DELIVERY; ATHEROSCLEROSIS; FXR; CHOLESTEROL
Issue Date
201508
Publisher
AMER CHEMICAL SOC
Citation
BIOCONJUGATE CHEMISTRY, v.26, no.8, pp.1597 - 1605
Abstract
Regulation of cholesterol and bile acid homeostasis has been attracting attention as a pharmaceutical target for the treatment of diseases, such as hypercholesterolaemia and type 2 diabetes. In recent years, small bile acid analogues have been developed for the purpose of apical sodium-dependent bile acid transporter (ASBT) inhibition. Here, we designed a novel hydrophilic ASBT inhibitor using oligomeric bile acid with a high affinity with ASBT. Polyacrylic acid-tetraDOCA conjugates (PATD) have the ability to bind to ASBT in order to induce hypocholesterolemic effects. Both the viability and the functionality of PATD were evaluated in vitro, showing that PATDs were effective in inhibiting the increases of cholesterol in the blood and oil in the liver induced by high fat diet (HFD). The results indicated that the newly developed biomaterials with oligomeric bile acids and a hydrophilic polymer are potent therapeutic agents for hyperlipidemia.
URI
http://hdl.handle.net/YU.REPOSITORY/31333http://dx.doi.org/10.1021/acs.bioconjchem.5b00230
ISSN
1043-1802
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약학대학 > 약학부 > Articles
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