Novel phospholipid analogues of pan-PPAR activator tetradecylthioacetic acid are more PPARα selective

被引：7

作者：

Bhurruth-Alcor, Yushma ^{[1
]}

Rost, Therese H. ^{[2
]}

Jorgensen, Michael R. ^{[1
]}

Rajender ^{[1
]}

Mueller, Melanie ^{[1
]}

Skorve, Jon ^{[2
]}

Berge, Rolf K. ^{[2
,3
]}

Miller, Andrew D. ^{[1
]}

机构：

[1] Univ London Imperial Coll Sci Technol & Med, Dept Chem, Imperial Coll Genet Therapies Ctr, London SW7 2AZ, England

[2] Univ Bergen, Inst Med, N-5021 Bergen, Norway

[3] Haukeland Hosp, Dept Heart Dis, N-5021 Bergen, Norway

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期

关键词：

Metabolic syndrome; Diabetes type II; PPAR; TTA; Phospholipids; 3-THIA FATTY-ACIDS; PEROXISOME PROLIFERATOR; GENE-EXPRESSION; RAT-LIVER; RECEPTORS; PATHWAYS;

D O I：

10.1016/j.bmcl.2009.11.115

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Tetradecylthioacetic acid (TTA) is a modified fatty acid that appears to improve insulin sensitivity, lower blood lipid levels, enhance fatty acid oxidation and promote anti-inflammatory action in vivo, through mechanisms partly dependent upon peroxisome proliferator-activated receptors (PPARs). In order to improve the biological efficacy of TTA as a PPAR agonist, two novel phospholipid analogue lyso tetradecylthioacetyl-L-alpha-phosphatidylcholine and di-tetradecylthioacetyl-L-alpha-phosphatidylglycerol have been developed. Here we report on the syntheses of these novel phospholipids and their relative potential to act as PPAR agonists in vitro, in comparison to TTA and other positive controls. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1252 / 1255

页数：4

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