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Synthesis and analysis of novel glycerolipids for the treatment of metabolic syndrome.

Abstract
Tetradecylthioacetic acid (TTA) 1 is a peroxisome proliferator-activated receptor (PPAR) agonist found to improve insulin sensitivity, lower blood lipid levels, enhance fatty acid oxidation, and promote anti-inflammation in vivo. In an attempt to enhance these properties, two key thioether fatty acid (Thefa) lipids, ditetradecylthioacetyl phosphatidylcholine 2 and tritetradecylthioacetyl glycerol 3, are synthesized and administered po to male Wistar rats at two different doses to study and compare metabolic outcomes relative to the administration of 1 alone after 6 days. Liposomal formulations of 1 and 2 are also prepared to evaluate acute metabolic responses (at 3 h) post i.v. injection. Across all metrics measured, 1-induced responses post po administration are in line with previous data. Responses induced from 3 are mostly equivalent to 1-induced responses. By contrast, 2-induced responses almost always outperform those of 1 and 3. Therefore, 2 may represent a new lead for the treatment of metabolic syndrome.
AuthorsMichael R Jorgensen, Yushma Bhurruth-Alcor, Therese Røst, Pavol Bohov, Melanie Müller, Cristina Guisado, Kostas Kostarelos, Endre Dyrøy, Rolf K Berge, Andrew D Miller, Jon Skorve
JournalJournal of medicinal chemistry (J Med Chem) Vol. 52 Issue 4 Pg. 1172-9 (Feb 26 2009) ISSN: 1520-4804 [Electronic] United States
PMID19175322 (Publication Type: Journal Article)
Chemical References
  • Glycerides
  • Peroxisome Proliferator-Activated Receptors
  • Phosphatidylcholines
  • Sulfides
  • 1-(carboxymethylthio)tetradecane
  • Glycerol
Topics
  • Animals
  • Glycerides (chemistry, pharmacology)
  • Glycerol
  • Male
  • Metabolic Syndrome (drug therapy)
  • Peroxisome Proliferator-Activated Receptors (agonists)
  • Phosphatidylcholines
  • Rats
  • Rats, Wistar
  • Sulfides (chemistry, pharmacology)

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