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

Jorgensen, M.R., Bhurruth-Alcor, Y., Rost, T., Bohov, P., Muller, M., Guisado, C., Kostarelos, K., Dyroy, E., Berge, R.K., Miller, A.D. and Skorve, J. (2009) Synthesis and analysis of novel glycerolipids for the treatment of metabolic syndrome. Journal of Medicinal Chemistry, 52 (4). pp. 1172-1179. 10.1021/jm801019s.

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DOI: 10.1021/jm801019s

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 two different doses to study and compare metabolic outcomes relative to the administration of 1 alone after 6 days. Liposomal formualtions of 1 and 2 are also prepared to evaluate responses post 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 theose of 1 and 3. Therefore, 2 may represent a new lead for the treatment of metabolic syndrome.

Item Type:Article
Additional Information:Full text available electronically from the School of Pharmacy Library.
Departments, units and centres:Department of Pharmaceutics > Centre for Drug Delivery Research
ID Code:1245
Journal or Publication Title:Journal of Medicinal Chemistry
Deposited By:Library Staff
Deposited On:26 Jun 2009 16:16
Last Modified:24 Feb 2012 10:40

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