Synthesis of tocopheryl succinate phospholipid conjugates and monitoring of phospholipase A₂ activity.
Tocopheryl succinates (TOSs) are, in contrast to tocopherols, highly cytotoxic against many cancer cells. In this study the enzyme activity of secretory phospholipase A(2) towards various succinate-phospholipid conjugates has been investigated. The synthesis of six novel phospholipids is described, including two TOS phospholipids conjugates. The studies revealed that the TOS conjugates are poor substrates for the enzyme whereas the phospholipids with alkyl and phenyl succinate moieties were hydrolyzed by the enzyme to a high extent.
Department of Chemistry, Technical University of Denmark, Kemitorvet, Building 201, DK-2800 Kgs. Lyngby, Denmark.
SourceBioorganic & medicinal chemistry 20:13 2012 Jul 1 pg 3972-8
MeSHCell Line, Tumor
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
Pub Type(s)Journal Article
Research Support, Non-U.S. Gov't