Synthesis of tocopheryl succinate phospholipid conjugates and monitoring of phospholipase A₂ activity.

Journal: Bioorganic & Medicinal Chemistry
Published:
Abstract

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.

Authors
Palle Pedersen, Hélène Viart, Fredrik Melander, Thomas Andresen, Robert Madsen, Mads Clausen