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

Palle Jacob Pedersen, Helene Marie-France Viart, Fredrik Melander, Thomas Lars Andresen, Robert Madsen, Mads Hartvig Clausen

Research output: Contribution to journalJournal articleResearchpeer-review

Abstract

Tocopheryl succinates (TOSs) are, in contrast to tocopherols, highly cytotoxic against many cancer cells. In this study the enzyme activity of secretory phospholipase A2 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.
Original languageEnglish
JournalBioorganic & Medicinal Chemistry
Volume20
Issue number13
Pages (from-to)3972-3978
ISSN0968-0896
DOIs
Publication statusPublished - 2012

Keywords

  • Drug delivery
  • Liposomes
  • Vitamin E
  • Phospholipase

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