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

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.

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  • Authors

    Pedersen PJ, Viart HM, Melander F, Andresen TL, Madsen R, Clausen MH

    Institution

    Department of Chemistry, Technical University of Denmark, Kemitorvet, Building 201, DK-2800 Kgs. Lyngby, Denmark.

    Source

    Bioorganic & medicinal chemistry 20:13 2012 Jul 1 pg 3972-8

    MeSH

    Cell Line, Tumor
    Humans
    Phospholipases A2
    Phospholipids
    Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
    Substrate Specificity
    Succinic Acid
    Tocopherols

    Pub Type(s)

    Journal Article
    Research Support, Non-U.S. Gov't

    Language

    eng

    PubMed ID

    22672983