Department of Chemistry, Technical University of Denmark, Kemitorvet, Building 201, DK-2800 Kgs. Lyngby, Denmark.
Bioorg Med Chem. 2012 Jul 1;20(13):3972-8. doi: 10.1016/j.bmc.2012.05.024. Epub 2012 May 17.
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.
生育酚琥珀酸酯（TOSs）与生育酚不同，对许多癌细胞具有高度细胞毒性。在这项研究中，研究了分泌型磷脂酶 A（2）对各种琥珀酸磷脂缀合物的酶活性。描述了六种新型磷脂的合成，包括两种 TOS 磷脂缀合物。研究表明，TOS 缀合物是该酶的不良底物，而具有烷基和苯基琥珀酸酯部分的磷脂则被酶高度水解。
