Crumpton S C, Goz B, Ishaq K S
Division of Medicinal Chemistry, School of Pharmacy, University of North Carolina, Chapel Hill 27514.
Anticancer Res. 1988 Nov-Dec;8(6):1361-6.
1-0-Alkyl diol and glyceryl ether lipids with a quaternary ammonium polar head group were synthesized and the cytotoxicity (IC50) tested against KB cells, with low 1-0-alkyl-cleavage activity, and rat hepatoma 77 cells with relatively high 1-0-alkyl-cleavage activity. The original premise was that the compounds would be inactivated by the cleavage enzyme and thus be selectively toxic to cells with less of the enzyme. Results with two other cell lines with equivalent cleavage enzyme, HL-60 and K562-4, however, are not consistent with this premise.
合成了具有季铵极性头部基团的1-0-烷基二醇和甘油醚脂质,并针对KB细胞(具有低1-0-烷基裂解活性)和大鼠肝癌77细胞(具有相对高的1-0-烷基裂解活性)测试了其细胞毒性(IC50)。最初的假设是这些化合物会被裂解酶灭活,因此对该酶含量较少的细胞具有选择性毒性。然而,另外两种具有同等裂解酶的细胞系HL-60和K562-4的实验结果与这一假设不一致。