Berkovic Dinko, Berkovic Katharina, Binder Claudia, Haase Detlef, Fleer Eduard A M
University Clinic of Göttingen, Department of Internal Medicine, Göttingen, Germany.
J Exp Ther Oncol. 2002 Jul-Aug;2(4):213-8. doi: 10.1046/j.1359-4117.2002.01036.x.
Hexadecylphosphocholine (HePC) is the first representative of the alkylphosphocholines (APC), a new group of biologically active compounds. HePC has pronounced antiproliferative effects on neoplastic cells in vitro and in vivo. The molecular mechanism by which HePC exerts its biological effects is still under investigation. Recently there has been growing evidence that HePC probably interferes with cellular signalling via phospholipases. It has been shown to inhibit both forms of phospholipase C (PLC), the phosphatidylinositol- and the phosphatidylcholine-specific PLC, and phospholipase A2. Here we present data showing that HePC inhibits the activity of phospholipase D in vitro, whereas the action of this enzyme in leukemic cell lines is not affected. Furthermore HePC does not seem to disturbed the activity of sphingomyelinase, another enzyme of phospholipid metabolism which has been shown to play an important role in cellular signalling as well.
十六烷基磷胆碱(HePC)是烷基磷胆碱(APC)的首个代表物,烷基磷胆碱是一类新型生物活性化合物。HePC在体外和体内对肿瘤细胞均有显著的抗增殖作用。HePC发挥其生物学效应的分子机制仍在研究中。最近,越来越多的证据表明,HePC可能通过磷脂酶干扰细胞信号传导。已证明它能抑制两种形式的磷脂酶C(PLC),即磷脂酰肌醇特异性PLC和磷脂酰胆碱特异性PLC,以及磷脂酶A2。在此我们展示的数据表明,HePC在体外抑制磷脂酶D的活性,而该酶在白血病细胞系中的作用不受影响。此外,HePC似乎并未干扰鞘磷脂酶的活性,鞘磷脂酶是磷脂代谢中的另一种酶,也已证明其在细胞信号传导中起重要作用。