Renis M, Cardile V, Russo A, Campisi A, Collovà F
Institute of Biochemistry, Faculty of Pharmacy, University of Catania, Catania, Italy.
Brain Res. 1998 Feb 2;783(1):143-50. doi: 10.1016/s0006-8993(97)01321-8.
The ether lipid 1-octadecyl-2-methyl-rac-glycero-3-phosphocholine (ET-18-OCH3) is a membrane interactive drug selectively cytotoxic toward neoplastic cells compared to normal cells. It induces apoptosis in human leukemic HL-60, T-lymphoid and in U937 myeloid cell lines and stimulates NO biosynthesis in cultured rat astrocytes. We have found a double action of ET-18-OCH3 in astrocytes which, at low doses, promotes a moderate induction of heat shock proteins of 70 kDa (HSP70) and the increase of glutamine synthetase (GS) activity. Conversely, at high doses, the drug shows toxic effects on astrocytes inducing decrease in GS activity, low molecular weight DNA formation, and release of lactic dehydrogenase (LDH) in the culture medium. Its analog compound platelet-activating factor (PAF) shares some of these biological aspects.
醚脂1-十八烷基-2-甲基-消旋甘油-3-磷酸胆碱（ET-18-OCH3）是一种与膜相互作用的药物，与正常细胞相比，它对肿瘤细胞具有选择性细胞毒性。它可诱导人白血病HL-60、T淋巴细胞和U937髓样细胞系凋亡，并刺激培养的大鼠星形胶质细胞中的一氧化氮生物合成。我们发现ET-18-OCH3在星形胶质细胞中具有双重作用，在低剂量时，它能适度诱导70 kDa热休克蛋白（HSP70）并增加谷氨酰胺合成酶（GS）活性。相反，在高剂量时，该药物对星形胶质细胞显示出毒性作用，导致GS活性降低、低分子量DNA形成以及培养基中乳酸脱氢酶（LDH）的释放。其类似化合物血小板活化因子（PAF）也具有其中一些生物学特性。
