Danhauser S, Berdel W E, Schick H D, Fromm M, Reichert A, Fink U, Busch R, Eibl H, Rastetter J
Department of Medicine I, Technische Universitaet, Munich, Federal Republic of Germany.
Lipids. 1987 Nov;22(11):911-5. doi: 10.1007/BF02535553.
Eleven lipids have been tested for cytotoxic (trypan blue dye exclusion) activity in cells from eight freshly explanted human leukemias in vitro. 4-Aminomethyl-1-[2,3-(di-N-decyloxy)N-propyl]-4-phenylpiperidine (CP-46,665), 1-mercapto-hexadecyl-2-methoxymethyl-rac-glycero-3-phosphocholine (BM 41.440), the 2-acetamide analog of platelet-activating factor (PAF) and 1-O-octadecyl-2-O-methyl-rac-glycero-3-phosphocholine (ET-18-OCH3) were found among the most active compounds. 2-Lysophosphatidylcholine (2-LPC) showed the lowest activity. However, in addition there was variation among the results regarding the activity of the 1-octadecyl-rac-glycero-3-phosphocholine (ET-18-OH) and its D- and L-forms, but a significantly higher cytotoxic activity of D-ET-18-OH compared with L-ET-18-OH on the basis of 2-LPC as control after an incubation time of 48 hr. We conclude that with the limited number of structures available, this type of study is not sufficient to yield further information about the mode of the accumulation and toxicity of this type of lipids.
在体外对来自8例新鲜移植的人类白血病的细胞进行了11种脂质的细胞毒性（台盼蓝染料排斥法）活性测试。4-氨基甲基-1-[2,3-（二-N-癸氧基）-N-丙基]-4-苯基哌啶（CP-46,665）、1-巯基十六烷基-2-甲氧基甲基-外消旋甘油-3-磷酸胆碱（BM 41.440）、血小板活化因子（PAF）的2-乙酰胺类似物以及1-O-十八烷基-2-O-甲基-外消旋甘油-3-磷酸胆碱（ET-18-OCH3）被发现是活性最强的化合物。2-溶血磷脂酰胆碱（2-LPC）的活性最低。然而，此外，关于1-十八烷基-外消旋甘油-3-磷酸胆碱（ET-18-OH）及其D型和L型的活性结果也存在差异，但在48小时孵育时间后，以2-LPC为对照，D-ET-18-OH的细胞毒性活性显著高于L-ET-18-OH。我们得出结论，鉴于可用结构数量有限，这类研究不足以提供关于此类脂质积累和毒性模式的更多信息。
