Anthony M L, Zhao M, Brindle K M
Department of Biochemistry, University of Cambridge, 80 Tennis Court Road, Old Addenbrookes Site, Cambridge CB2 1GA, United Kingdom.
J Biol Chem. 1999 Jul 9;274(28):19686-92. doi: 10.1074/jbc.274.28.19686.
Induction of apoptosis in HL-60 cells, using a variety of cytotoxic drugs, resulted, in all cases, in inhibition of CDP-choline:1, 2-diacylglycerol choline phosphotransferase, leading to an accumulation of its substrate, CDP-choline, and inhibition of phosphatidylcholine biosynthesis. Incubation of the cells with phosphatidylcholine reduced the number displaying an apoptotic morphology following drug treatment, and this was inversely related to the degree to which the drugs inhibited phosphatidylcholine biosynthesis. Inhibition of choline phosphotransferase by two of the drugs, farnesol and chelerythrine, was shown to be due to direct inhibition of the enzyme, while inhibition by the other drugs, etoposide and camptothecin, could be explained by the intracellular acidification that followed induction of apoptosis.
使用多种细胞毒性药物诱导HL-60细胞凋亡,在所有情况下均导致CDP-胆碱:1,2-二酰基甘油胆碱磷酸转移酶受到抑制,从而导致其底物CDP-胆碱积累,并抑制磷脂酰胆碱的生物合成。用磷脂酰胆碱孵育细胞可减少药物处理后呈现凋亡形态的细胞数量,且这与药物抑制磷脂酰胆碱生物合成的程度呈负相关。两种药物法尼醇和白屈菜红碱对胆碱磷酸转移酶的抑制作用被证明是由于对该酶的直接抑制,而其他药物依托泊苷和喜树碱的抑制作用可以通过凋亡诱导后细胞内酸化来解释。