新型烷化磷胆碱依鲁替尼通过半胱氨酸天冬氨酸蛋白酶（caspase）依赖性途径诱导 CLL 细胞凋亡。
Erufosine, a novel alkylphosphocholine, induces apoptosis in CLL through a caspase-dependent pathway.
机构信息
Clinic I of Internal Medicine, University of Cologne, Cologne, Germany.
出版信息
Leuk Res. 2010 Aug;34(8):1064-9. doi: 10.1016/j.leukres.2009.12.003. Epub 2010 Jan 21.
The alkylphosphocholine (APC) erufosine is a synthetic phospholipid analogue with antineoplastic activity. APC are known to interact with lipid metabolism and modulate cellular signaling pathways, particularly the phosphorylation of Akt. Here, in primary CLL cells induction of apoptosis was detected with an IC50 of 22muM whereas healthy donor PBMC were less sensitive towards erufosine. Treatment with erufosine caused dose-dependent cleavage of PARP, co-incubation with caspase inhibitor z-VAD almost completely abrogated the cytotoxic effect of erufosine indicating a caspase-dependent mechanism of erufosine. Erufosine was shown to induce apoptosis in primary CLL cells and merits further investigation regarding therapeutic options in CLL.
烷基磷酰胆碱（APC）埃罗福辛是一种具有抗肿瘤活性的合成磷脂类似物。APC 已知与脂质代谢相互作用，并调节细胞信号通路，特别是 Akt 的磷酸化。在这里，在原发性 CLL 细胞中，凋亡的诱导被检测到 IC50 为 22μM，而健康供体 PBMC 对埃罗福辛的敏感性较低。埃罗福辛处理导致 PARP 的剂量依赖性切割，与 caspase 抑制剂 z-VAD 共孵育几乎完全消除了埃罗福辛的细胞毒性作用，表明埃罗福辛的细胞凋亡依赖于 caspase。埃罗福辛被证明可诱导原发性 CLL 细胞凋亡，并在 CLL 的治疗选择方面值得进一步研究。
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