Pharmazentrum Frankfurt/ZAFES, Klinikum der Johann Wolfgang Goethe-Universität Frankfurt am Main, Germany.
Br J Pharmacol. 2010 Aug;160(7):1641-51. doi: 10.1111/j.1476-5381.2010.00818.x.
Sphingosine kinases (SKs) convert sphingosine to sphingosine 1-phosphate (S1P), which is a bioactive lipid that regulates a variety of cellular processes including proliferation, differentiation and migration.
We used the human endothelial cell line EA.hy926 to investigate the effect of nitric oxide (NO) donors on SK-1 expression, and on cell migration and tube formation.
We showed that exposure of EA.hy926 cells to Deta-NO (125-1000 microM) resulted in a time- and concentration-dependent up-regulation of SK-1 mRNA and protein expression, and activity with a first significant effect at 250 microM of Deta-NO. The increased SK-1 mRNA expression resulted from an enhanced SK-1 promoter activity. A similar effect was also seen with various other NO donors. In mechanistic terms, the NO-triggered effect occurred independently of cGMP, but involved the classical mitogen-activated protein kinase cascade because the MEK inhibitor U0126 abolished the NO-induced SK-1 expression. The effect of NO was also markedly reduced by the thiol-reducing agent N-acetylcysteine, suggesting a redox-dependent mechanism. Functionally, Deta-NO triggered an increase in the migration of endothelial cells in an adapted Boyden chamber assay, and also increased endothelial tube formation in a Matrigel assay. These responses were both abolished in cells depleted of SK-1.
These data show that NO donors up-regulate specifically SK-1 expression and activity in human endothelial cells, and SK-1 in turn critically contributes to the migratory capability and tube formation of endothelial cells. Thus, SK-1 may be considered an attractive novel target to interfere with pathological processes involving angiogenesis.
鞘氨醇激酶(SK)将鞘氨醇转化为鞘氨醇 1-磷酸(S1P),后者是一种生物活性脂质,可调节多种细胞过程,包括增殖、分化和迁移。
我们使用人内皮细胞系 EA.hy926 研究了一氧化氮(NO)供体对 SK-1 表达以及细胞迁移和管状形成的影响。
我们表明,EA.hy926 细胞暴露于 Deta-NO(125-1000 μM)会导致 SK-1 mRNA 和蛋白表达以及活性的时间和浓度依赖性上调,第一个显著作用发生在 250 μM 的 Deta-NO。增加的 SK-1 mRNA 表达是由于 SK-1 启动子活性增强所致。各种其他 NO 供体也表现出类似的作用。就机制而言,NO 触发的效应独立于 cGMP,但涉及经典的丝裂原活化蛋白激酶级联反应,因为 MEK 抑制剂 U0126 消除了 NO 诱导的 SK-1 表达。NO 的作用也被硫醇还原剂 N-乙酰半胱氨酸明显降低,表明存在氧化还原依赖的机制。在功能上,Deta-NO 在适应性 Boyden 室测定中触发内皮细胞迁移增加,并在 Matrigel 测定中增加内皮管状形成。在耗尽 SK-1 的细胞中,这些反应均被消除。
这些数据表明,NO 供体在人内皮细胞中特异性地上调 SK-1 的表达和活性,而 SK-1 反过来又对内皮细胞的迁移能力和管状形成至关重要。因此,SK-1 可被视为干扰涉及血管生成的病理过程的有吸引力的新靶标。