Department of Anesthesiology, First Affiliated Hospital of China Medical University, Heping District, Shenyang, China.
Clin Exp Immunol. 2010 Jun;160(3):450-6. doi: 10.1111/j.1365-2249.2010.04111.x. Epub 2010 Mar 16.
Many cellular stresses and inflammatory stimuli can activate p38 mitogen-activated protein kinase (MAPK), a serine/threonine kinase in the MAPK family. The different stimuli act via different receptors or signalling pathways to induce phosphorylation of the cytosolic protein p47(phox), one subunit of the nicotinamide adenine dinucleotide phosphate (NADPH) oxidase. Formyl-methionyl-leucyl-phenylalanine (fMLP) has been shown to induce the p38 MAPK phosphorylation during the respiratory burst in human neutrophils. Here, we show that treatment with S(+)-ketamine or R(-)-ketamine at different concentrations (50, 100, 200, 400 microM) reduced fMLP-induced superoxide anion generation and p47(phox) phosphorylation in neutrophils in a concentration-dependent manner (y = -0.093x + 93.35 for S(+)-ketamine and y = -0.0982x + 95.603 for R(-)-ketamine, respectively). While treatment with 50 microM ketamine inhibited fMLP-induced superoxide generation by 10%, treatment with 400 microM S(+)-ketamine and R(-)-ketamine reduced fMLP-induced superoxide generation to 60.5 +/- 8.3% and 60.0 +/- 8.5%, respectively, compared with that in neutrophils treated with fMLP alone. Furthermore, treatment with ketamine down-regulated both fMLP-induced p47(phox) and isoproterenol-induced p38 MAPK phosphorylation and superoxide production. Interestingly, treatment with SB203580, the p38 MAPK inhibitor, also mitigated fMLP-induced superoxide anion generation and p38 MAPK and p47(phox) phosphorylation as well as apoptosis in a concentration-dependent fashion in neutrophils. Therefore, ketamine racemes inhibited fMLP-induced superoxide anion generation and p47(phox) phosphorylation by modulating fMLP-mediated p38 MAPK activation in neutrophils.
许多细胞应激和炎症刺激可以激活丝裂原活化蛋白激酶(MAPK),这是 MAPK 家族中的一种丝氨酸/苏氨酸激酶。不同的刺激通过不同的受体或信号通路作用,诱导细胞溶质蛋白 p47(phox)的磷酸化,p47(phox)是烟酰胺腺嘌呤二核苷酸磷酸(NADPH)氧化酶的一个亚单位。已经表明,甲酰基-甲硫氨酸-亮氨酸-苯丙氨酸(fMLP)在人中性粒细胞的呼吸爆发期间诱导 p38 MAPK 磷酸化。在这里,我们表明,用不同浓度(50、100、200、400μM)的 S(+)-氯胺酮或 R(-)-氯胺酮处理以浓度依赖性方式减少 fMLP 诱导的超氧阴离子生成和中性粒细胞中 p47(phox)的磷酸化(对于 S(+)-氯胺酮为 y = -0.093x + 93.35,对于 R(-)-氯胺酮为 y = -0.0982x + 95.603)。虽然用 50μM 氯胺酮处理可抑制 fMLP 诱导的超氧化物生成 10%,但用 400μM S(+)-氯胺酮和 R(-)-氯胺酮处理可将 fMLP 诱导的超氧化物生成分别减少至 60.5 +/- 8.3%和 60.0 +/- 8.5%,与单独用 fMLP 处理的中性粒细胞相比。此外,氯胺酮处理还下调了 fMLP 诱导的 p47(phox)和异丙肾上腺素诱导的 p38 MAPK 磷酸化以及超氧化物生成。有趣的是,用 p38 MAPK 抑制剂 SB203580 处理也以浓度依赖的方式减轻了 fMLP 诱导的超氧阴离子生成以及 p38 MAPK 和 p47(phox)的磷酸化以及中性粒细胞中的凋亡。因此,氯胺酮外消旋体通过调节中性粒细胞中 fMLP 介导的 p38 MAPK 激活来抑制 fMLP 诱导的超氧阴离子生成和 p47(phox)磷酸化。