Riera Humberto, Afonso Valéry, Collin Pascal, Lomri Abderrahim
Unidad de Reumatología, Nivel plaza del Instituto Autónomo Hospital Universitario de Los Andes. Mérida, Venezuela.
INSERM U1029, Laboratoire de l'Angiogenèse et du Microenvironnement des Cancers, Pessac, France.
PLoS One. 2015 May 21;10(5):e0127571. doi: 10.1371/journal.pone.0127571. eCollection 2015.
Pyrrolidine dithiocarbamate (PDTC) known as antioxidant and specific inhibitor of NF-κB was also described as pro-oxidant by inducing cell death and reactive oxygen species (ROS) accumulation in cancer. However, the mechanism by which PDTC indices its pro-oxidant effect is unknown. Therefore, we aimed to evaluate the effect of PDTC on the human Cu/Zn superoxide dismutase 1 (SOD1) gene transcription in hematopoietic human cancer cell line U937. We herein show for the first time that PDTC decreases SOD1 transcripts, protein and promoter activity. Furthermore, SOD1 repression by PDTC was associated with an increase in oxidative stress as evidenced by ROS production. Electrophoretic mobility-shift assays (EMSA) show that PDTC increased binding of activating protein-1 (AP-1) in dose dependent-manner suggesting that the MAPkinase up-stream of AP-1 is involved. Ectopic NF-κB p65 subunit overexpression had no effect on SOD1 transcription. In contrast, in the presence of JNK inhibitor (SP600125), p65 induced a marked increase of SOD1 promoter, suggesting that JNK pathway is up-stream of NF-κB signaling and controls negatively its activity. Indeed, using JNK deficient cells, PDTC effect was not observed nether on SOD1 transcription or enzymatic activity, nor on ROS production. Finally, PDTC represses SOD1 in U937 cells through JNK/c-Jun phosphorylation. Taken together, these results suggest that PDTC acts as pro-oxidant compound in JNK/AP-1 dependent-manner by repressing the superoxide dismutase 1 gene leading to intracellular ROS accumulation.
吡咯烷二硫代氨基甲酸盐(PDTC)作为抗氧化剂和核因子-κB(NF-κB)的特异性抑制剂,也被描述为通过诱导癌细胞死亡和活性氧(ROS)积累而具有促氧化作用。然而,PDTC发挥其促氧化作用的机制尚不清楚。因此,我们旨在评估PDTC对造血性人类癌细胞系U937中人类铜锌超氧化物歧化酶1(SOD1)基因转录的影响。我们在此首次表明,PDTC可降低SOD1转录本、蛋白质和启动子活性。此外,PDTC对SOD1的抑制与ROS产生所证明的氧化应激增加有关。电泳迁移率变动分析(EMSA)表明,PDTC以剂量依赖性方式增加激活蛋白-1(AP-1)的结合,提示AP-1上游的丝裂原活化蛋白激酶(MAP激酶)参与其中。异位过表达NF-κB p65亚基对SOD1转录无影响。相反,在存在JNK抑制剂(SP600125)的情况下,p65可诱导SOD1启动子显著增加,提示JNK途径在NF-κB信号传导上游并对其活性起负调控作用。事实上,使用JNK缺陷细胞时,未观察到PDTC对SOD1转录、酶活性或ROS产生的影响。最后,PDTC通过JNK/c-Jun磷酸化在U937细胞中抑制SOD1。综上所述,这些结果表明,PDTC通过抑制超氧化物歧化酶1基因导致细胞内ROS积累,以JNK/AP-1依赖的方式作为促氧化化合物发挥作用。