Department of Chemistry and Biochemistry, Lebanese University, Rafic Hariri Educational Campus, Hadath, Lebanon.
Int J Biochem Cell Biol. 2012 Dec;44(12):2106-15. doi: 10.1016/j.biocel.2012.08.016. Epub 2012 Aug 22.
Previously we reported that the sesquiterpene lactone parthenolide induces oxidative stress in cardiac myocytes, which blocks Janus kinase (JAK) activation by the interleukin 6 (IL-6)-type cytokines. One implication suggested by this finding is that IL-6 signaling is dependent upon cellular anti-oxidant defenses or redox status. Therefore, the present study was undertaken to directly test the hypothesis that JAK1 signaling by the IL-6-type cytokines in cardiac myocytes is impaired by glutathione (GSH) depletion, since this tripeptide is one of the major anti-oxidant molecules and redox-buffers in cells. Cardiac myocytes were pretreated for 6h with l-buthionine-sulfoximine (BSO) to inhibit GSH synthesis. After 24h, cells were dosed with the IL-6-like cytokine, leukemia inhibitory factor (LIF). BSO treatment decreased GSH levels and dose-dependently attenuated activation of JAK1, Signal Transducer and Activator of Transcription 3 (STAT3), and extracellular signal regulated kinases 1 and 2 (ERK1/2). Addition of glutathione monoethyl ester, which is cleaved intracellularly to GSH, prevented attenuation of LIF-induced JAK1 and STAT3 activation, as did the reductant N-acetyl-cysteine. Unexpectedly, LIF-induced STAT1 activation was unaffected by GSH depletion. Evidence was found that STAT3 is more resistant than STAT1 to intermolecular disulfide bond formation under oxidizing conditions and more likely to retain the monomeric form, suggesting that conformational differences explain the differential effect of GSH depletion on STAT1 and STAT3. Overall, our findings indicate that activation of both JAK1 and STAT3 is redox-sensitive and the character of IL-6 type cytokine signaling in cardiac myocytes is sensitive to changes in the cellular redox status. In cardiac myocytes, activation of STAT1 may be favored over STAT3 under oxidizing conditions due to GSH depletion and/or augmented reactive oxygen species production, such as in ischemia-reperfusion and heart failure.
先前我们曾报道过,倍半萜内酯(一种植物化合物)白花前胡甲素可诱导心肌细胞产生氧化应激,从而阻断白细胞介素 6(IL-6)型细胞因子对 Janus 激酶(JAK)的激活。这一发现暗示着 IL-6 信号通路可能依赖于细胞抗氧化防御或氧化还原状态。因此,本研究旨在直接验证以下假设,即 IL-6 型细胞因子通过 JAK1 信号通路在心肌细胞中的作用因谷胱甘肽(GSH)耗竭而受损,因为三肽是细胞内主要的抗氧化分子和氧化还原缓冲剂之一。心肌细胞用 L-丁硫氧嘧啶(BSO)预处理 6 小时以抑制 GSH 的合成。24 小时后,用白细胞介素 6 样细胞因子白血病抑制因子(LIF)处理细胞。BSO 处理降低了 GSH 水平,并呈剂量依赖性地减弱了 JAK1、信号转导子和转录激活子 3(STAT3)和细胞外信号调节激酶 1 和 2(ERK1/2)的激活。GSH 单乙酯(可在细胞内分解为 GSH)的添加可防止 LIF 诱导的 JAK1 和 STAT3 激活减弱,还原剂 N-乙酰半胱氨酸也有此作用。出乎意料的是,GSH 耗竭对 LIF 诱导的 STAT1 激活没有影响。有证据表明,在氧化条件下,STAT3 比 STAT1 更能抵抗分子间二硫键的形成,并且更有可能保持单体形式,这表明构象差异解释了 GSH 耗竭对 STAT1 和 STAT3 的不同影响。总体而言,我们的研究结果表明,JAK1 和 STAT3 的激活均对氧化还原敏感,并且心肌细胞中 IL-6 型细胞因子信号的特征对细胞氧化还原状态的变化敏感。在心肌细胞中,由于 GSH 耗竭和/或活性氧物质(如在缺血再灌注和心力衰竭期间)产生增加,氧化条件下 STAT1 的激活可能优先于 STAT3。