Department of Pharmacology, Faculty of Pharmacy, Mersin University, Mersin, Turkey.
Department of Pharmacology, College of Medicine, Center for Health Sciences, University of Tennessee, Memphis, Tennessee.
Clin Exp Pharmacol Physiol. 2019 Feb;46(2):173-182. doi: 10.1111/1440-1681.13045.
We have previously demonstrated that the activation of the spleen tyrosine kinase (Syk)/inhibitory-κB (IκB)-α/nuclear factor-κB (NF-κB) p65 signalling pathway contributes to hypotension and inflammatory response in a rat models of zymosan (ZYM)-induced non-septic shock. The purpose of this study was to further examine the possible mechanism underlying the effect of inhibition of Syk by BAY61-3606 via NF-κB activity at the level of nuclear translocation regarding the production of vasodilator and proinflammatory mediators in lipopolysaccharide (LPS) (septic)- and ZYM (non-septic)-induced shock. Administration of LPS (10 mg/kg, ip) or ZYM (500 mg/kg, ip) to male Wistar rats decreased mean arterial pressure and increased heart rate that was associated with an increase in the activities of cyclooxygenase and nitric oxide synthase, tumour necrosis factor-α, and interleukin-8 levels, and NF-κB activation and nuclear translocation in sera and/or cardiovascular and renal tissues. BAY61-3606 (3 mg/kg, ip), the selective Syk inhibitor, given 1 hour after LPS- or ZYM injection reversed all the above-mentioned effects. These results suggest that Syk contributes to the LPS- or ZYM-induced hypotension and inflammation associated with transactivation of NF-κB in septic and non-septic shock.
我们之前已经证明,在酵母聚糖(ZYM)诱导的非感染性休克大鼠模型中,脾酪氨酸激酶(Syk)/抑制性κB(IκB)-α/核因子-κB(NF-κB)p65 信号通路的激活导致低血压和炎症反应。本研究的目的是进一步研究通过 NF-κB 活性在核易位水平上抑制 Syk 对脂多糖(LPS)(感染性)和 ZYM(非感染性)诱导的休克中血管扩张剂和促炎介质产生的可能机制。给予雄性 Wistar 大鼠 LPS(10mg/kg,ip)或 ZYM(500mg/kg,ip)可降低平均动脉压并增加心率,这与环加氧酶和一氧化氮合酶、肿瘤坏死因子-α和白细胞介素-8 水平的活性增加以及血清和/或心血管和肾脏组织中 NF-κB 的激活和核易位有关。选择性 Syk 抑制剂 BAY61-3606(3mg/kg,ip)在 LPS 或 ZYM 注射后 1 小时给予,可逆转上述所有作用。这些结果表明,Syk 参与 LPS 或 ZYM 诱导的低血压和炎症,与感染性和非感染性休克中 NF-κB 的转激活有关。