Mahavadi Sunila, Nalli Ancy D, Kumar Divya P, Hu Wenhui, Kuemmerle John F, Grider John R, Murthy Karnam S
Department of Physiology and Biophysics, Virginia Commonwealth University Program in Enteric Neuromuscular Sciences, Virginia Commonwealth University, Richmond, Virginia; and.
Department of Neuroscience, Temple University School of Medicine, Philadelphia, Pennsylvania.
Am J Physiol Cell Physiol. 2014 Aug 15;307(4):C402-11. doi: 10.1152/ajpcell.00123.2014. Epub 2014 Jun 18.
This study identified a distinctive pattern of expression and activity of adenylyl cyclase (AC) and phosphodiesterase (PDE) isoforms in mouse colonic longitudinal smooth muscle cells and determined the changes in their expression and/or activity in response to proinflammatory cytokines (IL-1β and TNF-α) in vitro and 2,4,6 trinitrobenzene sulphonic acid (TNBS)-induced colonic inflammation in vivo. AC5/6 and PDE4D5, expressed in circular muscle cells, were also expressed in longitudinal smooth muscle. cAMP formation was tightly regulated via feedback phosphorylation of AC5/6 and PDE4D5 by PKA. Inhibition of PKA activity by myristoylated PKI blocked phosphorylation of AC5/6 and PDE4D5 and enhanced cAMP formation. TNBS treatment in vivo and IL-1β and TNF-α in vitro induced inducible nitric oxide synthase (iNOS) expression, stimulated ERK1/2 activity, caused iNOS-mediated S-nitrosylation and inhibition of AC5/6, and induced phosphorylation of PDE4D5 and stimulated its activity. The resultant decrease in AC5/6 activity and increase in PDE4D5 activity decreased cAMP formation and smooth muscle relaxation. S-nitrosylation and inhibition of AC5/6 activity were reversed by the iNOS inhibitor 1400W, whereas phosphorylation and activation of PDE4D5 were reversed by the phosphatidylinositol 3-kinase inhibitor LY294002 and the ERK1/2 inhibitor PD98059. The effects of IL-1β or TNF-α on forskolin-stimulated cAMP formation and smooth muscle relaxation reflected inhibition of AC5/6 activity and activation of PDE4D5 and were partly reversed by 1400W or PD98059 and completely reversed by a combination of the two inhibitors. The changes in the cAMP/PKA signaling and smooth muscle relaxation contribute to colonic dysmotility during inflammation.
本研究确定了小鼠结肠纵行平滑肌细胞中腺苷酸环化酶(AC)和磷酸二酯酶(PDE)同工型的独特表达模式和活性,并确定了它们在体外对促炎细胞因子(IL-1β和TNF-α)以及在体内2,4,6-三硝基苯磺酸(TNBS)诱导的结肠炎症反应中表达和/或活性的变化。在环行肌细胞中表达的AC5/6和PDE4D5也在纵行平滑肌中表达。cAMP的形成通过PKA对AC5/6和PDE4D5的反馈磷酸化进行严格调控。肉豆蔻酰化的PKI对PKA活性的抑制阻断了AC5/6和PDE4D5的磷酸化并增强了cAMP的形成。体内TNBS处理以及体外IL-1β和TNF-α诱导了诱导型一氧化氮合酶(iNOS)的表达,刺激了ERK1/2活性,导致iNOS介导的S-亚硝基化并抑制AC5/6,诱导PDE4D5的磷酸化并刺激其活性。AC5/6活性的降低和PDE4D5活性的增加导致cAMP形成减少和平滑肌舒张。iNOS抑制剂1400W可逆转AC5/6的S-亚硝基化和活性抑制,而磷脂酰肌醇3-激酶抑制剂LY294002和ERK1/2抑制剂PD98059可逆转PDE4D5的磷酸化和激活。IL-1β或TNF-α对福斯可林刺激的cAMP形成和平滑肌舒张的影响反映了AC活动的抑制5/6和PDE4D5的激活,1400W或PD98059可部分逆转,两种抑制剂联合使用可完全逆转。cAMP/PKA信号传导和平滑肌舒张的变化导致炎症期间结肠运动障碍。