Hwang T H, Schwiebert E M, Guggino W B
Department of Physiology, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA.
Am J Physiol. 1996 Jun;270(6 Pt 1):C1611-23. doi: 10.1152/ajpcell.1996.270.6.C1611.
Stimulation of Cl- secretion across the airway epithelium by ATP or UTP as agonists has therapeutic implications for cystic fibrosis. Our results demonstrate that ATP stimulates Cl- secretion in rat tracheal epithelial cell monolayers in primary culture from the apical or basolateral side of the monolayer. Multiple types of ATP-sensitive Cl- conductances in intact monolayers were elucidated through inhibition by Cl- channel-blocking drugs. Multiple Cl- conductances stimulated by ATP and adenosine 3',5'-cyclic monophosphate (cAMP) (tested for comparison) were also deciphered more specifically by nystatin permeabilization of the basolateral membrane, subsequent imposition of symmetrical Cl-, I-, or Br- solutions to test halide permselectivity, inhibition by Cl- channel-blocking drugs, and construction of current-voltage plots to study time and voltage dependence of the currents. Apical ATP stimulates Cl- secretion through P2U (or P2Y2) purinergic receptors via both intracellular Ca2+ (Ca(2+)i)-dependent and Cai(2+)-independent signaling pathways by opening outwardly rectifying Cl- channels (ORCCs), cystic fibrosis transmembrane conductance regulator (CFTR) Cl- channels, and Cai(2+)-dependent Cl- channels. Basolateral ATP stimulates Cl- secretion via a combination of receptor subtypes (P2T and P2U) or a novel type of receptor (P2Y3), independent of Cai2+ or cAMP signaling by opening only CFTR channels. cAMP also stimulated multiple types of Cl- conductances, consistent with simultaneous activation of CFTR and ORCCs. Together, these results suggest that ATP as an agonist stimulates Cl- secretion via multiple purinergic receptors and multiple signal transduction pathways activated in different membrane domains of tracheal epithelia.
以ATP或UTP作为激动剂刺激气道上皮细胞的氯离子分泌对囊性纤维化具有治疗意义。我们的结果表明,ATP可从单层大鼠气管上皮细胞原代培养物的单层顶端或基底外侧刺激氯离子分泌。通过氯离子通道阻断药物的抑制作用,阐明了完整单层中多种类型的ATP敏感氯离子电导。通过制霉菌素通透基底外侧膜、随后施加对称的氯离子、碘离子或溴离子溶液以测试卤离子通透选择性、用氯离子通道阻断药物抑制以及构建电流-电压图以研究电流的时间和电压依赖性,还更具体地解读了由ATP和3',5'-环磷酸腺苷(cAMP)(作为对照进行测试)刺激的多种氯离子电导。顶端ATP通过P2U(或P2Y2)嘌呤能受体,经由细胞内钙离子(Ca(2+)i)依赖性和非Ca(2+)i依赖性信号通路,通过开放外向整流氯离子通道(ORCCs)、囊性纤维化跨膜电导调节因子(CFTR)氯离子通道和Ca(2+)依赖性氯离子通道来刺激氯离子分泌。基底外侧ATP通过受体亚型(P2T和P2U)或新型受体(P2Y3)的组合刺激氯离子分泌,仅通过开放CFTR通道而不依赖Ca(2+)或cAMP信号传导。cAMP也刺激多种类型的氯离子电导,这与CFTR和ORCCs的同时激活一致。总之,这些结果表明,ATP作为激动剂通过多种嘌呤能受体和在气管上皮细胞不同膜结构域中激活的多种信号转导途径刺激氯离子分泌。