Cuthbert A W, Supuran C T, MacVinish L J
Department of Medicine, University of Cambridge, Addenbrooke's Hospital, Level 5 Box 157, Hills Road, Cambridge CB2 2QQ, UK.
J Physiol. 2003 Aug 15;551(Pt 1):79-92. doi: 10.1113/jphysiol.2003.046482. Epub 2003 Jul 18.
Stimulation of Calu-3 epithelia with 7,8-benzoquinoline, under short circuit current conditions, produced a current increase that was completely accounted for by the net flux of chloride, measured simultaneously with 36Cl-. Nevertheless the current stimulated by 7,8-benzoquinoline was sensitive to acetazolamide, which caused up to 50 % inhibition of the stimulated current, the remainder being sensitive to the Na+-K+-2Cl- cotransport inhibitor bumetanide. The effects of acetazolamide could be mimicked by either amiloride or by the di-sodium salt of 4,4'-dinitrostilbene-2,2'-disulphonic acid (DNDS) added to the basolateral side of the epithelium, but their actions were not additive. Amiloride was needed in sufficient concentration to inhibit the sodium-proton exchanger NHE1. DNDS blocks both the chloride-bicarbonate exchanger AE2 and the sodium-bicarbonate transporter NBC1. However, since 7,8-benzoquinoline activates basolateral K+ channels, causing hyperpolarisation, it is unlikely NBC1 is active after addition of 7,8-benzoquinoline. The effect of DNDS is, therefore, mainly on AE2. It is concluded that chloride enters the basolateral aspect of the cells using the Na+-K+-2Cl- cotransporter and a parallel arrangement of NHE1 with AE2, these latter two being sensitive to acetazolamide because of their association with the cytoplasmic form of carbonic anhydrase CAII. The effects of acetazolamide could be mimicked by removal of HCO3-/CO2 from the bathing medium, and furthermore showed that the NHE1-AE2 mechanism is particularly important when the transport rate is high. Thus part of the current stimulated by 7,8-benzoquinoline and inhibited by acetazolamide or HCO3-/CO2 removal can be said to represent bicarbonate-dependent chloride secretion.
在短路电流条件下,用7,8 - 苯并喹啉刺激Calu - 3上皮细胞,产生的电流增加完全由与³⁶Cl⁻同时测量的氯离子净通量所解释。然而,7,8 - 苯并喹啉刺激产生的电流对乙酰唑胺敏感,乙酰唑胺可导致高达50%的刺激电流抑制,其余部分对Na⁺-K⁺-2Cl⁻共转运抑制剂布美他尼敏感。乙酰唑胺的作用可被添加到上皮细胞基底外侧的氨氯地平或4,4'-二硝基芪-2,2'-二磺酸二钠盐(DNDS)模拟,但它们的作用不是相加的。需要足够浓度的氨氯地平来抑制钠-质子交换体NHE1。DNDS可阻断氯-碳酸氢根交换体AE2和钠-碳酸氢根转运体NBC1。然而,由于7,8 - 苯并喹啉激活基底外侧K⁺通道,导致超极化,因此在添加7,8 - 苯并喹啉后NBC1不太可能是活跃的。因此,DNDS的作用主要在AE2上。结论是,氯离子利用Na⁺-K⁺-2Cl⁻共转运体以及NHE1与AE2的平行排列进入细胞的基底外侧,后两者对乙酰唑胺敏感,因为它们与细胞质形式的碳酸酐酶CAII相关。乙酰唑胺的作用可通过从浴液介质中去除HCO₃⁻/CO₂来模拟,并且进一步表明当转运速率较高时,NHE1 - AE2机制尤为重要。因此,由7,8 - 苯并喹啉刺激并被乙酰唑胺或去除HCO₃⁻/CO₂所抑制的部分电流可以说是代表了碳酸氢根依赖性氯分泌。