Calcium-activated chloride channels in a human biliary cell line: regulation by ca2+/calmodulin-dependent protein kinase. Schlenker, Thorsten, J. Gregory Fitz. Department of Medicine, Duke University Medical Center, Durham, NC 27710
APStracts 3:0048G, 1996.
Biliary epithelial cells contribute to bile formation through absorption and secretion of fluid and electrolytes. Recent studies indicate that membrane Cl- permeability is regulated in part by increases in intracellular Ca2+ concentration. Using the human Mz -ChA-1 cholangiocarcinoma cell line as a model, the purpose of these studies was to evaluate the effects of intracellular Ca2+ on channel activity, and to assess the possible roles of Ca2+-dependent kinases in channel regulation. Exposure to ionomycin (1 [mu]M) activated ion channels in the cell-attached configuration in 63/74 attempts, increasing open probability (Po) from 0 to 0.26 +/- 0.15 (n=17). Multiple channels were present in each patch, and the effects of ionomycin were reversed by subsequent addition of EGTA (2 mM) to the bath. With Cl--containing solutions, channels had a slope conductance of 14 +/- 4 pS (n=11) and the mean open time was estimated to be 5.3 +/- 1.8 ms. These channels were anion selective, and currents were carried by efflux of Cl- at the resting potential. Exposure to the Ca2+/calmodulin-dependent protein kinase (CaMKII) antagonist calmidazolium (100 [mu]M) decreased Po in ionomycin-stimulated cells to 0.02 +/- 0.06 (n=19). The protein kinase C antagonist chelerythrine (50 [mu]M) was without effect. In parallel studies in subconfluent cell monolayers, CaMKII antagonists were also potent inhibitors of ionomycin-stimulated 125I efflux. These findings indicate that Ca2+-dependent increases in membrane Cl- permeability are related in part to opening of 14 pS anion channels through a mechanism which depends upon both Ca2+ and CaMKII. These channels represent a potential target for pharmacologic modulation of biliary cell transport and function.

Received 8 August 1995; accepted in final form 15 February 1996.
APS Manuscript Number G340-5.
Article publication pending Am. J. Physiol. (Gastrointest. Liver
Physiology).
ISSN 1080-4757 Copyright 1996 The American Physiological Society.
Published in APStracts on 13 March 96