Journal
EUROPEAN JOURNAL OF PHARMACOLOGY
Volume 765, Issue -, Pages 34-41Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejphar.2015.08.011
Keywords
H+,K+-ATPase; Proton pump; DCPIB; Volume-regulated anion channel; LRRC8A
Categories
Funding
- Japan Society for the Promotion of Science [24659095, 25293047, 26460291, 25460282]
- Grants-in-Aid for Scientific Research [24659095, 25293047, 25460282] Funding Source: KAKEN
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4-(2-Butyl-6,7-dichloro-2-cyclopentylindan-1-on-5-yl)oxybutyric acid (DCPIB) has been used as an inhibitor of volume-regulated anion channel (VRAC), which is expressed in almost all cells (IC50 is around 4 mu M). Here, we found that DCPIB significantly inhibited the activities of gastric proton pump (H+,K+-ATPase) in isolated gastric tubulovesicles and the membrane sample of the H+,K+-ATPase-expressing cells, and their IC50 values were around 9 mu M. In the tubulovesicles, no significant expression of leucine rich repeat containing 8 family member A (LRRC8A), an essential component of VRAC, was observed. The inhibitory effect of DCPIB was also found in the membrane sample obtained from the cells in which LRRC8A had been knocked down. On the other hand, DCPIB had no significant effect on the activity of Na+,K+-ATPase or Ca2+-ATPase. In the H+,K+-ATPase-expressing cells, DCPIB inhibited the Rb-86(+) transport activity of H+,K+-ATPase but not that of Na+,K+-ATPase. DCPIB had no effect on the activity of Cl- channels other than VRAC in the cells. These results suggest that DCPIB directly inhibits H+,K+-ATPase activity. DCPIB may be a beneficial tool for studying the H+,K+-ATPase function in vitro. (C) 2015 Elsevier B.V. All rights reserved.
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