English
 
Help Privacy Policy Disclaimer
  Advanced SearchBrowse
  1. View item / 
  2. Item Summary

Item

ITEM ACTIONSEXPORT
Add to Basket
  Local TagsRelease HistoryDetailsSummary

Released
Journal Article

Epigallocatechin-3-gallate is an inhibitor of Na+,K+-ATPase by favoring the E1 conformation

MPS-Authors
/persons/resource/persons137890

Schwarz,  Wolfgang
Department of Biophysical Chemistry, Max Planck Institute of Biophysics, Max Planck Society;
Shanghai Research Center for Acupuncture and Medrians, Shanghai-Pudong 201203, China;

External Resource
No external resources are shared
Fulltext (restricted access)
There are currently no full texts shared for your IP range.
Fulltext (public)
There are no public fulltexts stored in PuRe
Supplementary Material (public)
There is no public supplementary material available
Citation

Ochiai, H., Takeda, K., Soeda, S., Tahara, Y., Takenaka, H., Abe, K., et al. (2009). Epigallocatechin-3-gallate is an inhibitor of Na+,K+-ATPase by favoring the E1 conformation. Biochemical Pharmacology, 78(8), 1069-1074. doi:10.1016/j.bcp.2009.06.007.


Cite as: https://hdl.handle.net/11858/00-001M-0000-0024-D745-D
Abstract
Four catechins, epigallocatechin-3-gallate, epigallocatechin, epicatechin-3-gallate, and epicatechin, inhibited activity of the Na+,K+-ATPase. The two galloyl-type catechins were more potent inhibitors, with IC50 values of about 1 μM, than were the other two catechins. Inhibition by epigallocatechin-3-gallate was noncompetitive with respect to ATP. Epigallocatechin-3-gallate reduced the affinity of vanadate, shifted the equilibrium of E1P and E2P toward E1P, and reduced the rate of the E1P to E2P transition. Epigallocatechin-3-gallate potently inhibited membrane-embedded P-type ATPases (gastric H+,K+-ATPase and sarcoplasmic reticulum Ca2+-ATPase) as well as the Na+,K+-ATPase, whereas soluble ATPases (bacterial F1-ATPase and myosin ATPase) were weakly inhibited. Solubilization of the Na+,K+-ATPase with a nonionic detergent reduced sensitivity to epigallocatechin-3-gallate with an elevation of IC50 to 10 μM. These results suggest that epigallocatechin-3-gallate exerts its inhibitory effect through interaction with plasma membrane phospholipid.