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dc.contributor.authorKheradpezhouh, E
dc.contributor.authorBarritt, Gregory John
dc.contributor.authorRychkov, Grigori Y
dc.date.accessioned2016-05-30T01:13:06Z
dc.date.available2016-05-30T01:13:06Z
dc.date.issued2015-11-10
dc.identifier.citationKheradpezhouh E, Barritt GJ, Rychkov GY. Curcumin inhibits activation of TRPM2 channels in rat hepatocytes. Redox Biol. 2016 Apr;7:1-7. doi: 10.1016/j.redox.2015.11.001.en
dc.identifier.issn2213-2317
dc.identifier.urihttp://hdl.handle.net/2328/36140
dc.descriptionThis is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).en
dc.description.abstractOxidative stress is a hallmark of many liver diseases including viral and drug-induced hepatitis, ischemia-reperfusion injury, and non-alcoholic steatohepatitis. One of the consequences of oxidative stress in the liver is deregulation of Ca(2+) homeostasis, resulting in a sustained elevation of the free cytosolic Ca(2+) concentration ([Ca(2+)]c) in hepatocytes, which leads to irreversible cellular damage. Recently it has been shown that liver damage induced by paracetamol and subsequent oxidative stress is, in large part, mediated by Ca(2+) entry through Transient Receptor Potential Melastatin 2 (TRPM2) channels. Involvement of TRPM2 channels in hepatocellular damage induced by oxidative stress makes TRPM2 a potential therapeutic target for treatment of a range of oxidative stress-related liver diseases. We report here the identification of curcumin ((1E,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione), a natural plant-derived polyphenol in turmeric spice, as a novel inhibitor of TRPM2 channel. Presence of 5µM curcumin in the incubation medium prevented the H2O2- and paracetamol-induced [Ca(2+)]c rise in rat hepatocytes. Furthermore, in patch clamping experiments incubation of hepatocytes with curcumin inhibited activation of TRPM2 current by intracellular ADPR with IC50 of approximately 50nM. These findings enhance understanding of the actions of curcumin and suggest that the known hepatoprotective properties of curcumin are, at least in part, mediated through inhibition of TRPM2 channels.en
dc.language.isoen
dc.publisherElsevieren
dc.rightsCrown Copyright 2015 Published by Elsevier B.V.en
dc.titleCurcumin inhibits activation of TRPM2 channels in rat hepatocytesen
dc.typeArticleen
dc.identifier.doihttps://doi.org/10.1016/j.redox.2015.11.001en
dc.rights.licenseCC-BY-NC-ND
local.contributor.authorOrcidLookupBarritt, Gregory John: https://orcid.org/0000-0002-7472-4250en_US


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