Curcumin potently blocks Kv1.4 potassium channels.
Curcumin, a major constituent of the spice turmeric, is a nutriceutical compound reported to possess therapeutic properties against a variety of diseases ranging from cancer to cystic fibrosis. In whole-cell patch-clamp experiments on bovine adrenal zona fasciculata (AZF) cells, curcumin reversibly inhibited the Kv1.4K+ current with an IC50 of 4.4 microM and a Hill coefficient of 2.32. Inhibition by curcumin was significantly enhanced by repeated depolarization; however, this agent did not alter the voltage-dependence of steady-state inactivation. Kv1.4 is the first voltage-gated ion channel demonstrated to be inhibited by curcumin. Furthermore, these results identify curcumin as one of the most potent antagonists of these K+ channels identified thus far. It remains to be seen whether any of the therapeutic actions of curcumin might originate with its ability to inhibit Kv1.4 or other voltage-gated K+ channel.
Liu
Haiyan
H
Department of Neuroscience, The Ohio State University, College of Medicine and Public Health, Columbus, OH 43210-1239, USA.
Danthi
Sanjay J
SJ
Enyeart
John J
JJ
D000311:Adrenal Glands / Q000187:drug effects / Q000378:metabolism; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002417:Cattle; D002478:Cells, Cultured; D003474:Curcumin / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D051665:Kv1.4 Potassium Channel / Q000037:antagonists & inhibitors*; D018408:Patch-Clamp Techniques
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D051665:Kv1.4 Potassium Channel; D003474:Curcumin