Modulation of Kv2.1 channels inactivation by curcumin.
BACKGROUND
The aim of the present study was to assess the effects of curcumin on the voltage-dependent Kv2.1 potassium channel.


METHODS
The whole-cell patch-clamp technique was used to explore the regulation of Kv2.1 channels expressed in HEK293 cells by curcumin.


RESULTS
Curcumin reduced the Kv2.1 currents; the inhibition occurred with a slow time course and was partially reversible. Curcumin did not alter the kinetics and voltage dependence of activation; however, the kinetics of open- and closed-state inactivation was accelerated by curcumin along with a hyperpolarizing shift in the voltage dependence of inactivation. Curcumin inhibition of Kv2.1 current was not use-dependent.


CONCLUSIONS
Overall, our data suggest that curcumin inhibits Kv2.1 channels by modulating the inactivation gating, which would be expected to impact cellular physiology.
Department of Physiology and Biophysics, Faculty of Medicine, Autonomous University of San Luis Potosí, Potosí, Mexico.
Iván A
IA
Aréchiga-Figueroa
Department of Physiology and Biophysics, Faculty of Medicine, Autonomous University of San Luis Potosí, Potosí, Mexico.
Mayra
M
Delgado-Ramírez
Department of Physiology and Biophysics, Faculty of Medicine, Autonomous University of San Luis Potosí, Potosí, Mexico.
Rita
R
Morán-Zendejas
Department of Physiology and Biophysics, Faculty of Medicine, Autonomous University of San Luis Potosí, Potosí, Mexico. Electronic address: aldo.rodriguez@uaslp.mx.
Aldo A
AA
Rodríguez-Menchaca
D003474:Curcumin / Q000494:pharmacology*; D057809:HEK293 Cells; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects; D007700:Kinetics; D008564:Membrane Potentials / Q000187:drug effects; D051669:Shab Potassium Channels / Q000037:antagonists & inhibitors*
D051669:Shab Potassium Channels; D003474:Curcumin
Curcumin; Inactivation; Kv2.1; Potassium channels