Int. J. Mol. Sci. 2013, 14(5), 9779-9789; doi:10.3390/ijms14059779
Article

Effects of (−)-Gallocatechin-3-Gallate on Tetrodotoxin-Resistant Voltage-Gated Sodium Channels in Rat Dorsal Root Ganglion Neurons

Received: 30 January 2013; in revised form: 10 April 2013 / Accepted: 24 April 2013 / Published: 7 May 2013
(This article belongs to the Special Issue Plant-Derived Pharmaceuticals by Molecular Farming 2012)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: The (−)-gallocatechin-3-gallate (GCG) concentration in some tea beverages can account for as much as 50% of the total catechins. It has been shown that catechins have analgesic properties. Voltage-gated sodium channels (Nav) mediate neuronal action potentials. Tetrodotoxin inhibits all Nav isoforms, but Nav1.8 and Nav1.9 are relatively tetrodotoxin-resistant compared to other isoforms and functionally linked to nociception. In this study, the effects of GCG on tetrodotoxin-resistant Na+ currents were investigated in rat primary cultures of dorsal root ganglion neurons via the whole-cell patch-clamp technique. We found that 1 μM GCG reduced the amplitudes of peak current density of tetrodotoxin-resistant Na+ currents significantly. Furthermore, the inhibition was accompanied by a depolarizing shift of the activation voltage and a hyperpolarizing shift of steady-state inactivation voltage. The percentage block of GCG (1 μM) on tetrodotoxin-resistant Na+ current was 45.1% ± 1.1% in 10 min. In addition, GCG did not produce frequency-dependent block of tetrodotoxin-resistant Na+ currents at stimulation frequencies of 1 Hz, 2 Hz and 5 Hz. On the basis of these findings, we propose that GCG may be a potential analgesic agent.
Keywords: catechins; (−)-gallocatechin-3-gallate; Na+ channel; dorsal root ganglion; tetrodotoxin-resistant
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MDPI and ACS Style

Zhang, Y.; Jia, Y.-Y.; Guo, J.-L.; Liu, P.-Q.; Jiang, J.-M. Effects of (−)-Gallocatechin-3-Gallate on Tetrodotoxin-Resistant Voltage-Gated Sodium Channels in Rat Dorsal Root Ganglion Neurons. Int. J. Mol. Sci. 2013, 14, 9779-9789.

AMA Style

Zhang Y, Jia Y-Y, Guo J-L, Liu P-Q, Jiang J-M. Effects of (−)-Gallocatechin-3-Gallate on Tetrodotoxin-Resistant Voltage-Gated Sodium Channels in Rat Dorsal Root Ganglion Neurons. International Journal of Molecular Sciences. 2013; 14(5):9779-9789.

Chicago/Turabian Style

Zhang, Yan; Jia, Yan-Yan; Guo, Jin-Lei; Liu, Pei-Qing; Jiang, Jian-Min. 2013. "Effects of (−)-Gallocatechin-3-Gallate on Tetrodotoxin-Resistant Voltage-Gated Sodium Channels in Rat Dorsal Root Ganglion Neurons." Int. J. Mol. Sci. 14, no. 5: 9779-9789.

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