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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

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Laboratory of Pharmacology and Toxicology, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China
* Author to whom correspondence should be addressed.
Received: 30 January 2013 / Revised: 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)
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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 catechins; (−)-gallocatechin-3-gallate; Na+ channel; dorsal root ganglion; tetrodotoxin-resistant
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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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.

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