Inhibitory Effects of Honokiol on the Voltage-Gated Potassium Channels in Freshly Isolated Mouse Dorsal Root Ganglion Neurons

Voltage-gated potassium (K V ) currents, subdivided into rapidly inactivating A-type currents ( I A ) and slowly inactivating delayed rectifier currents ( I K ), play a fundamental role in modulating pain by controlling neuronal excitability. The effects of Honokiol (Hon), a natural biphenolic compo...

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Veröffentlicht in:Neurochemical research 2018-02, Vol.43 (2), p.450-457
Hauptverfasser: Sheng, Anqi, Zhang, Yan, Li, Guang, Zhang, Guangqin
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Sprache:eng
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Zusammenfassung:Voltage-gated potassium (K V ) currents, subdivided into rapidly inactivating A-type currents ( I A ) and slowly inactivating delayed rectifier currents ( I K ), play a fundamental role in modulating pain by controlling neuronal excitability. The effects of Honokiol (Hon), a natural biphenolic compound derived from Magnolia officinalis , on K V currents were investigated in freshly isolated mouse dorsal root ganglion neurons using the whole-cell patch clamp technique. Results showed that Hon inhibited I A and I K in concentration-dependent manner. The IC 50 values for block of I A and I K were 30.5 and 25.7 µM, respectively. Hon (30 µM) shifted the steady-state activation curves of I A and I K to positive potentials by 17.6 and 16.7 mV, whereas inactivation and recovery from the inactivated state of I A were unaffected. These results suggest that Hon preferentially interacts with the active states of the I A and I K channels, and has no effect on the resting state and inactivated state of the I A channel. Blockade on K + channels by Hon may contribute to its antinociceptive effect, especially anti-inflammatory pain.
ISSN:0364-3190
1573-6903
DOI:10.1007/s11064-017-2440-4