Inhibitory effects of magnolol on voltage-gated Na⁺ and K⁺ channels of NG108-15 cells

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• 作者：Chi-Li Gong^a ; ¹ ; Kar-Lok Wong^b ; ^c ; ¹ ; Ka-Shun Cheng^b ; ¹ ; Chang-Shin Kuo^d ; Chia-Chia Chao^d ; Min-Fan Tsai^a ; Yuk-Man Leung^d ; ^{ymleung@mail.cmu.edu.tw}
• 关键词：Magnolol ; Voltage-gated Na+ channel ; Voltage-gated K+ channel ; Block ; NG108-15 cell
• 刊名：European Journal of Pharmacology
• 出版年：2012
• 期刊代码：24_00142999
• 类别：neu
• 出版时间：5 May, 2012
• 卷：682
• 期：1-3
• 页码：73-78
• 文件大小：658 K

摘要

Magnolol, a polyphenolic compound isolated from Houpu, a Chinese herb from the bark of Magnolia officinalis, has been reported to have in vitro and in vivo neuroprotective effects. In spite of these reported beneficial effects, studies on the direct impact of magnolol on neuronal ion channels have been scarce. Whether magnolol affects voltage-gated Na⁺ channels (VGSC) and voltage-gated K⁺ (Kv) channels is unknown. Using the whole-cell voltage-clamp method, we studied the effects of magnolol on voltage-gated ion channels in neuronal NG108-15 cells. Magnolol inhibited VGSC channels with mild state-dependence (IC₅₀ of 15 and 30 渭M, at holding potentials of 鈭?#xA0;70 and 鈭?#xA0;100 mV, respectively). No frequency-dependence was observed in magnolol block. Magnolol caused a left-shift of 18 mV in the steady-state inactivation curve but did not affect the voltage-dependence of activation. Magnolol inhibited Kv channels with an IC₅₀ of 21 渭M, and it caused a 20-mV left-shift in the steady-state inactivation curve without affecting the voltage-dependence of activation. In conclusion, magnolol is an inhibitor of both VGSC and Kv channels and these inhibitory effects may in part contribute to some of the reported neuroprotective effects of magnolol.