Gastrodin inhibits the activity of acid-sensing ion channels in rat primary sensory neurons

• Published in: European journal of pharmacology Vol. 731; pp. 50 - 57
• Main Authors: Qiu, Fang, Liu, Ting-Ting, Qu, Zu-Wei, Qiu, Chun-Yu, Yang, Zhifan, Hu, Wang-Ping
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 15.05.2014
• Subjects: Acid Sensing Ion Channel Blockers - pharmacology; Acid Sensing Ion Channels - metabolism; Acid-sensing ion channel; Animals; Benzyl Alcohols - pharmacology; Cell Membrane - drug effects; Cell Membrane - metabolism; Dorsal root ganglion neuron; Dose-Response Relationship, Drug; Electrophysiological Phenomena - drug effects; Electrophysiology; Formaldehyde - pharmacology; Ganglia, Spinal - cytology; Gastrodia elata; Gastrodin; Glucosides - pharmacology; Male; Nociception - drug effects; Pain; Proton-gated current; Protons; Rats; Rats, Sprague-Dawley; Sensory Receptor Cells - cytology; Sensory Receptor Cells - drug effects; Dorsal root ganglion neuron; Electrophysiology; Pain; Proton-gated current; Gastrodin; Acid-sensing ion channel
• ISSN: 0014-2999; 1879-0712
• DOI: 10.1016/j.ejphar.2014.02.044

Acid-sensing ion channels (ASICs), a family of proton-gated cation channels, are believed to mediate pain caused by extracellular acidification. Gastrodin is a main bioactive constituent of the traditional herbal Gastrodia elata Blume, which has been widely used in Oriental countries for centuries. As an analgesic, gastrodin has been used clinically to treat pain such as migraine and headache. However, the mechanisms underlying analgesic action of gastrodin are still poorly understood. Here, we have found that gastrodin inhibited the activity of native ASICs in rat dorsal root ganglion (DRG) neurons. Gastrodin dose-dependently inhibited proton-gated currents mediated by ASICs. Gastrodin shifted the proton concentration–response curve downwards, with a decrease of 36.92±6.23% in the maximum current response but with no significant change in the pH0.5 value. Moreover, gastrodin altered acid-evoked membrane excitability of rat DRG neurons and caused a significant decrease in the amplitude of the depolarization and the number of action potentials induced by acid stimuli. Finally, peripheral applied gastrodin relieved pain evoked by intraplantar injection of acetic acid in rats. Our results indicate that gastrodin can inhibit the activity of ASICs in the primary sensory neurons, which provided a novel mechanism underlying analgesic action of gastrodin.