title: Gastrodin inhibits the activity of acid-sensing ion channels in rat primary sensory neurons.
abstract: 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.
authors.affiliation: Department of Pharmacology, Hubei University of Science and Technology, 88 Xianning Road, Xianning 437100, Hubei, PR China; College of Life Sciences, Hubei University, Wuhan 430062, Hubei, PR China.
authors.forename: Fang
authors.initials: F
authors.lastname: Qiu
authors.affiliation: Department of Pharmacology, Hubei University of Science and Technology, 88 Xianning Road, Xianning 437100, Hubei, PR China.
authors.forename: Ting-Ting
authors.initials: TT
authors.lastname: Liu
authors.affiliation: Department of Pharmacology, Hubei University of Science and Technology, 88 Xianning Road, Xianning 437100, Hubei, PR China.
authors.forename: Zu-Wei
authors.initials: ZW
authors.lastname: Qu
authors.affiliation: Department of Pharmacology, Hubei University of Science and Technology, 88 Xianning Road, Xianning 437100, Hubei, PR China.
authors.forename: Chun-Yu
authors.initials: CY
authors.lastname: Qiu
authors.affiliation: College of Life Sciences, Hubei University, Wuhan 430062, Hubei, PR China.
authors.forename: Zhifan
authors.initials: Z
authors.lastname: Yang
authors.affiliation: Department of Pharmacology, Hubei University of Science and Technology, 88 Xianning Road, Xianning 437100, Hubei, PR China. Electronic address: wangping_hu@163.com.
authors.forename: Wang-Ping
authors.initials: WP
authors.lastname: Hu
mesh_terms: D062646:Acid Sensing Ion Channel Blockers / Q000494:pharmacology*; D062565:Acid Sensing Ion Channels / Q000378:metabolism*; D000818:Animals; D001592:Benzyl Alcohols / Q000494:pharmacology*; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D055724:Electrophysiological Phenomena / Q000187:drug effects; D005557:Formaldehyde / Q000494:pharmacology; D005727:Ganglia, Spinal / Q000166:cytology*; D005960:Glucosides / Q000494:pharmacology*; D008297:Male; D059225:Nociception / Q000187:drug effects; D011522:Protons; D051381:Rats; D017207:Rats, Sprague-Dawley; D011984:Sensory Receptor Cells / Q000166:cytology* / Q000187:drug effects*
chemical_list: D062646:Acid Sensing Ion Channel Blockers; D062565:Acid Sensing Ion Channels; D001592:Benzyl Alcohols; D005960:Glucosides; D011522:Protons; D005557:Formaldehyde; C045345:gastrodin
keywords: Acid-sensing ion channel; Dorsal root ganglion neuron; Electrophysiology; Gastrodin; Pain; Proton-gated current