title: The sodium channel of human excitable cells is a target for gambierol.
abstract: BACKGROUND
  Gambierol is a polycyclic ether toxin with the same biogenetic origin as ciguatoxins. Gambierol has been associated with neurological symptoms in humans even though its mechanism of action has not been fully characterized.
  
  
  METHODS
  We studied the effect of gambierol in human neuroblastoma cells by using bis-oxonol to measure membrane potential and FURA-2 to monitor intracellular calcium.
  
  
  RESULTS
  We found that this toxin: i) produced a membrane depolarization, ii) potentiated the effect of veratridine on membrane potential iii) decreased ciguatoxin-induced depolarization and iv) increased cytosolic calcium in neuroblastoma cells.
  
  
  CONCLUSIONS
  These results indicate that gambierol modulate ion fluxes by acting as a partial agonist of sodium channels.
authors.affiliation: Departamento de Farmacologia, Facultad de Veterinaria, Universidad de Santiago de Compostela, Lugo, Spain.
authors.forename: M Carmen
authors.initials: MC
authors.lastname: Louzao
authors.forename: Eva
authors.initials: E
authors.lastname: Cagide
authors.forename: Mercedes R
authors.initials: MR
authors.lastname: Vieytes
authors.forename: Makoto
authors.initials: M
authors.lastname: Sasaki
authors.forename: Haruhiko
authors.initials: H
authors.lastname: Fuwa
authors.forename: Takeshi
authors.initials: T
authors.lastname: Yasumoto
authors.forename: Luis M
authors.initials: LM
authors.lastname: Botana
mesh_terms: D002118:Calcium / Q000378:metabolism; D016764:Cell Polarity / Q000187:drug effects; D002922:Ciguatoxins / Q000494:pharmacology*; D004988:Ethers, Cyclic / Q000494:pharmacology*; D006801:Humans; D008564:Membrane Potentials / Q000187:drug effects; D009447:Neuroblastoma / Q000188:drug therapy / Q000378:metabolism; D009474:Neurons / Q000187:drug effects* / Q000378:metabolism; D011083:Polycyclic Compounds / Q000494:pharmacology*; D012530:Saxitoxin / Q000031:analogs & derivatives / Q000494:pharmacology; D015222:Sodium Channels / Q000187:drug effects* / Q000378:metabolism; D019831:Sodium-Calcium Exchanger / Q000037:antagonists & inhibitors / Q000187:drug effects / Q000378:metabolism; D014407:Tumor Cells, Cultured; D014701:Veratridine / Q000494:pharmacology; D035964:Oxocins
chemical_list: D002118:Calcium; D002922:Ciguatoxins; D004988:Ethers, Cyclic; D011083:Polycyclic Compounds; D012530:Saxitoxin; D015222:Sodium Channels; D019831:Sodium-Calcium Exchanger; D014701:Veratridine; C435770:gambierol; D035964:Oxocins; C082191:ciguatoxin 2; C034902:neosaxitoxin