Modulation of the nicotinic acetylcholine receptor by dioscorine in clonal rat phaeochlomocytoma (PC12) cells

Keiichi Nagata*, Gary L. Aistrup, Hiroshi Honda, Toshio Shono, Toshio Narahashi

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

Dioscorine is a toxin isolated from the tubers of tropical yam, Dioscorea hispida Schlussel that has insecticidal and antifeedant activities. The effects of dioscorine on the neuronal nicotinic acetylcholine receptor in rat clonal phaeochlomocytoma (PC12) cells were studied using whole-cell and single-channel patch clamp techniques. Dioscorine at concentrations of 0.45-450 μM accelerated the desensitization of current induced by 100 μM acetylcholine and suppressed the current in a dose-dependent manner. Dioscorine itself did not induce any current at concentrations ranging from 0.45 to 450 μM. At the single-channel level, 4.5-450 μM dioscorine, when co-applied with 10 μM acetylcholine, markedly shortened the open time and caused bursts to appear in a dose-dependent manner. The mean open time, mean closed time, and burst duration were decreased by dioscorine. These changes of single-channel kinetics result in a significant decrease in the total charge carried through the open channels, explaining the suppressive effect of dioscorine on acetylcholine-induced whole-cell currents. The suppressive effect of dioscorine on the acetylcholine-induced current is suggested to play an important role in the toxic actions in animals.

Original languageEnglish (US)
Pages (from-to)157-165
Number of pages9
JournalPesticide Biochemistry and Physiology
Volume64
Issue number3
DOIs
StatePublished - Jul 1999

ASJC Scopus subject areas

  • Agronomy and Crop Science
  • Health, Toxicology and Mutagenesis

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