Effects of protostane-type triterpenoids on the 5-HT3A receptor-mediated ion current in Xenopus oocytes

Brain Res. 2010 May 17;1331:20-7. doi: 10.1016/j.brainres.2010.03.041. Epub 2010 Mar 20.

Abstract

Alisol derivatives are unique protostane-type triterpenoid compounds that are isolated from Alismatis rhizoma, which is a well-known traditional medicine in East Asia. In the present study, we investigated the effects of protostane-type triterpenoids (AA, Alisol A; AB, Alisol B; AB-ac, Alisol B 23-acetate; AC-ac, Alisol C 23-aceteate) on 5-HT-induced currents mediated by the human 5-HT(3)A receptor expressed in Xenopus laevis oocytes. Co-treatment with triterpenoids regulated the 5-HT-induced inward peak current in a concentration-dependent and reversible manner. In addition, regulation of I(5-HT) by triterpenoids occurred in a non-competitive manner. Taken together, these results indicate that triterpenoids may regulate the 5-HT(3)A receptors that are expressed in Xenopus oocytes. Furthermore, this regulation of the ligand-gated ion channel activity by triterpenoids may be one of the pharmacological actions of Alismatis rhizoma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alismatales / chemistry*
  • Animals
  • Cholestenones / pharmacology*
  • Humans
  • Membrane Potentials / drug effects*
  • Oocytes / drug effects
  • Oocytes / metabolism
  • Patch-Clamp Techniques
  • Plant Extracts / pharmacology*
  • Receptors, Serotonin, 5-HT3 / drug effects*
  • Receptors, Serotonin, 5-HT3 / metabolism
  • Xenopus

Substances

  • Cholestenones
  • Plant Extracts
  • Receptors, Serotonin, 5-HT3
  • alisol B 23-acetate
  • alisol B
  • alisol A