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-HT3A 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 I5-HT by triterpenoids occurred in a non-competitive manner. Taken together, these results indicate that triterpenoids may regulate the 5-HT3A 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. © 2010 Elsevier B.V. All rights reserved.
5-HT3A receptor; Triterpenoid; Two-electrode voltage clamp
EMTREE drug terms: alisol a; alisol b; alisol B 23 acetate; alisol C 23 aceteate; serotonin 3A receptor; triterpenoid; unclassified drug
EMTREE medical terms: animal cell; article; concentration (parameters); controlled study; ion current; ion transport; nonhuman; oocyte; priority journal; regulatory mechanism; transport kinetics; Xenopus
MeSH: Alismatidae; Animals; Cholestenones; Humans; Membrane Potentials; Oocytes; Patch-Clamp Techniques; Plant Extracts; Receptors, Serotonin, 5-HT3; Xenopus
Medline is the source for the MeSH terms of this document.
Species Index: Xenopus laevis
Chemicals and CAS Registry Numbers: Cholestenones; Plant Extracts; Receptors, Serotonin, 5-HT3; alisol A, 19885-10-0; alisol B, 18649-93-9; alisol B 23-acetate