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.
- 5-HTA receptor
- Two-electrode voltage clamp