Effects of ginsenoside Rg2 on the 5-HT3A receptor-mediated ion current in Xenopus oocytes

Seok Choi, Jun Ho Lee, Seikwan Oh, Hyewhon Rhim, Sang Mok Lee, Seung Yeol Nah

Research output: Contribution to journalArticlepeer-review

43 Scopus citations

Abstract

Treatment of ginsenosides, major active ingredients of Panax ginseng, produces a variety of pharmacological or physiological responses with effects on the central and peripheral nervous systems. Recent reports showed that ginsenoside Rg2 inhibits nicotinic acetylcholine receptor-mediated Na+ influx and channel activity. In the present study, we investigated the effect of ginsenoside Rg2 on human 5-hydroxytryptamine3A (5-HT3A) receptor channel activity, which is also one of the ligand-gated ion channel families. The 5-HT 3A receptor was expressed in Xenopus oocytes, and the current was measured using the two-electrode voltage clamp technique. The ginsenoside Rg2 itself had no effect on the oocytes that were injected with H2O as well as on the oocytes that were injected with the 5-HT 3A receptor cRNA. In the oocytes that were injected with the 5-HT3A receptor cRNA, the pretreatment of ginsenoside Rg2 inhibited the 5-HT-induced inward peak current (I5-HT). The inhibitory effect of ginsenoside Rg2 on I5-HT was dose dependent and reversible. The half-inhibitory concentrations (IC50) of ginsenoside Rg2 was 22.3 ± 4.6 μM. The inhibition of I5-HT by ginsenoside Rg2 was non-competitive and voltage-independent. These results indicate that ginsenoside Rg2 might regulate the 5-HT3A receptors that are expressed in Xenopus oocytes. Further, this regulation on the ligand-gated ion channel activity by ginsenosides might be one of the pharmacological actions on Panax ginseng.

Original languageEnglish
Pages (from-to)108-113
Number of pages6
JournalMolecules and Cells
Volume15
Issue number1
StatePublished - Feb 2003

Keywords

  • 5-HT Receptor
  • Ginsenoside Rg
  • Ligand-gated Ion Channels
  • Panax Ginseng
  • Serotonin
  • Xenopus Oocytes

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