Effects of protopanaxatriol-ginsenoside metabolites on rat N-methyl-d-aspartic Acid receptor-mediated ion currents
- Effects of protopanaxatriol-ginsenoside metabolites on rat N-methyl-d-aspartic Acid receptor-mediated ion currents
- 신태준; 황성희; 최신혜; 이병환; 강지연; 김현중; R. Suzanne Zukin; 임혜원; 나승열
- Ginseng; Ginsenoside metabolites; N-methyl-D-aspartic acid receptor
- Issue Date
- The Korean Journal of Physiology & Pharmacology
- VOL 16, NO 2, 113-118
- Ginsenosides are low molecular weight glycosides found in ginseng that exhibit neuroprotective effects
through inhibition of N-methyl-D-aspartic acid (NMDA) receptor channel activity. Ginsenosides, like
other natural compounds, are metabolized by gastric juices and intestinal microorganisms to produce
ginsenoside metabolites. However, little is known about how ginsenoside metabolites regulate NMDA
receptor channel activity. In the present study, we investigated the effects of ginsenoside metabolites,
such as compound K (CK), protopanaxadiol (PPD), and protopanaxatriol (PPT), on oocytes that heterologously
express the rat NMDA receptor. NMDA receptor-mediated ion current (INMDA) was measured
using the 2-electrode voltage clamp technique. In oocytes injected with cRNAs encoding NMDA receptor
subunits, PPT, but not CK or PPD, reversibly inhibited INMDA in a concentration-dependent manner.
The IC50 for PPT on INMDA was 48.1±4.6 μM, was non-competitive with NMDA, and was independent
of the membrane holding potential. These results demonstrate the possibility that PPT interacts with
the NMDA receptor, although not at the NMDA binding site, and that the inhibitory effects of PPT
on INMDA could be related to ginseng-mediated neuroprotection.
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