Effects of protopanaxatriol-ginsenoside metabolites on rat N-methyl-d-aspartic Acid receptor-mediated ion currents

Title
Effects of protopanaxatriol-ginsenoside metabolites on rat N-methyl-d-aspartic Acid receptor-mediated ion currents
Authors
신태준황성희최신혜이병환강지연김현중R. Suzanne Zukin임혜원나승열
Keywords
Ginseng; Ginsenoside metabolites; N-methyl-D-aspartic acid receptor
Issue Date
2012-04
Publisher
The Korean Journal of Physiology & Pharmacology
Citation
VOL 16, NO 2, 113-118
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/42778
ISSN
12264512
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KIST Publication > Article
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