Ginsenoside Rk1 is a novel inhibitor of NMDA receptors in cultured rat hippocampal neurons 490

다국어 초록 (Multilingual Abstract)

Background: Ginsenoside Rk1, a saponin component isolated from heat-processed Panax ginseng Meyer,has been implicated in the regulation of antitumor and anti-inflammatory activities. Although ourprevious studies have demonstrated that ginsenoside Rg3 significantly attenuated the activation ofNMDA receptors (NMDARs) in hippocampal neurons, the effects of ginsenosides Rg5 and Rk1, which arederived from heat-mediated dehydration of ginsenoside Rg3, on neuronal NMDARs have not yet beenelucidated.
Methods: We examined the regulation of NMDARs by ginsenosides Rg5 and Rk1 in cultured rat hippocampalneurons using fura-2ebased calcium imaging and whole-cell patch-clamp recordings.
Results: The results from our investigation showed that ginsenosides Rg3 and Rg5 inhibited NMDARswith similar potencies. However, ginsenoside Rk1 inhibited NMDARs most effectively among the fivecompounds (Rg3, Rg5, Rk1, Rg5/Rk1 mixture, and protopanaxadiol) tested in cultured hippocampalneurons. Its inhibition is independent of the NMDA- and glycine-binding sites, and its action seems toinvolve in an interaction with the polyamine-binding site of the NMDAR channel complex.
Conclusion: Taken together, our results suggest that ginsenoside Rk1 might be a novel componentcontributable to the development of ginseng-based therapeutic treatments for neurodegenerativediseases.

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