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

Journal of Ginseng Research 2020년 44권 3호 p.490 ~ 495
 ( Ryoo Na-Yeon ) - Korea Institute of Science and Technology Center for Neuroscience

 ( Rahman Md. Ataur ) - Korea Institute of Science and Technology Center for Neuroscience
황홍익 ( Hwang Hong-Ik ) - Korea Institute of Science and Technology Center for Neuroscience
고성권 ( Ko Sung-Kwon ) - Semyung University Department of Oriental Medical Food and Nutrition
나승열 ( Nah Seung-Yeol ) - Konkuk University College of Veterinary Medicine
김형춘 ( Kim Hyoung-Chun ) - Kangwon National University College of Pharmacy
 ( Rhim Hye-Whon ) - Korea Institute of Science and Technology Center for Neuroscience

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 our previous studies have demonstrated that ginsenoside Rg3 significantly attenuated the activation of NMDA receptors (NMDARs) in hippocampal neurons, the effects of ginsenosides Rg5 and Rk1, which are derived from heat-mediated dehydration of ginsenoside Rg3, on neuronal NMDARs have not yet been elucidated.

Methods: We examined the regulation of NMDARs by ginsenosides Rg5 and Rk1 in cultured rat hippocampal neurons using fura-2?based calcium imaging and whole-cell patch-clamp recordings.

Results: The results from our investigation showed that ginsenosides Rg3 and Rg5 inhibited NMDARs with similar potencies. However, ginsenoside Rk1 inhibited NMDARs most effectively among the five compounds (Rg3, Rg5, Rk1, Rg5/Rk1 mixture, and protopanaxadiol) tested in cultured hippocampal neurons. Its inhibition is independent of the NMDA- and glycine-binding sites, and its action seems to involve 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 component contributable to the development of ginseng-based therapeutic treatments for neurodegenerative diseases.

키워드

Ginsenoside Rk1; Hippocampal neurons; Intracellular Ca2+; NMDA receptors; Whole-cell patch-clamp
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