NDLI: Gintonin, a Ginseng-Derived Lysophosphatidic Acid Receptor Ligand, Potentiates ATP-Gated P2X1 Receptor Channel Currents

Content Provider	PubMed Central
Author	Choi, Sun-hye Kim, Hyeon-joong Kim, Bo-ra Shin, Tae-joon Hwang, Sung-hee Lee, Byung-hwan Lee, Sang-mok Rhim, Hyewhon Nah, Seung-yeol
Copyright Year	2013
Abstract	Ginseng, the root of Panax ginseng C.A. Meyer, is used as a general tonic. Recently, we isolated a novel ginseng-derived lysophosphatidic acid (LPA) receptor ligand, gintonin. Gintonin activates G protein-coupled LPA receptors with high affinity in cells endogenously expressing LPA receptors, e.g., Xenopus oocytes. P2X receptors are ligand-gated ion channels activated by extracellular ATP, and 7 receptor subtypes (P2X1–P2X7) have been identified. Most of the P2X1 receptors are expressed in the smooth muscles of genitourinary organs involved in reproduction. A main characteristic of the P2X1 receptor is rapid desensitization after repeated ATP treatment of cells or tissues expressing P2X1 receptors. In the present study, we examined the effect of gintonin on P2X1 receptor channel activity. P2X1 receptors were heterologously expressed in Xenopus oocytes. ATP treatment of oocytes expressing P2X1 receptors induced large inward currents (IATP ), but repetitive ATP treatments induced a rapid desensitization of IATP . Gintonin treatment after P2X1 receptor desensitization potentiated IATP in a concentration-dependent manner. We further examined the signaling transduction pathways involved in gintonin-mediated potentiation of IATP . Gintonin-mediated IATP potentiation was blocked by Ki16425, an LPA1/3 receptor antagonist, a PKC inhibitor, a PLC inhibitor, and a PI4-Kinase inhibitor but not by a calcium chelator. In addition, mutations of the phosphoinositide binding site of the P2X1 receptor greatly attenuated the gintonin-mediated IATP potentiation. These results indicate that G protein-coupled LPA receptor activation by gintonin is coupled to the potentiation of the desensitized P2X1 receptor through a phosphoinositide-dependent pathway.
Related Links	http://dx.doi.org/10.1007/s10059-013-2293-x
Ending Page	150
Page Count	9
Starting Page	142
File Format	PDF
ISSN	02191032
e-ISSN	02191032
Journal	Molecules and Cells
Issue Number	2
Volume Number	35
Language	English
Publisher	Korea Society for Molecular and Cellular Biology
Publisher Date	2013-02-28
Access Restriction	Open
Rights Holder	Korea Society for Molecular and Cellular Biology
Subject Keyword	Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Cell Biology Medicine Molecular Biology

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Gintonin, a Ginseng-Derived Lysophosphatidic Acid Receptor Ligand, Potentiates ATP-Gated P2X1 Receptor Channel Currents