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The Inhibitory Effects of Korean Red Ginseng Saponins on 5- HT3A Receptor Channel Activity Are Coupled to Anti-Nausea and Anti-Vomiting Action

Kim Jong-Hoon    (Research Laboratory for the Study of Ginseng Signal Transduction and Dept. of Physiology College of Veterinary Medicine, Konkuk University   ); Lee Byung-Hwan    (Research Laboratory for the Study of Ginseng Signal Transduction and Dept. of Physiology College of Veterinary Medicine, Konkuk University   ); Jeong Sang Min    (Research Laboratory for the Study of Ginseng Signal Transduction and Dept. of Physiology College of Veterinary Medicine, Konkuk University   ); Nah Seung-Yeol    (Research Laboratory for the Study of Ginseng Signal Transduction and Dept. of Physiology College of Veterinary Medicine, Konkuk University  );
  • 초록

    We performed in vitro and in vivo studies to know whether the inhibitory effects of ginsenosides on $5-HT_{3A}$ receptor channel acctivity are coupled to anti-nausea and anti-vomiting action. In vitro study, we investigated the effect of compound K (CK) and M4, which are ginsenoside metabolites, on human $5-HT_{3A}$ receptor channel activity expressed in Xenopus oocytes using two-electrode voltage clamp technique. Treatment of CK or M4 themselves had no effect in both oocytes injected with $H_2O\;and\;5-HT_{3A}$ receptor cRNA. In oocytes injected with $5- HT_{3A}$ receptor cRNA, M4 treatment inhibited more potently 5-HT-induced inward peak current $(I_{5-HT})$ than CK with dose-dependent and reversible manner. The half-inhibitory concentrations $(IC_{50})$ of CK and M4 were $36.9\;\pm\;10.1\;and\;7.3\;\pm\;2.2\;{\mu}M$ , respectively. The inhibition of $I_{5-HT}$ by M4 was non-competitive and voltage-independent. These results indicate that M4 might regulate $5-HT_{3A}$ receptors. In vivo experiments, injection of cisplatin (7.5 mg/kg, i.v.) induced both nausea and vomiting with 1 h latency. These episodes reached to peak after 2 h and persisted for 4 h. Pre-treatment of GTS (500 mg/kg, p.o.) significantly reduced cisplatin-induced nausea and vomiting by $51\;\pm\;8.4\;and\;48.8\;\pm\;6.4\%$ during 4 h compared to GIS­untreated group, respectively. These results show the possibility that in vitro inhibition of $5-HT_{3A}$ receptor channel activity by ginsenosides might be coupled to in vivo anti-emetic activity.


  • 주제어

    Panax ginseng .   ginsenoside metabolites .   5-HT _{3A} receptor .   cisplatin .   emesis.  

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    2. 2005 "Effects of Korean Red Ginseng Extract on Cisplatin-Induced Nausea and Vomiting" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 28 (6): 680~684    
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    5. 2013 "Resveratrol Inhibits $GABA_C$ ${\rho}$ Receptor-Mediated Ion Currents Expressed in Xenopus Oocytes" The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology 17 (2): 175~180    
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  • Jeong, Sang-Min (12)

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