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KMID : 0352720050290010037
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Journal of Ginseng Research
2005 Volume.29 No. 1 p.37 ~ p.43
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The Inhibitory Effects of Korean Red Ginseng Saponins on 5-HT₃_A Receptor Channel Activity Are Coupled to Anti-Nausea and Anti-Vomiting Action
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Kim JH
Lee BH/Jeong SM/Nah SY
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Abstract
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We performed in vitro and in vivo studies to know whether the inhibitory effects of ginsenosides on 5-HT₃_A 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-HT₃_A 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 H₂O and 5-HT₃_A receptor cRNA. In oocytes injected with 5-HT₃_A 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±10.1 and 7.3±2.2㎛, respectively. The inhibition of l_5HT by M4 was non-competitive and voltage-independent. These results indicate that M4 might regulate 5-HT₃_A receptors. In vivo experiments, injection of cisplatin (7.5 ㎎/㎏, 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㎎/㎏, p.o.) significantly reduced cisplatin-induced nausea and vomiting by 51±8.4 and 48.8±6.4% during 4 h compared to GTS-untreated group, respectively. These results show the possibility that in vitro inhibition of 5-HT₃_A receptor channel activity by ginsenosides might be coupled to in vivo anti-emetic activity.
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