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[摘要]：Peppermint oil (Mentha x piperita L. (Lamiaceae)) has been shown to exert potent antiemetic properties, but its mode of action has not yet been elucidated. Among its active constituents (-)-menthol is the most important. Three different in vitro models were used to investigate the effects on 5-HT3 receptors (serotonin receptor subtype): [C-14] guanidinium influx into N1E-115 cells which express 5-HT3 receptors, isotonic contractions of the isolated rat ileum and equilibrium competition binding studies using a radioactively labelled 5-HT3 receptor antagonist ([H-3]GR65630) (3-(5-methyl-1H-imidazol-4-yl)-1-(1-methyl-1H-indol-3-yl)-1-propanone). Both peppermint oil and (-)-menthol inhibited [C-14] guanidinium influx through 5-HT3 receptor channels as well as contractions of the ileum induced by serotonin. Neither the peppermint oil nor (-)-menthol, however, was able to displace [H-3] GR65630 from 5-HT3 binding sites. It may be concluded that peppermint oil and (-)-menthol exert their antiemetic effect at least partly by acting on the 5-HT3 receptor ion-channel complex, probably by binding to a modulatory site distinct from the serotonin binding site. Copyright (C) 2010 JohnWiley & Sons, Ltd. |
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