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Effects of triterpenoids from Poria cocos Wolf on the serotonin type 3A receptor-mediated ion current in Xenopus oocytes
- Effects of triterpenoids from Poria cocos Wolf on the serotonin type 3A receptor-mediated ion current in Xenopus oocytes
- Lee J.-H.; Lee Y.J.; Shin J.-K.; Nam J.-W.; Nah S.-Y.; Kim S.-H.; Jeong J.-H.; Kim Y.; Shin M.; Hong M.; Seo E.-K.; Bae H.
- Ewha Authors
- SCOPUS Author ID
- Issue Date
- Journal Title
- European Journal of Pharmacology
- vol. 615, no. 41277, pp. 27 - 32
- SCI; SCIE; SCOPUS
- Poria cocos Wolf (P. cocos Wolf) is used to treat chronic gastritis, edema, nephrosis, gastric atony, acute gastroenteric catarrh, dizziness, emesis and vomiting. Triterpenoids are a class of natural compounds produced by P. cocos Wolf that contain acyclic 30-carbon precursors. In this study, we investigated the effect of triterpenoids (PA, Pachymic acid; DA, dehydroeburicoic acid; HA, 3β-hydroxylanosta-7,9(11),24-trien-21-oic acid) on human 5-hydroxytryptamine 3A (5-HT 3A) receptor channel activity, which is one of the ligand-gated ion channel families. The two-electrode voltage-clamp technique was used to examine the 5-HT3A mediated current. The inhibitory effect of triterpenoids on 5HT-induced inward current (I 5-HT) occurred in a concentration dependent and reversible manner. Furthermore, the half-inhibitory concentrations (IC 50) of PA, DA and HA were 3.2 ± 0.2, 5.5 ± 0.6 and 1.4 ± 0.2 μM, respectively. This corresponded to an order of potency for the inhibition of I 5-HT in oocytes expressing human 5-HT 3A receptor of HA > PA > DA. Finally, inhibition of I 5HT by triterpenoids occurred in a non-competitive manner, while inhibition by HA and PA showed more voltage-dependency. Taken together, these results indicate that triterpenoids may regulate the expressed 5-HT 3A receptors in Xenopus oocytes. Furthermore, this regulation of the ligand-gated ion channel activity by triterpenoids may be one of the pharmacological actions of P. cocos Wolf. © 2009 Elsevier B.V. All rights reserved.
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