Effects of triterpenoids from Poria cocos Wolf on the serotonin type 3A receptor-mediated ion current in Xenopus oocytes

Jun Ho Lee, Yoo Jin Lee, Jung Kyu Shin, Joo Won Nam, Seung Yeol Nah, Sung Hoon Kim, Jin-Hyun Jeong, Yangseok Kim, Minkyu Shin, Moochang Hong, Eun Kyoung Seo, Hyunsu Bae

Research output: Contribution to journalArticle

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Abstract

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-HT3A) 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 (I5-HT) occurred in a concentration dependent and reversible manner. Furthermore, the half-inhibitory concentrations (IC50) 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 I5-HT in oocytes expressing human 5-HT3A receptor of HA > PA > DA. Finally, inhibition of I5HT 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-HT3A 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.

Original languageEnglish
Pages (from-to)27-32
Number of pages6
JournalEuropean Journal of Pharmacology
Volume615
Issue number1-3
DOIs
Publication statusPublished - 2009 Aug 1

Fingerprint

Serotonin Receptors
Xenopus
Oocytes
Ligand-Gated Ion Channels
Ions
Vomiting
Nephrosis
Common Cold
Dizziness
Patch-Clamp Techniques
Gastritis
Inhibitory Concentration 50
Edema
Serotonin
Stomach
Electrodes
Carbon
Pharmacology
Wolfiporia

All Science Journal Classification (ASJC) codes

  • Pharmacology

Cite this

Lee, Jun Ho ; Lee, Yoo Jin ; Shin, Jung Kyu ; Nam, Joo Won ; Nah, Seung Yeol ; Kim, Sung Hoon ; Jeong, Jin-Hyun ; Kim, Yangseok ; Shin, Minkyu ; Hong, Moochang ; Seo, Eun Kyoung ; Bae, Hyunsu. / Effects of triterpenoids from Poria cocos Wolf on the serotonin type 3A receptor-mediated ion current in Xenopus oocytes. In: European Journal of Pharmacology. 2009 ; Vol. 615, No. 1-3. pp. 27-32.
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title = "Effects of triterpenoids from Poria cocos Wolf on the serotonin type 3A receptor-mediated ion current in Xenopus oocytes",
abstract = "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-HT3A) 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 (I5-HT) occurred in a concentration dependent and reversible manner. Furthermore, the half-inhibitory concentrations (IC50) 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 I5-HT in oocytes expressing human 5-HT3A receptor of HA > PA > DA. Finally, inhibition of I5HT 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-HT3A 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.",
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Lee, JH, Lee, YJ, Shin, JK, Nam, JW, Nah, SY, Kim, SH, Jeong, J-H, Kim, Y, Shin, M, Hong, M, Seo, EK & Bae, H 2009, 'Effects of triterpenoids from Poria cocos Wolf on the serotonin type 3A receptor-mediated ion current in Xenopus oocytes', European Journal of Pharmacology, vol. 615, no. 1-3, pp. 27-32. https://doi.org/10.1016/j.ejphar.2009.04.063

Effects of triterpenoids from Poria cocos Wolf on the serotonin type 3A receptor-mediated ion current in Xenopus oocytes. / Lee, Jun Ho; Lee, Yoo Jin; Shin, Jung Kyu; Nam, Joo Won; Nah, Seung Yeol; Kim, Sung Hoon; Jeong, Jin-Hyun; Kim, Yangseok; Shin, Minkyu; Hong, Moochang; Seo, Eun Kyoung; Bae, Hyunsu.

In: European Journal of Pharmacology, Vol. 615, No. 1-3, 01.08.2009, p. 27-32.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Effects of triterpenoids from Poria cocos Wolf on the serotonin type 3A receptor-mediated ion current in Xenopus oocytes

AU - Lee, Jun Ho

AU - Lee, Yoo Jin

AU - Shin, Jung Kyu

AU - Nam, Joo Won

AU - Nah, Seung Yeol

AU - Kim, Sung Hoon

AU - Jeong, Jin-Hyun

AU - Kim, Yangseok

AU - Shin, Minkyu

AU - Hong, Moochang

AU - Seo, Eun Kyoung

AU - Bae, Hyunsu

PY - 2009/8/1

Y1 - 2009/8/1

N2 - 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-HT3A) 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 (I5-HT) occurred in a concentration dependent and reversible manner. Furthermore, the half-inhibitory concentrations (IC50) 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 I5-HT in oocytes expressing human 5-HT3A receptor of HA > PA > DA. Finally, inhibition of I5HT 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-HT3A 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.

AB - 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-HT3A) 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 (I5-HT) occurred in a concentration dependent and reversible manner. Furthermore, the half-inhibitory concentrations (IC50) 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 I5-HT in oocytes expressing human 5-HT3A receptor of HA > PA > DA. Finally, inhibition of I5HT 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-HT3A 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.

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