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

doi: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

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

Department of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

39 Scopus citations

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-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 (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 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.

Original language	English
Pages (from-to)	27-32
Number of pages	6
Journal	European Journal of Pharmacology
Volume	615
Issue number	1-3
DOIs	https://doi.org/10.1016/j.ejphar.2009.04.063
State	Published - 1 Aug 2009

Bibliographical note

Funding Information:
This work was supported by the Korea Science and Engineering Foundation (KOSEF) grant funded by the Korean government (MEST) (No. 2009-0063466).

Keywords

Poria cocos Wolf
Serotonin type 3A receptor
Triterpenoid
Xenopus oocyte

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10.1016/j.ejphar.2009.04.063

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@article{3311cec501f34cffb1392bb5a9c610a4,

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.",

keywords = "Poria cocos Wolf, Serotonin type 3A receptor, Triterpenoid, Xenopus oocyte",

author = "Lee, \{Jun Ho\} and Lee, \{Yoo Jin\} and Shin, \{Jung Kyu\} and Nam, \{Joo Won\} and Nah, \{Seung Yeol\} and Kim, \{Sung Hoon\} and Jeong, \{Jin Hyun\} and Yangseok Kim and Minkyu Shin and Moochang Hong and Seo, \{Eun Kyoung\} and Hyunsu Bae",

note = "Funding Information: This work was supported by the Korea Science and Engineering Foundation (KOSEF) grant funded by the Korean government (MEST) (No. 2009-0063466).",

year = "2009",

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doi = "10.1016/j.ejphar.2009.04.063",

language = "English",

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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

N1 - Funding Information: This work was supported by the Korea Science and Engineering Foundation (KOSEF) grant funded by the Korean government (MEST) (No. 2009-0063466).

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.

KW - Poria cocos Wolf

KW - Serotonin type 3A receptor

KW - Triterpenoid

KW - Xenopus oocyte

UR - https://www.scopus.com/pages/publications/67449152244

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DO - 10.1016/j.ejphar.2009.04.063

M3 - Article

C2 - 19446542

AN - SCOPUS:67449152244

SN - 0014-2999

VL - 615

SP - 27

EP - 32

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 1-3

ER -

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

Abstract

Bibliographical note

Keywords

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