α-Bulnesene, a novel PAF receptor antagonist isolated from Pogostemon cablin

HuiChun Hsu; Wen Chia Yang; Wei Jern Tsai; Chien Chih Chen; Hui Yu Huang; Ying Chieh Tsai

doi:10.1016/j.bbrc.2006.05.006

α-Bulnesene, a novel PAF receptor antagonist isolated from Pogostemon cablin

HuiChun Hsu, Wen Chia Yang, Wei Jern Tsai, Chien Chih Chen, Hui Yu Huang, Ying Chieh Tsai

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

38 Citations (Scopus)

Abstract

α-Bulnesene is a sesquiterpenoid isolated from the water extract of Pogostemon cablin. It showed a potent and concentration-dependent inhibitory effect on platelet-activating factor (PAF) and arachidonic acid (AA) induced rabbit platelet aggregation. In a radioligand binding assay for the PAF receptor, α-bulnesene competitively inhibited [³H]PAF binding to the PAF receptor with an IC₅₀ value of 17.62 ± 5.68 μM. α-Bulnesene also dose-dependently inhibited PAF-induced intracellular Ca²⁺ increase in fluo-3/AM-loaded platelets (IC₅₀ values of 19.62 ± 1.32 μM). Furthermore, α-bulnesene inhibited AA-induced thromboxane B₂ (TXB₂) formation and prostaglandin E₂ (PGE₂) formation. These results indicate that the inhibitory effect of α-bulnesene on platelet aggregation was due to a dual activity; specifically the chemical blocked PAF-induced intracellular signal transduction and interfered with cyclooxygenase activity, which resulted in a decrease in thromboxane formation. This study is the first to demonstrate that α-bulnesene is a PAF receptor antagonist as well as an anti-platelet aggregation agent.

Original language	English
Pages (from-to)	1033-1038
Number of pages	6
Journal	Biochemical and Biophysical Research Communications
Volume	345
Issue number	3
DOIs	https://doi.org/10.1016/j.bbrc.2006.05.006
Publication status	Published - Jul 7 2006
Externally published	Yes

Keywords

α-Bulnesene
Arachidonic acid (AA)
Platelet aggregation
Platelet-activating factor (PAF)
Pogostemon cablin
Sesquiterpenoid

ASJC Scopus subject areas

Biophysics
Biochemistry
Molecular Biology
Cell Biology

Access to Document

10.1016/j.bbrc.2006.05.006

Cite this

@article{464b85fa3fd442ec95cb05d04579e006,

title = "α-Bulnesene, a novel PAF receptor antagonist isolated from Pogostemon cablin",

abstract = "α-Bulnesene is a sesquiterpenoid isolated from the water extract of Pogostemon cablin. It showed a potent and concentration-dependent inhibitory effect on platelet-activating factor (PAF) and arachidonic acid (AA) induced rabbit platelet aggregation. In a radioligand binding assay for the PAF receptor, α-bulnesene competitively inhibited [3H]PAF binding to the PAF receptor with an IC50 value of 17.62 ± 5.68 μM. α-Bulnesene also dose-dependently inhibited PAF-induced intracellular Ca2+ increase in fluo-3/AM-loaded platelets (IC50 values of 19.62 ± 1.32 μM). Furthermore, α-bulnesene inhibited AA-induced thromboxane B2 (TXB2) formation and prostaglandin E2 (PGE2) formation. These results indicate that the inhibitory effect of α-bulnesene on platelet aggregation was due to a dual activity; specifically the chemical blocked PAF-induced intracellular signal transduction and interfered with cyclooxygenase activity, which resulted in a decrease in thromboxane formation. This study is the first to demonstrate that α-bulnesene is a PAF receptor antagonist as well as an anti-platelet aggregation agent.",

keywords = "α-Bulnesene, Arachidonic acid (AA), Platelet aggregation, Platelet-activating factor (PAF), Pogostemon cablin, Sesquiterpenoid",

author = "HuiChun Hsu and Yang, {Wen Chia} and Tsai, {Wei Jern} and Chen, {Chien Chih} and Huang, {Hui Yu} and Tsai, {Ying Chieh}",

year = "2006",

month = jul,

day = "7",

doi = "10.1016/j.bbrc.2006.05.006",

language = "English",

volume = "345",

pages = "1033--1038",

journal = "Biochemical and Biophysical Research Communications",

issn = "0006-291X",

publisher = "Elsevier B.V.",

number = "3",

}

TY - JOUR

T1 - α-Bulnesene, a novel PAF receptor antagonist isolated from Pogostemon cablin

AU - Hsu, HuiChun

AU - Yang, Wen Chia

AU - Tsai, Wei Jern

AU - Chen, Chien Chih

AU - Huang, Hui Yu

AU - Tsai, Ying Chieh

PY - 2006/7/7

Y1 - 2006/7/7

N2 - α-Bulnesene is a sesquiterpenoid isolated from the water extract of Pogostemon cablin. It showed a potent and concentration-dependent inhibitory effect on platelet-activating factor (PAF) and arachidonic acid (AA) induced rabbit platelet aggregation. In a radioligand binding assay for the PAF receptor, α-bulnesene competitively inhibited [3H]PAF binding to the PAF receptor with an IC50 value of 17.62 ± 5.68 μM. α-Bulnesene also dose-dependently inhibited PAF-induced intracellular Ca2+ increase in fluo-3/AM-loaded platelets (IC50 values of 19.62 ± 1.32 μM). Furthermore, α-bulnesene inhibited AA-induced thromboxane B2 (TXB2) formation and prostaglandin E2 (PGE2) formation. These results indicate that the inhibitory effect of α-bulnesene on platelet aggregation was due to a dual activity; specifically the chemical blocked PAF-induced intracellular signal transduction and interfered with cyclooxygenase activity, which resulted in a decrease in thromboxane formation. This study is the first to demonstrate that α-bulnesene is a PAF receptor antagonist as well as an anti-platelet aggregation agent.

AB - α-Bulnesene is a sesquiterpenoid isolated from the water extract of Pogostemon cablin. It showed a potent and concentration-dependent inhibitory effect on platelet-activating factor (PAF) and arachidonic acid (AA) induced rabbit platelet aggregation. In a radioligand binding assay for the PAF receptor, α-bulnesene competitively inhibited [3H]PAF binding to the PAF receptor with an IC50 value of 17.62 ± 5.68 μM. α-Bulnesene also dose-dependently inhibited PAF-induced intracellular Ca2+ increase in fluo-3/AM-loaded platelets (IC50 values of 19.62 ± 1.32 μM). Furthermore, α-bulnesene inhibited AA-induced thromboxane B2 (TXB2) formation and prostaglandin E2 (PGE2) formation. These results indicate that the inhibitory effect of α-bulnesene on platelet aggregation was due to a dual activity; specifically the chemical blocked PAF-induced intracellular signal transduction and interfered with cyclooxygenase activity, which resulted in a decrease in thromboxane formation. This study is the first to demonstrate that α-bulnesene is a PAF receptor antagonist as well as an anti-platelet aggregation agent.

KW - α-Bulnesene

KW - Arachidonic acid (AA)

KW - Platelet aggregation

KW - Platelet-activating factor (PAF)

KW - Pogostemon cablin

KW - Sesquiterpenoid

UR - http://www.scopus.com/inward/record.url?scp=33646837647&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33646837647&partnerID=8YFLogxK

U2 - 10.1016/j.bbrc.2006.05.006

DO - 10.1016/j.bbrc.2006.05.006

M3 - Article

C2 - 16712790

AN - SCOPUS:33646837647

SN - 0006-291X

VL - 345

SP - 1033

EP - 1038

JO - Biochemical and Biophysical Research Communications

JF - Biochemical and Biophysical Research Communications

IS - 3

ER -

α-Bulnesene, a novel PAF receptor antagonist isolated from Pogostemon cablin

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this