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

48 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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

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

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10.1016/j.bbrc.2006.05.006

Cite this

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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\}",

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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

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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

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

Abstract

UN SDGs

Keywords

ASJC Scopus subject areas

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