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 journalArticle

34 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 languageEnglish
Pages (from-to)1033-1038
Number of pages6
JournalBiochemical and Biophysical Research Communications
Volume345
Issue number3
DOIs
Publication statusPublished - Jul 7 2006
Externally publishedYes

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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