Alpha-bulnesene, a novel PAF receptor antagonist isolated from Pogostemon cablin.

Abstract:

:Alpha-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, alpha-bulnesene competitively inhibited [(3)H]PAF binding to the PAF receptor with an IC(50) value of 17.62+/-5.68microM. alpha-Bulnesene also dose-dependently inhibited PAF-induced intracellular Ca(2+) increase in fluo-3/AM-loaded platelets (IC(50) values of 19.62+/-1.32microM). Furthermore, alpha-bulnesene inhibited AA-induced thromboxane B(2) (TXB(2)) formation and prostaglandin E(2) (PGE(2)) formation. These results indicate that the inhibitory effect of alpha-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 alpha-bulnesene is a PAF receptor antagonist as well as an anti-platelet aggregation agent.

authors

Hsu HC,Yang WC,Tsai WJ,Chen CC,Huang HY,Tsai YC

doi

10.1016/j.bbrc.2006.05.006

subject

Has Abstract

pub_date

2006-07-07 00:00:00

pages

1033-8

issue

3

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(06)01030-8

journal_volume

345

pub_type

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