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Characterisation of marrubenol, a diterpene extracted from Marrubium vulgare , as an L‐type calcium channel blocker
Author(s) -
El Bardai Sanae,
Wibo Maurice,
Hamaide MarieChristine,
Lyoussi Badiaa,
QuetinLeclercq Joëlle,
Morel Nicole
Publication year - 2003
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0705561
Subject(s) - contraction (grammar) , chemistry , calcium , voltage dependent calcium channel , muscle contraction , calcium channel blocker , smooth muscle , patch clamp , channel blocker , calcium channel , biophysics , aorta , endocrinology , medicine , biochemistry , biology , receptor , organic chemistry
The objective of the present study was to investigate the mechanism of the relaxant activity of marrubenol, a diterpenoid extracted from Marrubium vulgare . In rat aorta, marrubenol was a more potent inhibitor of the contraction evoked by 100 m M KCl (IC 50 : 11.8±0.3 μ M , maximum relaxation: 93±0.6%) than of the contraction evoked by noradrenaline (maximum relaxation: 30±1.5%). In fura‐2‐loaded aorta, marrubenol simultaneously inhibited the Ca 2+ signal and the contraction evoked by 100 m M KCl, and decreased the quenching rate of fura‐2 fluorescence by Mn 2+ . Patch‐clamp data obtained in aortic smooth muscle cells (A7r5) indicated that marrubenol inhibited Ba 2+ inward current in a voltage‐dependent manner ( K D : 8±2 and 40±6 μ M at holding potentials of −50 and −100 mV, respectively). These results showed that marrubenol inhibits smooth muscle contraction by blocking L‐type calcium channels.British Journal of Pharmacology (2003) 140 , 1211–1216. doi: 10.1038/sj.bjp.0705561