Characterisation of marrubenol, a diterpene extracted from Marrubium vulgare, as an L-type calcium channel blocker
(2003) British Journal of Pharmacology — Vol. 140, n° 7, p. 1211-1216 (2003)
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- 1. 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 mM KCl (IC50: 11.8+/-0.3 microM, maximum relaxation: 93+/-0.6%) than of the contraction evoked by noradrenaline (maximum relaxation: 30+/-1.5%). 2. In fura-2-loaded aorta, marrubenol simultaneously inhibited the Ca2+ signal and the contraction evoked by 100 mM KCl, and decreased the quenching rate of fura-2 fluorescence by Mn2+. 3. Patch-clamp data obtained in aortic smooth muscle cells (A7r5) indicated that marrubenol inhibited Ba2+ inward current in a voltage-dependent manner (KD: 8+/-2 and 40+/-6 microM at holding potentials of -50 and -100 mV, respectively). 4. These results showed that marrubenol inhibits smooth muscle contraction by blocking L-type calcium channels.
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El-Bardai, S., Wibo, M., Hamaide, M.-C., Lyoussi, B., Quetin-Leclercq, J., & Morel, N. (2003). Characterisation of marrubenol, a diterpene extracted from Marrubium vulgare, as an L-type calcium channel blocker. British Journal of Pharmacology, 140(7), 1211-1216. https://doi.org/10.1038/sj.bjp.0705561 (Original work published 2003)