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- Title
Characterisation of marrubenol, a diterpene extracted from Marrubium vulgare, as an L-type calcium channel blocker.
- Authors
Bardai, Sanae El; Wibo, Maurice; Hamaide, Marie-Christine; Lyoussi, Badiaa; Quetin-Leclercq, Joelle; Morel, Nicole
- Abstract
1 The objective of the present study was to investigate the mechanism of the rulaxant activity of marrubenol, a diterpenoid extracted from MarrubiumVulgare. In rat aorta, marrubenol was a more potent inhibitor of the contraclion evoked by 100 m M KCI IC[sub50]: 11.8 ±0.3μM, maximum relaxation. 93±0.6%) than of the confraction evoked by noradrenaline (maximum relaxation: 30±1.5%) 2 In fura-2-loaded aoria. marrubenol simultaneously inhibited the Ca[sup2+] signal and the contraction evoked by 100 m M KCI. and decreased the quenching rate of fura-2 flora fluoresence by Mn[sup2-] 3 Patch-clamp data obtained in aortic smooth muscle cells (A7r5) indicated that marrubenol inhibited Ba [sub2+] inward current in a voltage-dependent manner (K[subp] 8&plumn;2 and 40 ± 6μM at holding potentials of -50 and -100mV. respectively ). 4 These results showed that marrubenol inhibits smooth muscle contracion by blocking L-type culcium channels.
- Subjects
MARRUBIUM; CALCIUM antagonists; CALCIUM channels; ANTIHYPERTENSIVE agents; TRADITIONAL medicine; SMOOTH muscle; FURANS; THERAPEUTICS
- Publication
British Journal of Pharmacology, 2003, Vol 140, Issue 7, p1211
- ISSN
0007-1188
- Publication type
Article
- DOI
10.1038/sj.bjp.0705561