Journal
FITOTERAPIA
Volume 90, Issue -, Pages 85-93Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.fitote.2013.07.010
Keywords
Aconitum napellus L. subsp firmum; Diterpene alkaloids; GIRK; hERG; Cardiovascular ion channels
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Funding
- New Hungary Development Plan project [TAMOP-4.2.2.A-11/1/KONV-2012-0035, NKFP_07A1 RYT07_AF]
- Gedeon Richter Talentum Foundation
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Diterpene alkaloids neoline (1), napelline (2), isotalatizidine (3), karakoline (4), senbusine A (5), senbusine C (6), aconitine (7) and taurenine (8) were identified from Aconitum napellus L subsp.firmum, four (2-4, 6) of which are reported for the first time from this plant The structures were determined by means of LC-MS, 1D and 2D NMR spectroscopy, including H-1-H-1 COSY, NOESY, HSQC and HMBC experiments. Electrophysiological effects of the isolated compounds, together with nine diterpene alkaloids previously obtained from Aconitum toxicum and Consolida orientalis were investigated on stable transfected HEK-hERG (Kv11.1) and HEK-G1RK1/4 (Kir3.1 and Kir3.4) cell lines using automated patch clamp equipment Significant blocking activity on GIRK channel was exerted by aconitine (7) (45% at 10 mu M), but no blocking activities of the other investigated compounds were detected. The tested compounds were inactive on hERG channel in the tested concentration. The comparison of the previously reported metabolites of A. napellus subsp. firmum and compounds identified in our experiment reveals substantial variability of the alkaloid profile of this taxon. (C) 2013 Elsevier B.V. All rights reserved.
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