Vascular activity of a natural diterpene isolated from Croton zambesicus and of a structurally similar synthetic trachylobane.

Martinsen, Anneloes, Baccelli, Chiara, Navarro, Ismael, Abad, Antonio, Quetin-Leclercq, Joelle and Morel, Nicole (2010) Vascular activity of a natural diterpene isolated from Croton zambesicus and of a structurally similar synthetic trachylobane. Vascular Pharmacology, 52 (1). pp. 63-69. ISSN 1537-1891

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Abstract

The aim of this study was to determine the vasorelaxant activity of a natural diterpene extracted from Croton zambesicus, ent-18-hydroxy-trachyloban-3-one (DT6), and a synthetic diterpene of similar structure, ent-trachyloban-14,15-dione (DT10) in rat aorta. DT6 and DT10 inhibited aorta contraction in a concentration-dependent manner. Both were more potent inhibitors of KCl-evoked contraction than noradrenaline-evoked contraction. Nitric oxide (NO) synthase inhibition did not significantly affect DT6 effect whereas it significantly decreased DT10 inhibitory potency. In fura-2 loaded aorta rings, DT10 simultaneously inhibited KCl-evoked contraction and cytosolic calcium increase in a concentration-dependent manner. Furthermore, DT10 significantly inhibited calcium channel current recorded by the patch-clamp technique in human neuroblastoma cells SH-SY5Y. However, despite potentiation of 8-bromo-cGMP-response, DT6 and DT10 as verapamil depressed acetylcholine-evoked relaxation, DT6 being the most potent, while only DT6 and DT10 depressed SNAP-evoked relaxation. In conclusion, these data suggest that vasorelaxant activity of diterpenes (DT) is associated with the blockade of L-type voltage-operated calcium channels. Inhibition of NO-dependent relaxation by DT could be related to a decrease in NO availability.

Item Type: Article
Faculty \ School: Faculty of Medicine and Health Sciences > Norwich Medical School
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Depositing User: Pure Connector
Date Deposited: 21 Sep 2015 09:16
Last Modified: 22 Apr 2020 08:49
URI: https://ueaeprints.uea.ac.uk/id/eprint/54352
DOI: 10.1016/j.vph.2009.11.002

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