Article ID Journal Published Year Pages File Type
2480893 European Journal of Pharmaceutical Sciences 2013 8 Pages PDF
Abstract

The present study investigated the mechanisms underlying the vasorelaxant effects of the essential oil of Aniba canelilla (EOAC) and its main constituent 1-nitro-2-phenylethane (NP) in isolated superior mesenteric artery from spontaneously hypertensive rats (SHRs). At 0.1–1000 μg/mL, EOAC and NP relaxed SMA preparations pre-contracted with 75 mM KCl with IC50 (geometric mean [95% confidence interval]) values of 294.19 [158.20–94.64] and 501.27 [378.60–624.00] μg/mL, respectively); or with phenylephrine (PHE) (IC50s = 11.07 [6.40–15.68] and 7.91 [4.08–11.74) μg/mL, respectively). All these effects were reversible and remained unaltered by vascular endothelium removal. In preparations maintained under Ca2+-free conditions, EOAC and NP (both at 600 μg/mL) reduced the PHE-, but not the caffeine-induced contraction. In Ca2+-free and high K+ (75 mM) medium, the contractions produced by CaCl2 or BaCl2 were reduced or even abolished by EOAC and NP at 100 and 600 μg/mL, respectively. EOAC and NP (both at 10–1000 μg/mL) also relaxed the contraction evoked by phorbol dibutyrate (IC50 = 52.66 [10.82–94.64] and 39.13 [31.55–46.72] μg/mL, respectively). It is concluded that NP has a myogenic endothelium-independent vasorelaxant effects and appears to be the active principle of the EOAC. Vasorelaxant effect induced by both EOAC and NP is preferential to receptor-activated pathways and it appears to occur intracellularly more than a superficial action restricted to the membrane environment such as a simple blocking activity on a given receptor or ion channel.

Graphical abstractFigure optionsDownload full-size imageDownload high-quality image (226 K)Download as PowerPoint slide

Related Topics
Health Sciences Pharmacology, Toxicology and Pharmaceutical Science Drug Discovery
Authors
, , , , , , , ,