4.3 Article

Vasorelaxant effects of the monoterpenic phenol isomers, carvacrol and thymol, on rat isolated aorta

期刊

FUNDAMENTAL & CLINICAL PHARMACOLOGY
卷 24, 期 3, 页码 341-350

出版社

WILEY
DOI: 10.1111/j.1472-8206.2009.00768.x

关键词

carvacrol; excitation-contraction coupling; isolated aorta; thymol; vasorelaxant

资金

  1. Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES)
  2. Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)

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Various essential oils are rich in carvacrol, a monoterpenic phenol isomeric with thymol. This study was undertaken to assess the vasorelaxant effects of thymol and carvacrol in rat isolated aorta and the putative mechanisms underlying these effects. Thymol and carvacrol produced a concentration-dependent relaxation on the aortic ring preparations pre-contracted using KCl (IC50 value of 64.40 +/- 4.41 and 78.80 +/- 11.91 mu m, respectively) or using phenylephrine (PHE, 0.1 mu m) (IC50 value of 106.40 +/- 11.37 and 145.40 +/- 6.07 mu m, respectively) and inhibited the concentration-response curves of aortic rings to PHE or KCl. In Ca2+-free medium with ethylene glycol-bis(2-aminoethylether)-N,N,N',N'-tetraacetic acid (2 mm), thymol and carvacrol both at 1000 mu m completely abolished the phasic component of PHE-induced endothelium-containing ring contractions. At 400 mu m, thymol and carvacrol significantly reduced the CaCl2-induced contractions in Ca2+-free medium. Furthermore, both thymol and carvacrol (300 and 1000 mu m) significantly reduced the contraction evoked by phorbol dibutyrate (1 mu m), an activator of protein kinase C. Magnitude of this inhibitory effect was enhanced in the presence of the Ca2+ pump inhibitor, thapsigargin (1 mu m). At 1000 mu m, neither thymol nor carvacrol altered the resting potential of vascular smooth muscle cells. In conclusion, thymol and carvacrol induced an endothelium-independent relaxation in rat isolated aorta, an effect that seems mediated through some mechanisms probably involving a transduction pathway between Ca2+ release from sarcoplasmic reticulum and/or regulation of the Ca2+ sensitivity of the contractile system. Moreover, it's conceivable that thymol and carvacrol, at low concentrations, block the Ca2+ influx through the membrane.

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