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1.
Braz. j. med. biol. res ; 47(4): 328-333, 8/4/2014. graf
Artículo en Inglés | LILACS | ID: lil-705768

RESUMEN

In cardiac and skeletal muscle, eugenol (μM range) blocks excitation-contraction coupling. In skeletal muscle, however, larger doses of eugenol (mM range) induce calcium release from the sarcoplasmic reticulum. The effects of eugenol are therefore dependent on its concentration. In this study, we evaluated the effects of eugenol on the contractility of isolated, quiescent atrial trabeculae from male Wistar rats (250-300 g; n=131) and measured atrial ATP content. Eugenol (1, 3, 5, 7, and 10 mM) increased resting tension in a dose-dependent manner. Ryanodine [100 µM; a specific ryanodine receptor (RyR) blocker] and procaine (30 mM; a nonspecific RyR blocker) did not block the increased resting tension induced by eugenol regardless of whether extracellular calcium was present. The myosin-specific inhibitor 2,3-butanedione monoxime (BDM), however, reversed the increase in resting tension induced by eugenol. In Triton-skinned atrial trabeculae, in which all membranes were solubilized, eugenol did not change resting tension, maximum force produced, or the force vs pCa relationship (pCa=-log [Ca2+]). Given that eugenol reduced ATP concentration, the increase in resting tension observed in this study may have resulted from cooperative activation of cardiac thin filaments by strongly attached cross-bridges (rigor state).


Asunto(s)
Animales , Masculino , Calcio/fisiología , Eugenol/farmacología , Acoplamiento Excitación-Contracción/efectos de los fármacos , Atrios Cardíacos/efectos de los fármacos , Fuerza Muscular/efectos de los fármacos , Contracción Miocárdica/efectos de los fármacos , Adenosina Trifosfato/análisis , Anestésicos Locales/farmacología , Eugenol/administración & dosificación , Técnicas In Vitro , Luciferasas , Músculo Esquelético/efectos de los fármacos , Procaína/farmacología , Ratas Wistar , Rianodina/farmacología
2.
Braz. j. med. biol. res ; 38(3): 453-461, mar. 2005. graf
Artículo en Inglés | LILACS | ID: lil-394796

RESUMEN

Eucalyptol is an essential oil that relaxes bronchial and vascular smooth muscle although its direct actions on isolated myocardium have not been reported. We investigated a putative negative inotropic effect of the oil on left ventricular papillary muscles from male Wistar rats weighing 250 to 300 g, as well as its effects on isometric force, rate of force development, time parameters, post-rest potentiation, positive inotropic interventions produced by Ca2+ and isoproterenol, and on tetanic tension. The effects of 0.3 mM eucalyptol on myosin ATPase activity were also investigated. Eucalyptol (0.003 to 0.3 mM) reduced isometric tension, the rate of force development and time parameters. The oil reduced the force developed by steady-state contractions (50 percent at 0.3 mM) but did not alter sarcoplasmic reticulum function or post-rest contractions and produced a progressive increase in relative potentiation. Increased extracellular Ca2+ concentration (0.62 to 5 mM) and isoproterenol (20 nM) administration counteracted the negative inotropic effects of the oil. The activity of the contractile machinery evaluated by tetanic force development was reduced by 30 to 50 percent but myosin ATPase activity was not affected by eucalyptol (0.3 mM), supporting the idea of a reduction of sarcolemmal Ca2+ influx. The present results suggest that eucalyptol depresses force development, probably acting as a calcium channel blocker.


Asunto(s)
Animales , Masculino , Ratas , Ciclohexanoles/farmacología , Monoterpenos/farmacología , Contracción Miocárdica/efectos de los fármacos , Aceites Volátiles/farmacología , Músculos Papilares/efectos de los fármacos , Retículo Sarcoplasmático/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Contracción Isométrica/efectos de los fármacos , Ratas Wistar , Miosinas del Músculo Esquelético/efectos de los fármacos
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