Literature DB >> 24862086

Geraniol blocks calcium and potassium channels in the mammalian myocardium: useful effects to treat arrhythmias.

José Evaldo Rodrigues de Menezes-Filho1, Antônio Nei Santana Gondim, Jader Santos Cruz, Américo Azevedo de Souza, José Nilson Andrade Dos Santos, Eduardo Antônio Conde-Garcia, Damião Pergentino de Sousa, Michel Santana Santos, Evaleide Diniz de Oliveira, Carla Maria Lins de Vasconcelos.   

Abstract

Geraniol is a monoterpene present in several essential oils, and it is known to have a plethora of pharmacological activities. In this study, we explored the contractile and electrophysiological properties of geraniol and its antiarrhythmic effects in the heart. The geraniol effects on atrial contractility, L-type Ca(2+) current, K(+) currents, action potential (AP) parameters, ECG profile and on the arrhythmia induced by ouabain were evaluated. In the atrium, geraniol reduced the contractile force (~98%, EC = 1,510 ± 160 μM) and diminished the positive inotropism of CaCl2 and BAY K8644. In cardiomyocytes, the IC a,L was reduced by 50.7% (n = 5) after perfusion with 300 μM geraniol. Moreover, geraniol prolonged the AP duration (APD) measured at 50% (n = 5) after repolarization, without changing the resting potential. The increased APD could be attributed to the blockade of the transient outward K(+) current (Ito ) (59.7%, n = 4), the non-inactivation K(+) current (Iss ) (39.2%, n = 4) and the inward rectifier K(+) current (IK 1 ) (33.7%, n = 4). In isolated hearts, geraniol increased PRi and QTi without affecting the QRS complex (n = 6), and it reduced both the left ventricular pressure (83%) and heart rate (16.5%). Geraniol delayed the time to onset of ouabain-induced arrhythmias by 128%, preventing 30% of the increase in resting tension (n = 6). Geraniol exerts its negative inotropic and chronotropic responses in the heart by decreasing both L-type Ca(2+) and voltage-gated K(+) currents, ultimately acting against ouabain-induced arrhythmias.
© 2014 Nordic Association for the Publication of BCPT (former Nordic Pharmacological Society).

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Year:  2014        PMID: 24862086     DOI: 10.1111/bcpt.12274

Source DB:  PubMed          Journal:  Basic Clin Pharmacol Toxicol        ISSN: 1742-7835            Impact factor:   4.080


  6 in total

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