Geraniol Blocks Calcium and Potassium Channels in the Mammalian Myocardium: Useful Effects to Treat Arrhythmias.

Autor: Menezes‐Filho, José Evaldo Rodrigues, Gondim, Antônio Nei Santana, Cruz, Jader Santos, Souza, Américo Azevedo, Santos, José Nilson Andrade dos, Conde‐Garcia, Eduardo Antônio, Sousa, Damião Pergentino, Santos, Michel Santana, Oliveira, Evaleide Diniz, Vasconcelos, Carla Maria Lins
Předmět:
Zdroj: Basic & Clinical Pharmacology & Toxicology; Dec2014, Vol. 115 Issue 6, p534-544, 11p
Abstrakt: 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 Ca2+ 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 ICa,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 ( IK1) (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 Ca2+ and voltage-gated K+ currents, ultimately acting against ouabain-induced arrhythmias. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index