Türk Biyokimya Dergisi [Turkish Journal of Biochemistry], 2013, v. 38, n. 2, p. 126–132
Turkish Biochemical Society
Fecha de publicación :
Introduction: Econazole, an azole compound widely used as an antifungal drug, is currently investigated for additional therapeutic effects. In fact, the antitumoral properties of econazole have been recently demonstrated, both in vivo and at the cellular level. However, the precise mechanism of action behind its effects is still unclear.
Aim: To examine the effect of econazole on intracellular Ca2+ signaling pathways in a human adenocarcinoma cell line.
Methods: [Ca2+]i was measured in Fura 2-loaded HT29 cells by fluorescence. Fluorescence was recorded from 1ml aliquots of magnetically stirred HT29 cells using a Cary Eclipse Spectrophotometer (Varian Ltd., Madrid, Spain) with excitation wavelengths of 340 and 380 nm and emission at 510 nm.
Results: We have demonstrated that econazole has a dual effect on Ca2+ homeostasis. It caused a dose-dependent increase in [Ca2+]i. Both mobilization from thapsigargin-sensitive
stores and extracellular Ca2+ influx contributed to the effect. A phospholipase C-dependent pathway proved to be activated by econazole. In addition, econazole greatly inhibited a physiological activation of store-operated Ca2+ entry.
Conclusion: This study provides further molecular mechanism of econazole suggesting that this drug may modify the physiology of human adenocarcinoma HT29 cell line.