Econazole nitrate

Econazole nitrate is an effective inducer of micronuclei over a narrow dose range in cell lines V79, XEM2 and XEMd-MZ (expresses CYP1A2). ^[1] Econazole nitrate inhibits the proliferation of MCF-7 cells in a time- and dose-dependent manner by MTT method and colony forming assay. Econazole nitrate results in typical characteristics of apoptosis including the morphological changes and DNA fragmentation in MCF-7 cells. Econazole nitrate results in the decrease expression of procaspase-3, procaspase-9 and bcl-2. ^[2] Econazole inhibits ADP-ribose-activated currents in HEK-293 cells expressing recombinant human TRPM2 (hTRPM2). Econazole produces an essentially complete inhibition of the TRPM2-mediated current. ^[3] Econazole (25-50 mM) partially inhibits capacitative Ca2+ entry induced by cyclopiazonic acid, another endoplasmic reticulum Ca2+ pump inhibitor. Econazole induces Ca2+ influx via two separate pathways: one is sensitive to La3+, the other is not. ^[4] Econazole reversibly inhibits (Bu)(2)cAMP-stimulated progesterone production in a dose- and time-dependent manner in MA-10 cells without affecting total protein synthesis or P450(scc) and 3beta-hydroxysteroid dehydrogenase (3beta-HSD) enzyme expression or activity. ^[5] Econazole is a store-operated Ca2+ channel antagonist which induces cytotoxic cell death of leukemia. Econazole (5-20 mM) arrests human colon cancer cells at the G0/G1 phase of the cell cycle. Econazole induces COLO 205 cells apoptosis evidenced by ladder formation in DNA fragmentation assay and sub-G1 peak. ^[6]