Abstract

Esculetin (6,7-dihydrocoumarin) and the flavonoid quercetin (3,5,7,3',4' pentahydroxyflavone) show different pharmacological properties probably related to effects on redox homeostasis. Human leukemia NB4 cells were preincubated for 30 min or 2 h with either 100 μM esculetin or 25 μM quercetin. The cells were then treated with 1 mM H2O2 or 250 μM tert-butyl hydroperoxide (t-BHP) for 1 h. Pretreatments with quercetin prevented loss of cell viability (impermeability to PI) induced by H2O2 or t-BHP. Treatment with 1 mM H2O2 for 1 h produced lower apoptotic cells (26%) than 250 μM t-BHP (38%). Pretreatments with esculetin increased the apoptosis induced by H2O2 but reduced significantly the apoptosis produced by t-BHP. Quercetin reduced apoptosis produced by H2O2 and wholly protects against apoptosis induced by t-BHP. Superoxide was increased by treatment with H2O2 or t-BHP. Esculetin or quercetin increased the levels of superoxide in cells treated with H2O2 but reduced them in cells treated with t-BHP. Esculetin but not quercetin almost prevented peroxide production by H2O2. Our results show different effects of antioxidant treatment on leukemia cells and possible differential applications for antitumor therapy with either of those antioxidant compounds used.

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