A phenolic compound that acts as a 5-LO and 12-LO inhibitor
REVIEW Esculetin, a phenolic compound, acts as a 5-LO (5-lipoxygenase; 5-LOX) inhibitor. Esculetin is reported to display anti-inflammatory and antioxidant properties, as well as induce cell cycle arrest and apoptosis. In the presence of Esculetin and HA14-1 expression of the death receptor 4 (DR4) has been observed to be upregulated and extracellular-regulated kinase (ERK) to be activated. Other studies suggest that Esculetin upregulates death receptor 5 (DR5) protein expression, and enhances TRAIL-induced apoptosis. Additionally, reports demonstrate that Esculetin also inhibits the activity of 12-LO (12-lipoxygenase), and decreases leukotriene biosynthesis during 5-LO inhibition. IC50 data: ATPase: IC50 = 11.33 µM; A23187-induced LTC4 release: IC50 = 18 µM (mouse macrophage); A23187-induced PGE2 release: IC50 = 11 µM (mouse macrophage); Xanthine Oxidase: IC50 = 8.2 µM (human).
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