Ellagic acid

Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC₅₀ of 40 nM and a K_i of 20 nM. IC50 & Target:IC50: 40 nM (CK2)^[1]
Ki: 20 (CK2)^[1] In Vitro:Ellagic acid is a potent CK2 inhibitor, with an IC₅₀ of 40 nM and a K_i of 20 nM. Ellagic acid also blocks other kinases such as LYN, PKA, SYK, GSK3, FGR and CK1, with IC₅₀s of 2.9, 3.5, 4.3, 7.5, 9.4 and 13.0 μM, respectively, and shows no obvious effects on DYRK1a, CSK, NPM-ALK, RET and FLT3 (IC₅₀s > 40 μM). Ellagic acid (5-100 μM) shows inhibitory activities against Karpas299, SUDHL1, SR786, and FE-PD cell lines^[1]. Ellagic acid (10 μM) exhibits cytotoxic effects on MCF-7 cells after treatment of radiation. Ellagic acid (10 μM) in combination with Irradiation (IR) significantly abridges the capacity of MCF-7 cells to form colonies equated with individual treatments. Ellagic acid with IR also induces cell apoptosis, and facilitates the upregulation of pro-apopttotic Bax and downregulation of Bcl-2 in MCF-7 cells^[3]. In Vivo:Ellagic acid (EA; 10 mg/kg/day; p.o., 14 days) strongly decreases MDA brain content by 17%, and reduces the levels of brain TNF-α by 42% in rats. Ellagic acid markedly increases the reduced brain contents of 5-HT (39%), dopamine (DA, 71%), and norepinephrine (NE, 77%). Ellagic acid (10 mg/kg, p.o., 14 days) causes decreased histopathological changes induced by Doxorubicin in rats^[2].