Apigenin

Apigenin is a flavonoid compound found in many fruits and vegetables that selectively inhibits casein kinase 2 (CK2). Apigenin inhibits CK2 activity in the renal cortex with an IC₅₀ value of 30 µM to improve renal function in a rat model of glomerulonephritis.¹ CK2 inhibition by 20 µM apigenin decreases the degradation of IκBα and down-regulates NF-κB levels in WEHI-231 cells.² Apigenin at 5 µM is a potent inhibitor of the synthesis of the inflammatory mediators nitric oxide and prostaglandin E₂, reducing inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression by 56% and 64%, respectively, in the macrophage cell line J774A.1.³

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1. Yamada, M., Katsuma, S., Adachi, T., et al. Inhibition of protein kinase CK2 prevents the progression of glomerulonephritis. Proc. Natl. Acad. Sci. USA 102(21), 7736-7741 (2005).

2. Shen, J., Channavajhala, P., Seldin, D.C., et al. Phosphorylation by the protein kinase CK2 promotes calpain-mediated degradation of IκBα1. J. Immunol. 167(9), 4919-4925 (2001).

3. Raso, G.M., Meli, R., Di Carlo, G., et al. Inhibition of inducible nitric oxide synthase and cyclooxygenase-2 expression by flavonoids in macrophage J774A.1. Life Sci. 68(8), 921-931 (2001).