263711-74-6

Pale Yellow Crystalline Solid

The labelled aglucon of apiin and of apigenin-7-glucoside

Apigenin-d₅ is an internal standard for the quantificaiton of apigenin by GC- or LC-MS. 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. CK2 inhibition by 20 μM apigenin decreases the degradation of IκBα and down-regulates NF-κB levels in WEHI-231 cells. 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.

[1] MASATERU YAMADA. Inhibition of protein kinase CK2 prevents the progression of glomerulonephritis.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2005, 102 21: 7736-7741. DOI: 10.1073/pnas.0409818102
[2] JIAN SHEN. Phosphorylation by the Protein Kinase CK2 Promotes Calpain-Mediated Degradation of IκBα1[J]. The Journal of Immunology, 2001, 25 1: 4919-4925. DOI: 10.4049/jimmunol.167.9.4919
[3] GIUSEPPINA MATTACE RASO. Inhibition of inducible nitric oxide synthase and cyclooxygenase-2 expression by flavonoids in macrophage J774A.1[J]. Life sciences, 2001, 68 8: Pages 921-931. DOI: 10.1016/s0024-3205(00)00999-1