Inhibition of protein kinase CKII activity by resveratrol, a natural compound in red wine and grapes

• Published in: Life sciences (1973) 2002-09, Vol.71 (18), p.2145-2152
• Main Authors: Yoon, Soo-Hyun, Kim, Yun-Sook, Ghim, Sa-Youl, Song, Bang-Ho, Bae, Young-Seuk
• Format: Article
• Language: English
• Subjects: Adenosine Triphosphate - metabolism; Anticancer drug; Anticarcinogenic Agents - pharmacology; Casein Kinase II; Catalysis; Enzyme inhibitor; Enzyme Inhibitors - pharmacology; HeLa Cells; Humans; Indicators and Reagents; Kinetics; Phosphorylation; Protein kinase CKII; Protein-Serine-Threonine Kinases - antagonists & inhibitors; Resveratrol; Stilbenes - pharmacology; Vitis - chemistry; Wine - analysis
• ISSN: 0024-3205; 1879-0631
• DOI: 10.1016/S0024-3205(02)01997-5

Resveratrol is a phytoalexin found in grapes and other foods that has been shown to have anticancer and anti-inflammatory effects. Because protein kinase CKII is involved in cell proliferation and oncogenesis, we examined whether resveratrol could modulate CKII activity. Resveratrol was shown to inhibit the phosphotransferase activity of CKII with IC 50 of about 10 μM. Steady state studies revealed that resveratrol acted as a competitive inhibitor with respect to the substrate ATP. A value of 1.2 μM was obtained for the apparent K i. Resveratrol also inhibited the catalytic reaction of CKII with GTP as substrate. Furthermore, resveratrol inhibits endogenous CKII activity on protein substrates in HeLa cell lysates. These results suggest that resveratrol is likely to function by inhibiting oncogenic disease, at least in part, through the inhibition of CKII activity.