Inhibition of Protein Kinase CKII Activity by Euchrestaflavanone B Purified From Cudrania tricuspidata

Authors: Kim, Soon-Hee¹; Yoon, Soo-Hyun¹; Lee, Byong Won²; Park, Ki Hun³; Kim, Young Ho⁴; Bae, and Young-Seuk¹

Source: Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics, Volume 15, Number 6, 2005 , pp. 327-332(6)

Publisher: Cognizant Communication Corporation

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Abstract:

The CKII (EC 2.7.1.37) inhibitory compound was purified from the root barks of Cudrania tricuspidata and identified as (2 S)-2-[2,4-dihydroxy-5-(3-methyl-but-2-enyl)-phenyl]-5,7-dihyroxy-6-(3-methyl-but-2-enyl)-chroman-4-one (euchrestaflavanone B). Euchrestaflavanone B was shown to inhibit the phosphotransferase activity of CKII with IC₅₀ of about 78 μM. Steady-state studies revealed that euchrestaflavanone B acted as a competitive inhibitor with respect to the substrate ATP. A value of 16.4 μM was obtained for the apparent K _i. Concentration of 0.8 μM euchrestaflavanone B caused 50% growth inhibition of human cancer cells U937 and HeLa. Euchrestaflavanone B-induced cell death was characterized with the cleavage of poly(ADP-ribose) polymerase and procaspase-3, indicating that the inhibitor triggered apoptosis. Because protein kinase CKII is involved in cell proliferation and oncogenesis, these results suggest that euchrestaflavanone B may function by inhibiting oncogenic disease, at least in part, through the inhibition of CKII activity.

Keywords: Euchrestaflavanone B; Protein kinase CKII; Enzyme inhibitor; Apoptosis; Anticancer drug

Document Type: Research article

Affiliations: 1: Department of Biochemistry, College of Natural Sciences, Kyungpook National University, Daegu 702-701, Korea 2: Division of Applied Life Science, Department of Agricultural Chemistry, Gyeongsang National University, Jinju 660-701, Korea 3: *Department of Biochemistry, College of Natural Sciences, Kyungpook National University, Daegu 702-701, Korea 4: Department of Microbiology, College of Natural Sciences, Kyungpook National University, Daegu 702-701, Korea

Publication date: 2005-06-01

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Formerly: Oncology Research Incorporating Anti-Cancer Drug Design
Oncology Research Featuring Preclinical and Clincal Cancer Therapeutics publishes research of the highest quality that contributes to an understanding of cancer in areas of molecular biology, cell biology, biochemistry, biophysics, genetics, biology, endocrinology, and immunology, as well as studies on the mechanism of action of carcinogens and therapeutic agents, reports dealing with cancer prevention and epidemiology, and clinical trials delineating effective new therapeutic regimens.

Inhibition of Protein Kinase CKII Activity by Euchrestaflavanone B Purified From Cudrania tricuspidata

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