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DNA and Cell Biology
Catechin Conjugated with Fatty Acid Inhibits DNA Polymerase and Angiogenesis

To cite this article:
Kiminori Matsubara, Akiko Saito, Akira Tanaka, Noriyuki Nakajima, Reiko Akagi, Masaharu Mori, Yoshiyuki Mizushina. DNA and Cell Biology. February 2006, 25(2): 95-103. doi:10.1089/dna.2006.25.95.

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Kiminori Matsubara, Ph.D.
Department of Nutritional Science, Faculty of Health and Welfare Science, Okayama Prefectural University, Okayama, Japan.
Akiko Saito
Biotechnology Center, Toyama Prefecture, Toyama, Japan.
Akira Tanaka
Department of Bioresources Science, College of Technology, Toyama Prefectural University, Toyama, Japan.
Noriyuki Nakajima
Biotechnology Research Center, Toyama Prefectural University, Toyama, Japan.
Reiko Akagi
Department of Nutritional Science, Faculty of Health and Welfare Science, Okayama Prefectural University, Okayama, Japan.
Masaharu Mori
Department of Nursing, Faculty of Health and Welfare Science, Okayama Prefectural University, Okayama, Japan.
Yoshiyuki Mizushina
Department of Nutritional Science, Kobe-Gakuin University, Kobe, Japan.
High Technology Research Center, Kobe-Gakuin University, Kobe, Japan.

Catechins in green tea have anticancer and antiangiogenesis activities, with epigallocatechin-3-gallate (EGCG) being the most potent antiangiogenic tea catechin. This study examined whether chemical modification of catechin enhanced anticancer and antiangiogenic effects. Catechin, conjugated with fatty acid (acyl-catechin), strongly inhibited DNA polymerase, HL-60 cancer cell growth, and angiogenesis. Catechin conjugated with stearic acid [(2R,3S)-3′,4′,5,7-tetrahydroxyflavan-3-yl octadecanoate; catechin-C18] was the strongest inhibitor in DNA polymerase α and β and angiogenesis assays. Catechin-C18 also suppressed human endothelial cell (HUVEC) tube formation on the reconstituted basement membrane, suggesting that it affected not only DNA polymerases but also signal transduction pathways in HUVECs. These data indicate that acyl-catechins target both DNA polymerases and angiogenesis as anticancer agents. These results suggest that acylation of catechin is an effective chemical modification to improve the anticancer activity of catechin.

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Specific Inhibitors of Mammalian DNA Polymerase Species
Yoshiyuki MIZUSHINA
Bioscience, Biotechnology, and Biochemistry. Feb 2009, Vol. 73, No. 6: 1239-1251
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