IMR Press / FBE / Volume 3 / Issue 4 / DOI: 10.2741/E337

Frontiers in Bioscience-Elite (FBE) is published by IMR Press from Volume 13 Issue 2 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.

Acylated catechin derivatives: inhibitors of DNA polymerase and angiogenesis
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1 Laboratory of Food and Nutritional Sciences, Department of Nutritional Science, Kobe-Gakuin University, Nishi-ku, Kobe, Hyogo 651-2180, Japan
2 Cooperative Research Center of Life Sciences, Kobe-Gakuin University, Chuo-ku, Kobe, Hyogo 651- 8586, Japan
3 Department of Applied Chemistry, Faculty of Engineering, Osaka Electro-Communication University, Neyagawashi, Osaka 572-8530, Japan
4 Department of Biotechnology, Faculty of Engineering, Toyama Prefectural University, Imizu, Toyama 939-0398, Japan
5 Department of Bioresources Science, College of Technology, Toyama Prefectural University, Kosugi, Toyama 939-0398, Japan
6 Department of Human Life Science Education, Graduate School of Education, Hiroshima University, Higashi-Hiroshima, Hiroshima 739-8524, Japan

*Author to whom correspondence should be addressed.


Front. Biosci. (Elite Ed) 2011, 3(4), 1337–1348;
Published: 1 June 2011

We previously found that some catechins, such as epigallocatechin-3-O-gallate (EGCG), inhibit the activities of eukaryotic DNA polymerases (pols). In this study, we found that catechins conjugated with fatty acid (3-O-acylcatechins) are stronger inhibitors of mammalian pol than epicatechins conjugated with fatty acid (3-O-acylepicatechins). Moreover, 3-O-acylcatechins are more potent inhibitors of cultured cell growth both of the human colon carcinoma cell line (HCT116 cells) and human umbilical vein endothelial cell (HUVEC) line, as well as angiogenesis by comparison with 3-O-acylepicatechins. Catechin conjugated with stearic acid [(2R,3S)-3',4',5,7- tetrahydroxyflavan-3-yl octadecanoate; C-C18] was the strongest inhibitor in replicative pol alpha and repairrelated pol beta, as well as the cultured cell growth and angiogenesis assays in the compounds tested. C-C18 also suppressed HUVEC tube formation on reconstituted basement membrane suggesting that it affected not only pols but also signal transduction pathways in HUVECs. These data indicate that the acylated catechins target both pols and angiogenesis as anti-cancer agents. Moreover, the results suggest that acylation of catechin is an effective chemical modification to improve the anti-cancer activity of catechin.

Acylated catechin derivative
Cultured cell growth
DNA polymerase
Enzyme inhibitor
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