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首页> 外文期刊>Life sciences >Epicatechin conjugated with fatty acid is a potent inhibitor of DNA polymerase and angiogenesis.
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Epicatechin conjugated with fatty acid is a potent inhibitor of DNA polymerase and angiogenesis.

机译：与脂肪酸结合的表儿茶素是一种有效的DNA聚合酶和血管生成抑制剂。

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摘要

Anti-cancer and anti-angiogenesis effects of green tea catechins have been demonstrated. It has been found that chemical modification of tea catechins improves their biological activities. We examined the chemical modification of epicatechin enhanced anti-cancer and anti-angiogenic effects. Epicatechin conjugated with fatty acid (acyl-catechin) strongly inhibited DNA polymerase activity, HL-60 cancer cell growth and angiogenesis. Epicatechin conjugated with palmitic acid ((2R,3R)-3',4',5,7-tetrahydroxyflavan-3-yl hexadecanoate, epicatechin-C16) was the strongest inhibitor in DNA polymerase alpha, beta, lambda and angiogenesis assays. Epicatechin-C16 also suppressed human endothelial cell (HUVEC) tube formation on reconstituted basement membrane, suggesting that it affected not only DNA polymerase activity but also the signal transduction pathways needed for the tube formation in HUVECs. These results suggest that acylation of epicatechin is an effective chemical modification to improve the anti-cancer activity of epicatechin.
机译：绿茶儿茶素具有抗癌和抗血管生成作用。已经发现茶儿茶素的化学改性改善了它们的生物活性。我们检查了表儿茶素的化学修饰增强的抗癌和抗血管生成作用。表儿茶素与脂肪酸（酰基儿茶素）结合可强烈抑制DNA聚合酶活性，HL-60癌细胞生长和血管生成。在棕榈酸（（2R，3R）-3'，4'，5,7-四羟基黄烷-3-基十六烷酸酯，Epicatechin-C16）上缀合的表儿茶素是DNA聚合酶α，β，λ和血管生成测定中最强的抑制剂。 Epicatechin-C16还抑制了重组基底膜上的人内皮细胞（HUVEC）管的形成，表明它不仅影响DNA聚合酶的活性，而且还影响HUVECs管形成所需的信号转导途径。这些结果表明，表儿茶素的酰化是改善表儿茶素的抗癌活性的有效化学修饰。

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