Department of Chemistry, Indian Institute of Technology, Kharagpur 721 302, India.
Bioorg Med Chem. 2010 Sep 1;18(17):6538-46. doi: 10.1016/j.bmc.2010.06.077. Epub 2010 Jun 25.
The reported ribonuclease A inhibitory activity of the green tea extracts prompted us to synthesize novel catechin/epicatechin based conjugates with resorcinol and phloroglucinol with the aim to increase the number of phenolic OH groups. These are found to be more effective inhibitors of ribonuclease A as compared to catechin and epicatechin thus indicating the importance of number of phenolic OH groups for the inhibition of ribonucleolytic activity. Fluorescence studies have been carried out to evaluate the binding parameters. The protein-ligand docking studies are also performed to gain insight into the protein-polyphenols interactions. The epicatechin based polyphenols 1 and 2 also showed inhibition of angiogenin-induced angiogenesis, as determined by chorioallantoic membrane (CAM) assay.
绿茶提取物具有报道的核糖核酸酶 A 抑制活性，这促使我们合成新型以儿茶素/表儿茶素为基础的与间苯二酚和邻苯三酚的缀合物，目的是增加酚羟基的数量。与儿茶素和表儿茶素相比，这些化合物被发现是更有效的核糖核酸酶 A 抑制剂，这表明酚羟基数量对核糖核酸酶抑制活性的重要性。进行了荧光研究来评估结合参数。还进行了蛋白质-配体对接研究，以深入了解蛋白质-多酚相互作用。儿茶素基多酚 1 和 2 也显示出对绒毛尿囊膜（CAM）测定法测定的血管生成素诱导的血管生成的抑制作用。
