A.B. Hancock Jr. Memorial Laboratory for Cancer Research, Department of Biochemistry, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology, Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, Tennessee, USA.
Cancer Prev Res (Phila). 2011 Sep;4(9):1343-5. doi: 10.1158/1940-6207.CAPR-11-0372.
Green tea and its major polyphenolic flavonoid, epigallocatechin gallate (EGCG), have been credited with cancer chemopreventive activity for many years; the mechanism for this activity, however, has remained obscure. Now, as reported in this issue of the journal (beginning on page 1366), Urusova and colleagues showed direct binding of EGCG to the peptidyl prolyl cis/trans isomerase Pin1, which inhibited Pin1 enzymatic activity. They showed that Pin1 expression is required for EGCG effects on cell growth, c-Jun activation, and transcription regulation mediated by NF-κB and activator protein-1. The data provide a glimpse of the mechanism of action of EGCG and set a new bar for the future study of natural products with chemopreventive activity.
多年来，绿茶及其主要多酚类黄酮表没食子儿茶素没食子酸酯（EGCG）一直被认为具有抗癌化学预防作用；然而，这种活性的机制仍然不清楚。现在，正如本期杂志上的报道（从第 1366 页开始），Urusova 及其同事表明 EGCG 与肽基脯氨酰顺/反式异构酶 Pin1 的直接结合，抑制了 Pin1 的酶活性。他们表明，Pin1 的表达是 EGCG 对细胞生长、c-Jun 激活以及 NF-κB 和激活蛋白-1 介导的转录调节作用所必需的。这些数据提供了 EGCG 作用机制的一个 glimpse，并为具有化学预防活性的天然产物的未来研究设定了一个新的标准。
