The Prevention Program, Barbara Ann Karmanos Cancer Institute, and Department of Pathology, School of Medicine, Wayne State University, Detroit, MI, USA.
Cancer Lett. 2010 Jun 1;292(1):48-53. doi: 10.1016/j.canlet.2009.11.006. Epub 2009 Dec 3.
Epidemiological studies support the cancer-preventive effects of green tea and its main constituent (-)-epigallocatechin gallate [(-)-EGCG], however, (-)-EGCG is unstable under physiological conditions. Here we report that two novel fluoro-substituted (-)-EGCG analogs inhibited tumor growth with similar potency to that of Pro-EGCG (1) which has improved potency over parental compound (-)-EGCG in human breast cancer MDA-MB-231 xenografts. MDA-MB-231 tumors treated with each fluoro-substituted (-)-EGCG analog showed proteasome inhibition and apoptotic cell death, suggesting that the proteasome might be one of the cellular targets of fluoro-(-)-EGCGs and that proteasome inhibition is partially responsible for the observed antitumor activity.
流行病学研究支持绿茶及其主要成分(-)-表没食子儿茶素没食子酸酯((-)-EGCG)的抗癌作用,但(-)-EGCG 在生理条件下不稳定。在这里,我们报告了两种新型氟取代(-)-EGCG 类似物,它们抑制肿瘤生长的效力与 Pro-EGCG(1)相似,而 Pro-EGCG 在人乳腺癌 MDA-MB-231 异种移植瘤中的效力优于母体化合物(-)-EGCG。用每种氟取代(-)-EGCG 类似物处理的 MDA-MB-231 肿瘤显示蛋白酶体抑制和凋亡细胞死亡,这表明蛋白酶体可能是氟(-)-EGCG 的细胞靶标之一,而蛋白酶体抑制部分负责观察到的抗肿瘤活性。