绿茶多酚表没食子儿茶素-3-没食子酸酯D环上的对氨基取代基作为一种新型蛋白酶体抑制剂和癌细胞凋亡诱导剂。
A para-amino substituent on the D-ring of green tea polyphenol epigallocatechin-3-gallate as a novel proteasome inhibitor and cancer cell apoptosis inducer.
作者信息
Osanai Kumi, Landis-Piwowar Kristin R, Dou Q Ping, Chan Tak Hang
机构信息
Department of Applied Biology and Chemical Technology and the Open Laboratory of Chirotechnology, Institute of Molecular Technology for Drug Discovery and Synthesis, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, SAR, China.
出版信息
Bioorg Med Chem. 2007 Aug 1;15(15):5076-82. doi: 10.1016/j.bmc.2007.05.041. Epub 2007 May 18.
Abstract
Analogs of (-)-EGCG containing a para-amino group on the D-ring in place of the hydroxyl groups have been synthesized and their proteasome inhibitory activities were studied. We found that, the O-acetylated (-)-EGCG analogs possessing a p-NH(2) or p-NHBoc (Boc; tert-butoxycarbonyl) D-ring (5 and 7) act as novel tumor cellular proteasome inhibitors and apoptosis inducers with potency similar to natural (-)-EGCG and similar to (-)-EGCG peracetate. These data suggest that the acetylated amino-GTP analogs have the potential to be developed into novel anticancer agents.
摘要
已经合成了在D环上含有对氨基以取代羟基的（-）-表没食子儿茶素没食子酸酯（-）-EGCG类似物，并研究了它们的蛋白酶体抑制活性。我们发现，具有对氨基或对氨基叔丁氧羰基（Boc；叔丁氧羰基）D环的O-乙酰化（-）-EGCG类似物（5和7）作为新型肿瘤细胞蛋白酶体抑制剂和凋亡诱导剂，其效力与天然（-）-EGCG相似，且与全乙酰化（-）-EGCG相似。这些数据表明，乙酰化氨基-GTP类似物有潜力被开发成新型抗癌药物。
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