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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.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。
Bioorg Med Chem. 2007 Aug 1;15(15):5076-82. doi: 10.1016/j.bmc.2007.05.041. Epub 2007 May 18.

本文引用的文献

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The proteasome as a potential target for novel anticancer drugs and chemosensitizers.蛋白酶体作为新型抗癌药物和化学增敏剂的潜在靶点。
Drug Resist Updat. 2006 Dec;9(6):263-73. doi: 10.1016/j.drup.2006.11.001. Epub 2007 Jan 2.
2
Peracetylation as a means of enhancing in vitro bioactivity and bioavailability of epigallocatechin-3-gallate.过乙酰化作为提高表没食子儿茶素-3-没食子酸酯体外生物活性和生物利用度的一种手段。
Drug Metab Dispos. 2006 Dec;34(12):2111-6. doi: 10.1124/dmd.106.011460. Epub 2006 Sep 22.
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Synthetic peracetate tea polyphenols as potent proteasome inhibitors and apoptosis inducers in human cancer cells.合成过氧乙酸茶多酚作为人类癌细胞中有效的蛋白酶体抑制剂和凋亡诱导剂。
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A potential prodrug for a green tea polyphenol proteasome inhibitor: evaluation of the peracetate ester of (-)-epigallocatechin gallate [(-)-EGCG].一种绿茶多酚蛋白酶体抑制剂的潜在前体药物：（-）-表没食子儿茶素没食子酸酯[（-）-EGCG]过乙酸酯的评估。
Bioorg Med Chem. 2004 Nov 1;12(21):5587-93. doi: 10.1016/j.bmc.2004.08.002.
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Green tea and tea polyphenols in cancer prevention.绿茶及茶多酚在癌症预防中的作用
Front Biosci. 2004 Sep 1;9:2618-31. doi: 10.2741/1421.
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Study of the green tea polyphenols catechin-3-gallate (CG) and epicatechin-3-gallate (ECG) as proteasome inhibitors.绿茶多酚表没食子儿茶素没食子酸酯（CG）和表儿茶素没食子酸酯（ECG）作为蛋白酶体抑制剂的研究。
Bioorg Med Chem. 2004 Jul 1;12(13):3521-7. doi: 10.1016/j.bmc.2004.04.033.
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The development of proteasome inhibitors as anticancer drugs.蛋白酶体抑制剂作为抗癌药物的研发。
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Docking studies and model development of tea polyphenol proteasome inhibitors: applications to rational drug design.茶多酚蛋白酶体抑制剂的对接研究与模型开发：在合理药物设计中的应用。
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Enzymology of methylation of tea catechins and inhibition of catechol-O-methyltransferase by (-)-epigallocatechin gallate.茶儿茶素甲基化的酶学以及（-）-表没食子儿茶素没食子酸酯对儿茶酚-O-甲基转移酶的抑制作用
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Ester bond-containing tea polyphenols potently inhibit proteasome activity in vitro and in vivo.含酯键的茶多酚在体外和体内均能有效抑制蛋白酶体活性。
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从圣草中合成新型儿茶素（2R，3R）-表没食子儿茶素-3-O-（4-羟基苯甲酸酯）及其蛋白酶体抑制活性评估

Synthesis of (2R, 3R)-epigallocatechin-3-O-(4-hydroxybenzoate), a novel catechin from Cistus salvifolius, and evaluation of its proteasome inhibitory activities.

作者信息

Osanai Kumi, Huo Congde, 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 for Chiral Technology, the Institute of Molecular Technology for Drug Discovery and Synthesis, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong SAR, China.

出版信息

Tetrahedron. 2007 Aug 6;63(32):7565-7570. doi: 10.1016/j.tet.2007.05.043.

DOI:10.1016/j.tet.2007.05.043
PMID:21152270
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2998073/
Abstract

The total and semi syntheses of (2R, 3R)-epigallocatechin-3-O-(4-hydroxybenzoate), a novel catechin from Cistus salvifolius, was accomplished. The proteasome inhibition and cytotoxic activities of the synthetic compound and its acetyl derivative were studied and compared with (2R, 3R)-epigallocatechin-3-gallate (EGCG), the active component from green tea.

摘要

完成了来自圣栎叶石蚕的新型儿茶素（2R，3R）-表没食子儿茶素-3-O-（4-羟基苯甲酸酯）的全合成和半合成。研究了合成化合物及其乙酰衍生物的蛋白酶体抑制活性和细胞毒性，并与绿茶中的活性成分（2R，3R）-表没食子儿茶素-3-没食子酸酯（EGCG）进行了比较。