Laboratoire de Chimie Bioanalytique, Toxicologie et Chimie Physique Appliquée, Université Libre de Bruxelles (ULB), Brussels, Belgium.
Curr Med Chem. 2010;17(9):812-25. doi: 10.2174/092986710790712183.
Over eleven hundred publications reporting anticancer activities of polyphenols have appeared in the peer-reviewed literature. In addition, a search of the PubMed database using "polyphenols - cancer - review" as keywords produced over 320 hits for review articles (July 2009). Polyphenol anticancer activities include, among others, anti-oxidative, pro-apoptotic, DNA damaging, anti-angiogenic, and immunostimulatory effects. Targeting specific protein kinases to combat cancer represents a major focus of oncology research within the so-called targeted therapy approach. An exhaustive search of the PubMed database (July 2009) using "polyphenols - cancer - kinases" as keywords resulted in more than 130 hits, half of them having been published within the past five years. Furthermore, the PubMed database contains 25 reviews on the subject of anti-kinase activity of some specific polyphenols, including mainly curcumin and the green tea polyphenol (-)-epigallocatechin 3-gallate (EGCG). However, no attempt has been made yet to review this area of research in a comprehensive, general manner. The current review therefore aims to highlight those anticancer polyphenols that target specific kinases in various types of cancer. The present review also provides an in-depth analysis of polyphenol structure- activity relationships in relation to their anticancer activities and specific kinase targeting. Lastly, a number of polyphenols are identified as potential antitumor agents that could be used to combat biologically aggressive cancers, including metastasizing cancers, through the targeting of specific kinases.
已有一千一百多篇报道多酚类化合物抗癌活性的同行评议文献发表。此外，在 PubMed 数据库中使用“多酚-癌症-综述”作为关键字进行搜索，产生了超过 320 篇综述文章（2009 年 7 月）。多酚类化合物的抗癌活性包括抗氧化、促凋亡、DNA 损伤、抗血管生成和免疫刺激作用等。针对特定的蛋白激酶来治疗癌症是肿瘤学研究中所谓的靶向治疗方法的主要焦点。在 PubMed 数据库中使用“多酚-癌症-激酶”作为关键字进行全面搜索（2009 年 7 月），结果超过 130 次命中，其中一半是在过去五年内发表的。此外，PubMed 数据库中包含 25 篇关于某些特定多酚类化合物的抗激酶活性的综述，其中主要包括姜黄素和绿茶多酚（-）-表没食子儿茶素 3-没食子酸酯（EGCG）。然而，迄今为止，还没有人试图以全面、综合的方式来综述这一研究领域。因此，本综述旨在强调那些针对各种癌症中特定激酶的抗癌多酚类化合物。本综述还深入分析了多酚类化合物的结构-活性关系与其抗癌活性和特定激酶靶向之间的关系。最后，确定了一些多酚类化合物作为潜在的抗肿瘤药物，可通过靶向特定激酶来对抗具有生物侵袭性的癌症，包括转移性癌症。
