Department of Medical and Chemical Laboratory Diagnostics, General Hospital of Vienna, Medical University of Vienna, Waehringer Guertel 18-20, 1090 Vienna, Austria.
Pharm Res. 2010 Jun;27(6):1042-8. doi: 10.1007/s11095-010-0090-1. Epub 2010 Mar 16.
Resveratrol (3,4',5-trihydroxy-trans-stilbene) is a compound found in wine and is held responsible for a number of beneficial effects of red wine. Besides the prevention of heart disease and significant anti-inflammatory effects, resveratrol might inhibit tumor cell growth and even play a role in the aging process. We here describe the structure-activity relationship of resveratrol and analogues of resveratrol regarding the free radical scavenging and antitumor effects of this exciting natural compound. In addition, we have synthesized a number of analogues of resveratrol with the aim to further improve the beneficial effects of resveratrol. Our studies were based on the analysis of structural properties, which were responsible for the most important effects of this compound. Striking in vivo effects can be observed with hexahydroxystilbene (M8), the most effective synthetic analogue of resveratrol. We could show that M8 inhibits tumor as well as metastasis growth of human melanoma in two different animal models, alone and in combination with dacarbacine.
白藜芦醇（3,4',5-三羟基反式二苯乙烯）是一种存在于葡萄酒中的化合物，被认为是红葡萄酒具有多种有益作用的原因。除了预防心脏病和显著的抗炎作用外，白藜芦醇可能抑制肿瘤细胞生长，甚至在衰老过程中发挥作用。我们在这里描述了白藜芦醇及其类似物的构效关系，以了解这种令人兴奋的天然化合物的自由基清除和抗肿瘤作用。此外，我们还合成了一些白藜芦醇类似物，旨在进一步提高白藜芦醇的有益作用。我们的研究基于对结构特性的分析，这些特性对白藜芦醇的最重要作用负责。六羟基二苯乙烯（M8）是白藜芦醇最有效的合成类似物，在体内观察到了显著的效果。我们表明，M8 可以单独使用或与达卡巴嗪联合使用，抑制两种不同动物模型中的人类黑色素瘤肿瘤和转移生长。
