Resveratrol and Its Analogues – Is It a New Strategy of Anticancer Therapy?

S. Borys, R. Khozmi, W. Kranc, A. Bryja, M. Ješeta, B. Kempisty
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引用次数: 3

Abstract

Summary Resveratrol (RSV) is one of the polyphenols - metabolites common in plants,however it does not occur in animals. It occurs mainly in grape skin (Vitisvinifera), peanuts (Arachis hypogeal) and in the roots of (Polygonumcupidatum) a traditional Chinese curative plant. RSV has a preventive property against the most serious diseases of modern world such as cancer, neurodegenerative diseases and cardiovascular diseases. Due to pleiotropy, RSV is currently the main object of many research teams′ interest, which is shown by the significant number of publications devoted to this subject. Animal and human conducted studies have shown very low bioavailability of RSV (approx. 2%), which is the result of rapid biotransformation to sulphate and to a lesser extent, to the glucuronide conjugates as well. The studies on the improvement of RSV bioavailability, which have beencarried out for many years, have contributed to the synthesis of the analogues of more chemopreventive and more desirable pharmacokinetic properties. In order to enhance antiproliferative activity and RSV bioavailability, series of methyl analogues were synthesized and this will be described later in more detail. An example of such a derivative is DMU-212 (3,4,4’5-tetramethoxystilbene).
白藜芦醇及其类似物——它是抗癌治疗的新策略吗?
白藜芦醇(Resveratrol, RSV)是植物中常见的多酚代谢产物之一,但在动物中并不存在。它主要存在于葡萄皮(Vitisvinifera),花生(arachhis hypohypoal)和中国传统治疗植物(Polygonumcupidatum)的根中。RSV对现代世界最严重的疾病,如癌症、神经退行性疾病和心血管疾病具有预防作用。由于多效性,RSV目前是许多研究团队感兴趣的主要对象,这一点从大量致力于该主题的出版物中可以看出。动物和人类进行的研究表明,呼吸道合胞病毒的生物利用度非常低(约为1。2%),这是快速生物转化为硫酸盐的结果,在较小程度上,葡萄糖醛酸缀合物也是如此。多年来关于提高RSV生物利用度的研究,有助于合成更具有化学预防作用和更理想药代动力学性质的类似物。为了提高抗增殖活性和RSV的生物利用度,我们合成了一系列的甲基类似物,并将在后面详细描述。这种衍生物的一个例子是DMU-212(3,4,4 ' 5-四甲基二苯乙烯)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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