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黄酮类化合物作为抗癌剂:构效关系研究

Flavonoids as anticancer agents: structure-activity relationship study.

作者信息

López-Lázaro M

机构信息

Departamento de Farmacología, Facultad de Farmacia, Universidad de Sevilla, Spain.

出版信息

Curr Med Chem Anticancer Agents. 2002 Nov;2(6):691-714. doi: 10.2174/1568011023353714.

Abstract

The protection against some forms of cancer provided by many common foods has been observed in multiple epidemiological studies. Non-nutritive dietary compounds, such as flavonoids, have been considered as the responsible agents for such observations and since then, much research activity has been done about their potential anticancer effect. As a result, these compounds have been shown to regulate proliferation and cell death pathways leading to cancer. Thus, flavonoids such as the synthetic flavone, flavopiridol; the soy isoflavonoid, genistein; the tea catechin epigallocatechin gallate; or the common dietary flavonol, quercetin, are emerging as prospective anticancer drug candidates and some of them have already entered in clinical trials. In view of the therapeutic potential of flavonoids, many researchers have tried to elucidate possible structure-activity relationships that might lead to new drug discovery. However, and possibly due to the information being very scattered, there is very little understanding about a possible relationship between the flavonoid structure and their anticancer activity. Besides their therapeutic potential, since lots of flavonoids are present in our diet, a greater understanding of their anticancer properties might also modify our dietary habits in order to attack cancer with an effective weapon, prevention. This paper seeks to show, in a brief but comprehensive way, the anticancer properties of flavonoids. Through an understanding of the cancer process and its treatment, flavonoids are studied as possible useful compounds in cancer prevention and cancer therapy. Furthermore, this review attempts to compile and discuss the literature studying structure-activity relationships, in order to show structural requirements implicated in the anticancer activity of flavonoids, which might help to rationalize their development as antitumor agents.

摘要

多项流行病学研究观察到,许多常见食物能预防某些类型的癌症。非营养性膳食化合物,如类黄酮,被认为是导致这些观察结果的原因,从那时起,人们对其潜在的抗癌作用进行了大量研究。结果表明,这些化合物能够调节导致癌症的细胞增殖和细胞死亡途径。因此,诸如合成黄酮类化合物黄酮哌啶醇、大豆异黄酮染料木黄酮、茶儿茶素表没食子儿茶素没食子酸酯或常见膳食黄酮醇槲皮素等类黄酮,正成为有前景的抗癌药物候选物,其中一些已进入临床试验阶段。鉴于类黄酮的治疗潜力,许多研究人员试图阐明可能导致新药发现的结构 - 活性关系。然而,可能由于相关信息非常分散,人们对类黄酮结构与其抗癌活性之间的可能关系了解甚少。除了其治疗潜力外,由于我们的饮食中存在大量类黄酮,更深入地了解它们的抗癌特性也可能会改变我们的饮食习惯,以便用预防这一有效武器对抗癌症。本文旨在以简洁而全面的方式展示类黄酮的抗癌特性。通过了解癌症过程及其治疗方法,研究类黄酮作为癌症预防和癌症治疗中可能有用的化合物。此外,本综述试图汇编和讨论研究结构 - 活性关系的文献,以展示类黄酮抗癌活性所涉及的结构要求,这可能有助于合理开发其作为抗肿瘤药物。

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