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黄酮类化合物及相关化合物作为抗过敏物质。

Flavonoids and related compounds as anti-allergic substances.

作者信息

Kawai Mari, Hirano Toru, Higa Shinji, Arimitsu Junsuke, Maruta Michiru, Kuwahara Yusuke, Ohkawara Tomoharu, Hagihara Keisuke, Yamadori Tomoki, Shima Yoshihito, Ogata Atsushi, Kawase Ichiro, Tanaka Toshio

机构信息

Department of Respiratory Medicine, Allergy and Rheumatic Diseases, Osaka University Medical School, Osaka, Japan.

出版信息

Allergol Int. 2007 Jun;56(2):113-23. doi: 10.2332/allergolint.R-06-135. Epub 2007 Mar 1.

Abstract

The prevalence of allergic diseases has increased all over the world during the last two decades. Dietary change is considered to be one of the environmental factors that cause this increase and worsen allergic symptoms. If this is the case, an appropriate intake of foods or beverages with anti-allergic activities is expected to prevent the onset of allergic diseases and ameliorate allergic symptoms. Flavonoids, ubiquitously present in vegetables, fruits or teas possess anti-allergic activities. Flavonoids inhibit histamine release, synthesis of IL-4 and IL-13 and CD40 ligand expression by basophils. Analyses of structure-activity relationships of 45 flavones, flavonols and their related compounds showed that luteolin, ayanin, apigenin and fisetin were the strongest inhibitors of IL-4 production with an IC(50) value of 2-5 microM and determined a fundamental structure for the inhibitory activity. The inhibitory activity of flavonoids on IL-4 and CD40 ligand expression was possibly mediated through their inhibitory action on activation of nuclear factors of activated T cells and AP-1. Administration of flavonoids into atopic dermatitis-prone mice showed a preventative and ameliorative effect. Recent epidemiological studies reported that a low incidence of asthma was significantly observed in a population with a high intake of flavonoids. Thus, this evidence will be helpful for the development of low molecular compounds for allergic diseases and it is expected that a dietary menu including an appropriate intake of flavonoids may provide a form of complementary and alternative medicine and a preventative strategy for allergic diseases. Clinical studies to verify these points are now in progress.

摘要

在过去二十年中,过敏性疾病在全球范围内的患病率有所上升。饮食变化被认为是导致这种上升并加重过敏症状的环境因素之一。如果是这样,适当摄入具有抗过敏活性的食物或饮料有望预防过敏性疾病的发作并改善过敏症状。黄酮类化合物广泛存在于蔬菜、水果或茶中,具有抗过敏活性。黄酮类化合物可抑制组胺释放、IL-4和IL-13的合成以及嗜碱性粒细胞中CD40配体的表达。对45种黄酮、黄酮醇及其相关化合物的构效关系分析表明,木犀草素、花青素、芹菜素和漆黄素是最强的IL-4产生抑制剂,IC(50)值为2-5 microM,并确定了抑制活性的基本结构。黄酮类化合物对IL-4和CD40配体表达的抑制活性可能是通过它们对活化T细胞核因子和AP-1活化的抑制作用介导的。将黄酮类化合物施用于易患特应性皮炎的小鼠显示出预防和改善作用。最近的流行病学研究报告称,在黄酮类化合物摄入量高的人群中,哮喘发病率显著较低。因此,这一证据将有助于开发用于过敏性疾病的低分子化合物,并且预计包括适当摄入黄酮类化合物的饮食菜单可能提供一种补充和替代医学形式以及过敏性疾病的预防策略。目前正在进行验证这些观点的临床研究。

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