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黄酮类化合物作为药物研发中的优势骨架:当前进展

Flavones as a Privileged Scaffold in Drug Discovery: Current Developments.

作者信息

Boniface Pone K, Elizabeth Ferreira I

机构信息

Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of Sao Paulo, Sao Paulo, Brazil.

出版信息

Curr Org Synth. 2019;16(7):968-1001. doi: 10.2174/1570179416666190719125730.

DOI:10.2174/1570179416666190719125730
PMID:31984880
Abstract

BACKGROUND

Flavones are one of the main subclasses of flavonoids with diverse pharmacological properties. They have been reported to possess antimalarial, antimicrobial, anti-tuberculosis, anti-allergic, antioxidant, anti-inflammatory activities, among others.

OBJECTIVE

The present review summarizes the recent information on the pharmacological properties of naturally occurring and synthetic flavones.

METHODS

Scientific publications referring to natural and synthetic flavones in relation to their biological activities were hand-searched in databases such as SciFinder, PubMed (National Library of Medicine), Science Direct, Wiley, ACS, SciELO, Springer, among others.

RESULTS

As per the literature, seventy-five natural flavones were predicted as active compounds with reference to their IC50 (<20 µg/mL) in in vitro studies. Also, synthetic flavones were found active against several diseases.

CONCLUSION

As per the literature, flavones are important sources for the potential treatment of multifactorial diseases. However, efforts toward the development of flavone-based therapeutic agents are still needed. The appearance of new catalysts and chemical transformations is expected to provide avenues for the synthesis of unexplored flavones, leading to the discovery of flavones with new properties and biological activities.

摘要

背景

黄酮类化合物是黄酮的主要亚类之一,具有多种药理特性。据报道,它们具有抗疟疾、抗菌、抗结核、抗过敏、抗氧化、抗炎等活性。

目的

本综述总结了天然和合成黄酮药理特性的最新信息。

方法

在诸如SciFinder、PubMed(美国国立医学图书馆)、Science Direct、Wiley、ACS、SciELO、Springer等数据库中手动检索了有关天然和合成黄酮生物活性的科学出版物。

结果

根据文献,在体外研究中,七十五种天然黄酮被预测为活性化合物,其半数抑制浓度(IC50)<20μg/mL。此外,合成黄酮对多种疾病具有活性。

结论

根据文献,黄酮是潜在治疗多因素疾病的重要来源。然而,仍需要努力开发基于黄酮的治疗剂。新催化剂和化学转化的出现有望为未探索黄酮的合成提供途径,从而发现具有新特性和生物活性的黄酮。

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