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类黄酮衍生物在某些被忽视热带病中的治疗潜力。

Therapeutic Potential of Flavonoid Derivatives for Certain Neglected Tropical Diseases.

机构信息

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

出版信息

Curr Drug Targets. 2022;23(7):680-682. doi: 10.2174/1389450123666220309093827.

Abstract

BACKGROUND

Neglected tropical diseases (NTDs) are infectious diseases that mostly affect people living in tropical and subtropical regions, especially in impoverished areas. Ubiquitously found in plants, flavonoids are a group of compounds that have been reported to exhibit a wide range of biological activities against parasites (Leishmania sp., Trypanosoma cruzi, Trypanosoma brucei, Brugia malayi, etc.) that cause certain NTDs.

AIMS

The present study aims to highlight and discuss our recent reports on the implication of flavonoids in drug development for NTDs, such as leishmaniasis, Chagas disease, African trypanosomiasis, filariasis, among others.

RESULTS

Today, studies show that flavonoids exhibit in vitro antileishmanial, anti-trypanosomiasis, antifilarial activities, among others. Furthermore, the molecular hybridization of flavonoids with the triazole groups has led to the development of compounds with improved biological activity. The incorporation of chemical groups, such as NO, F, and Cl groups, during the process of design and synthesis, leads to the enhancement of pharmacological activity.

CONCLUSION

Flavonoids are useful metabolites that can be prospected as potential leads for the development of new agents against certain NTDs. However, research opportunities, including cytotoxicity and in vivo studies, mechanisms of action, bioavailability of these compounds, remain to be investigated in the future.

摘要

背景

被忽视的热带病(NTDs)是一类主要影响热带和亚热带地区人群,尤其是贫困地区人群的传染病。类黄酮广泛存在于植物中,据报道,其具有广泛的抗寄生虫(利什曼原虫、克氏锥虫、布氏冈比亚锥虫、马来丝虫等)生物活性,可用于治疗某些 NTDs。

目的

本研究旨在强调和讨论我们最近关于类黄酮在治疗 NTDs(如利什曼病、恰加斯病、非洲锥虫病、丝虫病等)药物开发中的应用的报告。

结果

如今,研究表明类黄酮具有体外抗利什曼原虫、抗锥虫、抗丝虫等活性。此外,类黄酮与三唑基团的分子杂交导致了具有改善生物活性的化合物的发展。在设计和合成过程中引入 NO、F 和 Cl 等化学基团可提高药理活性。

结论

类黄酮是一种有用的代谢物,可以作为开发针对某些 NTDs 的新型药物的潜在先导化合物。然而,仍需要进一步研究,包括细胞毒性和体内研究、作用机制、这些化合物的生物利用度等。

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