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柚皮素衍生物的合成与生物活性。

The synthesis and bioactivity of apigenin derivatives.

机构信息

Institute of Pharmacy and Pharmacology, Hengyang Medicinal School, University of South China, Hengyang, Hunan 421001, China.

Institute of Pharmacy and Pharmacology, Hengyang Medicinal School, University of South China, Hengyang, Hunan 421001, China; Department of Pharmacy, Hunan Vocational College of Science and Technology, Third ZhongyiShan Road, Changsha, Hunan 410004, China.

出版信息

Fitoterapia. 2024 Dec;179:106228. doi: 10.1016/j.fitote.2024.106228. Epub 2024 Sep 25.

Abstract

BACKGROUND

Apigenin, a naturally occurring compound with a flavone core structure, is known for its diverse bioactivities, including anti-inflammation, anti-toxicant, anti-cancer and so on. There has been significant interest in the medicinal chemistry community. To address these challenges, researchers have developed various derivatives of apigenin to address challenges such as poor water-solubility and low intestinal absorption, aiming to enhance the pharmacological activities and pharmacokinetic properties of this compound.

OBJECTIVE

In recent years, there has been a proliferation of apigenin derivatives with enhanced bioactivity. However, there is a lack of comprehensive reviews on the function-based modification of these derivatives. In this paper, we provide an overview of the apigenin derivatives with varying bioactivities and explored their structure activity relationships. And the functions of different groups of apigenin derivatives were also analyzed.

CONCLUSION

This review summarized the current achievements that could provide some clues for further study of apigenin-based drugs.

摘要

背景

芹菜素是一种具有黄酮核结构的天然化合物,具有多种生物活性,包括抗炎、解毒、抗癌等。这引起了医学界的极大兴趣。为了解决这些挑战,研究人员开发了各种芹菜素衍生物,以解决水溶性差和肠道吸收低等问题,旨在增强该化合物的药理活性和药代动力学特性。

目的

近年来,具有增强生物活性的芹菜素衍生物大量涌现。然而,对于这些衍生物基于功能的修饰缺乏全面的综述。本文综述了具有不同生物活性的芹菜素衍生物,并探讨了它们的构效关系。同时还分析了不同类型芹菜素衍生物的功能。

结论

本综述总结了目前的研究成果,为基于芹菜素的药物的进一步研究提供了一些线索。

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