Pharmacological and Nutritional Effects of Natural Coumarins and Their Structure–Activity Relationships,Molecular Nutrition & Food Research

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Pharmacological and Nutritional Effects of Natural Coumarins and Their Structure–Activity Relationships
Molecular Nutrition & Food Research ( IF 4.5 ) Pub Date : 2018-06-19 , DOI: 10.1002/mnfr.201701073
Jing-Jing Zhu ₁ , Jian-Guo Jiang ₁

Affiliation

Coumarins are fused benzene and pyrone ring systems with a wide spectrum of bioactivities, including antitumor, anti‐inflammation, antiviral, and antibacterial effects. In this paper, the current development of coumarin‐based drugs is introduced, and their structure–activity relationship is discussed by reviewing the relevant literature published in the past 20 years. Coumarin molecules can be customized by the target site to prevent systemic side effects by virtue of structural modification. The ortho‐phenolic hydroxyl on the benzene ring has remarkable antioxidant and antitumor activities. Coumarins with aryl groups at the C‐4 position have good activities in anti‐HIV, antitumor, anti‐inflammation, and analgesia. C‐3 phenylcoumarins have strong anti‐HIV and antioxidant effects. Tetracycline pyranocoumarins can significantly inhibit HIV; osthol structural analogues have antimicrobial activity. Praeruptorin C and its derivatives play an important role in lowering blood pressure and dilating coronary arteries, and khellactone derivatives have significant inhibitory effects on AIDS, cancer, and cardiovascular diseases. It is concluded that the specific site on the core structure of coumarin exhibits one or more activities due to the electronic or steric effects of the substituents. This review is intended to be conducive to rational design and development of more active and less toxic agents with a coumarin scaffold.

中文翻译：

天然香豆素的药理营养作用及其构效关系

香豆素是稠合的苯和吡喃酮环系统，具有广泛的生物活性，包括抗肿瘤、抗炎、抗病毒和抗菌作用。本文介绍了香豆素类药物的发展现状，并通过回顾近20年发表的相关文献，探讨了它们的构效关系。香豆素分子可以通过目标位点进行定制，以通过结构修饰来防止全身性副作用。苯环上的邻酚羟基具有显着的抗氧化和抗肿瘤活性。C-4位带有芳基的香豆素类化合物在抗HIV、抗肿瘤、抗炎、镇痛等方面具有良好的活性。C-3 苯基香豆素具有很强的抗 HIV 和抗氧化作用。四环素吡喃香豆素能显着抑制HIV；Osthol 结构类似物具有抗菌活性。Praeruptorin C及其衍生物在降低血压和扩张冠状动脉方面具有重要作用，kellactone衍生物对艾滋病、癌症和心血管疾病有显着抑制作用。可以得出结论，由于取代基的电子或空间效应，香豆素核心结构上的特定位点表现出一种或多种活性。本综述旨在有助于合理设计和开发活性更高、毒性更低的香豆素支架药物。和心血管疾病。可以得出结论，由于取代基的电子或空间效应，香豆素核心结构上的特定位点表现出一种或多种活性。本综述旨在有助于合理设计和开发活性更高、毒性更低的香豆素支架药物。和心血管疾病。可以得出结论，由于取代基的电子或空间效应，香豆素核心结构上的特定位点表现出一种或多种活性。本综述旨在有助于合理设计和开发活性更高、毒性更低的香豆素支架药物。

更新日期：2018-06-19

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