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黄酮类化合物的保肝活性及构效关系洞察

An Insight into the Hepatoprotective Activity and Structure-activity Relationships of Flavonoids.

作者信息

Majee Chandana, Mazumder Rupa, Choudhary Alka N

机构信息

Department of Pharmaceutical Chemistry, Noida Institute of Engineering and Technology, Greater Noida, UP, India.

Department of Pharmaceutics, Noida Institute of Engineering & Technology (Pharmacy Institute), 19 Knowledge Park II, Uttar Pradesh UP 201308, India.

出版信息

Mini Rev Med Chem. 2023;23(2):131-149. doi: 10.2174/1389557522666220602141142.

Abstract

BACKGROUND

Flavonoids are a class of polyphenolic bioactive compounds obtained from plants, which have a wide range of chemical structures and properties. More than 9000 distinct flavonoid molecules have been identified and have been found to regulate numerous developmental processes and play key biological roles in living organisms.

OBJECTIVE

This review aims to highlight the hepatoprotective potentiality of flavonoids and corelate their pharmacological activity with their chemical structure.

METHODS

With the advancement in the field of research related to phytochemicals, it is evident that flavonoids have versatile health benefits, viz., antioxidant property, free radical scavenging capacity, anticancer activity. The basic structures are C6-C3-C6 rings with various substitution patterns, resulting in a succession of subclass compounds, and the relationships between chemical structures and bioactivity have previously been investigated.

RESULTS

The hepatoprotective effects of bioactive flavonoids derived from plants have been widely linked to their antioxidant activity, antiinflammatory activity, effects on Sterol Regulatory Element- binding Proteins (SREBP), Peroxisome Proliferator-activated Receptor gamma (PPARγ) receptors, and inflammatory mediator cytokines according to numerous studies. The C2-C3 double bond at the A ring, as well as the hydroxyl groups of C3'or C4', and the carbonyl group at position C4, have been shown to augment their hepatoprotective activities; however, hydroxymethylation at C3' and C4' has been found to diminish the hepatoprotective activity.

CONCLUSION

The impact of flavonoid moieties and the structure-activity relationship of flavonoids related to combating various hepatic disorders have been vividly discussed in this review paper.

摘要

背景

黄酮类化合物是一类从植物中获取的多酚类生物活性化合物,具有广泛的化学结构和性质。已鉴定出9000多种不同的黄酮类分子,发现它们可调节众多发育过程,并在生物体中发挥关键生物学作用。

目的

本综述旨在突出黄酮类化合物的肝脏保护潜力,并将其药理活性与其化学结构相关联。

方法

随着植物化学相关研究领域的进展,很明显黄酮类化合物具有多种健康益处,即抗氧化特性、自由基清除能力、抗癌活性。其基本结构为具有各种取代模式的C6-C3-C6环,产生一系列亚类化合物,并且先前已经研究了化学结构与生物活性之间的关系。

结果

根据众多研究,源自植物的生物活性黄酮类化合物的肝脏保护作用与其抗氧化活性、抗炎活性、对固醇调节元件结合蛋白(SREBP)、过氧化物酶体增殖物激活受体γ(PPARγ)受体以及炎症介质细胞因子的影响密切相关。A环上的C2-C3双键以及C3'或C4'的羟基以及C4位的羰基已显示可增强其肝脏保护活性;然而,已发现C3'和C4'处的羟甲基化会降低肝脏保护活性。

结论

本综述论文生动地讨论了黄酮类部分的影响以及黄酮类化合物与对抗各种肝脏疾病相关的构效关系。

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