Department of Pharmacognosy, Faculty of Pharmacy with the Division of Laboratory Medicine, Medical University of Białystok, Białystok, Poland.
Department of Pharmacognosy, Medical University of Białystok, Student's Scientific Association, Białystok, Poland.
J Enzyme Inhib Med Chem. 2021 Dec;36(1):1016-1028. doi: 10.1080/14756366.2021.1927006.
Elastase is a proteolytic enzyme belonging to the family of hydrolases produced by human neutrophils, monocytes, macrophages, and endothelial cells. Human neutrophil elastase is known to play multiple roles in the human body, but an increase in its activity may cause a variety of diseases. Elastase inhibitors may prevent the development of psoriasis, chronic kidney disease, respiratory disorders (including COVID-19), immune disorders, and even cancers. Among polyphenolic compounds, some flavonoids and their derivatives, which are mostly found in herbal plants, have been revealed to influence elastase release and its action on human cells. This review focuses on elastase inhibitors that have been discovered from natural sources and are biochemically characterised as flavonoids. The inhibitory activity on elastase is a characteristic of flavonoid aglycones and their glycoside and methylated, acetylated and hydroxylated derivatives. The presented analysis of structure-activity relationship (SAR) enables the determination of the chemical groups responsible for evoking an inhibitory effect on elastase. Further study especially of the efficacy and safety of the described natural compounds is of interest in order to gain better understanding of their health-promoting potential.
弹性蛋白酶是一种属于水解酶家族的蛋白水解酶，由人中性粒细胞、单核细胞、巨噬细胞和内皮细胞产生。已知人中性粒细胞弹性蛋白酶在人体内发挥多种作用，但活性增加可能导致多种疾病。弹性蛋白酶抑制剂可能预防银屑病、慢性肾脏病、呼吸障碍（包括 COVID-19）、免疫紊乱甚至癌症的发生。在多酚类化合物中，一些黄酮类化合物及其衍生物，主要存在于植物药中，已被证明可以影响弹性蛋白酶的释放及其对人细胞的作用。本综述重点介绍了从天然来源中发现的、具有生化特征的黄酮类弹性蛋白酶抑制剂。对弹性蛋白酶的抑制活性是黄酮类苷元和它们的糖苷以及甲基化、乙酰化和羟基化衍生物的特征。对结构-活性关系（SAR）的分析使我们能够确定负责引发对弹性蛋白酶抑制作用的化学基团。进一步研究特别是描述的天然化合物的功效和安全性，以更好地了解它们的促进健康的潜力，是很有意义的。
