化学
阿卡波糖
酶
立体化学
生物化学
生物
淀粉酶
对接(动物)
IC50型
脂肪酶
活动站点
生物信息学
体外
水解
生物活性
水解酶
医学
护理部
基因
作者
Immacolata Faraone,Daniela Russo,Salvatore Genovese,Luigi Milella,Magnus Monné,Francesco Epifano,Serena Fiorito
出处
期刊:Phytochemistry
[Elsevier]
日期:2021-04-28
卷期号:187: 112781-112781
被引量:2
标识
DOI:10.1016/j.phytochem.2021.112781
摘要
Metabolic syndrome has several characteristic manifestations, including insulin resistance and dyslipidaemia, that demand therapeutic approaches, such as the inhibition of enzymes involved in nutrient absorption and digestion.This study aimed to evaluate the potential pharmacological use of natural compounds widespread in the plant kingdom and their semisynthetic compounds against target enzymes. Twenty-three oxyprenylated natural compoundswere investigated for their ability to inhibit α-amylase, α-glucosidase, and pancreatic lipase enzymes by in vitro assays. Moreover, in silico molecular docking was performed to analyse their binding capabilities into 3D structures. Farnesyloxyferulic acid, geranyloxyvanillic acid, nelumal A, and geranyloxyferulic acid showed the highest inhibition activity in all three in vitro enzyme assays. Moreover, in silico molecular docking of these four compounds was used to analyse their possible binding in 3D structures of the investigated enzymes. The results indicate that these compounds have considerable therapeutic potential for the treatment of metabolic syndrome, and further studies are warranted for their pharmacological development.
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