{"title":"In silico and in vitro Study of the Inhibitory Effect of Anti-inflammatory Drug Betamethasone on Two Lipases","authors":"Nia Samira, Benarous Khedidja, Abdelalim Fatima Zahra, Chellali Khadidja Nour Elyakine, Yousfi Mohamed","doi":"10.2174/1871523018666190906165944","DOIUrl":null,"url":null,"abstract":"Background For the first time, the anti-inflammatory drug betamethasone is investigated for its inhibitory activity against lipase. Objective This work aims to demonstrate the in vitro and in silico inhibitory effect of the anti-inflammatory drug betamethasone on the enzymatic activity of two lipases. Methods In vitro study using p-nitrophenyllaurate as lipase substrate is used to determine inhibition potency. Molecular Docking is performed using the Autodock Vina for drug molecule and two enzymes Candida rugosa lipase and human pancreatic lipase. Results Betamethasone represents a moderate inhibition effect with a value of IC50 of 0.36±0.01 mg/ml. Molecular docking allowed us to understand inhibitory – enzyme interactions and to confirm in vitro obtained results. Conclusion These experiments showed that betamethasone can be used in the treatment of diseases related to lipase activity.","PeriodicalId":35423,"journal":{"name":"Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2019-09-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1871523018666190906165944","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1871523018666190906165944","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"Medicine","Score":null,"Total":0}
引用次数: 0
Abstract
Background For the first time, the anti-inflammatory drug betamethasone is investigated for its inhibitory activity against lipase. Objective This work aims to demonstrate the in vitro and in silico inhibitory effect of the anti-inflammatory drug betamethasone on the enzymatic activity of two lipases. Methods In vitro study using p-nitrophenyllaurate as lipase substrate is used to determine inhibition potency. Molecular Docking is performed using the Autodock Vina for drug molecule and two enzymes Candida rugosa lipase and human pancreatic lipase. Results Betamethasone represents a moderate inhibition effect with a value of IC50 of 0.36±0.01 mg/ml. Molecular docking allowed us to understand inhibitory – enzyme interactions and to confirm in vitro obtained results. Conclusion These experiments showed that betamethasone can be used in the treatment of diseases related to lipase activity.
期刊介绍:
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new anti-inflammatory & anti-allergy agents. Publishing a series of timely in-depth reviews written by leaders in the field covering a range of current topics, Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in the field.