抗炎药倍他米松对两种脂肪酶抑制作用的计算机及体外研究

Q2 Medicine

Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry Pub Date : 2019-09-06 DOI:10.2174/1871523018666190906165944

Nia Samira, Benarous Khedidja, Abdelalim Fatima Zahra, Chellali Khadidja Nour Elyakine, Yousfi Mohamed

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引用次数: 0

摘要

背景首次研究了抗炎药物倍他米松对脂肪酶的抑制作用。目的研究抗炎药倍他米松对两种脂肪酶活性的体外和体内抑制作用。方法采用对硝基苯月桂酸酯作为脂肪酶底物的体外实验，测定其抑制效力。利用Autodock Vina对药物分子与念珠菌脂肪酶和人胰脂肪酶两种酶进行分子对接。结果倍他米松具有中等抑制作用，IC50值为0.36±0.01 mg/ml。分子对接使我们能够了解抑制酶的相互作用，并确认体外获得的结果。结论倍他米松可用于脂肪酶活性相关疾病的治疗。

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In silico and in vitro Study of the Inhibitory Effect of Anti-inflammatory Drug Betamethasone on Two Lipases

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.

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来源期刊

Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry Pharmacology, Toxicology and Pharmaceutics-Pharmacology

CiteScore

3.30

自引率

0.00%

发文量

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.