New Inhibition Detection Method to Evaluate the Human Salivary Alphaamylase Activity of Some Drugs, Molecular Docking, and SAR Studies.

Q2 Medicine

Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry Pub Date : 2021-01-01 DOI:10.2174/1871523019666200102111048

Nia Samira, Benarous Khedidja, Lakaas Manel, Sadeki Israa, Yousfi Mohamed

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引用次数: 3

Abstract

Background: For the first time, the investigation of six anti-inflammatory drugs and six antihistaminic drugs for inhibitory activities against alpha-amylase has been evaluated using a new inhibition detection method in order to find new treatments for some diseases caused by α-amylase.

Objective: The first part of this work was devoted to the evaluation of the inhibition activity of these drugs on salivary α-amylase in vitro. Then to study the nature of interactions and structure-activity relationship, using the Autodockvina program for molecular docking.

Materials and methods: The evaluation of the inhibitory activity of our drugs is achieved using a new method that has proved its sensitivity, quickness, and effectiveness.

Results: The results of this study show that betamethasone and loratadine are potent α-amylase inhibitors with IC50 values 0.7mg/ml and 1.03 mg/ml, respectively compared to acarbose with IC50=5.6 μg/ml.

Conclusion: The results showed that the loratadine and the betamethasone have a strong potential to inhibit the alpha-amylase.

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评价人唾液α淀粉酶活性的新抑制检测方法、分子对接及SAR研究。

背景:本文首次采用一种新的抑制检测方法，对6种抗炎药物和6种抗组胺药物对α-淀粉酶的抑制活性进行了研究，以期为某些α-淀粉酶引起的疾病寻找新的治疗方法。目的:第一部分体外评价这些药物对唾液α-淀粉酶的抑制活性。然后研究相互作用的性质和构效关系，利用Autodockvina程序进行分子对接。材料和方法:采用一种新的方法对药物的抑制活性进行评价，该方法具有敏感性、快速性和有效性。结果:本研究结果表明，倍他米松和氯雷他定是有效的α-淀粉酶抑制剂，IC50值分别为0.7mg/ml和1.03 mg/ml，而阿卡波糖的IC50值为5.6 μg/ml。结论:氯雷他定和倍他米松对-淀粉酶有较强的抑制作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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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.