{"title":"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。","authors":"Nia Samira, Benarous Khedidja, Lakaas Manel, Sadeki Israa, Yousfi Mohamed","doi":"10.2174/1871523019666200102111048","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>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.</p><p><strong>Objective: </strong>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.</p><p><strong>Materials and methods: </strong>The evaluation of the inhibitory activity of our drugs is achieved using a new method that has proved its sensitivity, quickness, and effectiveness.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>The results showed that the loratadine and the betamethasone have a strong potential to inhibit the alpha-amylase.</p>","PeriodicalId":35423,"journal":{"name":"Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"3","resultStr":"{\"title\":\"New Inhibition Detection Method to Evaluate the Human Salivary Alphaamylase Activity of Some Drugs, Molecular Docking, and SAR Studies.\",\"authors\":\"Nia Samira, Benarous Khedidja, Lakaas Manel, Sadeki Israa, Yousfi Mohamed\",\"doi\":\"10.2174/1871523019666200102111048\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>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.</p><p><strong>Objective: </strong>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.</p><p><strong>Materials and methods: </strong>The evaluation of the inhibitory activity of our drugs is achieved using a new method that has proved its sensitivity, quickness, and effectiveness.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>The results showed that the loratadine and the betamethasone have a strong potential to inhibit the alpha-amylase.</p>\",\"PeriodicalId\":35423,\"journal\":{\"name\":\"Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2021-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"3\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/1871523019666200102111048\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"Medicine\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1871523019666200102111048","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"Medicine","Score":null,"Total":0}
New Inhibition Detection Method to Evaluate the Human Salivary Alphaamylase Activity of Some Drugs, Molecular Docking, and SAR Studies.
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.
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.
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