Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme Activity
Human neutrophil elastase (HNE) is used as diagnostic biomarker for inflammation/infection. In this work, 10 ionic liquids (ILs) and 11 ionic liquids active pharmaceutical ingredients (ILs-APIs) were tested to evaluate the inhibition effect on the activity of porcine pancreatic elastase enzyme, freq...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-01-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/1/200 |
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| author | Fátima A. R. Mota Sarah A. P. Pereira André R. T. S. Araujo M. Lúcia M. F. S. Saraiva |
| author_facet | Fátima A. R. Mota Sarah A. P. Pereira André R. T. S. Araujo M. Lúcia M. F. S. Saraiva |
| author_sort | Fátima A. R. Mota |
| collection | DOAJ |
| description | Human neutrophil elastase (HNE) is used as diagnostic biomarker for inflammation/infection. In this work, 10 ionic liquids (ILs) and 11 ionic liquids active pharmaceutical ingredients (ILs-APIs) were tested to evaluate the inhibition effect on the activity of porcine pancreatic elastase enzyme, frequently employed as a model for HNE. The insertion of ionic liquids in some drugs is useful, as the insertion of ILs with inhibitory capacity will also slow down all processes in which this enzyme is involved. Therefore, a spectrophotometric method was performed to the determination of EC<sub>50</sub> values of the compounds tested. EC<sub>50</sub> values of 124 ± 4 mM to 289 ± 11 mM were obtained, with the most toxic IL for elastase being tetrabutylammonium acetate and the least toxic 1-butyl-3-methylimidazolium acetate. Moreover, sodium salicylate (raw material) presented the lower and benzethonium bistriflimide the higher EC<sub>50</sub> when compared with all the IL-APIs tested. This work provides significant information about the effect of the studied IL and IL-APIs in elastase enzyme activity. |
| first_indexed | 2024-03-10T13:32:04Z |
| format | Article |
| id | doaj.art-95f2100595d447f98a5fab2db8554c82 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T13:32:04Z |
| publishDate | 2021-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-95f2100595d447f98a5fab2db8554c822023-11-21T07:51:34ZengMDPI AGMolecules1420-30492021-01-0126120010.3390/molecules26010200Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme ActivityFátima A. R. Mota0Sarah A. P. Pereira1André R. T. S. Araujo2M. Lúcia M. F. S. Saraiva3LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, Porto University, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, PortugalLAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, Porto University, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, PortugalLAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, Porto University, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, PortugalLAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, Porto University, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, PortugalHuman neutrophil elastase (HNE) is used as diagnostic biomarker for inflammation/infection. In this work, 10 ionic liquids (ILs) and 11 ionic liquids active pharmaceutical ingredients (ILs-APIs) were tested to evaluate the inhibition effect on the activity of porcine pancreatic elastase enzyme, frequently employed as a model for HNE. The insertion of ionic liquids in some drugs is useful, as the insertion of ILs with inhibitory capacity will also slow down all processes in which this enzyme is involved. Therefore, a spectrophotometric method was performed to the determination of EC<sub>50</sub> values of the compounds tested. EC<sub>50</sub> values of 124 ± 4 mM to 289 ± 11 mM were obtained, with the most toxic IL for elastase being tetrabutylammonium acetate and the least toxic 1-butyl-3-methylimidazolium acetate. Moreover, sodium salicylate (raw material) presented the lower and benzethonium bistriflimide the higher EC<sub>50</sub> when compared with all the IL-APIs tested. This work provides significant information about the effect of the studied IL and IL-APIs in elastase enzyme activity.https://www.mdpi.com/1420-3049/26/1/200ionic liquidsionic liquids active pharmaceutical ingredientsenzyme activityelastaseinhibition |
| spellingShingle | Fátima A. R. Mota Sarah A. P. Pereira André R. T. S. Araujo M. Lúcia M. F. S. Saraiva Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme Activity Molecules ionic liquids ionic liquids active pharmaceutical ingredients enzyme activity elastase inhibition |
| title | Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme Activity |
| title_full | Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme Activity |
| title_fullStr | Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme Activity |
| title_full_unstemmed | Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme Activity |
| title_short | Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme Activity |
| title_sort | evaluation of ionic liquids and ionic liquids active pharmaceutical ingredients inhibition in elastase enzyme activity |
| topic | ionic liquids ionic liquids active pharmaceutical ingredients enzyme activity elastase inhibition |
| url | https://www.mdpi.com/1420-3049/26/1/200 |
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