Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme Activity

被引:15
|
作者
Mota, Fatima A. R. [1 ,2 ]
Pereira, Sarah A. P. [1 ]
Araujo, Andre R. T. S. [1 ,2 ]
Saraiva, M. Lucia M. F. S. [1 ]
机构
[1] Univ Porto, Fac Pharm, Dept Chem Sci, LAQV,REQUIMTE,Lab Appl Chem, Rua Jorge Viterbo Ferreira 228, P-4050313 Porto, Portugal
[2] Inst Politecn Guarda, Unidade Invest Desenvolvimento Interior, Av Dr Francisco de Sa Carneiro 50, P-6300559 Guarda, Portugal
来源
MOLECULES | 2021年 / 26卷 / 01期
关键词
ionic liquids; ionic liquids active pharmaceutical ingredients; enzyme activity; elastase; inhibition; HUMAN NEUTROPHIL ELASTASE; CATHEPSIN-G; TOXICITY; STABILITY;
D O I
10.3390/molecules26010200
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 EC50 values of the compounds tested. EC50 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 EC50 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.
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页数:14
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