评价离子液体和离子液体活性药物成分对弹性蛋白酶酶活性的抑制作用。
Evaluation of Ionic Liquids and Ionic Liquids Active Pharmaceutical Ingredients Inhibition in Elastase Enzyme Activity.
机构信息
LAQV, REQUIMTE, Department of Chemical Sciences, Laboratory of Applied Chemistry, Faculty of Pharmacy, Porto University, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
Unidade de Investigação para o Desenvolvimento do Interior, Instituto Politécnico da Guarda, Av. Dr. Francisco de Sá Carneiro, No. 50, 6300-559 Guarda, Portugal.
出版信息
Molecules. 2021 Jan 2;26(1):200. doi: 10.3390/molecules26010200.
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 values of the compounds tested. EC 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 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.
人中性粒细胞弹性蛋白酶（HNE）被用作炎症/感染的诊断生物标志物。在这项工作中，测试了 10 种离子液体（ILs）和 11 种离子液体活性药物成分（ILs-APIs），以评估它们对猪胰弹性蛋白酶酶活性的抑制作用，该酶常被用作 HNE 的模型。将离子液体插入某些药物中是有用的，因为具有抑制能力的 ILs 的插入也会减缓该酶参与的所有过程。因此，采用分光光度法测定了所测试化合物的 EC 值。得到的 EC 值为 124 ± 4 mM 至 289 ± 11 mM，对弹性蛋白酶毒性最大的 IL 是四丁基乙酸铵，毒性最小的是 1-丁基-3-甲基咪唑乙酸盐。此外，与所有测试的 IL-APIs 相比，水杨酸钠（原料）的 EC 值较低，苯扎氯铵双三氟甲烷磺酸盐的 EC 值较高。这项工作提供了关于研究中的 IL 和 IL-APIs 对弹性蛋白酶活性影响的重要信息。
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