Automatic Identification of Myeloperoxidase Natural Inhibitors in Plant Extracts.

The aim of this study is the development of an automated method for myeloperoxidase activity evaluation and its application in testing the inhibitory action of different plant extracts on the activity of the enzyme. This enzyme has its concentration increased in inflammatory and infectious processes, so it is a possible target to limit these processes. Therefore, an automatic sequential in-jection analysis (SIA) system was optimized and demonstrated that it is possible to obtain results with satisfactory accuracy and precision. With the developed method, plant extracts were studied, as promising candidates for MPO inhibition. In the group of selected plant extracts, IC50 values from 0.029 ± 0.002 mg/mL to 35.4 ± 3.5 mg/mL were obtained. Arbutus unedo L. proved to be the most inhibitory extract for MPO based on its phenolic compound content. The coupling of an automatic SIA method to MPO inhibition assays is a good alternative to other conventional methods, due to its simplicity and speed. This work also supports the pharmacological use of these species that inhibit MPO, and exhibit activity that may be related to the treatment of infection and inflammation.

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, 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.

Comparative analysis of electrochemical and optical sensors for detection of chronic wounds biomarkers: A review.

Chronic wounds (CW) present a significant healthcare challenge due to their prolonged healing time and associated complications. To effectively treat these wounds and prevent further deterioration, monitoring their healing progress is crucial. Traditional wound assessment methods relying on visual inspection and subjective evaluation are prone to inter-observer variability. Biomarkers play a critical role in objectively evaluating wound status and predicting healing outcomes, providing quantitative measures of wound healing progress, inflammation, infection, and tissue regeneration. Recent attention has been devoted to identifying and validating CW biomarkers. Various studies have investigated potential biomarkers, including growth factors, cytokines, proteases, and extracellular matrix components, shedding light on the complex molecular and cellular processes within CW. This knowledge enables a more targeted and personalized approach to wound management. Accurate and sensitive techniques are necessary for detecting CW biomarkers. Thus, this review compares and discusses the use of electrochemical and optical sensors for biomarker determination. The advantages and disadvantages of these sensors are highlighted. Differences in detection capabilities and characteristics such as non-invasiveness, portability, high sensitivity, specificity, simplicity, cost-effectiveness, compatibility with point-of-care applications, and real-time monitoring of wound biomarkers will be pointed out and compared. In summary, this work provides an overview of CW, explores the emerging field of CW biomarkers, and discusses methods for detecting these biomarkers, with a specific focus on optical and electrochemical sensors. The potential of further research and development in this field for advancing wound care and improving patient outcomes will also be noted.

Anticancer potential of NSAID-derived tris(pyrazolyl)methane ligands in iron(II) sandwich complexes.

Tris(pyrazolyl)methane (tpm), 2,2,2-tris(pyrazolyl)ethanol (tpmOH) and its esterification derivatives with ibuprofen and flurbiprofen (tpmIBU and tpmFLU) were used as ligands to obtain complexes of the type [Fe(tpmX)2]Cl2 (1-4). The tpmIBU and tpmFLU ligands and corresponding complexes 3 and 4 were characterized by IR and multinuclear NMR spectroscopy, and the structure of tpmIBU was elucidated by single crystal X-ray diffraction. Complexes 1-4 were also assessed for their behaviour in aqueous media (solubility in D2O, octanol/water partition coefficient, stability in physiological-like conditions). The antiproliferative activity of ligands and complexes was determined on A2780, A2780cis and A549 cancer cell lines and the non-cancerous HEK 293T and BJ cell lines. The ligands and complexes were investigated for their ability to inhibit COX-2 (cyclooxygenase) and HNE (4-hydroxynonenal) enzymes. Complexes 3 and 4 exhibited cytotoxicity that may be attributed predominantly to their bioactive fragments, while DNA binding and enhancement of ROS production do not appear to play any significant role.