Significance and impact of the study: Microorganisms such as Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella enterica subsp. enterica serovar Enteritidis and S. enterica subsp. enterica serovar Typhimurium can cause contamination in fresh or processed food products. The use of natural compounds, for instance carvacrol, can be an alternative to the use of synthetic bactericides. Our data demonstrate that the carvacrol nanoemulsion (NECV) had stability for up to 90 days, promoted inhibitory activity against all evaluated microorganisms , and improved antimicrobial activity against P. aeruginosa, S. aureus and S. Typhimurium when compared to free oil. These findings suggest that NECV can be evaluated as a food preservative to promote antimicrobial activity.
The compound (E)-2-cyano-N,3-diphenylacrylamide (JMPR-01) was structurally developed using bioisosteric modifications of a hybrid prototype as formed from fragments of indomethacin and paracetamol. Initially, in vitro assays were performed to determine cell viability (in macrophage cultures), and its ability to modulate the synthesis of nitrite and cytokines (IL-1β and TNFα) in non-cytotoxic concentrations. In vivo, anti-inflammatory activity was explored using the CFA-induced paw edema and zymosan-induced peritonitis models. To investigate possible molecular targets, molecular docking was performed with the following crystallographic structures: LT-A4-H, PDE4B, COX-2, 5-LOX, and iNOS. As results, we observed a significant reduction in the production of nitrite and IL-1β at all concentrations used, and also for TNFα with JMPR-01 at 50 and 25 μM. The anti-edematogenic activity of JMPR-01 (100 mg/kg) was significant, reducing edema at 2–6 h, similar to the dexamethasone control. In induced peritonitis, JMPR-01 reduced leukocyte migration by 61.8, 68.5, and 90.5% at respective doses of 5, 10, and 50 mg/kg. In silico, JMPR-01 presented satisfactory coupling; mainly with LT-A4-H, PDE4B, and iNOS. These preliminary results demonstrate the strong potential of JMPR-01 to become a drug for the treatment of inflammatory diseases.
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