RESUMEN
The current work aims to generate novel Schiff bases by reacting substituted aldehydes with amine derivatives catalyzed by a natural acid. The developed compounds underwent diverse physicochemical analyses including liquid chromatography-mass spectrometry, Fourier transform infrared spectroscopy, scanning electron microscopy, 1H- and 13C-nuclear magnetic resonance, and X-ray diffraction. Furthermore, differential thermogravimetric, thermogravimetric, and differential thermal analysis techniques were employed in a nitrogen-free environment to determine kinetic parameters. These data were then used in model-free isoconversional methods (e.g., Friedman, Kissinger-Akahira-Sunose, and Flynn-Wall-Ozawa). The Schiff bases were evaluated for their in vitro and in silico α-amylase inhibitory activity. Schiff base-2 displayed the highest inhibition compared with the reference drug acarbose. In comprehensive MTT assay cytotoxicity investigations, both Schiff bases showed strong anticancer capabilities against the human lung cancer cell line (A549). Moreover, this study demonstrated effectiveness of synthetic compounds in screening Caenorhabditis elegans for anti-Alzheimer's and stress resistance properties. The simplicity of its biology allowed precise evaluation of the effect of compounds on neuronal function and stress response. This research enhances drug discovery efforts for Alzheimer's and stress-related disorders, potentially improving patient outcomes.
RESUMEN
The present study investigated the prospect of improvement in pharmacokinetic (PK) parameters of marbofloxacin due to alpha-1-monolaurin pre-treatment in broiler chickens. Two groups of broilers were administered a single oral dose of marbofloxacin (5.00 mg kg-1 body weight): Group-I without pre-treatment and Group-II with alpha-1-monolaurin pre-treatment (4.00 g kg-1 feed for 10 days). Blood sampling was done periodically for both groups and plasma marbofloxacin concentrations were determined using ultra-high performance liquid chromatography. Pharmacokinetic parameters using non-compartmental modelling approach were calculated with the PKSolver software. Statistical analysis revealed significant differences in plasma marbofloxacin concentrations between the two groups at 1, 2, and 24 hr. Group-II birds exhibited a higher mean maximum plasma concentration (2.43 µg mL-1) at an earlier time (Tmax: 1.38 hr) compared to Group-I. The plasma concentrations of marbofloxacin were maintained above 0.10 and 0.18 µg mL-1 up to 24 hr in Group-I and Group-II broilers, respectively. Significant differences were observed in PK parameters such as the area under the curve and total body clearance. The mean relative oral bioavailability of Group-II birds compared to Group-I was 119.61%. The findings of the study provided evidence of PK parameters enhancement of marbofloxacin in the alpha-1-monolaurin pre-treated group. The calculated PK-pharmacodynamic indices for marbofloxacin predicted clinical efficaciousness in the broiler chickens.
RESUMEN
INTRODUCTION: Fluoroquinolones are most widely used for empirical treatment of gastrointestinal disease due to emergence of drug resistant strains to other antimicrobials. They are also indulged in cutaneous adverse drug reactions with varying form of severity. CASE PRESENTATION: A 43 year old male patient developed fixed drug eruptions after administration of tablet norfloxacin and metronidazole for treatment of colicky abdominal pain with diarrhoea. Erythematous rashes involved whole body including buccal mucosa. Causative drugs were stopped and patient was managed by local as well as systemic therapy and was recovered after 20 days. CONCLUSION: Awareness among healthcare professionals regarding FDEs and its management is essential to prevent mortality and morbidity and counsel patient regarding future use of drugs causing reactions with physician's advice.