Bioprospection of anti-inflammatory phytochemicals suggests rutaecarpine and quinine as promising 15-lipoxygenase inhibitors.

15-Lipoxygenase (15-LOX) belongs to the family of nonheme iron containing enzymes that catalyzes the peroxidation of polyunsaturated fatty acids (PUFAs) to generate eicosanoids that play an important role in signaling pathways. The role of 15-LOX has been demonstrated in atherosclerosis as well as other inflammatory diseases. In the present study, drug-like compounds were first screened from a set of anti-inflammatory phytochemicals based on Lipinski's rule of five (ROF) and in silico toxicity filters. Two lead compounds-quinine (QUIN) and rutaecarpine (RUT) were shortlisted by analyzing molecular interactions and binding energies of the filtered compounds with the target using molecular docking. Molecular dynamics simulation studies indicate stable trajectories of apo_15-LOX and docked complexes (15-LOX_QUIN and 15-LOX_RUT). In vitro 15-LOX inhibition studies shows that both QUIN and RUT have lower inhibitory concentration (IC50 ) value than the control (quercetin). Both QUIN and RUT exhibit moderate antioxidant activities. The cell viability study of these compounds suggests no significant toxicity in HEK-293 cell lines. Further, QUIN and RUT both did not show any inhibition against selected Gram-positive and Gram-negative bacterial species. Thus, based on our present findings, rutaecarpine and quinine may be suggested as promising 15-LOX inhibitor for the prevention of the atherosclerosis development.

Co-occurrence of antimicrobial resistance and virulence determinants in enterococci isolated from traditionally fermented fish products.

OBJECTIVES: Fermented foods frequently consumed in Northeast India can act as a reservoir for disseminating pathogenic organisms. Enterococci are often responsible for contamination of food products. This study investigated the antimicrobial resistance and co-existing virulence determinants of enterococci found in traditionally processed foods in India. METHODS: A total of 38 enterococci isolates identified as Enterococcus faecalis isolated from fermented fish samples from retail markets of Northeast India were selected for screening of pathogenic traits. RESULTS: Of the 38 isolates, 8 (21%) were able to hydrolyse gelatin and 13 (34%) showed protease activity. Screening for haemolytic activity of the isolates showed no positive test on sheep blood. The presence of virulence genes (gelE, agg, esp, cpd, efaAfs and cylA) was investigated by PCR. gelE, agg and esp were present in 17, 13 and 4 isolates, respectively. cpd and efaAfs were found in all isolates, whereas cylA was not detected. High resistance percentages to various antibiotics included kanamycin (63%), vancomycin and gentamicin (58%), tetracycline (53%) and rifampicin (50%). The vanA genotype was confirmed in 15 multidrug- and vancomycin-resistant strains. CONCLUSION: The simultaneous occurrence of virulence determinants and antimicrobial resistance in enterococci prevalent in the fermented fish products studied poses a potential threat of transmission to humans through the food chain. This study highlights the importance of E. faecalis as a reservoir of antimicrobial resistance and virulence factors and their potential transfer to humans. The findings reopen the issue of food safety regarding enterococci prevalent in traditionally processed fish products in the region.

A reusable magnetic nickel nanoparticle based catalyst for the aqueous synthesis of diverse heterocycles and their evaluation as potential anti-bacterial agent.

A library of biologically important heterocycles, viz. pyrazolyl pyrimidine-triones, bis(heterocyclyl)methanes were successfully synthesised by the condensation of barbituric acid, pyrazolone with an aldehyde and dimedone/4-hydoxy coumarin with various substituted aldehydes in aqueous medium at room temperature catalysed by nickel nanoparticles which proved to be an efficient magnetically recyclable catalyst. The method is simple, eco-friendly and gave excellent yields of the products without taking recourse to column chromatographic separation procedures. Computational method was employed to elucidate the selective formation of uncyclised product in reaction course. The biological activity of the synthesized compounds were investigated and the results demonstrated profound antibacterial activity.