Green synthesis of N,S-doped carbon dots for tartrazine detection and their antibacterial activities.

A simple, green and low-cost method was developed for the synthesis of highly fluorescent N,S-doped carbon dots (N,S-CDs) via the hydrothermal treatment of Gandha Prasarini (GP) leaves as a natural source of carbon, nitrogen and sulfur. The as-prepared N,S-CDs exhibited excitation-dependent green fluorescence emission (λex = 450 nm, λem = 525 nm) with excellent stability, and were used as a fluorescent probe for the selective detection of tartrazine with a limit of detection of 0.18 µM. The fluorescence quenching of N,S-CDs was due to the inner filter effect. The developed method has been employed for the determination of tartrazine in honey and soft drinks with satisfactory recovery ranging from 92 to 110.2%. In addition, the antibacterial activity of the N,S-CDs was explored against both Gram-negative bacteria, Escherichia coli (E. coli) and Pseudomonas aeruginosa (P. aeruginosa), and Gram-positive bacteria, Staphylococcus aureus (S. aureus). The antibacterial mechanism of the N,S-CDs was investigated. The results indicated that the antibacterial activity was due to the membrane damage of the bacteria by the N,S-CDs. Besides, the N,S-CDs showed negligible lytic effects on human erythrocytes. These findings will inspire further exploitation of CD-based nano-bactericides in biomedical applications.

Ce-catalyzed regioselective synthesis of pyrazoles from 1,2-diols via tandem oxidation and C-C/C-N bond formation.

A novel and efficient cerium-catalyzed tandem oxidation and intermolecular ring cyclization of vicinal diols with hydrazones has been achieved for the regioselective synthesis of pyrazole derivatives. The corresponding 1,3-di- and 1,3,5-trisubstituted pyrazoles were obtained in moderate to excellent yields. The reaction has the advantages of mild conditions, easily available starting materials, broad substrate scope and good functional group tolerance.

Lipid Flip-Flop-Inducing Antimicrobial Phytochemicals from Gymnema sylvestre are Bacterial Membrane Permeability Enhancers.

An amphiphilic phytochemical fraction isolated from methanol extract of Gymnema sylvestre leaf powder contained six terpenoids, two flavonoids, and one alkaloid that induced rapid flip-flop of fluorescent phospholipid analog in the phosphatidyl choline bilayer. Lipid-flipping activity of the methanol-extracted fraction of G. sylvestre (MEFGS) was dose-dependent and time-dependent with a rate constant k = (12.09 ± 0.94) mg-1 min-1 that was saturable at (40 ± 1) % flipping of the fluorescent lipid analogue. Interactions of MEFGS phytochemicals with large unilamelar vesicles led to time-dependent change in their rounded morphology into irregular shapes, indicating their membrane-destabilizing activity. MEFGS exhibited antibacterial activity on Escherichia coli (MTCC-118), Staphylococcus aureus (MTCC-212), and Pseudomonas aeruginosa (MTCC-1035) with IC50 values 0.5, 0.35, and 0.1 mg/mL, respectively. Phytochemicals in MEFGS increased membrane permeabilization in all three bacteria, as indicated by 23, 17, and 17% increase in the uptake of crystal violet, respectively. MEFGS enhanced membrane damage, resulting in a 3-5 fold increase in leakage of cytosolic ions, 0.5-2 fold increase in leakage of PO4 -, and 15-20% increase in loss of cellular proteins. MEFGS synergistically increased the efficacy of curcumin, amoxillin, ampicillin, and cefotaxime on S. aureus probably by enhancing their permeability into the bacterium. For the first time, our study reveals that phytochemicals from G. sylvestre enhance the permeability of the bacterial plasma membrane by facilitating flip-flop of membrane lipids. Lipid-flipping phytochemicals from G. sylvestre can be used as adjuvant therapeutics to enhance the efficacy of antibacterials by increasing their bioavailability in the target bacteria.

Fe-catalyzed one-pot synthesis of 1,3-di- and 1,3,5-trisubstituted pyrazoles from hydrazones and vicinal diols.

An iron-catalyzed route for the regioselective synthesis of 1,3- and 1,3,5-substituted pyrazoles from the reaction of diarylhydrazones and vicinal diols has been developed. This method was found to be practical with wide substrate scope.