A series of 15 previously reported N4-substituted isatin-3-thiosemicarbazones 3a-o has been screened for cytotoxic, antibacterial, antifungal and urease inhibitory activities. Compounds 3b, 3e and 3n proved to be active in cytotoxicity assay; 3e exhibited a high degree of cytotoxic activity (LD50 = 1.10 × 10− 5 M). Compound 3h exhibited significant antibacterial activity against B. subtilis, whereas compounds 3a, 3k and 3l displayed significant antifungal activity against one or more fungal strains i.e.T. longifusus, A. flavus and M. canis. In human urease enzyme inhibition assay, compounds 3g, 3k and 3m proved to be the most potent inhibitors, exhibiting relatively pronounced inhibition of the enzyme. These compounds, being non-toxic, could be potential candidates for orally effective therapeutic agents to treat certain clinical conditions induced by bacterial ureases like H. pylori urease. This study presents the first example of inhibition of urease by isatin-thiosemicarbazones and as such provides a solid basis for further research on such compounds to develop more potent inhibitors.
Hemicelluloses are biopolymers with versatile properties for biomedical applications. Herein, hemicellulose (arabinoxylan)-based antibacterial film dressings were prepared and characterized. Arabinoxylan was isolated from psyllium husk. Blank and gentamicin-loaded films were prepared by the solvent cast method using glycerol as the plasticizer. The appropriate composition of the films was obtained by varying the amounts of arabinoxylan, glycerol, and gentamicin. The films were found to be transparent, smooth, bubble-free, flexible, and easily peelable with 2% to 3% arabinoxylan. They had uniform thickness and swelled up to 60% of their initial size. The mechanical properties and water vapor transmission rate through the films were found to be suitable for wound-dressing application. Fourier transform infrared spectroscopy (FTIR) analysis confirmed drug–film compatibility. In an in vitro release study, more than 85% of the gentamicin was released from the films in 12 h. The antibacterial activities of the gentamicin-loaded films were found to be close to the standard gentamicin solution. The films were found to be cytocompatible in cell viability assay. These results suggested that hemicellulose-based films are promising materials for the dressing of infected wounds.