Synthesis and characterization of gold glyconanoparticles functionalized with sugars of sweet sorghum syrup

Gold glyconanoparticles were synthesized by a simple, rapid, and eco-friendly method by using sweet Sorghum syrup for application in biomedicine and biotechnology. The nanostructures of the prepared gold nanoparticles were confirmed by using UV-visible absorbance, TEM, SAED, FTIR, EDAX, XRD, and photoluminescence analyses. The formation of gold nanoparticles at both room and boiling temperatures and kinetics of the reaction were monitored by UV-visible spectroscopy and TEM studies. TEM analysis revealed that the obtained nanoparticles were mono-dispersed and spherical in shape with an average particle size of 7 nm. The size of the nanoparticles was influenced by the concentration of Sorghum syrup. The presence of elemental gold was confirmed by EDAX analysis. Based on the FTIR analysis, it was observed that the sugars present in the Sorghum syrup possibly acts as capping agents. The zeta potential analysis revealed that the glyconanoparticles were negatively charged with a potential of 25 mV. The XRD and SAED patterns also suggest that the nanoparticles were crystalline in nature and these particles were found to exhibit visible photoluminescence. Fructose and glucose present in sweet Sorghum syrup were demonstrated as responsible sugars for the reduction of gold ions, and sucrose stabilized the formed nanoparticles. The proposed mechanism for the formation and stabilization of gold glyconanoparticles is based on the phenomenon of ‘‘macromolecular crowding.’’ This is the first report on the use of sweet Sorghum syrup for the green synthesis of gold glyconanoparticles at both room and boiling temperature

Silver glyconanoparticles functionalized with sugars of sweet sorghum syrup as an antimicrobial agent

Bio-directed synthesis of metal nanoparticles is gaining importance due to their biocompatibility, low toxicity and eco-friendly nature. We used sweet sorghum syrup for a facile and cost-effective green synthesis of silver glyconanoparticles. Silver nanoparticles were formed due to reduction of silver ions when silver nitrate solution was treated with sorghum syrup solutions of different pH values. The nanoparticles were characterized by UV–vis, TEM (transmission electron microscopy), DLS (dynamic light scattering), EDAX (energy dispersive X-ray spectroscopy), FT-IR (fourier transform infrared spectroscopy) and XRD (X-ray diffraction spectroscopy). The silver glyconanoparticles exhibited a characteristic surface plasmon resonance around 385 nm. At pH 8.5, the nanoparticles were mono-dispersed and spherical in shape with average particle size of 11.2 nm. The XRD and SAED studies suggested that the nanoparticles were crystalline in nature. EDAX analysis showed the presence of elemental silver signal in the synthesized glyconanoparticles. FT-IR analysis revealed that glucose, fructose and sucrose present in sorghum syrup acted as capping ligands. Silver glyconanoparticles prepared at pH 8.5 had a zeta potential of −28.9 mV and were anionic charged. They exhibited strong antimicrobial activity against Gram-positive, Gram-negative and different Candida species at MIC values ranging between 2 and 32 μg ml−1. This is first report on sweet sorghum syrup sugars-derived silver glyconanoparticles with antimicrobial propert

Potential therapeutic applications of microbial surface-activecompounds

Numerous investigations of microbial surface-active compounds or biosurfactants over the past two decades have led to the discovery of many interesting physicochemical and biological properties including antimicrobial, anti-biofilm and therapeutic among many other pharmaceutical and medical applications. Microbial control and inhibition strategies involving the use of antibiotics are becoming continually challenged due to the emergence of resistant strains mostly embedded within biofilm formations that are difficult to eradicate. Different aspects of antimicrobial and anti-biofilm control are becoming issues of increasing importance in clinical, hygiene, therapeutic and other applications. Biosurfactants research has resulted in increasing interest into their ability to inhibit microbial activity and disperse microbial biofilms in addition to being mostly nontoxic and stable at extremes conditions. Some biosurfactants are now in use in clinical, food and environmental fields, whilst others remain under investigation and development. The dispersal properties of biosurfactants have been shown to rival that of conventional inhibitory agents against bacterial, fungal and yeast biofilms as well as viral membrane structures. This presents them as potential candidates for future uses in new generations of antimicrobial agents or as adjuvants to other antibiotics and use as preservatives for microbial suppression and eradication strategies

An azido-oxazolidinone antibiotic for live bacterial cell imaging and generation of antibiotic variants

An azide-functionalised analogue of the oxazolidinone antibiotic linezolid was synthesised and shown to retain antimicrobial activity. Using facile 'click' chemistry, this versatile intermediate can be further functionalised to explore antimicrobial structure-activity relationships or conjugated to fluorophores to generate fluorescent probes. Such probes can report bacteria and their location in a sample in real time. Modelling of the structures bound to the cognate 50S ribosome target demonstrates binding to the same site as linezolid is possible. The fluorescent probes were successfully used to image Gram-positive bacteria using confocal microscopy

Structure aided design of chimeric antibiotics

The rise of antibiotic resistance is of great clinical concern. One approach to reducing the development of resistance is to co-administer two or more antibiotics with different modes of action. However, it can be difficult to control the distribution and pharmacokinetics of two drugs to ensure both concentrations remain within the range of therapeutic efficacy whilst avoiding adverse effects. Hybrid drugs, where two drugs are linked together with a flexible linker, have been explored, but the resultant large, flexible molecules can have poor bioavailability. We have developed a chimeric approach using click chemistry where the pharmacophores of two drugs are overlapped into a single smaller, more drug-like molecule. Design and selection of compounds were assisted by in silico structural docking. We prepared a series of compounds that include candidates showing activity against the targets of both trimethoprim; dihydrofolate reductase, and ciprofloxacin; DNA gyrase and topoisomerase IV. The resultant triazole containing molecules show modest, but broad spectrum activities against drug sensitive and resistant Gram-negative and Gram-positive bacteria, with no observable cytotoxicity. (C) 2012 Elsevier Ltd. All rights reserved

Pharmacological targeting of the transcription factor SOX18 delays breast cancer in mice

Pharmacological targeting of transcription factors (TF) holds great promise for the development of new therapeutics, but strategies based on blockade of DNA binding, nuclear shuttling, or individual protein partner recruitment have yielded limited success. TFs typically engage in complex interaction networks, likely masking the effects of specifically inhibiting single protein-protein interactions. Here, we used a combination of genomic, proteomic and biophysical methods to discover a suite of protein-protein interactions involving the SOX18 TF, a known regulator of vascular development. We describe a small-molecule that disrupts a discrete subset of SOX18-dependent interactions. This compound selectively suppressed SOX18 transcriptional outputs in vitro and interfered with vascular development in zebrafish larvae. In a mouse pre-clinical model of breast cancer, treatment with this inhibitor significantly improved survival by reducing tumour vessel density and metastatic spread. Our studies validate an interactome-based molecular strategy to interfere with TF activity, for the development of novel disease therapeutic