Increased prevalence of methicillin-resistant Staphylococcus aureus (MRSA) has become a major threat to the health sector worldwide due to their virulence, limited therapeutic options and their distribution in both hospital and community settings. Discovery and development of new anti-MRSA agents as alternatives to the very few antibiotics left in the armamentarium are, thus, urgently required. Recently, an efflux mechanism in MRSA has been identified as one of the main contributors of resistance towards various structurally unrelated antibiotics. The potential of reserpine (a phytoalkaloid) as efflux pump inhibitor (EPI) against various microbes remains limited as the concentration needed for inhibition is toxic to humans. This study therefore aimed to evaluate 13 alkaloid compounds as potential inhibitory agents and/or potential EPIs against a panel of three MRSA isolates which not only differ in their susceptibility to vancomycin (amongst the last drugs available to treat serious MRSA infection), but also exhibited active efflux activity. Results indicated berberine's moderate inhibitiory activity against two MRSA isolates scoring a minimum inhibitory concentration (MIC) value of 125 microg/ml. Notable efflux inhibitory activity (ranging from two- to eightfold Ethidium Bromide MIC reduction) meanwhile was detected from quinine, piperine and harmaline using reserpine as the positive control. Findings from this study support the opinion that a vast number of potential phytocompounds with pharmacological potential await discovery. Therapeutic application of these compounds, however, warrants further investigation to ascertain their pharmacodynamics and safety aspects.
Galactomannan is a biopolymer polysaccharides mostly obtained from Leguminosae plant have shown an interesting capability as drug carrier. In this study, galactomannan from the seeds ofLeucaenaleucocephalaknown locally as ‘petai belalang’ was obtained by water extraction. The galactomannan was characterized structurally by nuclear magnetic resonance (NMR) and fourier transform infrared spectroscopy (FTIR). Highly molecular weight of galactomannan, > 2.56 x 106Da, was successfully extracted from the plant. Total carbohydrate content of this polysaccharides is 74.84% and composition of galactose and mannose have been confirm by high performance liquid chromatography (HPLC) which is 36.67% and 38.17% respectively. M/G ratio was determined as 1:1. Hence, galactomannan has been successfully extracted from the seeds ofLeucaenaleucocephala.
Galactomannan nanoparticles possess attractive properties such as biodegradable and biocompatible; significant in biomedical applications. Galactomannan (GA) isolated from the mature seed of a local plant, petai belalang known scientifically as Leucaena leucocephala were modified to acrylated galactomannan (AcGA) which acted as a precursor molecule for the preparation of crosslinked galactomannan nanoparticles (CL-GA). AcGA was synthesized using acryloyl chloride (AC) as a chemical modifier through esterification process. Trimethylolpropane triacrylate (TMPTA) was used as the crosslinker for the preparation of CL-GA. Successful conjugation of GA with acrylates was verified by 1H NMR and FTIR spectroscopies. Thermal properties of pure galactomannan, AcGA and CL-GA were measured using DSC to complement spectroscopic results. TEM images revealed the particle size of AcGA to be in the range of 30-100 nm; and increased to 200-850 nm range after the crosslinking process. Efficiency of CL-GA to trap crystal violet dye as a model drug was followed by UV Vis Spectroscopy. Results showed that CL-GA is capable of trapping crystal violet dye and has the potential to be used as a drug carrier.
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