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Self-association of bee propolis: effects on pharmaceutical applications
Jiri Trousil,Martin Hruby,Jiri Panek,Jana Matějková,Jan Kucka,Petr Stepanek 한국약제학회 2014 Journal of Pharmaceutical Investigation Vol.44 No.1
Propolis is a resinous product collected byhoneybees from various plant sources; it is widely used intraditional medicine and has been reported to have a broadspectrum of pharmacological effects (i.e., antibacterial,antifungal, antiviral and anti-inflammatory effects). Themost commonly used propolis formulations are gargles, inwhich propolis tinctures are diluted with water. The dilutionprocess is accompanied by nanoprecipitation, and thepropolis droplets are dispersed in the prepared gargle. Inthe present study, we investigated the dependence of theproperties of propolis nanodispersions on the method ofpreparation. The particle size was found to be approximately150 nm and was observed to decrease withincreasing dilution as the zeta potential of the particlesbecame more negative, which stabilized the dispersion. The dispersion dissolved upon alkalization and reprecipitatedduring acidification. The addition of salt destabilizedthe dispersion. The uptake of propolis from the dispersionwas modeled using 1-octanol and was found to be rapidand only slightly dependent on the nanoparticle size. Propolis susceptibility tests showed that the most effectivedispersion of propolis was tenfold-diluted EEP (P-80-10and JP-80-10). The disc diffusion method was used toevaluate the antibacterial activity of chosen dispersions ofpropolis against Staphylococcus aureus, Escherichia coliand Candida albicans. Propolis samples with differentlocations of origin exhibited different effects against thestrain of C. albicans.
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( Jana Mattova ),( Pavla Pouckova ),( Petr Urbanek ),( Martin Hruby ),( Jan Kucka ),( Miroslav Vetrik ),( Michaela Skodova ),( Petr Stepanek ),( Milos Petrik ),( Zbynek Novy ) 대한내과학회 2014 대한내과학회 추계학술대회 Vol.2014 No.1
Background: Wilson`s disease is a genetic disorder caused by a malfunction of ATPase 7B that leads to high accumulation of copper in the organism and consequent toxic effects. We propose a gentle therapy to eliminate the excessive copper content with oral administration of insoluble non-resorbable polymer sorbents containing selective chelating groups for copper ions (Cu²<sup>+</sup> ions). Methods: Polymeric beads with the chelating agents triethylenetetramine, N,N-di(2-pyridylmethyl)amine and 8-hydroxyquinoline were investigated. We performed a long term experiment with Wistar rats fed a diet containing the particular polymers. Further, we investigated non-resorbability of polymeric beads. We measured organ radioactivity after oral administration of 8-hydroxyquinoline on polymer radiolabelled with iodine-125. Non-resorbability was also tested with small animal PET/CT imaging (using copper-64) in NMR mice. Results: In a long-term experiment with Wistar rats fed a diet containing the polymers, we have found that there were no signs of polymer toxicity and the addition of polymers to the diet led to a significant reduction in the copper contents in the kidneys, brains, and livers of the rats. 8-hydroxyquinoline on polymer radiolabelled with iodine-125 was not absorbed from the digestive tract after oral administration. Non-resorbability was also confirmed with PET/CT imaging. Conclusions: We have shown that polymers containing specific ligands could potentially be novel therapeutics for Wilson`s disease. Polymeric beads significantly reduced copper content in selected organs and they are non-resorbable from digestive tract and fully eliminated in feces after oral administration.
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