Synthetic approaches for new labeling tags facilitating glycan analysis

This study is focused on the synthesis of labels based on the pyrene core bearing several ionizable quaternary amines and the efficient carbonyl-reactive group, such as primary amine or hydrazine

SMV-2017-732: Preparation, testing and delivery of isoelectric point standards

The project continues long-term cooperation of both participants. The low-molecular mass pI markers were synthesized and examined with aim to fill up and deliver the previously described compounds

Evaluation of stationary phases for HPLC based on nanofibers

In this study, the performance parameters were compared for the set of chromatographic columns filled with polyacrylonitrile nanofibers processed in the different manner. The advantages and challenges of the novel fillings were discussed

Monosaccharide anhydrides in atmospheric aerosols - optimization of separation and detection by means of LC-MS technique

We report a simple analytical method, based on high-performance liquid chromatography with mass spectrometric detection, which was developed and utilized to determine monosaccharide anhydrides in atmospheric aerosols

SMV-2017-743: Preparation, testing and delivery of isoelectric point standards

The project continues long-term cooperation of both participants. The low-molecular mass pI markers were synthesized and examined with aim to fill up and deliver the previously described compounds

Study on oligosaccharide composition of wort and beer samples by liquid chromatography/electrospray ionization tandem mass spectrometry

LC-MS technique was successfully applied to the description of oligosaccharides mixtures in wort and beer samples. Based on the important differences in MS/MS spectra the structural features of coeluted oligosaccharides were found

Study of the cell wall of Staphylococcus aureus and its sensitivity to enzybiotics

The endolysin resistant and sensitive strains of Staphylococcus aureus were compared by means of LC-MS based structural analysis of peptidoglycan isolated from their cell walls. The structural explanation of the resistance was suggested

Enzybiotics LYSSTAPH-S and LYSDERM-S as Potential Therapeutic Agents for Chronic MRSA Wound Infections

Antibacterial antibiotic therapy has played an important role in the treatment of bacterial infections for almost a century. The increasing resistance of pathogenic bacteria to antibiotics leads to an attempt to use previously neglected antibacterial therapies. Here we provide information on the two recombinantly modified antistaphylococcal enzymes derived from lysostaphin (LYSSTAPH-S) and endolysin (LYSDERM-S) derived from kayvirus 812F1 whose target sites reside in the bacterial cell wall. LYSSTAPH-S showed a stable antimicrobial effect over 24-h testing, even in concentrations lower than 1 µg/mL across a wide variety of epidemiologically important sequence types (STs) of methicillin-resistant Staphylococcus aureus (MRSA), especially in the stationary phase of growth (status comparable to chronic infections). LYSDERM-S showed a less potent antimicrobial effect that lasted only a few hours at concentrations of 15 μg/mL and higher. Our data indicate that these antimicrobial enzymes could be of substantial help in the treatment of chronic MRSA wound infections

Adamantane-substituted purines and their β-cyclodextrin complexes: Synthesis and biological activity

Cyclin-dependent kinases (CDKs) play an important role in the cell-division cycle. Synthetic inhibitors of CDKs are based on 2,6,9-trisubstituted purines and are developed as potential anticancer drugs; however, they have low solubility in water. In this study, we proved that the pharmaco-chemical properties of purine-based inhibitors can be improved by appropriate substitution with the adamantane moiety. We prepared ten new purine derivatives with adamantane skeletons that were linked at position 6 using phenylene spacers of variable geometry and polarity. We demonstrated that the adamantane skeleton does not compromise the biological activity, and some of the new purines displayed even higher inhibition activity towards CDK2/cyclin E than the parental compounds. These findings were supported by a docking study, which showed an adamantane scaffold inside the binding pocket participating in the complex stabilisation with non-polar interactions. In addition, we demonstrated that β-cyclodextrin (CD) increases the drug’s solubility in water, although this is at the cost of reducing the biochemical and cellular effect. Most likely, the drug concentration, which is necessary for target engagement, was decreased by competitive drug binding within the complex with β-CD. : © 2021 by the authors. Licensee MDPI, Basel, Switzerland.RVO: 68081715; Grantová Agentura České Republiky, GA ČR: GA 19-08410S; Univerzita Tomáše Bati ve Zlíně: IGA/FT/2021/001Internal Funding Agency of the Tomas Bata University in Zlin [IGA/FT/2021/001]; Czech Science FoundationGrant Agency of the Czech Republic [GA 19-08410S]; Institute of Analytical Chemistry of the Czech Academy of SciencesCzech Academy of Sciences [RVO: 68081715

Adamantane-bearing benzylamines and benzylamides: Novel building blocks for supramolecular systems with finely tuned binding properties towards β-cyclodextrin

Novel building blocks for the synthesis of supramolecular components based on adamantane-bearing benzylamines were prepared. The binding properties of these amines and the corresponding acetamides towards β-cyclodextrin (β-CD) were studied using mass spectrometry, NMR spectrometry, isothermal titration calorimetry and semi-empirical calculations. It was found that all of the examined guests predominantly formed 1:1 inclusion complexes in an enthalpy-driven manner with association constants of the order of 10 2-103 M-1. Stronger binding to the β-CD cavity was observed for guests with a longer spacer between the adamantane and benzene moieties and/or a 1,4-disubstituted benzene ring. © 2013 Taylor & Francis Group, LLC