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Disposition of New Synthetic Drugs in The Organism. Pharmacokinetics and Biotransformation Study. Toxicological Detection in Biological Materials.
Židková, Monika ; Balíková, Marie (advisor) ; Šustková, Magdaléna (referee) ; Šanda, Miloslav (referee)
The object of this thesis was the study on the pharmacokinetics and biotransformation of selected abused new synthetic drugs, specifically belonging to cathinone and aminoindane groups, in experimental rats. This work consisted of two parts: a biotransformation study of mephedrone, methylone, 5,6-methylenedioxy-2- aminoindane (MDAI) and a distribution profile study of mephedrone, methylone, MDAI and naphyrone. This document is presented as a commentary to the original papers, which were published in peer reviewed journals. The samples of blood and tissue (brain, lungs, liver) were taken at specific times after a subcutaneous single bolus dose of the studied drugs. The urine samples for the biotransformation studies were collected over a 24-hour period following the sc. dose. The LC/HRMS method was used for metabolite detection and quantitative analysis. Our findings not only included testing metabolites of the aforementioneddrugs against the synthesized reference standards, but also discovering previously unknown metabolites of these drugs. Ten phase I and five phase II metabolites aside from the parent drug were identified in urine after mephedrone administration by comparison of their spectra against those of reference standards and/or MS2 spectra of previously identified metabolites. The main...
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Larvae of flesh fly Neobellieria bullata as a source for novel antimicrobial peptides
Neubauerová, Tereza ; Macková, Martina ; Macek, Tomáš ; Šanda, Miloslav ; Voburka, Zdeněk
The antibiotic resistant strains of microorganisms are increasing threat for public health. Antimicrobial peptides from natural sources display a wide spectrum of activity. In our laboratory, several peptide fractions with antimicrobial acivity against gram-positive and gramnegative bacteria and fungi were isolated from larvae of flesh fly Neobellieria bullata. The presence of peptides was proved by tricine electrophoresis, molecular weights and sequences determination by MS and Edman sequencing, respectively. In comparison with database sequences we obtained structures present mainly in insect and amphibian antimicrobial peptides, but total matches were not higher than in 36%. Upon the obtained sequence motifs we designed structures of several synthetic peptides. These were synthetised on the Rink amide MBHA resin. Synthesis was performed according Fmoc/PyBOP-DIEA protocol. Antimicrobial activity of these peptides was determined.
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Isolation of antimicrobial peptides and proteins from tomato
Králová, M. ; Šanda, Miloslav ; Macková, M. ; Macek, Tomáš
Recent emerging problem is occurrence of multiresistant pathogens. This inconvenience makes people to search for new antimicrobials. One of possible ways is looking for natural antimicrobial peptides. In our project, green tissues of tomato (Solanum lycopersicum) were chosen for isolation of such peptides. Extracts obtained were fractionated by solid phase extraction and liquid chromatography. Antimicrobial activities were tested on model microorganisms. Several fractions exhibited antimicrobial activity against bacteria and fungi. In the extracts, precursors of two antifungal proteins were identified.
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