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Phase II biotransformation of NSAID flobufen
Babú, Yogeeta ; Wsól, Vladimír (advisor) ; Nobilis, Milan (referee) ; Kuchař, Miroslav (referee)
Xenobiotic chemicals are chemicals foreign to life that are usually derived synthetically or from an abiotic process. The synthetic xenobiotic chemicals are often of enormous value to human society and are usually the majority of the chemicals in such important groups of substances as petrochemicals, pesticides, plastics and pharmaceuticals, where the term drug is usually applied when referring to xenobiotics. Biotransformation is a major mechanism for drug elimination, as they undergo biotransformation after they enter the body. Biotransformation, which almost always produces metabolites that are more polar than the parent compound, usually terminates the pharmacologic action of the parent drug and, via excretion, increases removal of the drug from the body. However, other consequences are possible, including similar or different pharmacologic activity, or toxicological activity. The routes by which drugs may be biotransformed are many and varied and include oxidation, reduction, hydrolysis and conjugation reactions, among others. It is important that these pathways are understood, as the route of metabolism of a drug can determine its ultimate pharmacological or toxicological activity. Drug biotransformation is divided into two phases: Phase I, or functionalisation reactions and Phase II, or conjugative...
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Photocatalytic activity of titanium precursors treated in low temperature plasma
Brožek, Vlastimil ; Matějíček, Jiří ; Šrank, Z. ; Mastný, L. ; Janča, J.
In order to obtain compact photocatalytically active materials, the possibility of preparation of new titania forms by oxidation of titanium compounds, having different crystal structures and oxidation degree, was verified. Four model substances were chosen: titanium carbide, nitride, diboride and Ti2O3. These compounds were prepared in the form of high-specific-surface powder, as well as large-area compact free-standing parts by CVD, PVD and especially plasma spraying. After high temperature treatment in a water stabilized plasma, generated by the WSP torch, a measurable photoactivity was observed; this could be further improved by controlled oxidation below 450°C. Oxidation in an RF-generated oxygen plasma appeared more efficient, especially in shorter reaction times. However, the experiments have shown that even keeping the reactor walls at 450°C did not prevent the uncontrolled temperature rise inside, during the reaction of the oxygen plasma with titanium compounds.
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Effect of management on three moss species of fen meadows (Breidleria pratensis, Sphagnum warnstorfii, Tomentypnum nitens)
VELEHRADSKÁ, Tereza
Effects of different types of management (control, mown, mown + disturbed (gaps) + litter removed) on three moss species of fen meadows were studied. Experimental plots were established at sixteen sites in the Bohemian Forest, in the foothills of the Bohemian Forest and in Českomoravská vrchovina. Relevés and micromaps of bryophytes in the plots 0.5 × 0.5m were sampled at the beginning of the experiment during the summer season of 2010 and then after 3 seasons (during the summer season of 2012) of performing management. The age of the abandoned meadows was also determined and values of pH, conductivity and height of water level of each plot were measured. Positive influences of both types of management on the cover of Tomentypnum nitens and of management with creating gaps and remowing of litter on the cover of Breidleria pratensis were significant. Effect of management on the Sphagnum warnstorfii was significant only when processes of remaining on already occupied places and the expansion to new places were tested separately. Enviromental values did not significantly influence the change of cover of any species between 2010 and 2012. In conclusion, it is clear that diverse management with reasonable use of these practices (mowing, creation of gaps, litter removal) is desirable for maintaining of vital and diverse bryophyte layer.
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Utilization of molecular markers in oil seed rape breeding programmes
KRISTINOVÁ, Helena
Current breeding of oilseed rape is focused on breeding of F1 hybrids and the male sterility and self-incompatibility could play the significant role in hybrid breeding programmes. Plant breeders also more widely utilize molecular genetic techniques for selection of desirable plants/genotypes. Molecular methods are faster, more reliable and more specific than conventional ones, which are based mainly on morphological descriptors. The aim of my thesis was to optimize PCR analysis methods and to develop specific molecular markers for target plant selection in oilseed rape hybrid breeding programmes. The new marker for detection of fertility restoration gene (Rf) in CMS Ogu-INRA plants was tested. New primer pair RsPPRF2/RsPPRR2 was designed in the coding region of PPR-B protein, which participates in the restoration of fertility in CMS Ogu-INRA. Also newly designed primers BrSLGIIF/BrSLGIIR were tested in SI plants. The optimal annealing temperaturse of these primers was 58 °C. But amplification in some SC plants was also observed. The optimization of the PCR reaction was performed for all designed primers. The set of F1 SI hybrids created by crossing of two lines with different S II haplotypes was tested by using of the PCR-RFLP technique for detection of polymorphism in amplified fragments.
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Effect of management on three moss species of fen meadow \kur{Breidleria pratensis, Sphagnum warnstorfii, Tomentypnum nitens}
VELEHRADSKÁ, Tereza
Effects of different types of management (control, mown, mown + disturbed (gaps) + litter removed) on three moss species of fen meadows were studied. Experimental plots were established at sixteen sites in the Bohemian Forest, in the foothills of the Bohemian Forest and in Českomoravská vrchovina. Relevés and micromaps of bryophytes in the plots 0.5 × 0.5m were sampled at the beginning of the experiment during the summer season of 2010 and then after 3 seasons (during the summer season of 2012) of performing management. The age of the abandoned meadows was also determined and values of pH, conductivity and height of water level of each plot were measured. Positive influences of both types of management on the cover of Tomentypnum nitens and of management with creating gaps and remowing of litter on the cover of Breidleria pratensis were significant. Effect of management on the Sphagnum warnstorfii was significant only when processes of remaining on already occupied places and the expansion to new places were tested separately. Enviromental values did not significantly influence the change of cover of any species between 2010 and 2012. In conclusion, it is clear that diverse management with reasonable use of these practices (mowing, creation of gaps, litter removal) is desirable for maintaining of vital and diverse bryophyte layer.
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Abiotic stress resposes in apple (Malus domestica Borkh.) tissue cultures
Krsek, Daniel ; Pospíšilová, Jana (referee) ; Lipavská, Helena (advisor)
Abiotic stress factors, primarily those which disturb plant water balance, cause extensive crop losses. With regard to sessile lifestyle, many mechanisms how to cope with these unfavourable conditions were developed during evolution of plants. As common impact of many of these stresses like drought, salinity or low temperatures is of osmotic nature, the osmotic adjustment represents important part of plant stress response. Mostly, this component of stress reaction is provided by organic compounds, which are referred to as compatible solutes, including polyhydroxyl compounds (sucrose, sugar alcohols, cyclitols, and oligosacharides) and nitrogen-containing compounds (mainly proline). The effect of these solutes is not only osmotic, but also osmoprotective as they are able to preserve integrity of membranes and macromolecules by mimicking their water envelope. The compatible solutes also contribute to quenching of reactive oxygen species overproduced under these stress conditions. This study is focused on apple (Malus domestica) producing, beside sucrose, sugar alcohol sorbitol as primary photosynthetic product and transporting these carbohydrates along with raffinose family oligosaccharides (RFO) for a long distance. In vitro tissue cultures derived from leaves of two apple cultivars differing in...
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Stereoselective Aza-Annulations
Mandelová, Zuzana
This thesis was focused on enrichment of yet known findings in the area of aza-annulations for doubled azaannulation, which was coming up from ethyl 3-alkoxy-2-oxocyclohexancarboxylates ethyl 4-alkoxy-2-alkyl-3- oxopentanoates. Decahydrophenanthroline derivatives and appropriate spiro compounds should be prepared by this method in cyclic and acyclic row of reactions, respectively. Aza-annulations, their advantages, ways of realization and their usage in preparation of important chemical substances mainly from the area of alkaloids are complexly described in the text. Furthermore, tried methods of preparation of starting materials in cyclic and acyclic row of reactions, following praparations of enamines as well as proper aza-annulations, different arrangement of reaction conditions in an effort to get better yields of these reactions, and all the results are there also discussed in detail.
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Abiotic stress resposes in apple (Malus domestica Borkh.) tissue cultures
Krsek, Daniel
Abiotic stress factors, primarily those which disturb plant water balance, cause extensive crop losses. With regard to sessile lifestyle, many mechanisms how to cope with these unfavourable conditions were developed during evolution of plants. As common impact of many of these stresses like drought, salinity or low temperatures is of osmotic nature, the osmotic adjustment represents important part of plant stress response. Mostly, this component of stress reaction is provided by organic compounds, which are referred to as compatible solutes, including polyhydroxyl compounds (sucrose, sugar alcohols, cyclitols, and oligosacharides) and nitrogen-containing compounds (mainly proline). The effect of these solutes is not only osmotic, but also osmoprotective as they are able to preserve integrity of membranes and macromolecules by mimicking their water envelope. The compatible solutes also contribute to quenching of reactive oxygen species overproduced under these stress conditions. This study is focused on apple (Malus domestica) producing, beside sucrose, sugar alcohol sorbitol as primary photosynthetic product and transporting these carbohydrates along with raffinose family oligosaccharides (RFO) for a long distance. In vitro tissue cultures derived from leaves of two apple cultivars differing in...
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Synthesis of Pyridazines by Ring Transformation Reaction
Budilová, Hana ; Pour, Milan (referee) ; Klimešová, Věra (advisor)
Charles University in Prague The Faculty of Pharmacy in Hradec Králové The Department of Inorganic and Organic Chemistry Candidate: Hana Budilová Supervisors: Doc. RNDr. Věra Klimešová, CSc. Prof. Dr. Rainer Beckert Title of Diploma Thesis: Synthesis of Pyridazines by Ring Transformation Reaction Pyridazines are heterocyclic compounds with two adjacent nitrogen atoms. There are a lot of synthetic approaches to get pyridazine. A number of specific transformations from other heterocyclic systems have been reported. This thesis deals with the synthesis of pyridazines by transformation of a four-membered heterocycle. Some new derivatives of 1-methyl-3-(4-tolylamino)-4-(4-tolylimino)-6-(4'- substituted-phenyl)-1,4-dihydropyridazines were synthesized by a ring transformation of four- membered 2 -1,2-diazetine. This compound was obtained by a cycloacylation reaction of methylhydrazine and bis-oxalimidoyl chloride. NMR and mass spectrometry confirmed structures of prepared compounds. 1-Methyl-3-(4-tolylamino)-4-(4-tolylimino)-6-phenyl-1,4-dihydropyridazine had been previously proven to possess antimycobacterial activity. The new derivatives were tested against Mycobacterium tuberculosis My 331/88, M. avium My 330/88, M. kansasii My 235/80 and M. kansasii 6 509/96. MIC values of these compounds range...
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