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Phenolic acids in plants
Klížová, Lucie ; Karlíčková, Jana (advisor) ; Janoušek, Jiří (referee)
CHARLES UNIVERSITY PHARMACEUTICAL FACULTY IN HRADEC KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL BOTANY Title of the Diploma thesis: FENOLIC ACIDS IN PLANTS Candidate: Lucie Klížová Supervisor: PharmDr. Jana Karlíčková, Ph.D. Diploma thesis 2020/2021, pp. 153 Phenolic acids belongs between secondary metabolites, which are part of fruits, vegetables, cereals and other plants of different families. For example, it can be plants of family Lamiaceae, Asteraceae and Ericaceae, which contain significant amounts of these substances. In plants phenolic acids play an important role and they have many human health-promoting effects including antioxidant, anti-inflammatory, antiviral, antibacterial, antifungal, anticancer activity and other. Plants containing phenolic acids are preferably also used as antidiabetics, expectorants, insecticides, hypolipidemics, cardioprotective and neurological compounds, etc. The content of these compounds in plants may be different according to monitored cultivar, the place of growth, the time of harvest and many other aspects. Presence, identification and subsequent quantification of individual phenolic acids are usually done through the HPLC and MS methods and total content of these compounds is determined through the Folin-Ciocalteu method. The diploma thesis is a literature...
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Biotransformation of ferulic acid to sensory active compounds
Opial, Tomáš ; Pernicová, Iva (referee) ; Obruča, Stanislav (advisor)
The bachelor thesis deals with the biotransformation of ferulic acid to sensory active substances. The experiment was based on monitoring the biotransformation potential of selected microorganisms by high performance liquid chromatography (HPLC) method while the cultivation was performed in two parallel runs and samples with added ferulic acid were divided into 24-hour effect and 48-hour effect of ferulic acid on bacterial cultures. Thermophilic bacteria and halophilic bacterium Halomonas neptunia have been found to be the most suitable candidates for the biotransformation of ferulic acid to sensory active substances. In both samples of Schlegelella thermodepolymerans (DSM 15344 and DSM 15264) was formed 33 mg/l and 76 mg/l of vanillic acid and 81 mg/l and 71 mg/l of 4-vinylguaiacol after 24 hours of ferulic acid effect. In a sample with T. taiwanensis was formed 61 mg/l of vanillic acid and 32 mg/l of 4-vinylguaiacol after 48 hours of ferulic acid effect, and in a sample of R. xylanophilus was formed 56 mg/l of 4-vinylguaiacol. In the sample with H. neptunia after 24 hours of ferulic acid effect was formed 296 mg/l of vanillic acid, which was up to 59% of the conversion of the added ferulic acid and in a sample with H. organivorans after 24 hours of ferulic acid effect was formed 71 mg/l of vanillic acid. However, after 48 hours of ferulic acid effect, vanillic acid degraded. In addition to screening of biotransformation potential, the sequence of bacterial enzymes, involved in biotransformation, was also compared with protein sequences in the database using the BLAST search tool. The presence of genes encoding enzymes involved in biotransformation has been demonstrated for almost all used microorganisms except H. neptunia, for which no gene has been identified. The highest number of genes present in bacteria was with the enzymes feruloyl-CoA synthetase, enoyl-CoA hydratase/isomerase, acetoacetyl-CoA thiolase and vanillin dehydrogenase.
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Efficiency of Water Treatment Processes Using Activated Carbon
Hladíková, Lucie ; Kolesíková, Lucie (referee) ; Kučera, Tomáš (advisor)
The subject of the thesis is the issue of pesticides in the environment and the possibility of their removal through activated carbon. The thesis is divided into two parts, the search part and the practical part. The research part is focused on description of activated carbon. It also deals with the distribution of pesticides and their degradation in the environment. In the practical part, a laboratory experiment was carried out to determine the effectiveness of removing pesticides and metabolites from the test water on two types of activated carbon.
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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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Enzymatic modifications of bioactive flavonoids
Rydlová, Lenka ; Tesařová, Eva (advisor) ; Wimmer, Zdeněk (referee)
Extract from milk thistle (Silybum marianum (L.) Gaertn., synonym Carduus marianus L., Asteraceae) silymarin contains among others primarily bioactive flavonolignans. They have hepatoprotective and antioxidative effects and also anticancer, chemoprotective, dermatoprotective and hypocholesterolemic activity. This thesis focuses on the preparation of metabolites of the second phase of biotransformation unexplored flavonolignans 2,3-dehydrosilybin (DHSB), silychristin (SCH), 2,3-dehydrosilychristin (DHSCH). Pure sulfated derivatives were prepared using aryl sulfotransferase from Desulfitobacterium hafniense and p-nitrophenyl sulfate (p- NPS) as a donor. Flavonolignans yield exclusively monosulfates at the position C- 20 (C-19 in the case of silychristin and 2,3-dehydrosilychristin), except for 2,3- dehydrosilybin that gives also the 7,20-disulfated derivatives. For all samples were made antioxidant tests - DPPH assay (the highest activity had 2,3-dehydrosilychristin sulfate: IC50= 7,87 µM), Folin-Ciocalteau reduction assay (the highest activity had 2,3-dehydrosilychristin: 1,58 ekvivalents of gallic acid), ABTS+ scavenging (the highest activity had silychristin: 1,50 ekvivalents of vitamin C), inhibition of microsomal lipid peroxidation (the highest activity had 2,3-dehydrosilybin: IC50 = 10,6 µM),...
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HPLC Determination of Benzimidazoles
Slezáková, Šárka ; Kubíček, Vladimír (advisor) ; Lázníčková, Alice (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of biophysics and physical chemistry Candidate: Šárka Slezáková Supervisor: Ing. Vladimír Kubíček, CSc. Title of diploma thesis: HPLC Determination of Benzimidazoles In this thesis we have investigated the possibility of establishing benzimidazole with HILIC chromatography using a chromatographic column Ascentis Express HILIC 10.0 cm x 3.0 mm; 2.7 microns. Two groups of benzimidazoles were tested. The first one was focused on albendazole and its metabolites. Experiments with these substances did not produce satisfactory results, because the mobile phase composition which enables separation of the studied analytes was not found. The second group was formed by flubendazole and its reduced and hydrolyzed form. In this case, several mobile phase compositions were tested. Finally, distribution of individual analytes in a mixture, using a mobile phase ACN:HCOOH 0.03 mol/l (90:10), was successfully achieved. Ricobendazol was chosen as an internal standard. When separation conditions were found, calibration curve for the determination of reduced flubendazole in biological samples was subsequently constructed using ricobendazol as the internal standard with the use of fluorescence detection. Keywords: HILIC, HPLC, albendazole,...
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HPLC determination of silybin diastereoisomers in plasma of laboratory animals
Kolářová, Petra ; Tesařová, Eva (advisor) ; Bednář, Petr (referee)
Silybin is the main component of silymarin, a standardized extract obtained from the seeds of milk thistle (Silybum marianum). Flavonolignan silybin has antioxidant, hepatoprotective, chemoprotective and antitumor activities. Natural silybin occurs as an approximately equimolar mixture of two diastereoisomers - silybin A and silybin B. Analytical separation of these diastereoisomers is possible but preparative separation is complicated. The biological activity of the silybin A is different from the silybin B. Silybin diastereoisomers are mainly conjugated to glucuronides and sulfates in organism. A mixture of both silybin diasteroisomers is used in the majority of reported biological, chemical and pharmacokinetic studies. For the first time, optically pure silybin A and silybin B were used for pharmacokinetic study in this thesis. The object of this work was determination of the concentration of free and total silybin in rats plasma in relation to time. Theoretical introduction describes the current state of the problem of chemistry, pharmacology and pharmacokinetics of silybin diastereoisomers. Second part is focused on the selection of appropriate analytical column, chromatographic method and suitable procedure for preparation of biological samples for the determination of the silybin...
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The effect of metabolite terbuthylazine-2-hydroxy on early life stages of marbled crayfish
PEŘINOVÁ, Eliška
Terbuthylazine belongs to the group of pesticides on triazine-based for use in agriculture as herbicides. Terbuthylazine-2-hydroxy is the main metabolite of terbuthylazine. The aim of this study was evaluate the effect of terbuthylazine-2-hydroxy on mortality, growth, occurrence the deformations and the development of early life stages, and levels of oxidative stress, assess the activity of antioxidant enzymes of marbled crayfish (Procambarus fallax f. virginalis) and also augment data for assessing the impact of this metabolite on the environment. For assess of effect of this metabolite was used embryo larval toxicity test with crayfish. The effect of terbuthylazine-2-hydroxy was evaluated in four concentrations (0.75 g.l-1, 75 g.l-1, 375 g.l-1 and 750 g.l-1) for 62 days. Terbuthylazine-2-hydroxy in concentrations 375 g.l-1 and 750 g.l-1 caused decrease of activity superoxide dismutase (SOD) and the levels lipid peroxidation (measured as TBARS) and inhibition of growth. Inhibition of growth was also observed in the group exposed to 75 g.l-1 of terbuthylazine-2-hydroxy. Additionally, there was delay in ontogenetic development of crayfish exposed to concentration 750 g.l-1. The real tested concentration of 75 g.l-1 terbuthylazine-2-hydroxy had no effect to monitored indices in the early life stages of marbled crayfish. Terbuthylazine-2-hydroxy caused oxidative damage of cellular lipids and proteins, changes in antioxidant activity, reduction of growth, delay in ontogenetic development of marbled crayfish.
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