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Natural compounds isolated from plants at the Faculty of Pharmacy in Hradec Králové as potential inhibitors of aldo-ketoreductase 1A1 (AKR1A1)
Karásková, Jitka ; Novotná, Eva (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles Universtity Pharmaceutical Faculty in Hradec Králové Department of Biochemical Sciences Candidate: Bc. Jitka Karásková Supervisor: RNDr. Eva Novotná, Ph.D. Title of diploma thesis: Natural compounds isolated from plants at the Faculty of Pharmacy in Hradec Králové as potential inhibitors of aldo-ketoreductase 1A1 (AKR1A1) Aldo-keto reductase 1A1 is an enzyme belonging to the aldo-keto reductase superfamily. It is a monomeric, cytosolic enzyme that is able to reduce carbonyl groups within a wide range of substrates. The enzyme is expressed in almost every tissue in the body, most represented in hepatocytes, renal cells and salivary glands, where it contributes to the reduction of endogenous substrates and the first phase of biotransformation of xenobiotics. AKR1A1 catalyzes NADPH-dependent reduction of aldehydes and ketones to their corresponding primary and secondary alcohols. Enzyme substrates include, for example, mevalonate; anthracycline antibiotics doxorubicin or daunorubicin; some pro-carcinogens that are activated by the reaction into carcinogens, such as: trans- dihydrodiol metabolites of polycyclic aromatic hydrocarbons. Generally, it is involved in the metabolism of lipids and carbohydrates that contain an aldehyde function. The increased expression and activity of AKR1A1 has been...
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Effect of anthelmintics on activity of selected biotranformation enzymes in plants
Hanulíková, Markéta ; Raisová Stuchlíková, Lucie (advisor) ; Jansová, Hana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Markéta Hanulíková Supervisor: RNDr. Lucie Raisová Stuchlíková, Ph.D. Consultant: RNDr. Radka Podlipná, Ph.D. Title of diploma thesis: Effect of anthelminthics on activity of selected biotransformation enzymes Anthelmintics belong between the drugs widly used in veterinary medicine. In the environment, these drugs represent a significant source of pollution with a negative impact on micro-organism and entire ecosystems. The fate of anthelmintics and their effect on plants has not yet been studied sufficiently. The aim of this work was to investigate the effect of two frequently used anthelmintics, fenbendazole (FEN) and ivermectin (IVM) on antioxidant enzymes peroxidase (POX), catalase (CAT), ascorbate peroxidase (APX), glutathione reductase (GR), glutathione-S-transferase (GST) and superoxide dismutase (SOD) in model plant Arabidospsis thaliana. In this study was used in vitro cell suspension of Arabidospsis thaliana. Enzyme activity was measured spectrophotometrically in samples taken after 8, 24 and 72 hours. At samples exposed to effect of FEN the activity of SOD enzyme increased, on the other hand the activity of GST enzyme decreased. The presence of IVM has an inhibitory effect on GR, GST...
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Biotransformation of monepantel in plant (Campanula rotundifolia, Plantago lanceolata)
Crhová, Anna ; Raisová Stuchlíková, Lucie (advisor) ; Vokřál, Ivan (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Bc. Anna Crhová Supervisor: RNDr. Lucie Stuchlíková Raisová, Ph.D. Title of diploma thesis: Biotransformation of monepantel in plants (Campanula rotundifolia, Plantago lanceolata) Anthelmintics are veterinary drugs used to eliminate disease caused by parasitic worms. Monepantel (MOP) is a representative of amino-acetonitrile derivatives. This relatively new group of drugs is effective on helminthic strains, which are resistant to classic therapy (benzimidazoles, makrocyklic lactones, imidazothiazoles). Due to high consuption of these drugs, it is important to find out their fate in the exposed organisms. Anthelmintics are in contact with the environment and they can affect terrestrial and aquatic organisms. Their various forms can be accumulate in plants. These plants can be eaten by the animal, which may lead to development of resistance in helminths. In addition, the physiology of plants and animals may be disrupt and, consequently, biodiversity loss may occur. The aim of this study was to determine the biotransformation processes occurring in ribwort plantain (Plantago lanceolata) and harebell (Campanula rotundifolia) after low concentrations of MOP. Suspensions of both plants cells...
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Metabolomic analysis of bile acids in various biological samples.
Hadravská, Pavlína ; Skálová, Lenka (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences University of Eastern Finland in Kuopio, School of Pharmacy Department of Pharmaceutical Chemistry Candidate: Pavlína Hadravská Supervisor: prof. RNDr. Lenka Skálová, Ph.D. Consultant: prof. Seppo Auriola Title of Diploma thesis: Metabolomic analysis of bile acids in various biological samples This thesis aimed to establish a suitable qualitative and quantitative analysis of selected bile acids in mouse liver, human plasma and especially in human hair. Nine selected bile acids were analyzed (cholic acid, deoxycholic acid, chenodeoxycholic acid, ursodeoxycholic acid, lithocholic acid, taurocholic acid, taurodeoxycholic acid, glycocholic acid and glycochenodeoxycholic acid). An identification and a quantification of the bile acids have been performed by UHPLC with two types of hybrid mass spectrometers (Quadrupole connected to Time of Flight and Quadrupole connected to Orbitrap). We tried to develop a method that allows a detection of both unconjugated bile acids and their glycine- and taurine-conjugates in biological samples. To develop and optimize this method, mouse liver and human plasma were used. Afterwards, the method was used to detect bile acids in human hair, because the bile acids could serve as...
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HPLC-high resolution mass spectrometry analysis of in vitro and in vivo metabolism of scoparone
Novák, Filip ; Matoušková, Petra (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences University of Eastern Finland in Kuopio, School of Pharmacy Department of Pharmaceutical Chemistry Candidate: Filip Novák Supervisor: Ing. Petra Matoušková, Ph.D. Consultant: prof. Seppo Auriola Title of Diploma thesis: HPLC-high resolution mass spectrometry analysis of in vitro and in vivo metabolism of scoparone Scoparone is an active ingredient of Artemisia scoparia, a medicinal plant used in traditional Chinese medicine. It has been studied for various pharmacological effects such as upregulation of conjugation enzymes included in excretion of bilirubin, reduction of proinflammatory cytokines, lowering of plasma lipids levels and inhibition of platelet aggregation. In this thesis, metabolism of scoparone was studied by LC-MS method using Q-ToF device. Scoparone was incubated with liver microsomes obtained from 6 different mammal species to study in vitro oxidation. In total, six metabolites were detected in the incubation samples. Scopoletin and isoscopoletin were identified as major metabolites in every species, however, the rates of scoparone oxidation as well as a ratio of formed isoscopoletin and scopoletin varied. Furthermore, in vivo metabolites in human were studied in urine samples obtained from...
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Effect of anthelmintics on activity of selected biotranformation enzymes in plants
Hanulíková, Markéta ; Raisová Stuchlíková, Lucie (advisor) ; Jansová, Hana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Markéta Hanulíková Supervisor: RNDr. Lucie Raisová Stuchlíková, Ph.D. Consultant: RNDr. Radka Podlipná, Ph.D. Title of diploma thesis: Effect of anthelminthics on activity of selected biotransformation enzymes Anthelmintics belong between the drugs widly used in veterinary medicine. In the environment, these drugs represent a significant source of pollution with a negative impact on micro-organism and entire ecosystems. The fate of anthelmintics and their effect on plants has not yet been studied sufficiently. The aim of this work was to investigate the effect of two frequently used anthelmintics, fenbendazole (FEN) and ivermectin (IVM) on antioxidant enzymes peroxidase (POX), catalase (CAT), ascorbate peroxidase (APX), glutathione reductase (GR), glutathione-S-transferase (GST) and superoxide dismutase (SOD) in model plant Arabidospsis thaliana. In this study was used in vitro cell suspension of Arabidospsis thaliana. Enzyme activity was measured spectrophotometrically in samples taken after 8, 24 and 72 hours. At samples exposed to effect of FEN the activity of SOD enzyme increased, on the other hand the activity of GST enzyme decreased. The presence of IVM has an inhibitory effect on GR, GST...
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HPLC-high resolution mass spectrometry analysis of in vitro and in vivo metabolism of scoparone
Novák, Filip ; Matoušková, Petra (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences University of Eastern Finland in Kuopio, School of Pharmacy Department of Pharmaceutical Chemistry Candidate: Filip Novák Supervisor: Ing. Petra Matoušková, Ph.D. Consultant: prof. Seppo Auriola Title of Diploma thesis: HPLC-high resolution mass spectrometry analysis of in vitro and in vivo metabolism of scoparone Scoparone is an active ingredient of Artemisia scoparia, a medicinal plant used in traditional Chinese medicine. It has been studied for various pharmacological effects such as upregulation of conjugation enzymes included in excretion of bilirubin, reduction of proinflammatory cytokines, lowering of plasma lipids levels and inhibition of platelet aggregation. In this thesis, metabolism of scoparone was studied by LC-MS method using Q-ToF device. Scoparone was incubated with liver microsomes obtained from 6 different mammal species to study in vitro oxidation. In total, six metabolites were detected in the incubation samples. Scopoletin and isoscopoletin were identified as major metabolites in every species, however, the rates of scoparone oxidation as well as a ratio of formed isoscopoletin and scopoletin varied. Furthermore, in vivo metabolites in human were studied in urine samples obtained from...
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Metabolomic analysis of bile acids in various biological samples.
Hadravská, Pavlína ; Skálová, Lenka (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences University of Eastern Finland in Kuopio, School of Pharmacy Department of Pharmaceutical Chemistry Candidate: Pavlína Hadravská Supervisor: prof. RNDr. Lenka Skálová, Ph.D. Consultant: prof. Seppo Auriola Title of Diploma thesis: Metabolomic analysis of bile acids in various biological samples This thesis aimed to establish a suitable qualitative and quantitative analysis of selected bile acids in mouse liver, human plasma and especially in human hair. Nine selected bile acids were analyzed (cholic acid, deoxycholic acid, chenodeoxycholic acid, ursodeoxycholic acid, lithocholic acid, taurocholic acid, taurodeoxycholic acid, glycocholic acid and glycochenodeoxycholic acid). An identification and a quantification of the bile acids have been performed by UHPLC with two types of hybrid mass spectrometers (Quadrupole connected to Time of Flight and Quadrupole connected to Orbitrap). We tried to develop a method that allows a detection of both unconjugated bile acids and their glycine- and taurine-conjugates in biological samples. To develop and optimize this method, mouse liver and human plasma were used. Afterwards, the method was used to detect bile acids in human hair, because the bile acids could serve as...
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