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The pharmacokinetics of isoflavonoides
Ungerová, Lucie ; Pourová, Jana (advisor) ; Mladěnka, Přemysl (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Lucie Ungerová Supervisor: PharmDr. Jana Pourová, Ph.D. Title of diploma thesis: The pharmakokinetics of isoflavonoids The aim of this diploma thesis is to summarize currently available informations about the pharmacokinetics of the polyfenolic compounds from a large group of flavonoids, isoflavonoids. Isoflavonoids are coumpounds found in many plant families, but especially in some members of Fabaceae family. One of the main well-known sources are soy beans containing the most famous isoflavones - genistein and daidzein, their pharmakokinetics is the main theme of this diploma thesis. Since isoflavonoids are mainly contained in the diet, their oral administration is very relevant. Isoflanonoids in the human diet occurs predominantly in the form of glykosides and therefore, after ingestion, they have to be deglycosylated by β- glucosidase enzyme family to aglycones. After that they are able to pass through the intestine into the systemic circulation and they are available for action. This is already happening in the oral cavity and the absorption occurs in the small intestine. The intestinal bacterial microflora composition is also very important for pharmacokinetics, for example I can mention...
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Evaluation of the efficacy of new acetylcholinesterase inhibitors by Ellman's method
Mackurová, Michaela ; Čečková, Martina (advisor) ; Pourová, Jana (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Performed at: University of defence in Brno, Faculty of Military Health Sciences in Hradec Králové, Department of Toxicology and Military Pharmacology Candidate: Michaela Mackurová Leader of diploma thesis: Doc. PharmDr. Martina Čečková, Ph.D. Supervisor: mjr. PharmDr. Vendula Hepnarová, Ph.D. Title of diploma thesis: Measurement of the efficacy of new acetylcholinesterase inhibitors using the Ellman method Cholinesterases (ChEs) belong to an important group of enzymes in our body. The best known acetylcholinesterase and butyrylcholinesterase play an important role in the treatment of many diseases, including Alzheimer's disease (AD). It is a neurodegenerative disease that occurs mainly in the elderly. It is one of the most common forms of dementia and its incidence is still increasing. To date, no effective therapy for AD has been developed, only symptomatic treatment is available. It is therefore necessary to look for therapeutics that would be able to stop or cure this serious disease. The aim of this work was to determine the inhibitory contraction of newly synthesized potential drugs AD against both ChEs. A total of 27 tacrine derivatives were tested, which were enriched with substituents...
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The in vitro effects of selected substances on isolated rat aorta
Beránková, Anna ; Pourová, Jana (advisor) ; Vopršalová, Marie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Anna Beránková Supervisor: PharmDr. Jana Pourová, Ph.D. Title of diploma thesis: The in vitro effects of selected substances on isolated rat aorta Flavonoids are a numerous group of secondary plant metabolites. Flavonoid compounds are substances widely extended in nature and many of them have a positive influence on human health, primarily for their vasodilatory, antioxidant and anti- inflammatory effects. Three substances were selected for this diploma theses: two substances of isoflavonoid group, genistin and genistein, and the end product of genistein metabolism, 4-ethylphenol. The aim of this work is examination of vasorelaxant effects of this substances in vitro. Vasorelaxing potential of tested substances was tested in vitro in isolated aortic rings of Wistar rat. The effect of increasing doses of individual substances in precontracted aortic rings with intact endothelium was measured. From the obtained values of vessel tension, the DRC curves and EC50 values were created. The results were evaluated. The results analysis shows, that genistein (EC50 2,903.10-5 M) had the most significant activity. Also genistin (EC50 4,045.10-4 M) and high doses of 4-ethylphenol (EC50 1,509.10-3 M) caused...
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Vasodilatory effects of bisphenol AF ex vivo
Kuchařová, Nela ; Pourová, Jana (advisor) ; Vopršalová, Marie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Nela Kuchařová Supervisor: PharmDr. Jana Pourová, Ph.D. Title of diploma thesis: Vasodilatory effects of bisphenol AF ex vivo Bisphenols are organic compounds used in the manufacture of plastics, resins, varnishes and lot of other products. However, their effects on human body are associated with a number of adverse effect that need to be investigated in more detail. The aim of this diploma thesis was to determine whether bisphenol AF has vasodilating effects ex vivo and to verify the mechanism of the relaxing effect. The experiments were performed on an isolated thoracic aorta of a Wistar rat. Bisphenol AF was added cumulatively to the precontracted aorta at increasing concentrations and we monitored whether vasodilation was induced. In testing the mechanism of action, we used inhibitors of the mechanisms tested during the experiment. The obtained results were evaluated using the GraphPad Prism program. The results show that bisphenol AF has a dose-dependent ex vivo vasodilatory effect (EC50 = 57.16 μmol/l). The mechanism of this effect is the blockage of voltagegated calcium channels on the vascular smooth muscle cell. The participation of other tested mechanisms has not been confirmed. Key...
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Food interactions of antibiotics
Nováková, Veronika ; Pourová, Jana (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Veronika Nováková Supervisor: PharmDr. Jana Pourová, Ph.D. Title of diploma thesis: Food interactions of antibiotics Diploma thesis deals with clinically significant interactions between antibiotics and food. It defines basic concepts such as antibiotics, food, drug interactions and also drug-food interactions. The main part of the work deals with the characteristics of individual groups of antibiotics, describes their mechanism of action, including the antimicrobial spectrum, the main side effects and deals with the already mentioned interactions with food and beverages. St. John's wort, grapefruit, alcohol, or polyvalent ions in particular play an important role in these interactions, which can have a significant effect on the course of antibiotic therapy. The next part of this work deals with the effect of probiotics on the natural intestinal microflora, which is disrupted by antibiotics. The last part of the thesis deals with the issue of antibiotic resistance and the principles of correct and appropriate use of antibiotics, which have an impact not only on minimizing the emergence and development of bacterial resistance, but also help to prevent interactions, including drug-food...
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Study of vasodilatory effects of selected silymarin flavonolignans ex vivo on isolated rats aorta
Šimánková, Lenka ; Pourová, Jana (advisor) ; Vopršalová, Marie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Mgr. Lenka Šimánková Supervisor: PharmDr. Jana Pourová, Ph.D. Title of rigorous thesis: Study of vasodilatory effect of selected silymarin's flavonolignans ex vivo on isolated rat's aorta. Flavonolignans are a group of compounds which include the complex substance of silymarin, which is found and obtained from a plant named Milk Thistle (Silybum marianum). Several studies show its antioxidant and anti-inflammatory effects. Its main effect for which it is used in medicine is hepatoprotective activity. The aim of this work is to find out whether selected flavonolignans of silymarin complex vasoor their sulfated metabolites may have vasorelaxant effects. Five selected substances (2,3 dehydrosilybin, silychristin and their sulfated conjugates 2,3-dehydrosilybin-20-O-sulphate, 2,3-dehydrosilybin- 7,20-O-disulphate a silychristin-19-O- sulphate) were tested ex vivo on the Wistar rat aorta. Both tested flavonolignans had vasorelaxant effects comparable to those of the respective monosulfates. In contrast, 2,3- dehydrosilybin disulfate was completely ineffective.
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The ex vivo study of mechanism of vasodilatation effect of 3,4,-dihydroxyphenylacetic acid and 4-methylcatechol
Hodinová, Veronika ; Pourová, Jana (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Mgr. Veronika Hodinová Supervisor: PharmDr. Jana Pourová, Ph.D. Title of rigorous thesis: The ex vivo study of mechanism of vasodilatation effect of 3,4-dihydroxyphenylacetic acid and 4-methylcatechol The aim of this thesis was to prove some mechanisms of vasorelaxation effects caused by two colonic metabolites of flavonoids, 3,4-dihydroxyphenylacetic acid and 4-methylcatechol, by the ex vivo method of isolated rat's aorta. We confirmed the vasorelaxation effects in both of the metabolites. We found out the mechanisms of vasorelaxation effect by experiments with the inhibitor of cyclooxygenase and also by experiments with inhibitors of calcium-activated potassium channels. We found out that the cyclooxygenase as well as some subtypes of calcium-activated potassium channels have both participated in the vasodilatation effect of 3,4-dihydroxyphenylacetic acid. We were not able to confirm the mechanism of vasodilatation effect of 4-methylcatechol, the results were ambiguous. The participation of the inhibition of cyclooxygenase is unlikely.
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Mechanism of the vasorelaxant effect of biochanin A studied ex vivovon isolated rat aorta
Katiová, Diana ; Pourová, Jana (advisor) ; Trejtnar, František (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxikology Consultant: PharmDr. Jana Pourová, Ph.D. Consultant specialist: Mgr. Thomas Migkos Student: Diana Katiová Title of Thesis: Mechanism of the vasorelaxant effect of biochanin A studied ex vivo on isolated rat aorta Flavonoids are secondary plant metabolities which are known for thein wide range of effects. Many of them have beneficial effects on the human organism. Thay have anti-inflammatory properties, antioxidant activity and positive effect on cardiovascular system. The main aim of this thesis was to determine possible vasorelaxant mechanisms of action of selected isoflavonoid biochanin A. The vasorelaxation potential was verified in ex vivo conditions on isolated rat aortic rings. The results has confirmed dose-dependent induced vasodilatation. Our experiments confirm that the vasodilatatory effect of biochanin A is independent on the function of endotel. Beside that the experimental part of this thesis is dealing with the effect of this substance on Ca2+ channels of L-type in the plasma membrane and whether vasorelaxant effect is dependent on extracelullar Ca2+ . Our results confirm that similarly as nifedipine biochanin A blocks these channels as well. Moreover biochanin A in the medium without...
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The ex vivo effects of selected silymarin flavonolygnans on isolated rat aorta
Sloukgi, Tatiana ; Pourová, Jana (advisor) ; Mladěnka, Přemysl (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Tatiana Sloukgi Supervisor: PharmDr. Jana Pourová, Ph.D. Title of Diploma Thesis: The effect of Silymarin Flavonolignans and their sulfated conjugates on blood vessels ex vivo. Silymarin flavonolignans have recently shown some positive effects on the cardiovascular system. In this work, we studied the vasodilatory effect on rat aorta ex vivo of three silymarin conjugates, silybin A-20-sulfate, silybin B-20-sulfate and 2,3- dehydrosilychristin-19-O-sulfate, and one parent flavonolignan 2,3- dehydrosilychristin. For each substance, a concentration response curve was created and the concentration that produces 50% of maximum relaxation was determined (EC50). All substances exerted very low or no vasodilatory activity. Finally, we focused on the mechanism of action of silybin A. We tested whether its vasorelaxant activity depends on the presence of intact endothelium. The vasorelaxant effect of silybin A on isolated rat aorta ex vivo was clearly endothelium-dependent.
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Cardiovascular effects of silymarin
Ryzová, Leona ; Pourová, Jana (advisor) ; Vopršalová, Marie (referee)
1 ABSTRACT Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Leona Ryzová Supervisor: PharmDr. Jana Pourová, Ph.D. Title of diploma thesis: Cardiovascular effects of silymarin Aim: The aim of the diploma thesis is to summarize the existing knowledge about the mixture of natural plant substances collectively referred to as silymarin and to map the results of the latest studies focusing on the cardiovascular effects of silymarin. Main findings: Available data suggest that silymarin has positive effects on the human body, including hepatoprotective, choleretic and cholagogic, neuroprotective, anticancer and antiviral, anti-inflammatory and positive effects on diabetes mellitus. Positive effects on the cardiovascular system include protective effects on the vascular endothelium, antioxidant effects, beneficial effects on blood lipids, regulation of blood aggregation and antidiabetic effects. Although the conclusions from cardiovascular studies are not always the same, most confirm the positive effect of silymarin on the cardiovascular system. A necessary part of future research will be the search for new dosage forms in order to increase the bioavailability of silymarin, which so far limits its clinical application. Conclusion: Silymarin is a mixture of...
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