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Interactions of essential amino acids with iron ions
Nadějová, Jana ; Karlíčková, Jana (advisor) ; Siatka, Tomáš (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Candidate: Jana Nadějová Supervisor: PharmDr. Jana Karlíčková, Ph.D. Title of Thesis: Interaction of essential amino acids with iron ions Iron is an important trace element that is needed for the proper functioning of the body. Lack of iron, as well as an excess of iron, can lead to pathological conditions, so it is necessary to control the level of iron in the blood and in case of overloading the body with iron, its chelation can be considered a possible therapeutic tool. Chelators for these therapeutic purposes should be the body's own substance. Amino acids are therefore ideal candidates for the regulation of iron homeostasis in the body, so this thesis focuses on some of them. The individual amino acids are linked by a peptide bond to form proteins. Proteinogenic amino acids are divided into essential, which must be ingested through food, and nonessential, which the body can create on its own. The aim of this study was to compare the iron-chelating and iron-reducing activity of the essential amino acids L-histidine, L-methionine, and the nonessential amino acids L- cysteine, its dimer L-cystine, L-aspartic and L-glutamic acid. The research also included a substance derived from...
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Interaction of chalcones with transition metals II.
Šulcová, Martina ; Macáková, Kateřina (advisor) ; Mladěnka, Přemysl (referee)
Charles University in Prague Faculty of Phramacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Martina Šulcová Supervisor: Assoc. Prof. Ing. Kateřina Macáková, Ph.D. Title of the diploma thesis: Interaction of chalcones with transition metals II. Copper is one of the essencial elements in human body which is involved in the functioning of many enzymes and metabolic pathways. Although it appears in trace amounts in the body, its functions are irreplaceable. However, the ion level must be kept in balance by the various mechanisms of the body. If there is an excess or deficiency of copper in the body, this condition can lead to the development of health issues. Chalcones are substances belonging to the group of flavonoids. Their polyphenolic structure does not have a closed ring C. Studies describe their anticancer, anti-inflammatory, antiviral, antidiabetic, antibacterial, antioxidant, immunosuppressive and other properties. Chosen substances in the group of dihydrochalcones (naringin dihydrochalcone, neohesperidin dihydrochalcone, phloretin, phlorizin) and chalcones (isoliquiritigenin, licochalcone A) were tested for their chelation and reduction activity of the copper ions in this diploma thesis. The activity was measured at different pH environments (7.5; 6.8; 5.5 and 4.5) and...
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The impact of synthetic chelators from the group of 4-acylpyrazole-5-ones on alcohol dehydrogenase
Sobolová, Zuzana ; Mladěnka, Přemysl (advisor) ; Jirkovský, Eduard (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Zuzana Sobolová Supervisor: Prof. Přemysl Mladěnka, Pharm.D., Ph.D. Consultant: Marcel Hrubša, MS.c. Title of diploma thesis: The impact of synthetic chelators from the group of 4-acylpyrazole-5-ones on alcohol dehydrogenase Inhibitors of alcohol dehydrogenase play a key role in the treatment of poisoning caused by methanol, ethanol, ethylene glycol, and their toxic metabolites. Such treatment can therefore be considered as life-saving. In clinical practice, a single substance, fomepizole, is used. This thesis is aimed at investigation of the effect of eleven experimental chelators from the 4- acylpyrazol-5-ones group on equine and yeast alcohol dehydrogenases, and the possible definition of structural features that would be the most suitable for interaction with this enzyme. Due to the ability of these substances to chelate zinc ions, it is believed that they could inhibit an enzyme that has a zinc molecule in the structure. The measurement itself is based on principle of increase in absorbance during the enzymatic reaction, which is caused by the formation of NADH. This measurement is relatively simple, efficient and, due to used kinetic method, also less susceptible to be affected by...
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Searching for natural cobalt chelators
Kadlecová, Kateřina ; Karlíčková, Jana (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Student: Kateřina Kadlecová Supervisor: PharmDr. Jana Karlíčková, Ph.D. Title of diploma: Searching for natural cobalt chelators Cobalt, as a trace element, is mostly found in the human body as the central atom of vitamin B12. Its deficiency is manifested by psychological impairment, memory loss, dementia or megaloblastic anemia. In excess amount, it is toxic to the body, which has been most described in patients with MoM hip replacement surgery. Cobalt causes damage to surrounding tissue until it is destroyed, or also cardiotoxicity, thyroid hypofunction, memory and hearing loss. Flavonoids are natural polyphenolic compounds with the ability to bind metals, scavenge free radicals and hence protect against oxidative stress. The aim of the work was to determine the cobalt chelating activity of a row of flavonoids using spectrofotometric measurements in vitro at 4 pathophysiologically relevant pH conditions (pH 4.5, 5.5, 6.8 and 7.5). Of the test substances, only 3-hydroxyflavon and baicalein showed chelation activity. 3-hydroxyflavon in a 1:1 ratio achieved 100 % chelation at pH 7.5 and about 60 % at pH 6.8. Baicalein was reactive at pH 7.5 and 6.8, when at 10:1 it was able to bind about 50...
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Search for an efficient cobalt chelator
Nosková, Karolína ; Mladěnka, Přemysl (advisor) ; Smutný, Tomáš (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Karolína Nosková Supervisor: prof. Přemysl Mladěnka, PharmD., Ph.D. Consultant: Monika Moravcová, MSc. Title of diploma thesis: Search for an efficient cobalt chelator Cobalt, as part of vitamin B12, is an essential trace element for human organism. However, long-term exposure to high doses leads to toxicity. Chronic cobalt intoxication is currently most commonly observed after the implantation of cobalt-containing prostheses, which in some cases do not work properly and cobalt is released from them by mechanical friction or corrosion. That not only leads to a local reaction, but cobalt ions also enter the blood and lymphatic circulation and thus cause a systemic reaction. The intoxication is then manifested by neurological, cardiovascular and endocrine symptoms, which can lead to irreversible changes or even to the death. However, a chelator that would be able to effectively and selectively bind cobalt and thus effectively treat intoxication is not available in clinical practice. The aim of this thesis was a search for an efficient cobalt chelator among known metal chelators. Chelation was measured in vitro by a method based on spectrophotometric detection of unchelated cobalt ions at...
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Searching for natural cobalt chelators
Kadlecová, Kateřina ; Karlíčková, Jana (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Student: Kateřina Kadlecová Supervisor: PharmDr. Jana Karlíčková, Ph.D. Title of diploma: Searching for natural cobalt chelators Cobalt, as a trace element, is mostly found in the human body as the central atom of vitamin B12. Its deficiency is manifested by psychological impairment, memory loss, dementia or megaloblastic anemia. In excess amount, it is toxic to the body, which has been most described in patients with MoM hip replacement surgery. Cobalt causes damage to surrounding tissue until it is destroyed, or also cardiotoxicity, thyroid hypofunction, memory and hearing loss. Flavonoids are natural polyphenolic compounds with the ability to bind metals, scavenge free radicals and hence protect against oxidative stress. The aim of the work was to determine the cobalt chelating activity of a row of flavonoids using spectrofotometric measurements in vitro at 4 pathophysiologically relevant pH conditions (pH 4.5, 5.5, 6.8 and 7.5). Of the test substances, only 3-hydroxyflavon and baicalein showed chelation activity. 3-hydroxyflavon in a 1:1 ratio achieved 100 % chelation at pH 7.5 and about 60 % at pH 6.8. Baicalein was reactive at pH 7.5 and 6.8, when at 10:1 it was able to bind about 50...
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Interactions of essential amino acids with iron ions
Nadějová, Jana ; Karlíčková, Jana (advisor) ; Siatka, Tomáš (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Candidate: Jana Nadějová Supervisor: PharmDr. Jana Karlíčková, Ph.D. Title of Thesis: Interaction of essential amino acids with iron ions Iron is an important trace element that is needed for the proper functioning of the body. Lack of iron, as well as an excess of iron, can lead to pathological conditions, so it is necessary to control the level of iron in the blood and in case of overloading the body with iron, its chelation can be considered a possible therapeutic tool. Chelators for these therapeutic purposes should be the body's own substance. Amino acids are therefore ideal candidates for the regulation of iron homeostasis in the body, so this thesis focuses on some of them. The individual amino acids are linked by a peptide bond to form proteins. Proteinogenic amino acids are divided into essential, which must be ingested through food, and nonessential, which the body can create on its own. The aim of this study was to compare the iron-chelating and iron-reducing activity of the essential amino acids L-histidine, L-methionine, and the nonessential amino acids L- cysteine, its dimer L-cystine, L-aspartic and L-glutamic acid. The research also included a substance derived from...
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Search for an efficient cobalt chelator
Nosková, Karolína ; Mladěnka, Přemysl (advisor) ; Smutný, Tomáš (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Karolína Nosková Supervisor: prof. Přemysl Mladěnka, PharmD., Ph.D. Consultant: Monika Moravcová, MSc. Title of diploma thesis: Search for an efficient cobalt chelator Cobalt, as part of vitamin B12, is an essential trace element for human organism. However, long-term exposure to high doses leads to toxicity. Chronic cobalt intoxication is currently most commonly observed after the implantation of cobalt-containing prostheses, which in some cases do not work properly and cobalt is released from them by mechanical friction or corrosion. That not only leads to a local reaction, but cobalt ions also enter the blood and lymphatic circulation and thus cause a systemic reaction. The intoxication is then manifested by neurological, cardiovascular and endocrine symptoms, which can lead to irreversible changes or even to the death. However, a chelator that would be able to effectively and selectively bind cobalt and thus effectively treat intoxication is not available in clinical practice. The aim of this thesis was a search for an efficient cobalt chelator among known metal chelators. Chelation was measured in vitro by a method based on spectrophotometric detection of unchelated cobalt ions at...
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Iron-chelating properties of fruit extracts of various elderberries
Gorová, Barbora ; Mladěnka, Přemysl (advisor) ; Kašparová, Marie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Barbora Gorová Supervisor: Assoc Prof. Přemysl Mladěnka, Pharm.D., Ph.D. Title of thesis: Iron-chelating properties of fruit extracts of various elderberries Inorganic iron is the major food source of iron in humans. It plays role in many biochemical reactions. Thus, iron metabolism disorders can lead to different diseases associated with lack of iron or iron overload. One of the possible treatment modalities of the latter represents the administration of iron chelators. Elderberry, Sambucus nigra L. (Adoxaceae), has been used in traditional medicine. The fruits of elderberry are a rich source of cyanidin-based anthocyanins as the main component. There are important differences, both in chemical and physical properties between several cultivars of elderberry. Anthocyanins might interact with metals in the gastrointestinal tract by formation of chelates. However, data on metal interactions with anthocyanins are sparse. The main aim of this study was to perform the analysis of interaction of iron with elderberry fruit extracts as a rich and cheap source of anthocyanins with cyanidin as the aglycon. In this in vitro study ten elderberry fruit exctracts were tested for iron chelating activities...
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Iron-chelating acitivity of selected alkaloids III.
Dočekalová, Linda ; Macáková, Kateřina (advisor) ; Siatka, Tomáš (referee)
Dočekalová L., Iron-chelating activity of selected alkaloids III, Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical botanic and ecology, Hradec Králové, 2016, 60 pp. Iron is important trace element necessary for human organism. When excess it develops free radicals and structures of organism are harmed. It can lead to organ failure. Excess is solved with chelators, the most used is deferoxamine. But his terapeutic regimen is disadvantageous and it has a lot of side effects. That's reason for searching for substances with better features. This paper focuses on studium of iron-chelating activity of selected alkaloids from family Amaryllidaceae. Concretely, it's galanthamine, undulatine, buphanisine, caranine, 1-O- acetylbulbisine, homolycorine, tazettine, galanthamine, chlidanthine, ambelline, haemanthamine, haemanthidine, hamayne, 9-O-demethylgalanthine and lycoramine. As standard for comparison of activity was used deferoxamine. Activity was measured by spectrophotometer. As indicator was used ferrozine. Chelatation was measured for ferrous ionts and for total iron, where hydroxylamine as reduction agent was used. Ferrous ionts was measured also with pH alteration. Highest activity reached deferoxamine in all executed measurements. In...
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