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Interaction of chalcones with transition metals I.
Faberová, Jana ; Macáková, Kateřina (advisor) ; Karlíčková, Jana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidat: Jana Faberová Supervisor: doc. Ing. Kateřina Macáková, Ph.D. Title of Thesis: Interaction of chalcones with transition metals I. Iron is a biogenic metal element with unpaired d-electrons that plays a key role in the survival of unicellular organisms, plants and mammals. The electron shell of the iron atom is able to easily bind and release electrons and thus contribute to the proper function of the organism. Iron is necessary to ensure the transport of respiratory gases, cell differentiation and the functioning of some specific enzymes. However, despite the clearly positive effect of iron on human health, inappropriately low or high level of iron in the body can cause the development many diseases. Chalcones are plant polyphenols belonging to the family of flavonoids, secondary metabolites of plants. The term chalcone generally refers to a chemical structure with an ,-unsaturated ketone system based on 1,3-diphenylprop-2-en-1-on. These substances have a wide spectrum of biological activities and in the right amount can be good for human health. The aim of this diploma thesis was to monitor the iron-chelating and iron-reducting activity of selected chalcones: isoliquiritigenin, licochalcon A,...
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Preparation of a method for detection of the extent of chelation of calcium and magnesium ions
Konečný, Lukáš ; Mladěnka, Přemysl (advisor) ; Jáč, Pavel (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Lukáš Konečný Supervisor: prof. Přemysl Mladěnka, Pharm.D., Ph.D. Title of Thesis: Preparation of a method for detection of the extent of chelation of calcium and magnesium ions Calcium and magnesium are biogenic elements belonging to the second group of the periodic table. Calcium is the fifth most abundant element in the human body. In addition to its important role in bone homeostasis, calcium is involved in other processes such as blood clotting, muscle contraction and regulation of nerve excitability Magnesium is the cofactor of many enzymatic reactions essential for a row of physiological functions. The aim of this work was to propose a novel screening method for determination of the degree of calcium and magnesium chelation. In the first step the UV-vis spectra of the selected indicator o-cresolphthalein complexone and its complexes with calcium and magnesium were measured. This was followed by verification of the linearity and the determination of the sensitivity of the method. Concurrently the stability of the indicator and its complexes with both ions was measured. In the last step, the suitability of the method was verified on a standard chelator ethylenediaminetetraacetic acid...
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Can essential amino acids be considered as copper chelators?
Holotíková, Nikola ; Karlíčková, Jana (advisor) ; Tůmová, Lenka (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Nikola Holotíková Supervisor: PharmDr. Jana Karlíčková, Ph.D. Title of Thesis: Can essential amino acids be considered as copper chelators? Copper is a trace element playing an important role in the human organism. Copper levels in the body have to be carefully controlled because disruption of copper homeostasis can cause oxidative damage which may lead to various pathologies. Chelation of copper can potentially be used as a therapeutic tool. Medical chelators should ideally mimic chelators, especially peptides and proteins which are important for regulation of copper homeostasis. Their structure is formed by amino acids linked by peptide bonds. For this reason, the study is focused on selected amino acids. Proteinogenic amino acids are classified into essential and nonessential. Essential amino acids must be obtained from the diet. The aim of this study was to compare the copper chelation and reduction activity of essential amino acids L-histidine and L-methionine, and nonessential amino acids L-cysteine, its dimer L-cystine, L-aspartic acid and L-glutamic acid. Also a L-cysteine-derived compound, N-acetylcysteine, was tested. All of them were tested using spectrophotometric methods at pHs which...
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Search of effective cobalt chelators - 8-hydroxyquinolines
Pelnářová, Karolína ; Mladěnka, Přemysl (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Karolína Pelnářová Supervisor: Prof. Přemysl Mladěnka, PharmD., Ph.D. Consultant: Václav Tvrdý, MSc.; Marcel Hrubša, MSc. Title of diploma thesis: Searching of effective cobalt chelators - 8-hydroxyquinolines Cobalt is one of the essential trace elements present in the human body. It forms a part of the organometallic complex of vitamin B12, which is essential for many physiological functions. Both overload and lack of cobalt in the body is associated with pathological conditions. Manifestations of deficiency can lead up to pernicious anemia or hypofunction of the thyroid gland. Cobalt intoxication can occur in an industrial environment, such as by cobalt metal dust during heavy metal processing, or by its release due to corrosion from orthopedic prostheses. Systemic toxicity is manifested by a number of endocrine, cardiovascular and neurological symptoms. The main aim of this diploma thesis was to find effective chelators of cobalt from the group of substances derived from 8-hydroxyquinoline. In vitro spectrophotometric measurement was used to determine the degree of chelation. The effect of chelation was also monitored ex vivo in rat erythrocytes. All tested chelators - 8-hydroxyquinoline,...
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Copper-chelating properties of isoflavonoids
Horňasová, Veronika ; Mladěnka, Přemysl (advisor) ; Spilková, Jiřina (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Veronika Horňasová Supervisor: Assoc. Prof. Přemysl Mladěnka, Ph.D. Title of diploma thesis: Copper-chelating properties of isoflavonoids Copper is an essential trace element that plays a crucial role in our organism. It is involved in many physiological processes. On the other hand, free copper may be toxic for the organism and therefore copper homeostasis must be carefully controlled. Copper chelators represent a promising component of therapeutic strategies not only in absolute but also in relative (local) excess of copper. Especially substances which are expected to have a lower risk for side effects, such as isoflavones, may be beneficial in the treatment of Wilson's disease as well as neurodegenerative diseases or cancer. Isoflavones belong to one of the subclasses of flavonoids. Their biological effects are quite large - anti-inflammatory, antioxidant, cardio- and neuroprotective and anti-tumor. In this diploma thesis chelating properties of a group of ten isoflavones were tested by two indicators - hematoxylin and bathocuproin. In order to determine the chelating properties, a spectrophotometric measurement was used. It is a precise and rapid method. From the tested compounds,...
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Interactions of alkaloids with transition metals III.
Cymbál, Martin ; Macáková, Kateřina (advisor) ; Tůmová, Lenka (referee)
Charles University Pharmaceutical Faculty in Hradec Králové Department of Pharmaceutical Botany Candidate: Bc. Martin Cymbál, DiS. Supervisor: doc. Ing. Kateřina Macáková, Ph.D. Diploma thesis 2019/2020: Interactions of alkaloids with transition metals III., pp. 86. Copper is one of the important trace elements in the body. It regulates various enzymatic pathways. This work monitors the chelating and reducing activity of isochinoline alkaloids of the family Amaryllidaceae. The alkaloids of Amaryllidaceae have a large number of effects such as analgesic, narcotic, antiarrhythmic, antihypertensive, bronchodilatory, chemotherapeutic, antiparasitic, uteretonic, locally anesthetic, mydriatic and many other significant effects. An important representative is galanthamine hydrobromide, which is therapeutically used and is an inhibitor of acetylcholinesterase. Galanthamine type alkaloids (galanthamine, galanthamine hydrobromide, chlidanthine), lycorine type (lycorine, galanthine), haemanthamine type (haemanthnamine, vittatine) and montanine type (montanine) were studied. The methodology of the work was to determine the chelating and reducing activity with the use of the hematoxylin indicator and bathocuproindisulfonic acid, at different pH or in dimethylsulfoxide. Of the alkaloids studied, galanthamine and...
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Interactions of alkaloids with transition metals II.
Šilhová, Markéta ; Macáková, Kateřina (advisor) ; Tůmová, Lenka (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Botany Consultant: Ing. Kateřina Macáková, Ph. D. Student: Markéta Šilhová Title of Thesis: Interactions of alkaloids with transition metals II. Copper is an important component of the human body. It is involved in the right functioning of organ systems and is also a part of many important body enzymes. It is necessary to maintain a balanced amount of copper in the body in order to avoid excess or deficiency, which can lead to various diseases. The aim of this diploma thesis was to determine the copper chelating and copper reducing effects of isoquinoline alkaloids berberine chloride, canadine, corydaline, sculerine, sinactine, stylopine, tetrahydropalmatine, allocryptopine, protopine, corycavamine and cryptopine. In experimental measurements the determination of chelation of copper ions with hemytoxyline and the determination of chelation and reduction of copper ions using disodium salt of bathocuproindisulfonic acid was performed. The highest reducing activity was exhibited by scoulerine, whose structure in comparison with other alkaloids contains hydroxyl groups and which has been exhibited in the past to inhibit the growth of tumour cell. The lowest reducing activity was measured for protopine alkaloids and...
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Interactions of alkaloids with transition metals III.
Cymbál, Martin ; Macáková, Kateřina (advisor) ; Tůmová, Lenka (referee)
Charles University Pharmaceutical Faculty in Hradec Králové Department of Pharmaceutical Botany Candidate: Bc. Martin Cymbál, DiS. Supervisor: doc. Ing. Kateřina Macáková, Ph.D. Diploma thesis 2019/2020: Interactions of alkaloids with transition metals III., pp. 86. Copper is one of the important trace elements in the body. It regulates various enzymatic pathways. This work monitors the chelating and reducing activity of isochinoline alkaloids of the family Amaryllidaceae. The alkaloids of Amaryllidaceae have a large number of effects such as analgesic, narcotic, antiarrhythmic, antihypertensive, bronchodilatory, chemotherapeutic, antiparasitic, uteretonic, locally anesthetic, mydriatic and many other significant effects. An important representative is galanthamine hydrobromide, which is therapeutically used and is an inhibitor of acetylcholinesterase. Galanthamine type alkaloids (galanthamine, galanthamine hydrobromide, chlidanthine), lycorine type (lycorine, galanthine), haemanthamine type (haemanthnamine, vittatine) and montanine type (montanine) were studied. The methodology of the work was to determine the chelating and reducing activity with the use of the hematoxylin indicator and bathocuproindisulfonic acid, at different pH or in dimethylsulfoxide. Of the alkaloids studied, galanthamine and...
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Interactions of alkaloids with transition metals IV.
Loskotová, Lenka ; Macáková, Kateřina (advisor) ; Karlíčková, Jana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Bc. Lenka Loskotová Supervisor: doc. Ing. Kateřina Macáková, Ph.D. Title of Thesis: Interactions of alkaloids with transition metals IV. Copper is a biogenic trace element that participates in the proper function of an organism. It is part of a number of enzymes and participates in metabolic processes in the human body. The level of copper in the organism should be regulated to avoid its excess or deficit, as pathologies could occur. Alkaloids are natural nitrogenous substances of alkaline nature. We find many biological activities in them. The aim of this thesis was to measure copper-chelating and copper- reducing activity of isoquinoline alkaloids: corypalmine, thalictricavine, 8-oxoberberine, fumarilin, norisocorydine and laurotetanine. Alkaloid activity was measured at different pH environments (4.5; 5.5; 6.8 and 7.5) and in the DMSO environment by a spectrophotometric method using hematoxyline and acid disodium salt bathocuproindisulfonic. Based on the results, structure-effect relationships were derived. In experimental measurement, it was found that none of us tested alkaloids showed chelating activity. Reduction activity has been demonstrated in all test substances. The lowest activity...
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Preparation of a novel method for screeing of cobalt chelators
Moravcová, Monika ; Mladěnka, Přemysl (advisor) ; Karlíčková, Jana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Monika Moravcová Supervisor: Assoc. Prof. Přemysl Mladěnka, Pharm.D., Ph.D. Title of thesis: Preparation of a Novel Method for Screening of Cobalt Chelators Cobalt as a structural part of the vitamin B12 is an essential microelement for living organisms including humans. However, its excess is associated with pathological conditions. Cobalt poisoning can be caused for example by exposure to cobalt metal dust during the production of hard metals or follow the corrosion of metal hip prosthesis. Patients intoxicated by cobalt can develop different manifestations including neurological impairment, hypothyroidism or cardiomyopathy. The aim of this work is to prepare a standardized, rapid, cheap but precise method for the screening of cobalt chelators. For this purpose, spectrophotometric detection using 1-nitroso-2-nafphhol-3,6-disulfonic acid disodium salt as the indicator was used. Firstly, it was found that the addition of cobalt ions led to a clear bathochromic shift of the maximum absorbance of the indicator. The relationship between the absorbance and cobalt concentration was highly linear from 470 to 560 nm at all 4 tested pH conditions (4.5, 5.5, 6.8 and 7.5). The sensitivity of the method...
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