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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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Determination of the stoichiometry of the copper complexes with dehydrosilybine A
Klimková, Kateřina ; Mladěnka, Přemysl (advisor) ; Hrdina, Radomír (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Kateřina Klimková Supervisor: Assoc. Prof. Přemysl Mladěnka, Pharm. D., Ph.D. Consultant: Assoc. Prof. Kateřina Valentová, Ph.D. Title of Thesis: Determination of the stoichiometry of the copper complexes with dehydrosilybin A Silymarin, the standardized extract of the milk thistle (Silybum marianum), is a widely used approved over-the-counter drug that is recommended for a number of liver diseases. Silymarin contains as one of its components 2,3-dehydrosilybinA, which has an appropriate metal binding site in its structure. In general, flavonolignans, due to their structure, can interact with transition metals in the gastrointestinal tract by forming complexes. This property can be useful for the protection against excessive amounts of metals in the body. The aim of this in vitro study was to analyse the interaction of 2,3-dehydrosilybin A with copper, which plays a crucial role in the organism as a cofactor of many enzymes. Although being an essential element, it can, however, be toxic at elevated levels. Stoichiometry, as one of the most important characteristics of the complex, was determined by UV-Vis spectrophotometry in four (patho)physiological pH conditions (4.5; 5.5; 6.8; 7.5)...
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Iron-chelating effects of flavonoid metabolites - small polyphenolic substances
Vavřichová, Nikol ; Macáková, Kateřina (advisor) ; Karlíčková, Jana (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical botanic and ekology Candidate: Nikol Vavřichová Supervisor: Ing. Kateřina Macáková Ph.D. Title of diploma thesis: Iron - chelating effects of flavonoid metabolites - small polyphenolic substances (2015/2016) Iron is a trace element which is necessary for function of an organism. There is no specific excretion mechanism for iron, therefore any deflection causes deficiency or abundance. Iron abundance leads to hemochromatosis. An application of iron chelators is a treatment of choice for hemochromatosis. There are three clinically used chelators for treatment of iron overload: deferoxamine, deferasirox and deferiprone. These drugs are inappropriate for therapy (side effects, dosage form). Therefore there is a place for serching for new types of medicine for treatment of hemochromatosis. Flavonoids are natural substances with positive influence on a human organism. The most investigated effects are antioxidant and chelating activity. As flavonoids are metabolised in a human body, there is an arising question if flavonoid metabolites are also able to chelate iron ions. For this work we chose derivates of benzoic acid: benzoic acid, 3 - hydroxybenzoic acid, 4 - hydroxybenzoic acid, 2,4 - dihydroxybenzoic...
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Determination of the stoichiometry of the copper complexes with dehydrosilybine A
Klimková, Kateřina ; Mladěnka, Přemysl (advisor) ; Hrdina, Radomír (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Kateřina Klimková Supervisor: Assoc. Prof. Přemysl Mladěnka, Pharm. D., Ph.D. Consultant: Assoc. Prof. Kateřina Valentová, Ph.D. Title of Thesis: Determination of the stoichiometry of the copper complexes with dehydrosilybin A Silymarin, the standardized extract of the milk thistle (Silybum marianum), is a widely used approved over-the-counter drug that is recommended for a number of liver diseases. Silymarin contains as one of its components 2,3-dehydrosilybinA, which has an appropriate metal binding site in its structure. In general, flavonolignans, due to their structure, can interact with transition metals in the gastrointestinal tract by forming complexes. This property can be useful for the protection against excessive amounts of metals in the body. The aim of this in vitro study was to analyse the interaction of 2,3-dehydrosilybin A with copper, which plays a crucial role in the organism as a cofactor of many enzymes. Although being an essential element, it can, however, be toxic at elevated levels. Stoichiometry, as one of the most important characteristics of the complex, was determined by UV-Vis spectrophotometry in four (patho)physiological pH conditions (4.5; 5.5; 6.8; 7.5)...
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Interaction of phenylpropionic acids with copper
Zemanová, Kamila ; Karlíčková, Jana (advisor) ; Matysová, Ludmila (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Kamila Zemanová Supervisor: PharmDr. Jana Karlíčková, Ph.D. Title of Thesis: Interaction of phenylpropionic acids with copper Copper is an essential trace element which is essential for our body. It has a significant effect on the correct functioning of important organs and it plays an important role in the transfer of electrons at the major enzymatic pathways as a prostetic group. On the other hand, excess or deficiency of copper in the human body can cause many diseases. Phenylpropionic acids are group of substances which can have antioxidant, anti-inflammatory and anticancer effects. They are involved in the scavenging of free radicals and reactive oxygen species. In this diploma thesis, I tested copper chelating activity of six phenylpropionic acids at different pHs by spectrofotometric methods using a hematoxylin and a bathocuproinedisulfonic acid disodium salt as an indicator. 3-(3,4-dihydroxyphenyl)propionic acid showed the highest chelating potential but only using a hematoxylin. KEYWORDS: Copper, Phenylpropionic acids, Antioxidants, Chelating activity, Hematoxylin, Bathocuproin
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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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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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Interactions of alkaloids with transition metals I.
Rzepecká, Radka ; Macáková, Kateřina (advisor) ; Karlíčková, Jana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Radka Rzepecká Supervisor: Ing. Kateřina Macáková, Ph.D. Title of Thesis: Interactions of alkaloids with transition metals I. Copper is one of the essential trace elements that are necessary for the proper functioning of the organism. Copper is a significant component of many enzymes that affect various metabolic processes in the human body. It is important that the level of copper in the body is regulated because its deficit or excess lead to a variety of pathological conditions. Alkaloids are secondary plant metabolites that are distinguished by numerous biological activities. In this thesis the copper-chelating and copper-reducing activity of eleven isoquinoline alkaloids was measured: boldine, isocorydine, (+)-bulbocapnine, (+)-corydine, glaucine, (-)-sinoacutine, (-)-californidine, (-)-escholtzine, platycerine, (-)-fumaricine, and (+)- parfumine. Alkaloid activity was measured at four (patho) physiological pH values by a verified spectrophotometric method using two indicators: bathocuproinedisulfonic acid disodium salt and hematoxylin. Based on the results, structure-effect relationships were derived. The results show that none of the tested substances was able to chelate copper ions. In...
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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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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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