National Repository of Grey Literature 26 records found  1 - 10nextend  jump to record: Search took 0.00 seconds. 
Study of the expression and toxicity of catechol derivates in MCF-7 cell line
Kleplová, Dominika ; Carazo Fernández, Alejandro (advisor) ; Vokřál, Ivan (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Dominika Kleplová Supervisor: PharmDr. Alejandro Carazo, PhD. Title of the Diploma thesis: Study of the expression and toxicity of catechol derivatives in MCF-7 cell line Estrogens perform many important functions in the human body. They act by binding to estrogen receptors (ER) and thus regulate reproduction, the menstrual cycle, bone density, cholesterol metabolism or brain function. They also play an important role in the development and onset of breast cancer, where the amount of ER expressed is used as a very important biomarker in patients suffering from this disease. Despite ongoing research, breast cancer is considered to have the highest mortality rate. Catechols are organic compounds. In the human body, they can occur as metabolites in the degradation of benzene and estrogens or other endogenous compounds such as neurotransmitters and their precursors. Catechols are known to be involved in redox processes in the body, to exert antioxidant and toxic effects, to interfere with protein function and to cause DNA strand breaks. Their positive effect on breast cancer therapy is the subject of research, but it has not yet been fully explored. The subject of this thesis is to study the...
Precision-cut placental slices as a model to study inflammatory response
Bolboli, Bahareh ; Štaud, František (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Bahareh Bolboli Supervisor: Prof. PharmDr. František Štaud, Ph.D. Consultant: Kasin Yadunandam Anandam, Ph.D. Title of the diploma thesis: Precision-cut placental slices as a model to study inflammatory response. Maternal inflammation during pregnancy is a recognized factor linked to an array of complications and potential neurodevelopmental and neuropsychiatric risks for offspring. Placenta isthe crucial interface between maternal and fetal domains. This organ not only shapes fetal development but also possesses the ability to respond to inflammatory stimulations, potentially in a sex-specific manner. Nonetheless, the fundamental immunoregulatory mechanisms orchestrating such responses remain unclear. To bridge this knowledge gap, our study harnessed an innovative approach: the ex vivo precision-cut placental slice model using rat placentas. This experimental design was tailored to probe acute inflammatory responses. Precision-cut placental slices, precisely 200 µm thick, were meticulously generated from both male and female rat placentas. These slices were subjected to varying concentrations of Lipopolysaccharide (LPS) or Polyinosinic: polycytidylic acid (Poly I:C) for discrete periods of 4...
Search for new natural alpha-glucosidase inhibitors
Kašpárková, Michaela ; Karlíčková, Jana (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Student: Michaela Kašpárková Supervisor: PharmDr. Jana Karlíčková, Ph.D. Title of diploma thesis: Search for new natural α-glucosidase inhibitors α-glucosidase is one of the main enzymes that break down carbohydrates in the digestive tract. Its physiological function is mainly the cleavage of α-(1,4) bonds of oligosaccharides and enabling the absorption of D-glucose into the bloodstream. As a result, there is an increase in postprandial blood glucose values, which is not desirable in patients with diabetes or in people with a high risk of developing it. Flavonoids are natural polyphenolic substances found in many natural components of our food. These substances are known for their positive effects on human health, which also include the ability to inhibit the α-glucosidase enzyme. Therefore, the aim of this work was to determine the inhibitory activity of flavonoids against the α-glucosidase enzyme and the subsequent assessment of the structure-activity relationship. Using twenty-two selected flavonoids belonging to five different structural groups, the inhibitory activity on the yeast α-glucosidase from Saccharomyces cerevisiae was determined by spectrophotometric measurements in vitro....
Chelation of copper ions by thiol containing chelators
Kladivová, Andrea ; Mladěnka, Přemysl (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Andrea Kladivová Consultant: Václav Tvrdý, MSc. Supervisor: Assoc. Prof. Přemysl Mladěnka, PharmD., Ph.D. Title of diploma thesis: Chelation of copper ions by thiol containing chelators Copper is an essential trace element that is important for many physiological functions. On the other hand, disruption of copper homeostasis associated with its elevated level is dangerous for the organism, because of the formation of free radicals. Copper chelators can represent an effective tool in the treatment of such conditions. Due to the ability of a thiol group to bind metal ions and form a chelate, thiol containing chelators are promising compounds for the reduction of copper levels. Within this diploma thesis, four compounds containing a thiol group were tested for the ability to chelate copper ions. Spectrophotometric measurement was used for this determination. It is a simple, fast but precise method for determination of the chelation properties in vitro. In addition, the ability of these compounds to reduce cupric ions was examined. When using the basic hematoxylin method, all the tested substances proved they can chelate copper. Their efficacy was practically identical except for the...
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...
Vasodilatory effects of catechol derivatives ex vivo
Šmídová, Kristýna ; Pourová, Jana (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Kristýna Šmídová Supervisor: doc. PharmDr. Jana Pourová, Ph.D. Title of diploma thesis: Vasodilatory effects of catechol derivatives ex vivo Polyphenols, including flavonoids, are a broad group of natural substances with significant effects on human health, including the prevention of cardiovascular diseases. Their metabolites can also be active, with clinical effects which may even exceed those of the parent compounds. The aim of this diploma thesis was to verify vasodilatory effects of one flavonoid metabolite type, a series of catechol derivatives and elucidate the mechanism of action of the most potent substance. The established ex vivo method of isolated aortic rings of Wistar rats with isotonic registration of tissue contraction and dilation (software S.P.E.L. Advanced Kymograph Software) was used. In the experiments with the rat aorta precontracted by norepinephrin, 3-methoxycatechol was the most effective vasodilator (EC50 = 7,6 µmol.l-1). In the mechanistic study, we found out that its effect is endothelium-independent, and that 3-methoxycatechol enhances the vasodilatory effect of sodium nitropruside. However, the specific mechanism responsible for vasodilation was not identified and...
Study of the expression and toxicity of catechol derivates in breast cancer cell lines
Vyoralová, Tereza ; Carazo Fernández, Alejandro (advisor) ; Jirkovský, Eduard (referee)
Studium exprese a toxicity derivátů katecholu v prsních nádorových buněčných liniích, Tereza Vyoralová ABSTRACT Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Tereza Vyoralová Supervisor: PharmDr. Alejandro Carazo Ph.D. Title of the diploma thesis: Study of the expression and toxicity of catechol derivates in breast cancer cell lines Estrogens have several important functions in the human organism and are also involved in the formation and development of breast cancer. These effects are mediated by binding to estrogen receptors (ER) and show complex spectrum of effects such as regulation of reproduction, menstrual cycle, brain function, bone density or mobilization of cholesterol. In addition the presence and quantification of ER in breast cancer is currently used as one of the most important predictive biomarkers in patients suffering from this disease. The occurence and activity of ER correlates with the response of breast cancer to hormonal treatment and with the patient's prognosis. Despite intensive research, breast cancer is still ranked among the cancers with the highest lethality. Catechols are organic compounds that are naturally present in food as pollutants, but also can be found in the human body, where they play an important role as...
The impact of compounds from cigarette smoke on blood coagulation in vitro
Afshari, Mohammadreza ; Carazo Fernández, Alejandro (advisor) ; Karlíčková, Jana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Mohammadreza Afshari Supervisors: Pharm Dr Alejandro Carazo Fernández, Ph.D. Thesis title: The impact of compounds from cigarette smoke on blood coagulation in vitro Hemostasis is the physiological process that stops bleeding at the site of an injury while maintaining normal blood flow elsewhere in the circulation. It is characterized by the equilibrium between proteins, enzymes, and other biological factors. Hemostasis is one of the most important biological processes in our body and any alteration in the function can affect the health of the individual severely. Nowadays the world is experiencing an epidemy of cigarette smoking and many people are socially and economically affected by the health impact of cigarette smoking. Cigarette smoking has been proven to increase the chance of the development of various cardiovascular diseases such as atherosclerosis, coronary heart disease, stroke, and peripheral arterial disease, among others. Despite the large number of studies conducted on the effect of cigarette smoke on the cardiovascular system, there are only scarce studies that directly evaluate the effect and impact of cigarette smoke on the hemostasis and their effect on specific steps....
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...
Vasodilatory effects of catechol derivatives ex vivo
Šmídová, Kristýna ; Pourová, Jana (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Kristýna Šmídová Supervisor: doc. PharmDr. Jana Pourová, Ph.D. Title of diploma thesis: Vasodilatory effects of catechol derivatives ex vivo Polyphenols, including flavonoids, are a broad group of natural substances with significant effects on human health, including the prevention of cardiovascular diseases. Their metabolites can also be active, with clinical effects which may even exceed those of the parent compounds. The aim of this diploma thesis was to verify vasodilatory effects of one flavonoid metabolite type, a series of catechol derivatives and elucidate the mechanism of action of the most potent substance. The established ex vivo method of isolated aortic rings of Wistar rats with isotonic registration of tissue contraction and dilation (software S.P.E.L. Advanced Kymograph Software) was used. In the experiments with the rat aorta precontracted by norepinephrin, 3-methoxycatechol was the most effective vasodilator (EC50 = 7,6 µmol.l-1). In the mechanistic study, we found out that its effect is endothelium-independent, and that 3-methoxycatechol enhances the vasodilatory effect of sodium nitropruside. However, the specific mechanism responsible for vasodilation was not identified and...

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