National Repository of Grey Literature 115 records found  1 - 10nextend  jump to record: Search took 0.00 seconds. 
Potential toxicity of terpenes and their effects in liver cells
Zárybnický, Tomáš ; Boušová, Iva (advisor) ; Anzenbacherová, Eva (referee) ; Trejtnar, František (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Mgr. Tomáš Zárybnický Supervisor: assoc. prof. PharmDr. Iva Boušová, Ph.D. Consultant: assoc. prof. Ing. Petra Matoušková, Ph.D. Title of Doctoral Thesis: Potential toxicity of terpenes and their effects in liver cells The public interest in herbal products, supplements, extracts or isolated active compounds has been increasing during last decades. The aim of this doctoral thesis was to study selected compounds from the group of monoterpenes and sesquiterpenes and their interactions with liver cells: interactions with drug metabolising enzymes, their potential liver toxicity and looking for novel mechanisms of action. The literature about hepatotoxic properties of several monoterpenes and sesquiterpenes, that showed liver toxicity, was summarized first. Then, the study was aimed toward a known hepatotoxicant (R)-pulegone and its presumed metabolite (R)- menthofuran. The toxicity results in precision-cut human liver slices have shown that (R)- menthofuran was less toxic to human liver and that the reason may be inter-species differences between human and mice. Several sesquiterpenes (farnesol, cis-nerolidol, trans-nerolidol, α-humulene, β-caryophyllene, and caryophyllene oxide) have previously...
Recent knowledge on drug effect on male fertility
Klapková, Tereza ; Trejtnar, František (advisor) ; Hyršová, Lucie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Tereza Klapková Supervisor: Assoc. Prof. PharmDr. František Trejtnar, CSc. Title of diploma thesis: Recent knowledge on drug effect on male fertility Among the various types of side effects presented in clinically used drugs, negative effects on male reproductive functions can be find. This issue seems to be important and current especially due to the general trend of the decrease in fertility in men and the increasing drug use in younger age groups. The aim of this diploma thesis was to create an overview summarizing current expert knowledge on the effect of drugs on male fertility. For this purpose, we selected relevant publications in the PubMed database, perform their analysis and create the text ofthe thesis. The review focuses mainly on groups of drugs that are often clinically used and discussed in relation to male fertility, such as drugs acting on the cardiovascular system, antimicrobial drugs, drugs used in pain therapy, antidepressants, antiepileptics, antipsychotics, immunosuppressants and some other drugs. In addition to standard drugs, the review also includes several important natural substances, which are used as adjunctive therapy of various diseases or are important from a...
Study of transport mediated by drug transporters in model cell systems
Znamínková, Jana ; Hyršová, Lucie (advisor) ; Trejtnar, František (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Jana Znamínková Supervisor: PharmDr. Lucie Hyršová, PhD. Title of diploma thesis: Study of transport mediated by drug transporters in model cell systems Liver is the main biotransformation organ of human organism. Not every substance can cross the cell membrane of hepatocytes by simple diffusion. Transport of such substances across the membrane is mediated by specialized transport proteins. Uptake transporters localized on the basolateral membrane of hepatocytes play a crucial role in uptake of compounds from blood into hepatocytes, where the biotransformation takes place. OCT1 transporter belongs between important members of this group, it transports organic cations. Efflux transporters localized on the apical membrane are responsible for transport of substances from hepatocytes to bile canalicular and these transporters mediate their elimination in this way. BCRP is an example of this group of transporters. Drug transporters represent one of the most important mechanisms of drug-drug interactions due to their wide range of substrates. The aim of this study was to evaluate the function of novel cell models using substrate and inhibitors of these transporters. Stably transfected MDCK II cells...
Changes in expression of biotransformation enzymes in nematodes affected by albendazole
Štěrbová, Karolína ; Skálová, Lenka (advisor) ; Trejtnar, František (referee)
5 ABSTRACT Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Bc. Karolína Štěrbová Supervisor: prof. RNDr. Lenka Skálová Ph.D. Title of diploma thesis: Changes in expression of biotransformation enzymes in nematodes affected by albendazole Barber's pole worm (Haemonchus contortus) is highly pathogenic parasitic nematode, which assaults gastrointestinal system of small ruminants. Disease. Which caused is named by the agent haemonchoses. Long-term infection leads to develop of anaemia, lose weight of host and often even death. For treatment of this disease, synthetic antiparasitic drugs called anthelmintics are used. However, worldwide problem is growth of resistance against all used anthelmintics. Cause of this problem is probably common and unreasonable using of anthelmintics and the exposure of the parasites to sub-lethal doses. This thesis is focused on study of the mechanisms of resistance of barber's pole worm to albendazole, anthelmintic belonging to benzimidazoles group. The increased expression of biotransformation enzymes could contribute to resistance development. In our study, the influence of albendazole on expression of selected genes in adults of H. contortus from the ISE (Inbread Susceptible Edinburgh) strain was studied. Worms...
Analysis of drug problems at hospital department from the pharmacist's point of view
Dvořáčková, Eliška ; Vlček, Jiří (advisor) ; Trejtnar, František (referee) ; Urbánek, Karel (referee)
práce v anglickém jazyce Title: Analysis of drug problems at hospital department from the pharmacist's point of view Introduction: Chronic kidney disease is a medical and economic problem. It affects 10-13 % of the population in European countries and incidence is increasing with every decade of life. The most common cause of kidney failure in patients over 50 years of age is associated with 2. type diabetes and hypertension. Chronic kidney disease is associated with risk of mortality, hospitalization and decreased quality of life. Clinical pharmacist as a specialist in a field of pharmacotherapy collaborates with other health professionals to optimize pharmacotherapy. Proactive approach with active prevention of drug related problems (DRPs) is preferre. Identification and minimization of drug problems together with optimization of pharmacotherapy are the main objectives of clinical pharmacy. Where the prerequisite for the detection and resolution of drug problems is not only knowledge of pharmacology but also other medical disciplines such as biochemistry, microbiology, pathophysiology and epidemiology. This work is one of the first publications of this type in the Czech Republic, which reveals a review of pharmacotherapy in patients with chronic kidney disease and the integration of a pharmacist...
The study of properties of radiolabelled monoclonal antibodies for imaging in oncology
Janoušek, Jiří ; Trejtnar, František (advisor) ; Kozempel, Ján (referee) ; Lázníčková, Alice (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Jiří Janoušek, MSc. Supervisor: Assoc. Prof. PharmDr. František Trejtnar, CSc. Consultant: Mgr. Pavel Bárta, Ph.D. Title of doctoral thesis: The study of properties of radiolabelled monoclonal antibodies for imaging in oncology Monoclonal antibodies belong to the group of targeted biological drugs that are currently successfully applied in various medical specialties, including oncology. The ability to specifically bind to antigens present in a tumour tissue is their significant attribute that can be used for imaging tumours in Nuclear Medicine. Receptors for vascular endothelial growth factor (VEGFR) and epidermal growth factor (EGFR) are possible tumour specific targets that are characteristic for some types of proliferating tumour tissue. The attachment of appropriate radionuclide is necessary for the potential radiodiagnostic use of monoclonal antibody. This task requires chemical modification of the antibody molecule that can damage its immunoreactivity and the binding to the target receptor. The aim of the doctoral thesis was to study the influence of labelling conditions with selected diagnostic radionuclides on radiochemical characteristics, in vitro receptor specific binding and...
In vitro evaluation of novel Toll-like receptor ligands I.
Hudáková, Kristína ; Trejtnar, František (advisor) ; Soukup, Ondřej (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Kristína Hudáková Supervisor: doc. PharmDr. František Trejtnar, CSc. Title of diploma thesis: In vitro evaluation of novel Toll-like receptor ligands I Vaccination against preventable infections prevents millions of deaths each year. Their immunity enhancing activity is strengthened by the presence of vaccine adjuvants. Development of vaccine adjuvants leads to improved safety profile and also can play a vital role in the research of new vaccines against pathogens against which the vaccines currently do not exist. The main aim of this diploma thesis was to verify the ability of rationally developed small molecule ligands to influence Toll-like receptors and thus their potential to be utilized as vaccine adjuvants. The assay was carried out using modified cell lines continually expressing the human TLR4 or TLR8 whose activation leads to production of secreted embryonic alkaline phosphatase. Ten analyzed substances labelled as DM 001 - DM 010 were examined for their agonistic and also antagonistic properties while interacting with the TLRs. Immunomodulatory activity of these tested samples was then determined by quantification of secreted alkaline phosphatase with the help of a colorimetric...
Interactions of resveratrol derivatives with PXR receptor
Marešová, Veronika ; Pávek, Petr (advisor) ; Trejtnar, František (referee)
Charles University in Prague Department of Pharmacology & Toxicology Student: Supervisor: Prof Title of diploma thesis: Interactions of resveratrol derivatives with PXR receptor Derivatives of resveratrol belong between natural substances contained mainly in red wine and grapefruit. These compounds with stilbene-like structure show antioxidant activity. Pregnane X receptor (PXR) regulates expression of the most important biotransformation enzymes in human liver and intestine including cytochrome P450 3A4 (CYP3A4). Interaction of resveratrol and PXR have already been studied, but published data are contradictory. In my diploma thesis, I studied interaction of resveratrol and its derivatives with PXR. For this purpose, gene reporter assay with quantitative real-time polymerase chain reaction (qRT-PCR) was introduced. It was not possible to conduct experiments in standard way because both resveratrol and its derivatives inhibit lusiferase activities. I studied also effects of resveratrol and its derivatives on expression of CYP3A4 mRNA on differentiated HepaRG cell line. New method gene reporter method with qRT-PCR detection of luciferase was established on hepatoma cell line HepG2 transfected with CYP3A4 reporter construct. Concertation dependent effects of resveratrol and its derivatives were...
The changes in expression of selected drug-metabolizing enzymes in parasites after exposition to sublethal doses of drugs
Pasák, Michael ; Skálová, Lenka (advisor) ; Trejtnar, František (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Bc. Michael Pasák Supervisor: prof. RNDr. Lenka Skálová, Ph.D. Title of diploma thesis: The changes in expression of selected drug-metabolizing enzymes in parasites after exposition to sublethal doses of drugs The parasite, which causes significant losses of small ruminants through a disease called haemonchosis, is the abomasal nematode Haemonchus contortus. IVM is one of the anthelmintics used in veterinary medicine to eliminate haemonchosis. The main problem with this parasite is the presence of drug resistance to almost all administered anthelmintics including IVM. It is believed that xenobiotic-metabolizing enzymes such as cytochromes P450 (CYPs) and membrane efflux transporters P- glycoproteins (P-gps), play the role in resistance in H. contortus. This study focuses on the effect of sublethal doses of IVM on expression of selected CYPs and P-gps. Females and males of susceptible ISE strain H. contortus were separated before our experiment. After incubation of nematodes with three different concentrations of IVM, RNA was isolated and the changes in expression of selected genes were analyzed using qPCR. Significant sex-differences were observed in inducibility of tested genes. Significant...
The study of properties of radiolabelled monoclonal antibodies for imaging in oncology
Janoušek, Jiří ; Trejtnar, František (advisor) ; Kozempel, Ján (referee) ; Lázníčková, Alice (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Jiří Janoušek, MSc. Supervisor: Assoc. Prof. PharmDr. František Trejtnar, CSc. Consultant: Mgr. Pavel Bárta, Ph.D. Title of doctoral thesis: The study of properties of radiolabelled monoclonal antibodies for imaging in oncology Monoclonal antibodies belong to the group of targeted biological drugs that are currently successfully applied in various medical specialties, including oncology. The ability to specifically bind to antigens present in a tumour tissue is their significant attribute that can be used for imaging tumours in Nuclear Medicine. Receptors for vascular endothelial growth factor (VEGFR) and epidermal growth factor (EGFR) are possible tumour specific targets that are characteristic for some types of proliferating tumour tissue. The attachment of appropriate radionuclide is necessary for the potential radiodiagnostic use of monoclonal antibody. This task requires chemical modification of the antibody molecule that can damage its immunoreactivity and the binding to the target receptor. The aim of the doctoral thesis was to study the influence of labelling conditions with selected diagnostic radionuclides on radiochemical characteristics, in vitro receptor specific binding and...

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