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Macrocyclic complexes as models for copper(II) bonding in cupredoxins: Proof of concept
Ulrichová, Tereza ; Hermann, Petr (advisor) ; Hudeček, Jiří (referee)
Currently, modified electron transport metaloproteins with presence ion Cu(II) in their active site are most commonly used to study kinetics of electron transfer. One of the most studied model protein is cupredoxin azurin from P. aeruginosa with standard redox potential approximately 310-360 nm (depends on experimental conditions and techniques). Ion Cu(II) in azurin is coordinated by the side chain atoms of His46 , His117 , Cys112 , Met121 and carbonyl of Gly45 . The aim of this work was to prepare macrocyclic ligand, 1-[1H-imidazol-2- yl)methyl]-1,4,7-triazacycklononanu (LIM ), which would be able to form stable complexes with both of copper ions Cu(II) and Cu(I). Such as macrocyclic complexes could be utilized as low molecular models of active sites in proteins. The ligand was prepared using five-step synthesis employing protection of macrocycle, reduction and subsequent bromation of 1H- imidazol-2-karbaldehyd, and following alkylation reaction. Deprotection of macrocycle revealed final product of ligand. All reaction intermediates and prepared ligand were characterized by NMR and MS. Potentiometric titrations determined ligand protonation constant (log K1 = 10,62, log K2 = 6,65, log K3 = 4,91), which describe acid-base properties of a ligand in an aqueous solution. Similarly, the coordination...
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Lipid-based nanoparticles for the delivery of naphthoquinone derivatives for the treatment of psoriasis
Ulrichová, Tereza ; Hrubý, Martin (advisor) ; Poučková, Pavla (referee)
Psoriasis is an autoimmune chronic skin disease with a global prevalence of around 2-4%. Pharmacological treatment currently serves mainly to suppress the symptoms of the disease. However, many drugs have major side effects and therapy must often be discontinued. On the other hand, advances in understanding the pathophysiology of psoriasis have pointed out several molecular targets to be considered for future treatment. Traditional Chinese medicine has been using herbal extracts containing various types of 1,4-naphthoquinones for psoriasis treatment. These naphthoquinones have attracted much attention from the pharmaceutical industry for their structural diversity and wide range of pharmacological effects. Colored 1,4-naphthoquinones shikonin, juglon and their derivatives have already been tested on a numerous cell lines and animal models. The problem is their limited solubility in water, thermolability and susceptibility to oxidation and polymerization. Topical application is complicated by their strong binding to the upper layer of the skin, which causes skin discoloration that is difficult to wash off and reduces their penetration into the deeper layers of the skin, where their therapeutic effect is needed. To solve these problems, we developed within this thesis colorless prodrugs based on...
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Macrocyclic complexes as models for copper(II) bonding in cupredoxins: Proof of concept
Ulrichová, Tereza ; Hermann, Petr (advisor) ; Hudeček, Jiří (referee)
Currently, modified electron transport metaloproteins with presence ion Cu(II) in their active site are most commonly used to study kinetics of electron transfer. One of the most studied model protein is cupredoxin azurin from P. aeruginosa with standard redox potential approximately 310-360 nm (depends on experimental conditions and techniques). Ion Cu(II) in azurin is coordinated by the side chain atoms of His46 , His117 , Cys112 , Met121 and carbonyl of Gly45 . The aim of this work was to prepare macrocyclic ligand, 1-[1H-imidazol-2- yl)methyl]-1,4,7-triazacycklononanu (LIM ), which would be able to form stable complexes with both of copper ions Cu(II) and Cu(I). Such as macrocyclic complexes could be utilized as low molecular models of active sites in proteins. The ligand was prepared using five-step synthesis employing protection of macrocycle, reduction and subsequent bromation of 1H- imidazol-2-karbaldehyd, and following alkylation reaction. Deprotection of macrocycle revealed final product of ligand. All reaction intermediates and prepared ligand were characterized by NMR and MS. Potentiometric titrations determined ligand protonation constant (log K1 = 10,62, log K2 = 6,65, log K3 = 4,91), which describe acid-base properties of a ligand in an aqueous solution. Similarly, the coordination...
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How does the teaching qualification influence the elaboration of colour modification of Wartegg drawing test
ULRICHOVÁ, Tereza
This bachelor´s thesis deals with processing of colours modifications of Wartegg drawing test (WZT) done by secondary school teachers. Aim of the work is comparrison of WZT processing ways of humanistic discipline teachers with natural science disciplines teachers. Theoretical part of the work deals with characteristics of projective methods and with charateristics of WZT and its colours modifications. The theoretical part further describes symbolism of colours and defines the proffession of a teacher. Empirical part of the work is concerned with description of distinctions and concordances between 28 WZT processings done by humanistic disciplines teachers and 28 WZT processings done by natural scinence disciplines teachers.
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