National Repository of Grey Literature 138 records found  1 - 10nextend  jump to record: Search took 0.01 seconds. 
Preparation and Evaluation of New Ligands Targeting Organic Cation Transporters in the Central Nervous System for the Treatment of Depression
Monteiro, Andrea ; Roh, Jaroslav (advisor) ; Vávrová, Kateřina (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Student: Andrea Monteiro Supervisor: Assoc. Prof. PharmDr. Jaroslav Roh, Ph.D. Specialized supervisors: Nicolas Pietrancosta, Ph.D. Sophie Gautron, Ph.D. Title: Preparation and Evaluation of New Ligands Targeting Organic Cation Transporters in the Central Nervous System for the Treatment of Depression Brain organic cation transporters (OCT2, OCT3) are polyspecific facilitated diffusion transporters that regulate aminergic tonus and have a complementary role to high-affinity monoamine transporters (serotonine transporter SERT, noradrenaline transporter NET and dopamine transporter DAT) in monoamine clearance in the brain. Their complementary characteristics compared to the high-affinity transporters (widespread distribution, broader pharmacological profile) and their involvement in mood-related functions make brain OCT relevant and original targets for the development of novel antidepressants. H2-cyanome is a newly developed prodrug of cyanome that targets OCT. This prodrug showed promising antidepressant efficacy in a rodent model of chronic depression. Despite the positive impact of this prodrug on antidepressant efficacy, its limitation is its high affinity for 1 adrenergic receptors that may...
Study of barrier lipids in the skin and skin models
Sochorová, Michaela ; Vávrová, Kateřina (advisor) ; Zimčík, Petr (referee) ; Salavec, Miloslav (referee)
1 Abstract Charles University, Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Candidate: Mgr. Michaela Sochorová Supervisor: prof. PharmDr. Kateřina Vávrová, Ph.D. Title of doctoral thesis: Study of barrier lipids in the skin and skin models The barrier lipids are found in the intercellular spaces of the uppermost layer of epidermis - stratum corneum (SC). These lipids comprise an approximately equimolar mixture of ceramides (Cer), fatty acids (FA) and cholesterol (Chol). The composition and organization of the lipid mixture is unique and provides a barrier, which protects organism against harmful effects from the surroundings and, at the same time, it protects body from excessive water loss and contributes to homeostasis maintenance. Skin barrier disruption, including altered barrier lipid composition and organization, was described in many skin diseases, for example atopic dermatitis, psoriasis or skin cancer. Study and therapy of these diseases are limited by their complex pathophysiology and a lack of biological material (human skin). Therefore, skin models are appropriate and useful tools for study of skin diseases. The skin models differ in their simplicity/complexity and their preparation therefore they can provide different information. Model lipid membranes are...
Synthesis and study of 1-O-acylceramides
Jon, Vojtěch ; Vávrová, Kateřina (advisor) ; Opálka, Lukáš (referee)
The extracellular matrix of the uppermost layer of the skin, the stratum corneum (SC), consists of ceramides (Cer), cholesterol (Chol), free fatty acids (FFA) and cholesteryl sulfate (CholS). Cer play an important role in the correct barrier function of mammalian epidermis. A new type of sphingolipids, i.e., 1-O-acyl-Cer, have been found in human SC very recently; however, their role in the SC is unknown. These Cer species contain sphingosine (S) that is N- acylated with non-hydroxylated or α- hydroxylated fatty acid, and moreover, hydroxyl group at C1 in sphingosine is esterified by an additional fatty acid (lignoceric acid, C24 or palmitic acid, C16). Because 1-O-acyl-Cer are not commercially available, we aimed to synthesize physiological 1-O-acyl Cer, i.e., Cer-24NS16, Cer-16NS16 and Cer-24AS16. Moreover, we aimed to study their behaviour on permeability and microstructure of model skin lipid membranes. The 1-O-acyl-Cer were synthesized by an acylation of Cer-NS16 or Cer-AS16 with palmitic or lignoceric acid using N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide and 4- dimethylaminopyridine. Cer-AS16 was prepared by α-bromination of palmitic acid, substitution of bromine by hydroxyl and N-acylation of sphingosine by the prepared acid in the presence N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide...
Study of azaphthalocyanines as fluorescence quenchers in oligodeoxynucleotide probes
Demuth, Jiří ; Nováková, Veronika (advisor) ; Hocek, Michal (referee) ; Vávrová, Kateřina (referee)
Charles University, Faculty of Pharmacy in Hradec Kralove Department: Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Author: Mgr. Jiří Demuth Supervisor: doc. PharmDr. Veronika Nováková, Ph.D. Consultant: prof. PharmDr. Petr Zimčík, Ph.D. Doctoral Thesis: Study of azaphthalocyanines suitable for quenching of fluorescence in oligodeoxynucleotide probes Phthalocyanines (Pcs) and azaphthalocyanines (AzaPcs) are planar macrocyclic compounds. These synthetic compounds are derived from naturally occurring dyes - porphyrins. Pcs and AzaPcs have very interesting photophysical properties due to their extensive 18 -electron conjugated system. They are used in electrotechnics, material industry or in medicinal applications. Octaalkylamino substituted tetrapyrazinoporphyrazines (TPyzPzs), which belong to AzaPc family, can quench fluorescence of other molecules due to the ultrafast intramolecular charge transfer. This thesis studies this quenching ability of TPyzPzs with the aim to develop efficient fluorescence probes. Such probes could find application in a variety of experiments across scientific disciplines i.e. - biochemistry, forensic or genetic analysis. Synthetic part of dissertation thesis is a continuation of previous investigation of TPyzPzs in our research group. It describes...
Synthesis and study of ceramides with deuterated acyl chain
Hudská, Klára ; Vávrová, Kateřina (advisor) ; Nováková, Veronika (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic Chemistry Candidate: Klára Hudská Supervisor: Doc. PharmDr. Kateřina Vávrová, Ph.D. Title of Diploma Thesis: Synthesis and study of ceramides with deuterated acyl chain Ceramides are a complex group of lipids belonging to sphingolipids. They are the most important component in stratum corneum and play an essential role in protecting the skin from excessive water loss and other environmental damages. Despite the fact that ceramides are a subject of intensive research, the exact effect of their structure on barrier skin function has not been fully explained. The aim of this diploma thesis was to synthesize a series of ceramides derived from sphingosin with deuterated acyl chains with chain lenght 4C, 16C and 24C and their study using Fourier transform infrared spectroscopy to understand the behaviour of ceramides in SC and their structure-activity relationships. The study of the synthesized ceramides using ATR-FTIR spectroscopy revealed that, at skin temperature, lipid chains are arranged in orthorhombic subcell, mostly with all-trans conformation. While the CerNS24 prefers extended conformation with its acyl associated with the acyl of LA and cholesterol associated with the sphingosin chain in...
Study of lipid membranes with lysolipids as models of atopic dermatitis
Pospíšilová, Markéta ; Vávrová, Kateřina (advisor) ; Zbytovská, Jarmila (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of inorganic and organic chemistry Candidate: Pospíšilová, Markéta Supervisor: Assoc. Prof. PharmDr. Kateřina Vávrová, Ph.D. Title of Diploma Thesis: Study of lipid membranes with lysolipids as models of atopic dermatitis We are protected against the harmful influence of the external environment by a skin barrier, which is located in the stratum corneum. The skin barrier also prevents excessive water loss through the skin. Ceramides have the most important role in the barrier function of the skin. The healthy skin's ceramides are synthesized of glucosylceramide and sphingomyelin via enzymes sphingomyelinase and glucocerebrosidase. If there is a lack of ceramide in the stratum corneum, which means, if these mechanisms work insufficiently, it gives rise to atopic dermatitis. In the stratum corneum of a patient who suffers from atopic dermatitis are glucosylceramide and sphingomyelin hydrolyzed by glucosylceramide/sphingomyeline deacylase which leads to free fatty acids and lysolipids (glucosylsphingosine and sphingosinephosphorylcholine) generation. In this work, we prepared model membranes which simulate a composition of lipids of the stratum corneum of a patient with atopic dermatitis, in which ceramides are replaced by...
Isosters of transkarbam 12 as transdermal penetration enhancers
Šíma, Martin ; Hrabálek, Alexandr (advisor) ; Vávrová, Kateřina (referee)
SUMMARY: Diploma thesis - Isosters of Transkarbam 12 as skin penetration enhancers Transkarbam 12 (5-(dodecyloxycarbonyl)pentylammonium-5-(dodecyloxycarbo- nyl)pentylcarbamate, T12) is a highly effective skin permeation enhancer. In this diploma thesis, T12 analogs with carbamate and carbonate function groups replacing the ester one were synthetised, and evaluated in vitro as skin permeation enhancers on excised porcine skin, using theophiline as a model drug. The results were expressed by an enhancing ratio and compared with the biological activity of T12. The enhancing activity decreases in the following sequence: ester, carbonate, carbamate. The results thus show that it is the ester group in the molecule of T12 which is essential for its extraordinary effect. In addition, homologues with a different length of the ending and connecting carbon chains were evaluated. While the length of the connecting carbon chain does not influence the biological activity significantly, nonyl to decyl ending carbon chains show the highest acceleration ability. It indicates that the length of the carbon chain, and not its lipofility, is important for the enhancing activity.
Synthesis and study of 1-O-acylceramides
Jon, Vojtěch ; Vávrová, Kateřina (advisor) ; Opálka, Lukáš (referee)
The extracellular matrix of the uppermost layer of the skin, the stratum corneum (SC), consists of ceramides (Cer), cholesterol (Chol), free fatty acids (FFA) and cholesteryl sulfate (CholS). Cer play an important role in the correct barrier function of mammalian epidermis. A new type of sphingolipids, i.e., 1-O-acyl-Cer, have been found in human SC very recently; however, their role in the SC is unknown. These Cer species contain sphingosine (S) that is N- acylated with non-hydroxylated or α- hydroxylated fatty acid, and moreover, hydroxyl group at C1 in sphingosine is esterified by an additional fatty acid (lignoceric acid, C24 or palmitic acid, C16). Because 1-O-acyl-Cer are not commercially available, we aimed to synthesize physiological 1-O-acyl Cer, i.e., Cer-24NS16, Cer-16NS16 and Cer-24AS16. Moreover, we aimed to study their behaviour on permeability and microstructure of model skin lipid membranes. The 1-O-acyl-Cer were synthesized by an acylation of Cer-NS16 or Cer-AS16 with palmitic or lignoceric acid using N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide and 4- dimethylaminopyridine. Cer-AS16 was prepared by α-bromination of palmitic acid, substitution of bromine by hydroxyl and N-acylation of sphingosine by the prepared acid in the presence N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide...

National Repository of Grey Literature : 138 records found   1 - 10nextend  jump to record:
See also: similar author names
1 Vavrová, Katarína
18 VÁVROVÁ, Kateřina
2 Vávrová, Karolína
18 Vávrová, Kateřina
2 Vávrová, Katka
5 Vávrová, Klára
1 Vávrová, Květa
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