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Asymetrically substituted ureas as a skin permeation enhancers
Šíma, Martin ; Hrabálek, Alexandr (advisor) ; Vávrová, Kateřina (referee)
PharmDr. Martin Šíma Asymetrically substituted ureas as a skin permeation enhancers ABSTRACT: Transkarbam 12 (5-(dodecyloxycarbonyl)pentylammonium-5-(dodecyloxycarbo-nyl)pentylcarbamate, T12) is a highly effective skin permeation enhancer. In this rigorous thesis, T12 analogs with urea function group 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 biological activity of T12 and its analogs from previous studies (alkane, ketone, amide, carbamate, and carbonate). Similarly to analogs from previous studies, there was a significant decrease in the enhancing potency. The results thus show that the ester group in the molecule of T12 is essential for its extraordinary effect.
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Anti-adhesive activity of bovine whey oligosaccharides against Neisseria meningitis
Janůšová, Barbora ; Vávrová, Kateřina (advisor) ; Pour, Milan (referee)
RESUME Neisseria meningitidis, je lidský patogen způsobující život ohrožující onemocnění. Tato onemocnění jsou velice závažná a mohou být smrtelná již za několika hodin po manifestaci prvních příznaků. Proto je nezbytně nutná rychlá diagnóza a okamžité nasazení antibiotik. Avšak díky zvýšenému výskytu rezistentních bakteriálních kmenů se stává léčba i prevence velmi obtížná, a jsou tedy hledány nové způsoby terapie. Jedním z nových přístupů může být antiadhesivní terapie využívající glykanů, které zabraňují adhesi bakterií na hostitelské tkáně. Oligosacharidy a glykokonjugáty izolované z kravského a mateřského mléka prokázaly antiadhesivní účinky proti mnoho patogenům, stejně tak i proti N. meningitidis. Tyto komponenty by mohly být tedy využity jako bioaktivní přísada do potravin, a snižovat tak incidenci bakterielních onemocnění. Toto využití je však velmi ekonomicky náročné, a jsou tedy hledány jiné zdroje, které by mohly snížit náklady. Takový zdroj představuje syrovátka vznikající jako odpadní produkt při výrobě sýrů. Cílem této práce tedy bylo izolovat oligosacharidy z kravské syrovátky, separovat je na neutrální a acidické a otestovat jejich antiadhesivní účinky. Pro separaci izolovaných oligosacharidů bylo užito gelové a iontově výměnné chromatografie. Schopnost oligosacharidů zabránit adhesi N....
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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.
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Synthesis of human ω-O-acylceramides and evaluation of their effects on barrier properties of skin lipid membranes
Opálka, Lukáš ; Vávrová, Kateřina (advisor) ; Hampl, František (referee) ; Kučerka, Norbert (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic chemistry Candidate: Mgr. Lukáš Opálka Supervisor: doc. PharmDr. Kateřina Vávrová, Ph.D. Title of doctoral thesis: Synthesis of human ω-O-acylceramides and evaluation of their effects on barrier properties of skin lipid membranes The main objective of this work was to synthesize and study human acylceramides (acylCer, ceramides of the EO type) with the focus on the relationships between the acylCer concentration , structure of their polar head, their ability to form lamellar phases and permeability of model lipid membranes. Another objective was to synthesize ceramide-1-phosphates for the study of their signaling role in skin barrier and an analogue of ganglioside GM1 with shorter acyl chain as a standard for analysis of these lipids. Ceramides (Cer) belong to the family of sphingolipids. They are the central molecules in sphingolipid metabolism, they participate on cell regulatory processes and the formation of human skin lipid barrier. The main skin barrier is situated in the stratum corneum (SC), which is the uppermost layer of skin. The purpose of SC is to maintain homeostasis of the inner environment and to prevent the penetration of exogenous substances, allergens and bacteria to the...
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Synthesis and study of ceramide analogues
Školová, Barbora ; Vávrová, Kateřina (advisor) ; Matějka, Pavel (referee) ; Šklubalová, Zdeňka (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of inorganic and organic chemistry Candidate: Mgr. Barbora Školová Supervisor: doc. PharmDr. Kateřina Vávrová, Ph.D. Title of doctoral thesis: Synthesis and study of ceramide analogues Ceramides (Cer) together with free fatty acids and cholesterol form intercellular lamellar space of the uppermost skin layer (stratum corneum, SC). This lipid matrix presents the proper skin barrier - it protects organism against outer environment and keeps its homeostasis as well. The composition and arrangement of the intercellular lipid matrix is essential for the skin barrier properties. In spite of this fact, the organization of SC lipids at the molecular level is not fully elucidated. The aim of this work is to contribute to more detailed insight into organization of skin barrier using SC lipid model membranes, in particular to find the structural parameters in ceramide molecules, which play a role in the maintenance of the skin barrier. The SC model membranes present a useful tool to study SC lipids, they mimic physiological or pathological conditions in the skin. The obtained results should be used in diagnosing or therapy of skin diseases characteristic with impaired barrier function, such as atopic dermatitis or psoriasis....
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Land Analysis needful for complex landscaping
Vávrová, Kateřina ; Kottová, Blanka (advisor) ; Klára, Klára (referee)
This thesis deals with a detailed analysis of available data for the area, which is the cadastral area Malý Bor district Klatovy, which subsequently serves as a major
base for the actual process of implementing the komplex landscaping. It also includes my own field research.
In the first part are described in detail and explained the particular concepts related to the landscape, landscaping, and for them the important materials. In another part is defined the researched area and it is described in terms
of historical, typological, geomorphological, geological, climatic, hydrological, phytogeographical and geobiocenological.
In the following part there is the description of the available materials and economic land use. With all these available data have been maked particular analyzes that lead to evaluation road infrastructure, water and wind erosion, the situation of nature and landscape protection, water management measures and landscape greenery. Everything is completed by findings from the field research
and my own photographs. On these findings are based and individual recommendations or warnings, which serve as comments in a case of implementation of comprehensive landscaping.
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