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Antiproliferative, antioxidant and anti-inflammatory activity of quinones, terpenoids and their derivatives
Přibylová, Marie ; Vaněk, Tomáš (advisor) ; Smrček, Stanislav (referee) ; Hájek, Miroslav (referee)
Plant compounds play an important role in human medicine. They are a source of new drugs or serve as an inspiration for drugs' development. This thesis presents a study about syntheses of derivatives and biological activities of two groups of natural products, quinones and terpenoids. Terpenoids are plant secondary metabolites which are known for their antimicrobial, anti-inflammatory and anti-tumoral activities. We have focused on two representatives, paclitaxel and carvacrol. GnRH-paclitaxel anti-tumor conjugates potentially suitable for targeted delivery to cancer cells were prepared. Their antiproliferative activities in vitro were evaluated on MCF-7 cancer cell line and cytotoxicity in rat hepatocytes. Carvacrol and its derivative were tested for its possible anti- inflammatory effect, which was assessed in vitro as their potential to inhibit prostaglandin E2 biosynthesis via cyclooxygenase pathway. Quinones, other targets of the thesis, are well-known for biological activities similar to terpenoids. Thymoquinone, juglone and their derivatives were tested in vitro as inhibitors of cyclooxygenases and 5-lipoxygenase. Derivatives of juglone were prepared to help us to suggest structure-activity relationship of this compound. Thymoquinone and its derivatives were evaluated for their antioxidant capacity...
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Redox Dependence of Excitation Quenching by Quinones in Bacteriochlorophyll Agregates
Paleček, David
Harvesting only 4 % of light striking the Earth could possibly fulfill present energy demands of a mankind. Chlorosome of green sulfur bacteria is re- garded as suitable light-harvesting system for photosynthesis imitation. This work presents comparison of absorption and hole burning spectra of artificially prepared aggregates similar to chlorosomes with different compositions in order to verify the proposed role of quinones in excitation quenching and its redox de- pendence. Absorption spectra at room and helium temperature showed a resem- blance between artificial aggregates and chlorosomes. Hole burning experiments verified the role of quinones in excitation quenching under aerobic conditions. Even more pronounced excitation quenching was observed under anaerobic con- ditions. Significant improvements of the original experimental set-up provided better experimental data which raised many further question that are worth trying to answer in the future.
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Oxidativní enzymy v hroznech révy vinné
Brázda, Martin
The main objective of the Thesis is to understand the oxidation of must, especially enzymatic oxidation. It is caused by the oxidative enzymes that are already present on the grapes in vineyard, especially on those badly infected by mushroom diseases. The two main oxidative enzymes that need to be targeted are tyrosinase and laccase, collectively called polyphenoloxidasi (PPO). These most active oxidative enzymes, which already oxidize the must in the beginning of wine production and degrade the quality of future wine, belong to the group of oxidoreductases where oxygen is a catalyst for enzymatic activity and the phenolic compounds are substrates. Another main goal of the Thesis is to determine polyphenol oxidase activity on several samples of varieties and to compare how it affects other wine parameters such as acids, sugar content, etc. We will discus the oxidation of caftaric acid and its subsequent conversion to quinones. Quinones are just the product of the oxidation of phenolic compounds due to the activity of these enzymes. Caftaric and coutaric acids are the most oxidizable compounds for these enzymes and will therefore be discussed in more detail. It is also necessary to focus on possible protection against enzymatic oxidation.
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Redox Dependence of Excitation Quenching by Quinones in Bacteriochlorophyll Agregates
Paleček, David
Harvesting only 4 % of light striking the Earth could possibly fulfill present energy demands of a mankind. Chlorosome of green sulfur bacteria is re- garded as suitable light-harvesting system for photosynthesis imitation. This work presents comparison of absorption and hole burning spectra of artificially prepared aggregates similar to chlorosomes with different compositions in order to verify the proposed role of quinones in excitation quenching and its redox de- pendence. Absorption spectra at room and helium temperature showed a resem- blance between artificial aggregates and chlorosomes. Hole burning experiments verified the role of quinones in excitation quenching under aerobic conditions. Even more pronounced excitation quenching was observed under anaerobic con- ditions. Significant improvements of the original experimental set-up provided better experimental data which raised many further question that are worth trying to answer in the future.
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Antiproliferative, antioxidant and anti-inflammatory activity of quinones, terpenoids and their derivatives
Přibylová, Marie ; Vaněk, Tomáš (advisor) ; Smrček, Stanislav (referee) ; Hájek, Miroslav (referee)
Plant compounds play an important role in human medicine. They are a source of new drugs or serve as an inspiration for drugs' development. This thesis presents a study about syntheses of derivatives and biological activities of two groups of natural products, quinones and terpenoids. Terpenoids are plant secondary metabolites which are known for their antimicrobial, anti-inflammatory and anti-tumoral activities. We have focused on two representatives, paclitaxel and carvacrol. GnRH-paclitaxel anti-tumor conjugates potentially suitable for targeted delivery to cancer cells were prepared. Their antiproliferative activities in vitro were evaluated on MCF-7 cancer cell line and cytotoxicity in rat hepatocytes. Carvacrol and its derivative were tested for its possible anti- inflammatory effect, which was assessed in vitro as their potential to inhibit prostaglandin E2 biosynthesis via cyclooxygenase pathway. Quinones, other targets of the thesis, are well-known for biological activities similar to terpenoids. Thymoquinone, juglone and their derivatives were tested in vitro as inhibitors of cyclooxygenases and 5-lipoxygenase. Derivatives of juglone were prepared to help us to suggest structure-activity relationship of this compound. Thymoquinone and its derivatives were evaluated for their antioxidant capacity...
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Vliv redoxního stavu na zhášení excitace v bakteriochlorofylových agregátech
Paleček, David ; Dědic, Roman (advisor) ; Polívka, Tomáš (referee)
Harvesting only 4 % of light striking the Earth could possibly fulfill present energy demands of a mankind. Chlorosome of green sulfur bacteria is re- garded as suitable light-harvesting system for photosynthesis imitation. This work presents comparison of absorption and hole burning spectra of artificially prepared aggregates similar to chlorosomes with different compositions in order to verify the proposed role of quinones in excitation quenching and its redox de- pendence. Absorption spectra at room and helium temperature showed a resem- blance between artificial aggregates and chlorosomes. Hole burning experiments verified the role of quinones in excitation quenching under aerobic conditions. Even more pronounced excitation quenching was observed under anaerobic con- ditions. Significant improvements of the original experimental set-up provided better experimental data which raised many further question that are worth trying to answer in the future.
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