Dohnalova A: Alkaloids of Amaryllidaceae family: isolation, structural identification, biological activity. I; Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové, 2017, 64 p. The Amaryllidaceae family includes bulbous, beautifully flowering plants that have been used for thousands of years in traditional medicine. The major chemical compounds found in this particular plant family are alkaloids, namely Amaryllidaceae alkaloids. Until now, more than 500 isoquinoline alkaloids have been discovered, which exhibit a diverse biological activity including antitumor and antibacterial. They are also able to inhibit acetylcholinesterase. The aim of the diploma thesis was to process 34 kg of fresh bulbs of Narcissus cv. PROFESSOR EINSTEIN and to prepare an alkaloidal extract. This extract was further divided by column chromatography to almost 500 fractions which were merged based on TLC into 27 subfractions. The subfractione No. 17 was selected for isolation of at least one pure alkaloid. Preparative TLC was used for the the isolation. One pure compound was obtained in crystalic form which was then subjected to structural analysis by EI-MS and NMR methods. Further studies of biological activities were performed in...

Baková I.: Isolation of alkaloids of the species Magnolia soulangeana Soul.-Bod. and study of their biological activity. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové, 2017. Key words: Magnolia solulangeana, secondary metabolites, alkaloids, biological activity. Secondary metabolites of plants are responsible for various biological activities. Alkaloids were described as a potentially suitable for Alzheimer's disease therapy (AD) through their inhibition activities against cholinesterases. Nowadays, these substances are important medicine for AD, therefore a screening of herbal drugs is still a current topic. An alkaloid extract of Magnolia × soulangeana flowers was tested in a preliminary testing on anticholinesterase activity. Because of the promising results, it was chosen for an isolation and identification possible effective alkaloids. The extract was separated by a column chromatography using aluminium oxide and a step gradient elution. Alkaloids were isolated by a repeated preparative thin-layer chromatography. Individual alkaloids were identified by a structural analysis (NMR, MS) and then their optical activity was measured. Substances were tested for an inhibition activity against human...

Orientador: Glaúcia Maria Pastore / Tese (doutorado) - Universidade Estadua de Campinas, Faculdade de Engenharia de Alimentos / Made available in DSpace on 2018-08-18T10:58:19Z (GMT). No. of bitstreams: 1 Malta_LucianaGomes_D.pdf: 3416128 bytes, checksum: dec89a08c54c6d1964d67b3fdcd3b259 (MD5) Previous issue date: 2011 / Resumo: A ingestão de muitas frutas convencionais, exóticas e nativas está associada com a redução do risco de doenças crônicas não transmissíveis e até mesmo o câncer. Neste contexto, o presente trabalho tem como proposta estudar atividades biológicas bem como identificar e quantificar os compostos fenólicos das frutas do Cerrado brasileiro, Guapeva (Pouteria cf. guardneriana Radlk.), Murici (Byrsonima verbascifolia Rich.) e Gabiroba (Compomanesia cambessedeana O. Berg.). Além dos compostos fenólicos, foram investigadas as atividades antioxidante, antiinflamatória, antimutagência, antigenotóxica, antiproliferativa e citotóxica. Os compostos fenólicos foram extraídos com etanol 95% e com água. Os fenólicos lipofílicos foram extraídos, a partir da fruta, com hexano. A quantificação dos compostos fenólicos foi realizada e os extratos etanólicos apresentaram melhores resultados quando comparados com os aquosos. O extrato etanólico da Gabiroba concentração de fenólicos de 4610,46 mg Ácido Gálico/100g fruta fresca, sendo superior a todos os outros extratos. Também foi realizada a quantificação dos flavonóides totais, mas apenas para os extratos etanólicos, e a semente da Guapeva apresentou o resultado mais relevante, no valor de 2915,62 mg Catequina/100g fruta fresca. Os extratos do Cerrados foram avaliados quanto a capacidade antioxidante in vitro através dos métodos 2,2- Diphenyl ¿ 1- picrylhydrazil (DPPH), Trolox Equivalent Antioxidant Capacity (TEAC), Oxygen Radical Absorbance Capacity (ORAC) e Peroxyl Radical cavenging Capacity (PSC). Os resultados do teste DPPH foram expostos de duas formas diferentes, como equivalentes de Trolox onde o extrato etanólico da casca da Guapeva destacou-se por apresentar maior potencial antioxidante nos 3 tempos analisados (30, 60 e 90 minutos) e também como IC50, onde o extrato etanólico da Gabiroba apresentou melhor resultado no valor de 11,10 µg/mL de fruta fresca. Para o teste TEAC os extratos etanólicos da casca da Guapeva e a Gabiroba apresentaram maior potencial antioxidante, com resultados de 1543,53 e 1014,25 µM Trolox Equivalentes/100g fruta fresca, respectivamente. Já para os ensaios ORAC e PSC o extrato etanólico da Gabiroba apresentou maior atividade, com resultados de 43780,00 µM TE/100g de fruta e 2342,52 µM Vitamina C/100 g fruta fresca, respectivamente. A identificação e quantificação dos compostos fenólicos presentes nos extratos foram realizadas por Cromatografia líquida de alta eficiência. Foram identificados Ácido ferrúlico, Resveratrol, Etil galato, Catequina, Propil galato e Epicatequina. Ratos foram tratados com os extratos de frutas e o plasma foi coletado 30, 60 e 90 minutos após a gavagem para análise pelos métodos ORAC, TEAC e fenóis totais. O extrato de casca da Guapeva apresentou maior concentração de fenóis totais após trinta minutos da ingestão e o Murici após 1 hora. Através da análise TEAC, todos os extratos apresentaram maior atividade antioxidante no tempo de 30 minutos quando comparado com os demais tempos. No ensaio ORAC todos os extratos apresentaram maior potencial nos períodos de 30 e 60 minutos. A identificação dos compostos fenólicos no plasma foi determinada por Espectrometria de Massas, sendo que apenas a Catequina foi identificada no grupo que foi tratado com Gabiroba. O potencial antimutagênico/mutagênico foi determinado pelo teste in vivo de Micronúcleos. Todos os extratos mostraram-se antimutagênicos e não mutagênicos. O extrato com maior efeito protetor contra a droga Ciclofosfamida foi o Murici 400 mg extrato/kg P.C. com efeito redutor de 97,71%. A avaliação do efeito antiinflamatório foi realizada pelo teste de Edema de pata, induzido por Carragenina e todos os extratos apresentaram ação antiinflamatória. Também verificou-se que a partir da segunda hora após a injeção da Carragenina, o efeito antiinflamatório apresentado por todos extratos, aumentou. O efeito antigenotóxico foi avaliado pelo ensaio Cometa in vivo. Todos os extratos avaliados não danificaram o DNA e os que apresentaram maior proteção contra dano/lesão no DNA foram a polpa, casca e semente da Guapeva na concentração de 200 mg extrato/kg P.C. e o Murici na concentração de 400 mg extrato/kg P.C. Oito linhagens tumorais humanas foram utilizadas na determinação do potencial antiproliferativo, apenas a Guapeva casca, polpa e o Murici apresentaram início de efeito citostático. A atividade citotóxica e antiproliferativa foi avaliada em hepatocarcinoma humano (HepG2), a semente da fruta Guapeva apresentou citotoxicidade, e a casca e polpa da fruta Guapeva, assim como a Gabiroba se destacaram no potencial antiproliferativo com valores de 11,75; 12,57 e 8,35 mg/mL. O potencial antioxidante celular foi avaliado e a casca da fruta Guapeva apresentou maior atividade, no valor de 99,91 µmol Quercetina/100g fruta de fresca. De acordo com nosso conhecimento, este foi o estudo mais aprofundado sobre as propriedades biológicas das frutas do Cerrado, e que possivelmente possibilitará a utilização destes como alimento funcional / Abstract: There is an association between the conventional intake of many fruits (exotic native species) with reduced risk of chronic diseases and even cancer. In this context, this work aims to study the biological activities, identify and quantify the phenolic compounds of Cerrado's fruits, the Guapeva (Pouteria cf. Guardneriana Radlk), Murici (verbascifolia Byrsonima Rich) and Gabiroba (Compomanesia cambessedeana O. Berg). In addition, we investigated the antioxidant, anti-inflammatory, antimutagenic, antigenotoxic, antiproliferative and cytotoxic properties of these fruits. Phenolic compounds were extracted with 95% ethanol and water. The lipophilic phenolics were extracted from the fruit with hexane. The quantification of phenolic compounds was performed and the ethanol extracts presented better results when compared with aqueous extracts. The Gabiroba extract showed the total phenolic concentration of 4610.46 mg Gallic acid/100g fresh fruit, higher than all other analyzed extracts. Total flavonoids were also quantified, but only the ethanol extracts were used. The seed of the Guapeva presented the most relevant results, amounting to 2915.62 mg Catechin /100g fresh fruit. The Cerrado's extracts were evaluated for antioxidant capacity in vitro using the methods 2,2- Diphenyl ¿ 1- picrylhydrazil (DPPH), Trolox Equivalent Antioxidant Capacity (TEAC), Oxygen Radical Absorbance Capacity (ORAC) e Peroxyl Radical cavenging Capacity (PSC). The DPPH test results were presented in two different ways, one as Trolox equivalents, in which the ethanol extract of the peel of the Guapeva resulted in the highest antioxidant potential for the three analyzed times (30, 60 and 90 minutes) and the other way as EC50, in which it was observed that the ethanol extract of Gabiroba had the best result with a value of 11.10 µg/mL of fresh fruit. From the TEAC test, ethanol extracts of the peel of Guapeva and Gabiroba showed higher antioxidant potential, the results were 1543.53 and 1014.25 uM Trolox Equivalents/100g of fresh fruit, respectively. For the ORAC and PSC tests, the ethanol extract of the Gabiroba presented the highest activity, with results of 43,780.00 µM TE/100g of fresh fruit and 2342.52 µM Vitamin C/100g of fresh fruit, respectively. The identification and quantification of phenolic compounds in the extracts were performed by high performance liquid chromatography. The following standards were identified: Ferrulic acid, resveratrol, ethyl gallate, catechin, Propyl gallate, and epicatechin. Rats were treated with the extract of fruits and plasma was collected 30, 60 and 90 min after gavage for analysis by the methods ORAC, TEAC and Total phenolics. The peel of the Guapeva extract showed the highest concentration of phenolics thirty minutes after treatment and the Murici presented the highest concentration after 1 hour of ingestion. For the TEAC test, all extracts showed higher antioxidant activity at 30 minutes compared to the other analyzed periods. For the ORAC assay, all the extracts had the greatest potential in periods between 30 and 60 minutes. The identification of phenolic compounds in plasma was determined by mass spectrometry, and only the Catechin was identified in the group of animals that received the Gabiroba extract. The antimutagenic / mutagenic test was determined by in vivo micronucleus test. None of the extracts show mutagenic properties. The extract with the greatest protective effect against Cyclophosphamide drug was the Murici at 400 mg extract / kg body weight, presenting reduction effect of 97.71%. The evaluation of anti-inflammatory effect was accomplished by testing the paw edema induced by the Carrageenan drug and it was observed that all extracts showed anti-inflammatory properties. It was also found that from the second hour after injection of Carrageenan, all extracts presented an increase of anti-inflammatory effects. The antigenotoxic effect was evaluated by Comet assay in vivo. All the extracts evaluated did not induce DNA damage, the extracts that provided greater protection against DNA damage were the pulp, peel and seed of Guapeva at 200 mg extract/kg body weight and Murici at 400 mg extract/kg body. Eight human tumor cell lines were used to determine the potential antiproliferative effects of the fruits, however just the peel, pulp of Guapeva and Murici showed cytostatic effects. The antiproliferative and cytotoxicity activities were evaluated in human hepatocellular carcinoma cells (HepG2). The seeds of Guapeva presented cytotoxicity, and the peel and pulp of Guapeva, and Gabiroba showed the highest antiproliferative potential with values of 11.75, 12.57 and 8.35 mg/mL, respectively. The cellular antioxidant potential was tested and the peel of the Guapeva showed the highest activity, amounting to 99.91 µmol Quercetin/100g fresh fruit. This study furthers the investigation of the biological properties of the fruits of the Cerrado, and possibly allow the use of these as functional food / Doutorado / Tecnologia de Alimentos / Doutor em Tecnologia de Alimentos

Orientador: Ronaldo Aloise Pilli / Dissertação (mestrado) - Universidade Estadual de Campinas, Instituto de Quimica / Made available in DSpace on 2018-08-14T13:10:56Z (GMT). No. of bitstreams: 1 Marquissolo_Cilene_M.pdf: 4919703 bytes, checksum: f834b50c778a98043d8f699e6b2947b9 (MD5) Previous issue date: 2009 / Resumo: Este trabalho tem como objetivo preparar análogos furânicos da goniotalamina 31, 32 e 33 em suas duas formas enantioméricas, utilizando-se a alilação catalítica e assimétrica nas condições de Keck e a reação de metátese de olefinas para fechamento de anel. Estes análogos foram obtidos em bons rendimentos e excelentes razões enantioméricas. Estes novos compostos foram submetidos a testes de atividade antiproliferativa frente a nove linhagens de células tumorais e a bioensaios in vitro contra a forma tripomastigota do Trypanosoma cruzi e contra a forma promastigota de Leishmania major e Leishmania brasiliensis. No que diz respeito à atividade antiproliferativa, exceto para as linhagens de melanoma e cólon, os compostos testados apresentaram maior potência do que o controle positivo, doxorrubicina. Adicionalmente, os compostos 31, 32 e 33 mostraram-se mais ativos que a goniotalamina (1), exceto para as linhagens de mama e ovário. Os bioensaios de citotoxicidade com células não infectadas (LLC-MK2) mostraram que os compostos apresentaram baixa citotoxicidade. Com relação à atividade tripanocida, embora o composto (S)-31 tenha se apresentado como o composto mais ativo, mostrou alta citotoxicidade em células não-infectadas. (S)-32 é o composto que apresenta atividade mais interessante contra T. cruzi, além do menor valor de citotoxicidade e alto índice de segurança. Para a atividade leishmanicida, o análogo (S)-31 apresentou-se como o composto mais ativo para ambas as espécies de Leishmania, mostrando-se cerca de 6,5 vezes mais ativo que o controle positivo para Leishmania brasiliensis e cerca de 14,6 vezes para Leishmania major. Os ensaios de citotoxicidade revelaram valores de concentração superiores aos valores de IC50, indicando baixa toxicidade. Para Leishmania brasiliensis e Leishmania major, (R)-31 e (S)-31 mostraram-se como os compostos mais ativos e apresentaram bons índices de segurança. O análogo 33 não apresentou atividade expressiva em nenhum dos testes realizados indicando que a presença do grupo nitro ligado ao anel furânico é de grande importância para as atividades biológicas avaliadas / Abstract: This work describes the preparation of furan analogues of goniothalamin (compounds 31, 32 and 33) in both enantiomeric forms through the utilization of Keck asymmetric allylation and ring-closing methatesis reaction. These analogues were prepared in good overall yield and excellent enantiomeric ratio. These novel compounds were evaluated as antiproliferative agents against a panel of nine cancer cell lines and in vitro bioassays against the tripomastigote form of Trypanosoma cruzi and promastigote form of Leishmania major and Leishmania brasiliensis. Compounds 31-33 were more potent than the positive control (doxorubicin) in the antiproliferative experiments, except for melanoma and colon cancer cells. Additionally compounds 31-33 were more active than goniothalamin (1), except for breast and ovary cancer cells. Regarding their tripanocidal activity, compound (S)-31 was shown to be very toxic to non-infected cells despite its being highly active. Compound (S)-32 was the most promising one against T. cruzi due to its low toxicity and high insurance level. As to the leishmanicidal activity, the analogue (S)-31 was shown to be the most active for both Leishmania species investigated being 6,5 times more active than the positive control for Leishmania brasiliensis and about 14,6 times for Leishmania major, The citotoxicity assays revealed low toxicity against non-infected cells. For Leishmania brasiliensis and Leishmania major (R)-31 and (S)-31 were shown to be more active one and also displayed the best insurance level. Analogue 33 did not display any significant biological activity in our assays indicating that the nitrofuran moiety is very important for the biological activities investigated / Mestrado / Quimica Organica / Mestre em Química

A matéria orgânica do solo (MOS) é composta de uma mistura complexa e heterogênea de compostos orgânicos, sendo as substâncias húmicas (SH) a fração mais recalcitrante da MOS. As SH têm grande influência sobre as propriedades químicas e biológicas do solo, contribuindo como fonte de energia para microrganismos e também contribuindo com a disponibilidade de nutrientes. Além disso, as SH podem contribuir de forma expressiva para o desenvolvimento e produção das plantas cultivadas. Neste sentido, o objetivo deste trabalho foi avaliar a atividade e diversidade da comunidade bacteriana do solo, a disponibilidade de nutrientes e a produtividade da cultura de trigo após aplicação de doses crescentes de SH. Dois experimentos foram montados e avaliados, sendo um ensaio de incubação com um solo arenoso e outro um experimento de casa de vegetação com plantas de trigo em dois solos tropicais distintos (textura arenosa e argilosa). Houve um estímulo à atividade microbiana em ambos os experimentos, sendo este estímulo transitório, o que provavelmente ocorreu devido a um efeito priming provocado pela adição de SH. No entanto não houve alteração na estrutura da comunidade bacteriana pela adição de SH, o que pode ser devido ao fato de ser um material recalcitrante e já presente no solo. Também houve aumento na disponibilidade de fósforo, potássio, cálcio e nitrogênio, bem como da CTC, tanto em solo arenoso quanto argiloso, expressando o efeito das SH na melhoria das propriedades químicas de solos tropicais. Além disso, um efeito significativo foi visto em parâmetros relacionados à produtividade do trigo. Houve aumento de massa seca de raízes e parte aérea, além de aumento no peso e número de grãos, o que pode se refletir em aumento considerável de produtividade. Esses resultados são importantes por mostrarem que mesmo a fração mais recalcitrante da MOS pode influenciar positivamente aspectos químicos e biológicos do solo, contribuindo com a melhoria do sistema de produção e também com maiores produtividades vegetais. / The soil organic matter (SOM) is composed of a complex and heterogeneous mixture of organic compounds, in which the humic substances (HS) are considered to be the most recalcitrant fraction. HS have great influence on chemical and biological soil properties, contributing as energy source for microorganisms and as nutrient reservoir for plants. Furthermore, HS can contribute significantly to the development and production of crop plants. Therefore, the objective of this study was to evaluate the activity and diversity of the soil bacterial community, nutrient availability and productivity of a wheat crop after application of increasing doses of HS. For this purpose, two experiments were performed and evaluated, one is an incubation essay with a sandy soil and the other a greenhouse experiment with wheat plants using two distinct tropical soils as substrates (sandy and clayey). Microbial activity was stimulated in both experiments, and this transient stimulus may have been due to a priming effect caused by the addition of HS. However, there was no change in the bacterial community structure which may be due to the fact that HS is a recalcitrant material and already present in the soil. Nevertheless, we found an increase in the availability of phosphorus, potassium, calcium and nitrogen, as well as in the CEC in both, sandy and clayey soils, showing that HS do improve chemical properties of tropical soils. Furthermore, we found a significant effect on wheat productivity related parameters. There was an increase of dry weight of roots and shoots, as well as increased weight and number of grains, which may be reflected in a significant increase in productivity. These results are important because they show that even the most recalcitrant SOM fraction can positively influence soil chemical and biological aspects, contributing to the improvement of the production system and also to higher plant productivity.

Submitted by Ricardo Cedraz Duque Moliterno (ricardo.moliterno@uefs.br) on 2016-01-19T23:08:21Z No. of bitstreams: 1 TESE DOUTORADO VERS?O FINAL.pdf: 3041272 bytes, checksum: e0025693076836f6a3804cc2aaf6a529 (MD5) / Made available in DSpace on 2016-01-19T23:08:21Z (GMT). No. of bitstreams: 1 TESE DOUTORADO VERS?O FINAL.pdf: 3041272 bytes, checksum: e0025693076836f6a3804cc2aaf6a529 (MD5) Previous issue date: 2015-09-28 / Essential oils are complex mixtures of various isolates of plant secondary metabolites. Due to the increased use of these aromatic compounds, research has been developed, and the development of new products. This study analyzed the antimicrobial, cytotoxic and immunomodulatory activities in addition to the phytochemical profile of essential oils Achyrocline satureoides and Ageratum conyzoides. The micro-organisms most sensitive to oils were Staphylococcus aureus CCMB 262 and Candida kruzei CCMB 287. The essential oil of A. conyzoides was considered non-toxic in the tested conditions. In the assessment of the immune response induced by oils, although they were not statistically significant differences between the concentrations tested and control, it was observed that the essential oils inhibited the production of IL-8 and IL-12 cytokines with exception of the species A. satureoides at a concentration of 100 mg / mL. This behavior may suggest the capacity reduction of the inflammatory response. The chromatographic analysis of essential oils of A. satureoides demonstrated a chemical profile consistent with the literature where the major components were ?-Pinene, E-caryophyllene, ?-copaene, ?-humulene, d-cadinene. Since the analysis of oils A. conyzoides showed conflicting results in the literature which suggests a new chemotype, since the presence of precocenos the chemical analysis was not observed. / Os ?leos essenciais s?o misturas complexas de metab?litos secund?rios isolados de diversas plantas. Devido ao aumento do uso destes compostos arom?ticos, pesquisas v?m sendo desenvolvidas, al?m do desenvolvimento de novos produtos. O presente trabalho analisou as atividades antimicrobiana, citot?xica e imunomoduladora, al?m do perfil fitoqu?mico de ?leos essenciais de Achyrocline satureoides e Ageratum conyzoides. Os micro-organismos mais sens?veis aos ?leos foram Staphylococcus aureus CCMB 262 e Candida kruzei CCMB 287. O ?leo essencial de A. conyzoides foi considerado at?xico nas condi??es testadas. Em rela??o ? avalia??o da resposta imune induzida pelos ?leos, apesar de n?o terem sido encontradas diferen?as estatisticamente significantes entre as concentra??es testadas e o controle, p?de-se observar que os ?leos essenciais inibiram a produ??o das citocinas IL-8 e IL-12, com exce??o da esp?cie A. satureoides na concentra??o de 100 ?g/mL. Este comportamento pode sugerir a capacidade de redu??o da resposta inflamat?ria. As an?lises cromatogr?ficas dos ?leos essenciais de A. satureoides demonstrou um perfil qu?mico em concord?ncia com a literatura onde os componentes majorit?rios foram ?-Pineno, E-Cariofileno, ?-Copaeno, ?-Humuleno, d-Cadineno. J? as an?lises dos ?leos de A. conyzoides apresentou resultados divergentes da literatura o que nos sugere um novo quimiotipo, uma vez que n?o foi observada a presen?a de precocenos nas an?lises qu?micas.

4 ABSTRACT Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Viera Bodoríková Supervisor: doc. Ing. Lucie Cahlíková, Ph.D. Title of Diploma thesis: Synthesis of haemanthamine derivatives and their biological activity Haemanthamine, an isoquinoline Amarillidaceae alkaloid, exhibits a wide and important range of biological activities, including antitumor, antiviral, antioxidant, antimalarial and anticonvulsant. Biological activity of haemanthamine relatives closely with its structure. By modifying the different parts of the molecule, we can identify some structure-activity relationships. With this aim, the thirteen semisynthetic analogues of alkaloid haemathamine were prepared and purified using analytic and preparative TLC methods. The obtained substances were then subjected to structural analysis, specifically, there were used MS, HRMS, 1D and 2D NMR spectroscopic techniques. Prepared compounds were tested on its possibility to inhibit human erythrocytic acetylcholinesterase (HuAChE) and human serum butyrylcholinesterase (HuBuChE). The most promising biological activities have been shown by aromatic esters labelled as LC- 70 (IC50 HuAChE = 0,12 ± 0,01 µM) and LC-73 (IC50 HuAChE =0,17 ± 0,01 µM). The cytotoxic activity of prepared compounds has been...

This thesis deals with the study of the biological activity of humic substances. Based on the literature review preparation procedures were optimized in order to develop new hydrogel forms containing humic substances and biopolymers with high swelling capacity. Besides methodology for the rapid assessment of the biological activity obtained in laboratory conditions were designed and tested. The experimental part focused on characterization of hydrogel samples by means of routine physico-chemical methods, the main attention was paid to sorption of water and release of humic substances into solution. Then the prepared hydrogel materials were tested focusing on the growth effects on the maize. The absorption of mineral nutrients by the roots of plants were studied as well. The motivation of this work comes from the potential of agricultural and environmental applications of such hydrogel materials resulting in a renewal of previously exhausted organic content of soils and consequent interruption of substantial soil degradation.

Tato práce představuje pilotní studii testující souvislosti mezi biologickými vlastnostmi a strukturou huminových kyselin extrahovaných z původního a modifikovaného jihomoravského lignitu, důl Mír, Mikulčice. V první části práce byly testovány metody vhodné ke zvýšení výtěžku huminových kyselin extrahovaných z lignitu. Oxidace lignitu v plynné fázi nepřinesla uspokojivé zvýšení výtěžku a byla instrumentálně poměrně náročná. Dále proto byla zkoumána jen oxidace v kapalné fázi a modifikace nízkomolekulárními organickými kyselinami. Modifikace organickými kyselinami byla inspirována procesy podporujícími biologické funkce v rizosféře, t.j. kořenový systém vylučuje exudáty způsobující změny v supramolekulové struktuře okolní organické hmoty čímž zlepšuje její mobilitu a prostupnost buněčnými stěnami. Primární struktura huminových kyselin připravených v této práci byla zkoumána prostřednictvím elementární analýzy a spektrálních metod (13C CPMAS NMR, EPR a UV-VIS spektroskopie). Navzdory tomu, že primární struktura vykazovala jen malé rozdíly, měření biologické aktivity a genotoxického potenciálu prokázalo, že huminové kyseliny a jejich humáty získané z lignitu s rozdílnou předúpravou vykazují odlišnou bioaktivitu. Proto byla dále zkoumána supramolekulární struktura vzorků ve zředěných roztocích, a to prostřednictvím vysokoúčinné vylučovací chromatografie, měření ultrazvukové rychlosti a hustoty. Testovány byly dva různé protionty – draselný a amonný. Získané výsledky potvrdily předpoklad, že pozorované změny v kvalitě humátů jsou závislé na protiiontu, koncentraci humátu v roztoku a také na metodě předúpravy původního lignitu. Obě zvolené metody předúpravy lignitu prokázaly svůj potenciál produkovat huminové kyseliny s rozmanitými biologickými vlastnostmi, aplikovatelné v zemědělství, životním prostředí a potenciálně i ve farmakologii.

Charles University, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmaceutical Botany (16-16130) Author: Tkáčová Beáta Supervisor: PharmDr. Kateřina Breiterová, Ph.D. Title of thesis: Alkaloids of Narcissus species cultivars and their biological activity I. Key words: Narcissus, alkaloids, biological activity, Alzheimer's disease. The main aim of this diploma thesis was to obtain summary alkaloid extracts from bulbs of five species cultivars (Narcissus cv. Acropolis, Delta, White Marvel, Kedron, Scarlet Gem) and one variety (Narcissus albus var. plenus odoratus), labeled as AL-450, AL-457, AL-460, AL-463, AL-467 and AL-508, from which samples were subsequently prepared for GC-MS analysis and screening of biological activities (cholinesterase inhibitory activity and cytotoxicity). Totally, 18 alkaloids were identified by GC-MS analysis, comparing their mass spectra. Identified alkaloids include 3-O-demethylmaritidine, 11,12-dehydroanhydrolycorine, assoanine, dehydroassoanine, galanthamine, galanthine, haemanthamine, hippeastrine, incartine, lycoramine, lycorine, narwedine, norpluvine, pancracine, pluvine, pseudolycorine and tazettine. Samples of cultivars AL-457, AL-460, AL-463 and AL-508, showed relatively promising hAChE inhibitory activity in screening assay (c = 50 µg/ml),...