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Amaryllidaceae alkaloids of montanine type and their derivatives as potential drugs.
Maafi, Negar ; Cahlíková, Lucie (advisor) ; Šmejkal, Karel (referee) ; Havlík, Jaroslav (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Candidate: Negar Maafi Supervisor: Prof. Ing. Lucie Cahlíková, Ph.D. Title of Doctoral Thesis: Amaryllidaceae alkaloids of montanine type and their derivatives as potential drugs. Based on the knowledge of the biological activity of montanine-type alkaloids of Amaryllidaceae, these alkaloids were selected for the preparation of their semisynthetic derivatives to study the relationship between structure and the activity. Derivatives of montanine-type alkaloids were prepared using haemanthamine and montanine as starting substances. The montanine-type alkaloid 3-O- methylpancracine was prepared using intramolecular rearrangement of haemanthamine. Previously isolated montanine from bulbs of Hippeastrum x hybridum cv. Ferrari was used in synthesize of derivatives. In total, more than 80 aliphatic and aromatic derivatives of montanine and 3-O- methylpancracine have been prepared. All compounds were identified using 1D- and 2D-NMR, MS, HRMS, and so forth. The prepared derivatives were screened for a wide range of biological activities (inhibitory potential against hAChE/hBuChE, antimycobacterial, antibacterial and antifungal activity, cytotoxicity, and others). In the hAChE/hBuChE study, the...
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Metabolic Profile of Panax ginseng Bioactive Substance in Plant Material of Varies Origin.
Bacílková, Anna ; Klusoňová, Hana (advisor) ; Havlík, Jaroslav (referee)
Author: Anna Bacílková Title: Metabolic profiles of bioactive components of Panax ginseng C. A. Meyer from different herbal sources Diploma thesis Publishing place: Charles University in Prague, Faculty of Pharmacy in Hradec Králové The field of study - pharmacy In this diploma thesis, I was concerned with the determination and quantification of 12 ginsenosides in 11 commercial ginseng preparations from the species Panax ginseng C. A. Meyer available in the Czech Republic. Ginsenosides are triterpenes saponins considered to be main bioactive principles of ginseng. The two-dimensional thin layer chromatography and high performance liquid chromatography with UV detection was used for the identification and quantitative determination of these compounds. The methods applied are based on comparison of the retention times and retention factors of samples and a mixture of standards. The content of ginsenoside Rf was used as a marker to differentiate Panax ginseng C. A. Meyer from other species. Ginsenosides were detected only in 8 from 11 preparations. There was also significant product-to-product variability in concentrations and proportions of ginsenosides. The content of ginsenosides was also compared with available data from manufacturer and the measured concentrations of marker compounds differed...
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Metabolic Profile of Panax ginseng Bioactive Substance in Plant Material of Varies Origin.
Bacílková, Anna ; Havlík, Jaroslav (referee) ; Klusoňová, Hana (advisor)
Author: Anna Bacílková Title: Metabolic profiles of bioactive components of Panax ginseng C. A. Meyer from different herbal sources Diploma thesis Publishing place: Charles University in Prague, Faculty of Pharmacy in Hradec Králové The field of study - pharmacy In this diploma thesis, I was concerned with the determination and quantification of 12 ginsenosides in 11 commercial ginseng preparations from the species Panax ginseng C. A. Meyer available in the Czech Republic. Ginsenosides are triterpenes saponins considered to be main bioactive principles of ginseng. The two-dimensional thin layer chromatography and high performance liquid chromatography with UV detection was used for the identification and quantitative determination of these compounds. The methods applied are based on comparison of the retention times and retention factors of samples and a mixture of standards. The content of ginsenoside Rf was used as a marker to differentiate Panax ginseng C. A. Meyer from other species. Ginsenosides were detected only in 8 from 11 preparations. There was also significant product-to-product variability in concentrations and proportions of ginsenosides. The content of ginsenosides was also compared with available data from manufacturer and the measured concentrations of marker compounds differed...
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Microbiota of the digestive tract of bees and related insect and the influencing facftors
Hroncová, Zuzana ; Havlík, Jaroslav (advisor) ; Kalous, Lukáš (referee)
This thesis consists of six research chapters, out of which, five have already been published in research journals, 1 is in the process of submission and the last chapter presents original unpublished confidential data in the process of manuscript preparation.
The research presented in this thesis concerns the complex mechanisms of bees and wasps immune system focused on microbiota as component of immunity. As shown in the introduction, highly social and managed species of bees like honey bees and bumble bees, play key roles in natural and agricultural ecosystems worldwide. Recent losses of bees have been attributed to pesticide exposure, poor nutrition, increased parasite loads and habitat degradation. Over the past several years, governments, beekeepers, and the general public worldwide have become concerned by increased losses of honey bee colonies, calling for more research on how to keep colonies healthy. Our main aim was to explore the complex mechanisms of bees and related species gut bacterial populations, their links to insect immunity and investigate the opportunities for an intervention. Part of our aim was to characterise the bumble bee and wasp gut microbiota using 16S RNA sequencing in a search for potentially novel bacterial species.
We have tried to explain how microbiome interacts with the host and showed that major members of these communities appear to benefit the host. The simple gut communities of social bees present ideal model systems to investigate the underlying evolutionary and genetic processes of such interactions. Information based on our results may help in the design of proper probiotic supplementation strategies with respect to physiological conditions in the honey bee gut.
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Antioxidant, anti-proliferative and immunomodulatory effect of fruits, vegetables and mushrooms in vitro
Doskočil, Ivo ; Havlík, Jaroslav (advisor) ; Orsák, Matyáš (referee)
Recently there has been an increasing interest in discovering of new species of plants and mushrooms which have antioxidant or anti proliferative activity. The interest is caused by the fact that these species have medicinal and food utilization. These properties of plants and mushrooms can be used when dealing with many diseases which may be connected with oxidative stress (inflammatory bowel disease, cardiovascular disease, hypertension, and tumour disease, etc.).
The thesis propounds characteristics of in vitro antioxidant and anti proliferative activity of 19 types of juices and 28 methanol extracts of fruits and vegetables, which are common parts of a diet. In the thesis there are also characteristics of 13 ethanol extracts of edible mushrooms of the order of Polypore (Popyporales). Antioxidant activity was quantifie by 2, 2 diphenyl 1 picrylhydrazyl (DPPH), oxygen radical absorbance capacity (ORAC), and inhibition of nitric oxide (NO) production. Cytotoxicity was measured by MTT (3 (4,5 dimethylthiazol 2 yl) 2,5 diphenyltetrazolium bromide. Immunomodulatory activity was determined by an assay of phagocytic activity of human neutrophil granulocytes. Further a total phenolic content (TPC) and total beta glucan content were investigated; these are considered to be the potentially active constituents participating in mentioned activities.
From the obtained results it is evident that juices (TPC = 1603.2 mg GAE/L; ORAC = 438.5 umol TE/g)
and a bilberry (Vaccinium myrtillus) fruit extract (ORAC 836.6 umol TE/g; DPPH = 404.6 umol TE/g) showed
the highest antioxidant activity of all tested samples of fruits and vegetables. Capsicum (Capsicum L.)
juices (TPC = 642.1 mg GAE/L; ORAC = 127.9 umol TE/g) and a radish (Raphanus sativus L.) extract
(ORAC 724.5 umol TE/g; DPPH = 52.2 umol TE/g) also proved to have the high values of antioxidant activity. From the tested fruits and vegetables the following inhibited to produce a nitric oxide: onion (Allium cepa L) juices (lowered the NO production by 57%), tangerine juices (Citrus reticulata Blanco)(by 52%), broccoli (Brassica oleracea var. botrytis italic) extract (by 21%), and orange (Citrus sinensis Pers.) extract (by 10%). Concerning edible
mushrooms, Lentinus tigrinus (Bull.) Fr. (TPC = 216.2 umol GAE/g of extract), Ganoderma lucidum (Curtis) P. Kras (TPC = 257.9 umol GAE/g of extract), and Royoporus badius (Pers.) A.B. De (TPC = 257.8 umol GAE/g of extract) presented the highest phenolic content. Sparassis crispa (Wulfen) Fr. (117.4 mg/g of extract) had the highest content of beta glucan. Substantial effect on phagocytic activity of granulocytes was noticed in connection with Neolentinus lepideus (Fr.) Redhead & Ginns, Polyporus squamosus (Huds.) Fr., and S. crispa. In connection with the latter of mentioned mushrooms, a moderate inhibitory effect towards HT 29 human colorectal adenocarcinoma cell line
(IC50 = 107 ug/ml of extract) was noticed.
The results indicate that the tested plants and mushrooms can be beneficial when reducing the negative effects of oxidative stress. The oxidative stress has been recognized as a contributing factor to a whole range of diseases and the reduction of the oxidative stress may lead to the decrease in the possibility of the diseases´ progression. The results show the possible favourable effects on the human health. When evaluating the results, the following fact should be taken into consideration; the in vitro tests and screenings are considered to be the first phase of systematic research of the effects and serve for the choice of respondents for further detailed studies.
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Comparison of HPLC a GC-MS method for pesticide determination in soil
Chalbia Václavíková, Alena ; Kočárek, Martin (advisor) ; Havlík, Jaroslav (referee)
Physical and chemical properties of pesticides may vary significantly. Pesticides can be acidic, neutral or alkaline. Some compounds containing phosphorus, other sulfur, nitrogen or halogens. These atoms can be important for the detection of pesticides. Some of the compounds are volatile, others on the contrary not evaporate, which is also one of the important properties for chromatography. The diversity of pesticides actually makes it impossible to create a universal method, which is very impractical in terms of quality and time determination. Because that pesticides are one of the most chemicals in most countries. In the food and drinking water are limits on pesticides in order to avoid negative impact on public health. For residues in soil or surface water limits are set. (Lutz et al., 2006)
The objective of this thesis is to evaluate the possibility of using two types of chromatographs with different detectors for the analysis of pesticide. Pendimethalin which was chosen for this work, will be analyzed usinga liquid chromatograph with UV detektor and gas chromatography with mass detector. Both this method will be compared as well two extraction methods (Soxhlet extraction and shaking), and two extraction agents (methanol and acetonitrile).
Another point of the work is to provethe hypothesis that, for the determination of pendimethalin in soil is by gas chromatography using a mass spectrometer in comparison with the high performance liquid chromatography time and more expensive, but will achieve a higher yield and a lower detection limit of the pesticide.
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Cell culture-based model for the evaluation of adhesive properties of probiotic bacteria
Theodorou, Vasiliki ; Havlík, Jaroslav (advisor) ; Tauchen, Jan (referee)
Probiotic microorganisms, defined as living microorganisms which when administered in adequate amounts confer a health benefit to the host, and their adhesion and colonization of intestinal epithelium, are critical factors in maintaining probiotic efficacy. Polyphenols are a large and heterogeneous group of phytochemicals in plant-based foods, such as tea, coffee, wine, cocoa, cereal grains, soy, fruits and berries. In the last decade, there has been much interest in the health benefits of dietary plant polyphenols that arise from their potential ability to promote adhesion of probiotic bacteria to the human intestinal epithelium.
The purpose of this study was to investigate the effect of four polyphenols: isoquercetrin, phloretin, procyanidin B2 and rutin on the adhesion ability of two potentially probiotic strains (Lactobacillus casei, Lactobacillus gasseri) to in vitro human intestinal epithelial model consisting of Caco-2 and mucus-secreting HT29-MTX co-culture.
The adhesion of Lactobacillus casei after treating the co-culture cell lines with isoquercetrin, phloretin, and rutin was increased by 49.76, 72.97, 63.66 % respectively, whereas procyanidin B2 inhibited the adhesion 20.25% compared with the control sample. The adhesion of Lactobacillus gasseri after treatment of the co-culture with isoquercetrin, phloretin, procyanidin B2 and rutin was increased by 35.45, 31.28, 45.69, 25.01 % respectively compared with the control sample.
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In vitro anti-proliferation activity alkaloids the Amaryllidaceae
Panenková, Kristýna ; Havlík, Jaroslav (advisor) ; Jarošová, Veronika (referee)
Summary
Natural phytochemicals are currently used in the treatment of many diseases. Cancers are just ones of them and they are ranked among the most common and the most serious. Phytochemicals in the form of cytostatics are used in chemotherapeutic treatment of cancer. In future there could be included among cytostatics also some alkaloids from the family
of Amaryllidaceae, whose testing for a selective cytostatic effect on tumor cell lines
of colorectal carcinoma Caco-2 and HT-29 and on normal cell lines of human intestinal epithelial FHs 74 Int is a subject of this thesis.
There were tested 17 alkaloids isolated from plants of Chlidanthusfragrans, Zephyranthes robusta and Nerine bowdenii. Particularly alkaloids from plant Zephyranthes robusta namely haemanthamine with this values: IC50 = 0.99 plus/minus 0.14 microM for tumor cells, Caco-2, 0.59 plus/minus 0.01 microM for tumor cells HT-29 and 19.47 plus/minus 8.86 microM for normal cells
FHs 74 Int, Lycorine with values IC50 = 0.99 plus/minus 0.08 microM for tumor cells Caco-2, 1.2 plus/minus 0.01 microM for tumor cells HT-29 and 22.68 plus/minus 0.09 microM for normal cells FHs 74 Int and Haemanthidin with values IC50 = 3.29 plus/minus 0.91 microM to tumor cells Caco-2, 1.72 plus/minus 0.11 microM to tumor cells HT-29, and 11.63 plus/minus 0.86 microM for normal cells FHs 74 Int proved a significant
anti-proliferative activity.
From these results there is evident the selectivity against colorectal cancer cell lines. For this reason, those tested alkaloids are suitable for further testing and for study of their biological activity against tumor cells in the terms of in vitro and in vivo.
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Comparison of school catering policies in the Czech Republic and other european countries
Lídlová, Barbora ; Havlík, Jaroslav (advisor) ; Anna, Anna (referee)
The school lunch provides an important opportunity for learning healthy habits, and well-balanced school meals have been linked to improved concentration in class, better educational outcomes and fewer sick days. School lunches are diverse across Europe. Many countries in Europe have policies to help schools provide nutritionally balanced meals which also reflect the general eating culture of each nation. The most advanced systems of school meals include those in Finland and Sweden, where all school meals are fully funded by the government. In 2014 first children between the ages of five and seven received a free school lunch in The United Kingdom. In England, school meals have increased their level due to the fact that renowned chef Jamie Oliver noticed how poor quality school meals had. The Jamie Oliver Food Foundation was founded in 2002 and run three core food education programmes in schools. Recently, a very interesting topic is organic food in school meals, and less use of convenient food. Italy has become a pioneer in Europe to use organic and local products in school meals. 40 % of their served food has an organic origin. Across France are all vending machines banned from school since 2005. Countries which do not have compulsory system of school catering services are e.g. Norway, Netherlands and Belgium. Czech school meals are one of the best in Europe. And not just in terms of a comprehensive system of school lunches, but also by the availability of full hot school lunches of high quality for all children. School canteens in Czech Republic based their nutrient ration on recommended daily nutrients intake, which provide daily need of essential nutrients and vitamins. These daily intakes are part of Decree 107 of 2005. In these days, in Czech Republic is discussed question of the ban on vending machines. And in February 2015, it has been decreed to ban the sale of unhealthy snacks and beverages in Czech schools approved by the Chamber of Deputies of the Parliament of the Czech Republic.
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