|
Biological activity of plant metabolites. XIV. Influence of alkaloids from Chelidonium majus L.on acetylcholinesterase
Kubincová, Dagmar ; Opletal, Lubomír (advisor) ; Karlíčková, Jana (referee)
Kubincová, D.: Biological activity of plant metabolites XIV; Influence of alkaloids from Chelidonium majus L. on acetylcholinesterase. Rigorous work, Charles University in Prague, Faculty of Pharmacy Hradec Králové, 74 pp. Key words: Alzheimer's disease, alkaloids, Chelidonium majus, acetylcholinesterase, biological aktivity. Within the screening of plants that contain alkaloids inhibiting the activity of the human erythrocytic acetylcholinesterase Greater celadine (Chelidonium majus L., Papaveraceae) was studied. 41.8 kg of the whole dry plant (the aerial part with the roots) served for the isolation of alkaloids. Mixtures of pseudocyanides of benzophenanthridine alkaloids, phenolic bases, and the alkaloids precipitated from either chloroform-soluble or chloroform-insoluble chlorides were obtained from the purified ethanolic extract. My task was to separate bases from the chlorides insoluble in chloroform. Using both column and thin layer chromatography protopine as a base was isolated. The identity of the isolated alkaloid was determined by means of an authentic standard and by comparing its physico-chemical characteristics with the published data. The isolated compound inhibited the human erythrocytic acetylcholinesterase with IC50 1,12.10-3 M. Comparing its biological activity with that of...
|
|
Chemical constituents of stems and leaves of Vaccinium myrtillus
Hybelbauerová, Simona
Bilberry (Vaccinium myrtillus L., Ericaceae), also known as European blueberry, has a long history in European folk medicine of being widely used in the form of fruits, tinctures, teas and other herbal formulas for the treatment of diarrhoea, circulatory diseases, eye conditions, inflammation and diabetes. Unlike the berry's fruits, the other vegetative organs have attracted much less attention. This PhD thesis was interested in stemps and leaves of Vaccinium myrtillus. Successive fractionation of the MeOH extract of Vaccinium myrtillus stems and leaves furnished 20 isolated compounds, including two new 2,4-pentanediol coumarates, (E)-(2S,4R)-4- (-D-glucopyranosyloxy)-pent-2-yl-p-coumarate 1 and its aglycone 2, new triterpenoid 3,12- dihydroxyolean-28→13-olid 3 and 17 known compounds: 2,4- pentanediol glucoside, -amyrin, -amyrin, oleanolic acid, ursolic acid, glutinol, - sitosterol, - sitosterolglucoside- tocoferol, methyl--D-fructofuranoside, methyl--D-fructofuranoside, methyl--D-fructopyranoside, saccharose, 2-deoxy-D-ribono-1,4-lactone, myo-inositol, quercetin and monotropein, whose structures were elucidated by comparing their physical and NMR data with those reported in the literature. 1 2 3
|
|
Biological Active Plant Metabolites I. Alkaloids of Corydalis cava (L.) Schweigg. & Körte (Fumariaceae) and Screening of Their Biological Properties
Sekula, Marek ; Jahodář, Luděk (referee) ; Cahlíková, Lucie (advisor)
Sekula, M.: Biological Active Plant Metabolites I. Alkaloids of Corydalis cava (L.) Schweigg. & Körte (Fumariaceae) and Screening of Their Biological Properties. Rigorous thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2010, 65 p. Within the screening of plants that contains alkaloids inhibiting the activity of the human erythtocytic acetylcholinesterase and human serum butyrylcholinesterase Corydalis cava (L.) Schweigg. & Körte (Fumariaceae) was studied. This work connect to my diploma thesis (2009). The task was to separate mixture of alkaloids from extract "B-chloroform" subfraction F1. This subfraction was prepared within the frame of diploma thesis. From this mixture, using preparative TLC, were isolated two compounds F1-1A and F1-1C in the form of free bases. On the basis of MS, NMR and IR spektroskopy the isolated alkaloid F1-1A was identified as 3-(1-(6,7- dimethoxy-3,4-dihydroisoquinolin-1-yl)ethyl)-2,6-dimethoxy-phenol. It is the first isolation and description of this compound. Structural analysis of compound F1-1C is continuing. The isolated compound F1-1A inhibited the human erythrocyte acetylcholinesterase and human blood serum butyrylcholinesterase with IC50 for AChE (127,6×10-6 M) and with...
|
|
Biological activity of plant metabolites XI. Alkaloids of Corydalis cava (L.) Schweigg & Körte (Fumariaceae) and their influence on acetylcholinesterase
Sekula, Marek ; Cahlíková, Lucie (referee) ; Opletal, Lubomír (advisor)
Sekula, M.: Biological activity of plant metabolites XI.; Alkaloids of Corydalis cava (L.) Schweigg. & Körte (Fumariaceae) and their activity on acetylcholinesterase. Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2009, 61 p. Within the screening of plants that contains alkaloids inhibiting the aktivity of the human erythtocytic acetylcholinesterase and human serum butyrylcholinesterase Turkey Corn (Corydalis cava (L.) Schweigg. & Körte, Fumariaceae) was studied. 11,3 kg of the dry roots served for the isolation of alkaloids. Extrakt "B-chloroform" wich contain mixture of terciary alkaloids bad diethylether-insoluble were obtained from the purified ethanolic extract. The task was to separate mixture of alkaloids from extrakt "B-chloroform". Using both column and thin layer chromatography sinoacutine as a base was isolated. The identity of the isolated alkaloid as determined by means of comparing its physico-chemical characteristics with the published data. The isolated sinoacutine inhibited the human erythrocytic acetylcholinesterase and human serum butyrylcholinesterase with IC50 for AChE (1,510 × 10-3 M) and with IC50 for BuChE (1,806 × 10-3 M). Comparing its biological aktivity with that of...
|
|
Biological activity of plant metabolites X. Alkaloids of Corydalis cava (L.) Schweigg & Körte (Fumariaceae) and their influence on acetylcholinesterase
Průša, Jan ; Cahlíková, Lucie (referee) ; Opletal, Lubomír (advisor)
Průša, J.: Biological aktivity of plant metabolites XI.;Alkaloids of Corydalis cava (L.) Schweigg. & Körte (Fumariaceae) and their activity on acetylcholinesterase and butyrylcholinesterase. Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2009, 52 pages. Within the screening of plants that contains alkaloids inhibiting activity of the human erythrocytic acetylcholinesterase Corydalis cava (L.) Schweigg. & Körte, (Fumariaceae) was studied. 11,8kg of the roots served for the isolation of alkaloids. Mixtures of various structurally types of isochinolic alkaloids were obtained from the purified ethanolic extrakt. My task was to separate alkaloids of the B extract in chloroform (68,6 g). Using both column chromatography and crystallization 8-trichloromethyl-7,8-dihydropalmatin was isolated. The 8-trichloromethyl-7,8-dihydropalmatin is an artefact of palmatin rising during extraction by chlorinated solvents (with help of 1 H-NMR, ESI-MS and comparing its physico- chemical characteristics with the published data). The isolated compound inhibited the human erythrotic acetylcholinesterase with IC50 = 0,08292 mM and butyrylcholinesterase IC50 > 0,745 mM. Comparing its biological activity with the standard of...
|
|
Biological effect of plant metabolites II. Isolation of alkaloids from Eschscholzia californica Cham.
Linzerová, Michaela ; Karlíčková, Jana (advisor) ; Macáková, Kateřina (referee)
Linzerová, M.: A Biological Effect of Plant Metabolits II. The Isolation of Alkaloids from Eschscholzia californica Cham. A diploma work, Charles University in Praque, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2009, 66 pages Extract J1 from plant Eschscholzia californica Cham. was separated. The separation was performed on a chromatografic column filled by silica gel, mixture of chloroform-ethanol 100+0 to 45+55 was chosen as eluent. For detection was taken thin-layer chromatography. A polar mixture of ethanol-acetic acid-water (60+30+10) was chosen as eleunt mixture. Detection was evaluated by UV radiation and spray of Dragendorff reagent. The fractions containing the highest concentracion of alkaloids were coupled and purified. Two different alkaloids were obtained. The structures of these alkaloids were found out by NMR method. Keywords: Californian Poppy, Eschscholzia californica, alkaloids, column chromatography, Alzheimer disease, benzophenanthridin alkaloids
|
|
Accumulation and biotransformation of nitramines in plant tissue
Šídlová, Petra ; Skálová, Lenka (advisor) ; Szotáková, Barbora (referee)
Explosives are toxic, recalcitrant to degradation and contaminate large areas of land and ground water. Remediation of these xenobiotics is difficult and an enormous logistical task. Phytoremediation is a technique that offers an environment friendly, low-cost alternative to current remediation techniques. However this approach is hindered by the low metabolic abilities of plants towards these xenobiotic compounds and the phytotoxicity of these compounds. The fate of the explosives RDX (hexahydro-1,3,5-trinitro-1,3,5-triazine) and HMX (octahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine) on exposure to plant was investigated in hydroponic system of sunflower (Heliantus annuus L.) and hemp (Cannabis sativa L.) approximately for more than 10 days. Exposure levels were: 10mg/l and 50mg/l RDX, respectively HMX for sunflower; 25mg/l and 50mg/l RDX , 5mg/l and 50mg/l HMX for hemp. Their ecotoxicites were characterized by the test based on the inhibition of elongation of primary roots 3days-old mustard and hemp seedlings. Extracts of plants were analyzed by HPLC (liquid chromatography). These study showed that RDX and HMX was taken up by both plant species. The accumulation of these nitramines was observed more in the roots than in the aerial parts of the plants, except for RDX in hemp, where the...
|
|
Hard and soft exudates detection in retinal images
Válková, Hana ; Lamoš, Martin (referee) ; Kolář, Radim (advisor)
The thesis deals with automatic detection of soft and hard exudates in retinal images of the human eye. In its introduction the thesis describes the issue of diabetes in relation to the damage to the retina of the eye. What is described in the first place is diabetic retinopathy, its symptoms and progression of the disease. Another section is devoted to describing DIARETDB1, the freely accessible database which besides other things contains a set of images showing various degrees of disease, evaluation of images from the experts and the evaluation protocol. The next section discusses several methods for automatic detection of hard and soft exudates. The practical part of the bachelor’s thesis is aimed at image pre-processing with respect to the normalization of retinal images, the selected method for adaptive transformation of contrast was implemented. This part also containts description of chosen methology of thresholding, feature extraction based on lesions intensity and its surroundings, use of Ho Kashyap classifier is described, classification of lesions in images is followed. In conclusion realized methods is evaluated.
|
|
Isolation and characterisation of biologically active substances
Kettnerová, Eliška ; Nesměrák, Karel (advisor) ; Musilová, Adéla (referee)
This Bachelor thesis aims at isolation and partial identification of biologically active substances which are produced by actinomycetes and can be potentially applied in medicine. Cultivation broths of actinomycetes containing their metabolites were purified and pre-concentrated by solid phase extraction. Then, the bioassay of the extracts by Kirby-Bauer test using the sensitive strain Kocuria rhizophila was performed. Biologically active metabolites were analyzed and isolated by ultra- performance liquid chromatography with photo diode array detector. Isolated substances were assayed by mass spectrometry, which yielded relative molecular mass values of the unknown compounds. The values were compared with relative molecular masses of compounds listed in a chemical database, which involves natural products including antibiotics. We revealed that the unknown biologically active substances do not refer to any already discovered compound present in the database suggesting that the unknown compounds may be novel. More mass spectrometry and nuclear resonance experiments have to be carried out in order to elucidate their structure. Key words: actinomycetes, antibiotics, SPE, UPLC, HPLC Subject heading: analysis of secondary metabolites, bioassay test, isolation of biologically active compounds,...
|
|
Analysis of pigments from integument of Graphosoma semipunctatum.
Krajíček, Jan ; Svobodová, Eva (referee) ; Bosáková, Zuzana (advisor)
Pterines belong to an important group of compounds, acting as pigments in many species. Some of them are probably responsible for characteristic coloration of the insect group (Hereroptera). This coloration is considered to be a visual warning signal for optically orientating predators (birds, lizards etc.). In this work, pterines in the species of Graphosoma semipunctatum have been investigated by high performance liquid chromatography. To develope an appropriate separation method, the reverse-phase separation mode with C18 stationary phase (Spherisorb ODS 2) and binary mobile phase (organic modifier/buffer or water) was used. The effect of type and content of organic modifiers (methanol, ethanol, tetrahydrofuran) and concentration of phosphate buffer pH 3.0 (10 - 30 mM) in the mobile phases on retention and separation behavior of the studied pterines (leukopterin, biopterin, xanthopterin, isoxanthopterin and erythropterin) was studied. Under the optimized separation conditions (5/95 (v/v) methanol/20 mM phosphate buffer, pH 3.0, flow rate 0.7 ml.min-1 , UV detection at 290 nm), the extract from the integument of Graphosoma semipunctatum was analyzed.
|
guest ::
