|
|
Study of biological activity of alkaloids isolated from Fumaria officinalis L. (Fumariaceae) I.
Kostelník, Jan ; Chlebek, Jakub (advisor) ; Cahlíková, Lucie (referee)
Kostelník, J.: Study of biological activity of alkaloids isolated from Fumaria officinalis L. (Fumariaceae) I. Diploma thesis, Charles University in Prague,Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2014, 63 p. The aim of this study was to isolate alkaloids from joined fraction no. 55-67 (A2) obtained from the total alkaloid fraction of extract of Fumaria officinalis L. (Fumariaceae) plant. Using chromatography methods three alkaloids were isolated and then identified by structural analysis (GC-MS, NMR). Three alkaloids were isolated by using common chromagografic methods and then identified by structural analyses optical rotation and melting point as (-)-O- methylfumarophycine, (-)-sinactine a (-)-stylopine. Inhibitory activity of isolated alkaloids was assessed against human erythrocyte acetylcholinesterase, human butyrylcholineesterase and prolyl oligopeptidase. The results were expressed as IC50 values ((-)-stylopine: IC50 AChE and IC50 BuChE > 1000 μM, IC50 POP > 1000 mM; (-)-O-methylfumarophycine: IC50 AChE = 963.10 ± 135.98 µM, IC50 BuChE = 1771.0 ± 380.94 µM, IC50 POP - unmeasured; (-)-sinactine IC50 AChE = 632.0 ± 68.12 µM, IC50 BuChE = 8154.3 ± 981.42 µM, IC50 POP = IC50 POP = 52.9 ± 1.8 µM). None of alkaloids isolated showed...
|
|
|
Study of biological activity of alkaloids isolated from Fumaria officinalis L. (Fumariaceae) II.
Malý, Lukáš ; Chlebek, Jakub (advisor) ; Opletal, Lubomír (referee)
Malý, L.: Study of biological activity of alkaloids isolated from Fumaria officinalis L. (Fumariaceae) II. Diploma Thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2014, 49 pp. Obtained diethylether extract of Fumaria officinalis L. was separated to fractions in column chromatography with petrol, chloroform and ethanol. Preparative TLC and crystalisation led to isolation of five alkaloids from fraction. Alkaloids were identified by GC-MS and NMR specters, optical rotation and melting point as protopine, cryptopine, (-)-fumaricine, (+)-fumariline and (+)-parfumidine. Isolated alkaloids were tested for their inhibition activity towards acetyl- and butyrylcholinesterase and towards prolyloligopeptidase. Activities were compared with standards. Natural inhibitor galanthamine showed IC50 AChE 1.710 ± 0.065 µM, IC50 BuChE 42.30 ± 1.30 µM. Best inhibition activity showed protopine (IC50 AChE 345.4 ± 24 µM, IC50 BuChE 239.6 ± 22.3 µM) and cryptopine (IC50 AChE 477.71 ± 47.33 µM, IC50 BuChE 270.82 ± 39.12 µM). The highest prolyloligopeptidase inhibition activity showed (+)-parfumidine with IC50 POP 99.2 µM, which was more active than used natural inhibitor baicaline (IC50 POP 605.9 ± 0.021 µM). Synthetic POP...
|
|
|
Neurotropic and antioxidative activity of some selected species of monocotyledonous alkaloidal plants in vitro. VIII.
Breiterová, Kateřina ; Cahlíková, Lucie (advisor) ; Ločárek, Miroslav (referee)
Author: Kateřina Breiterová Title: Neurotropic and antioxidative activity of some selected species of monocotyledonous alkaloidal plants in vitro. VIII. Diploma thesis Charles Univerzity in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology 2015, 101 p. More than 50 % cases of dementia are nowadays caused byAlzheimer's disease (AD). AD is a progressive neurodegenerative disease and it causes gradual memory loss, disorientation and behavioral disorders which affect patient's social and occupational life. AD is characteristic by loss of neurons in some regions of brain - for example hippocampus and cortex. Ethiopathogenesis of this disease is not completely known - that is why the treatment is still just symptomatic. Formation of β-amyloid deposits in brain tissue plays an important role - it is a protein which creates extracellular plagues around neurites and causes their degeneration and death. Intracellular tangles are made up of the changed τ-protein. These tangles also cause death of the neuronal cell. The degeneration of neurons is supported by reactive oxygen radicals too. The another problem is a glutamatergic system disorder. This set of excitatory amino acids is important for correct long-term memory formation. Patients with AD suffer from...
|
|
|
Study of biological activity of isolated alkaloids from Argemone grandiflora (Papaveraceae)I.
Adamcová, Markéta ; Chlebek, Jakub (advisor) ; Opletal, Lubomír (referee)
Adamcová, M.: Study of biological activity of alkaloids isolated from Argemone grandiflora (Papaveraceae) I. Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2015. The aim of this study was isolation of substances from total diethyl ether alkaloid extract of Argemone grandiflora Sweet, their identification and assessment of their inhibition activity towards acetylcholinesterase, butyrylcholinesterase and prolyl oligopeptidase. Using common chromatografic methods, four alkaloids were isolated, that was identified as (+)-laudanosine, protopine, (-)-argemonine a (-)-platycerine. These substances was tested for their inhibition activity IC50: (+)-laudanosine (IC50 AChE = 617,00 ± 46,55 μM, IC50 BuChE = 644,77 ± 55,52 μM, IC50 POP = not mesured yet); protopine (IC50 AChE = 229,98 ± 21,02 μM, IC50 BuChE = 208,87 ± 17,67 μM, IC50 POP ˃ 1000 μM); (-)-argemonine (IC50 AChE = 4677,75 ± 1241,08 μM, IC50 BuChE = 885,45 ± 119,50 μM, IC50 POP = 337 ± 83,1 μM); (-)-platycerine (IC50 AChE = 223,65 ± 19,61 μM, IC50 BuChE = 1651,25 ± 327,7 μM, IC50 POP = 687 ± 74 μM). In comparison with the standards galanthamine (IC50 AChE = 1,710 ± 0,065 μM, IC50 BuChE = 42,30 ± 1,30 μM) and huperzine A (IC50 AChE = 0,033 ± 0,001...
|
|
|
Biological aktivity of secondary plants metabolites III. Alkaloids of Narcissus tazetta L.
Panchartková, Markéta ; Ločárek, Miroslav (advisor) ; Opletal, Lubomír (referee)
Panchartková, M.: Biological aktivity of secondary plants metabolites III. Alkaloids of Narcissus tazetta L., Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové, 2015, 67s. Plants from the Amaryllidaceae family contain alkaloids that have multiple biological effects. There is described antiviral, antitumor, antibacterial, antimalarial and anti-fungal effect. Activity against human cholinesterases is important too. The aim of this thesis was to prepare seven alkaloid extracts of individual cultivars of the plants Narcissus and then to realize their GC/MS analysis. Thanks to this analysis, several different structural types of alkaloids from the Amaryllidaceae family were identified. The most frequently identified alkaloids were homolycorine, lycorine, tazettine and galanthamine type. This was followed by the measuring of biological activity against human acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE). The highest inhibitory activity IC50 identified the alkaloidal extract of the Narcissus jonquilla cv. New baby with the values in relation to HuAChE 13,78 ± 1,48 and in relation to HuBuChE 96,12 ± 9,55. The main reason was probably the highest content of galanthamine of all cultivars,...
|
|
|
Biological aktivity of secondary plants metabolites I. Alkaloids of Narcissus jonquilla L.
Nováková, Dana ; Ločárek, Miroslav (advisor) ; Chlebek, Jakub (referee)
Nováková D.: Biological activity of secondary plants metabolites I. Alkaloids of Narcissus jonquilla L. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2015, pp. 70. The aim of the diploma thesis was a preparation of alkaloid extracts to identification of alkaloid patterns and measure cholinesterase inhibitory activity. This activity is useful for treating Alzheimer's disease. Alkaloid extracts of seven Narcissus jonquilla L. (Amaryllidaceae) varieties (Sundial, Sundisc, Sweetness, Waterperry, Simplex, Twinkling Yellow, Yazz) were studied with respect to their acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE) inhibitory activity and alkaloid patterns. Twenty-three alkaloids were determined by GC/MS, and ten of them identified from their mass spectra and retention times. All samples exhibited content of galanthamine, most samples contained lycorine and tazettine. Promising HuAChE inhibition activity was demonstrated by Narcissus jonquilla L. cv. Waterperry with IC50 values of 6.53 ± 0.88 μg/mL. The strongest inhibitory activity against HuBuChE was detected in extract from Narcissus jonquilla L. cv. Sundisc with IC50 value of 5.09 ± 0.64 μg/mL. Keywords: Alzheimer's disease, Amaryllidaceae, Narcissus,...
|
|
|
Biological activity of plant metabolites XXIII. Alkaloids of Corydalis cava (L.) SCHWEIGG. & KÖRTE and their effect on acetylcholinesterase and butyrylcholinesterase.
Kaluzsná, Blanka ; Opletal, Lubomír (advisor) ; Cahlíková, Lucie (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Bc. Blanka Kaluzsná Supervisor: Prof. RNDr. Lubomír Opletal, CSc. Title of Diploma Thesis: Biological activity of plant metabolites XXIII. alkaloids of Corydalis cava (l.) Schweigg. & Körte and their effect on acetylcholinesterase and butyrylcholinesterase An ether extract which contained tertiary basic alkaloids was prepared from the dry bulb of Corydalis cava (L.) SCHWEIGG. & KÖRTE. A subfaction labeled 2/B was obtained by column chromatography and crystallization. Three alkaloids were isolated by preparative TLC and they were identified by GC/MS and 1 H a 13 C NMR analyzes as (+)-canadine, (+)-tetrahydropalmatine and domestine. Isolated alkaloids were tested by spectrophotometric Ellman method for inhibitory activity against human erythrocyte acetylcholinesterase (HuAChE) and plasma butyrylcholinesterase (HuBuChE). In comparison with the refernce substances, from these isolated alkaloids only (+)-canadine showed an relatively high inhibitory activity against HuAChE (12,4 µM). (+)-Tetrahydropalmatine and (+)-domestine had no significant inhibitory activity in this direction, against both HuAChE and HuBuChE. Key words: Corydalis cava, (+)-canadine, (+)-tetrahydropalmatine,...
|
|
|
Magnetic particles as a reversible carrier for enzyme electrodes
Janíček, Zdeněk ; Žeravík,, Jiří (referee) ; Skládal,, Petr (advisor)
Master’s thesis contains information about the enzymes, biosensors, enzyme biosensors and magnetic particles. Cholinesterasa (ChE) is the generally name for the two related enzymes, mutually differing appearance and biological functions. Acetylcholinesterasa (AChE) is necessary for the transmission of nervous excitement. AChE is located at cholinergic synapses, where is the hydrolysis of the neurotransmitter acetylcholine and this termination by the nervous excitement. Butyrylcholinesterasa (BChE) is related to AChE and it is present in serum. Experimental part was focused on electrochemical biosensors with cholinesterase enzyme using magnetic particles for reversible reconstruction layer. Cholinesterase immobilization was carried out on the magnetic particles by covalent binding after glutaraldehyde activated. The measurement of activity take place with acetylthiocholin as a substrate in a flow system, magnetic particles were captured before the platinum electrode and produced by thiocholin is detected amperometric. The aim was to measure inhibition of AChE. Significant inhibition ChE is caused by certain drugs and pesticides based on organophosphates. There was tested by inhibition of AChE pesticide dichlorvos. Emphasis was on finding possible experimental conditions for the creation of the automated procedure to measure the AChE activity, which was based on auto-injector and pumps of Gilson, together with a 735 programme for the definition of the working configuration, preparation of measurement scripts and implementation of application methods.
|
|
|
Arrow poisons, their us in toxicology and medicine
BÁRTOVÁ, Lucie
Abstract The introduction of physiologically and therapeutically effective drugs in anaesthetic treatment has meant a significant change. Their discovery has thus contributed to a minimisation of their negative effects on a living organism. As a result, anaesthesiology has become more controllable and safer. These new drugs translate into more comfort for the patient in the course of anaesthesiology as well as his or her rapid recovery resulting in a shorter period of hospitalisation. The research of new physiologically and therapeutically effective substances is a pre-requisition of a potential higher standard of medical care. Older substances, e.g. Alkuronium and Gallamin, which, due to their undesirable effects, have come out of use, have lost their significance. Nowadays, these substances have been generally replaced by substances with an intermedial effect, e.g. Rokuronium and Cisatrakurium, which, compared with Alkuronium and Gallamin, show a minimum of undesirable effects. One of the foremost objectives of the current pharmaceutical research is to find a replacement of Sukcinylcholin, which, in spite of its known side effects, has had a non-substitutable position in urgent intubation. As a result, its use is limited to out-patient application and a certain selection of patient categories. Let us hope that we shall see a replacement of Sukcinylcholin being introduced in treatment in the near future. This would mean a final solution of problems arising from its side effects limiting its scope of application.
|
|
|
Isolation and chromosomal localization of acetylcholinesterase genes in the codling moth, \kur{Cydia pomonella}
SÝKOROVÁ, Miroslava
The codling moth, Cydia pomonella (Lepidoptera; Tortricoidea) is a major pest of pome fruitand walnut orchards in the world. Due to the intensive chemical control C. pomonella has developed a high resistance to various insecticides. One of the mechanisms of the resistance is acetylcholinesterase insensitivity to carbamates and organophosphates. The insensitivity is based on mutations in one of two genes for acetylcholinesterase. This study deals with testing a hypothesis suggesting that one gene coding for acetylcholinesterase in the codling moth was translocated to the Z sex chromosome. The hypothesis has been latersupported by sex-linked inheritance of insecticide resistance in a related species, Grapholita molesta, and also by a large size of sex hromosomes in the codling moth.
|
guest ::
