Synthesis and interaction of secondary N-nitrosamines with acetylcholinesterase
- Authors: Mmutle, Tsietso Bernard
- Date: 1991
- Subjects: Chemistry, Physical and theoretical , Enzyme kinetics
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:4058 , http://hdl.handle.net/10962/d1004119 , Chemistry, Physical and theoretical , Enzyme kinetics
- Description: Secondary N-nitrosamines: diphenylnitrosamine (DPhNA), dimethylnitrosamine (DMNA), diethylnitrosamine (DENA), dipropylnitrosamine (DPNA), dibutylnitrosamine (DBNA), diethanolnitrosamine (DEtNA), methylnitrosoglycine (MNGly), nitrosopyrrolidine (NPyr), nitrosomorpholine (NMor) and nitrosopiperidine (NPip) were synthesised and their interaction with acetylcholinesterase (AChE) was investigated. Analyses of kinetic results show that DMNA (Ki=34.78 μM); DENA (Ki=54.24 μM); DPNA(Ki=60.36 μM); DBNA(Ki=95.54 μM); DEtNA(Ki=43.68 μM)MNGly (Ki=30.18 μM); NPip (Ki=123 μM); NPyr (Ki=66.07 μM), NMor (Ki=73.93 μM) and DPhNA (Ki=20.32 μM) are competitive and reversible inhibitors of acetylcholinesterase, with respect to the substrate, acetylthiocholine chloride, ATChCl. With time they act as irreversible covalent inhibitors with dipropy1nitrosamine producing 72% inactivation after 60 minutes. Scatchard analyses of f1uorometric titrations, (Kd=0.75mM-4.09mM); gel chromatography (Kd=O. 80mM-4. 60mM) and equilibrium dia1ysis (Kd=O. 71mM- 4.21mM) for MNG1y, DMNA, DEtNA, DENA, DPNA, NPyr, DSNA, NMor and NPip show that these compounds have weaker affinity for the enzyme, as compared to the much tightly binding aromatic DPhNA, Kd values (0.65mM, 0.68mM and 0.68mM) for fluorometric experiments, gel chromatography and equilibrium dialysis respectively. In all cases, the number of binding sites of acetylcholinesterase averaged to four.
- Full Text:
- Date Issued: 1991
- Authors: Mmutle, Tsietso Bernard
- Date: 1991
- Subjects: Chemistry, Physical and theoretical , Enzyme kinetics
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:4058 , http://hdl.handle.net/10962/d1004119 , Chemistry, Physical and theoretical , Enzyme kinetics
- Description: Secondary N-nitrosamines: diphenylnitrosamine (DPhNA), dimethylnitrosamine (DMNA), diethylnitrosamine (DENA), dipropylnitrosamine (DPNA), dibutylnitrosamine (DBNA), diethanolnitrosamine (DEtNA), methylnitrosoglycine (MNGly), nitrosopyrrolidine (NPyr), nitrosomorpholine (NMor) and nitrosopiperidine (NPip) were synthesised and their interaction with acetylcholinesterase (AChE) was investigated. Analyses of kinetic results show that DMNA (Ki=34.78 μM); DENA (Ki=54.24 μM); DPNA(Ki=60.36 μM); DBNA(Ki=95.54 μM); DEtNA(Ki=43.68 μM)MNGly (Ki=30.18 μM); NPip (Ki=123 μM); NPyr (Ki=66.07 μM), NMor (Ki=73.93 μM) and DPhNA (Ki=20.32 μM) are competitive and reversible inhibitors of acetylcholinesterase, with respect to the substrate, acetylthiocholine chloride, ATChCl. With time they act as irreversible covalent inhibitors with dipropy1nitrosamine producing 72% inactivation after 60 minutes. Scatchard analyses of f1uorometric titrations, (Kd=0.75mM-4.09mM); gel chromatography (Kd=O. 80mM-4. 60mM) and equilibrium dia1ysis (Kd=O. 71mM- 4.21mM) for MNG1y, DMNA, DEtNA, DENA, DPNA, NPyr, DSNA, NMor and NPip show that these compounds have weaker affinity for the enzyme, as compared to the much tightly binding aromatic DPhNA, Kd values (0.65mM, 0.68mM and 0.68mM) for fluorometric experiments, gel chromatography and equilibrium dialysis respectively. In all cases, the number of binding sites of acetylcholinesterase averaged to four.
- Full Text:
- Date Issued: 1991
Chemistry and the white knight : inaugural lecture delivered at Rhodes University
- Authors: Letcher, T.M.
- Date: 1981
- Subjects: Chemistry, Physical and theoretical
- Language: English
- Type: Text
- Identifier: vital:647 , http://hdl.handle.net/10962/d1020716 , ISBN 0868100749
- Description: Inaugural lecture delivered at Rhodes University , Rhodes University Libraries (Digitisation)
- Full Text:
- Date Issued: 1981
- Authors: Letcher, T.M.
- Date: 1981
- Subjects: Chemistry, Physical and theoretical
- Language: English
- Type: Text
- Identifier: vital:647 , http://hdl.handle.net/10962/d1020716 , ISBN 0868100749
- Description: Inaugural lecture delivered at Rhodes University , Rhodes University Libraries (Digitisation)
- Full Text:
- Date Issued: 1981
A study of the properties and methods of analysis of high molecular weight N-nitrosamines
- Authors: Kelly, Felix Thomas
- Date: 1974 , 2013-10-29
- Subjects: Nitrosoamines , Chemistry, Physical and theoretical
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:4421 , http://hdl.handle.net/10962/d1006878 , Nitrosoamines , Chemistry, Physical and theoretical
- Description: Various high molecular weight dialkylnitrosamines were prepared including, for the first time, methyl-n-octadecylnitrosamine and di-n-dodecylnitrosamine. The infrared, ultraviolet and mass spectra of a selection of these compounds were recorded and studied. Gel permeation chromatography was used for the isolation of individual nitrosamines in standard nitrosamine mixtures, while ion-exchange chromatography effected complete clean-up of amine-contaminated nitrosamine solutions. Thin-layer and gas-liquid chromatographic methods were developed for the detection, separation and analysis of nanogram quantities of these lipophilic nitrosamines. In addition the above chromatographic systems were used for the analysis of distillates of spiked wheat flour samples. High recoveries of dicyclopentylnitrosamine, di-n-heptylnitrosamine and di-n-octylnitrosamine, from the spiked wheat flour samples, were achieved using a specially developed freeze-drying/vacuum distillation technique, the distillates obtained being relatively free from major contaminants. , KMBT_363 , Adobe Acrobat 9.54 Paper Capture Plug-in
- Full Text:
- Date Issued: 1974
- Authors: Kelly, Felix Thomas
- Date: 1974 , 2013-10-29
- Subjects: Nitrosoamines , Chemistry, Physical and theoretical
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:4421 , http://hdl.handle.net/10962/d1006878 , Nitrosoamines , Chemistry, Physical and theoretical
- Description: Various high molecular weight dialkylnitrosamines were prepared including, for the first time, methyl-n-octadecylnitrosamine and di-n-dodecylnitrosamine. The infrared, ultraviolet and mass spectra of a selection of these compounds were recorded and studied. Gel permeation chromatography was used for the isolation of individual nitrosamines in standard nitrosamine mixtures, while ion-exchange chromatography effected complete clean-up of amine-contaminated nitrosamine solutions. Thin-layer and gas-liquid chromatographic methods were developed for the detection, separation and analysis of nanogram quantities of these lipophilic nitrosamines. In addition the above chromatographic systems were used for the analysis of distillates of spiked wheat flour samples. High recoveries of dicyclopentylnitrosamine, di-n-heptylnitrosamine and di-n-octylnitrosamine, from the spiked wheat flour samples, were achieved using a specially developed freeze-drying/vacuum distillation technique, the distillates obtained being relatively free from major contaminants. , KMBT_363 , Adobe Acrobat 9.54 Paper Capture Plug-in
- Full Text:
- Date Issued: 1974
The solubility of barium sulphate in water at 25°
- Authors: Rosseinsky, D R
- Date: 1957
- Subjects: Chemistry, Physical and theoretical , Solubility , Barium sulfate
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:4491 , http://hdl.handle.net/10962/d1013097
- Description: Barium sulphate is a widely used analytical precipitate and for this reason its properties have been extensively studied. The variety of results encountered with barium sulphate samples prepared by different methods is an indication of the complex nature of this interesting substance. Intro., p. 8.
- Full Text:
- Date Issued: 1957
- Authors: Rosseinsky, D R
- Date: 1957
- Subjects: Chemistry, Physical and theoretical , Solubility , Barium sulfate
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:4491 , http://hdl.handle.net/10962/d1013097
- Description: Barium sulphate is a widely used analytical precipitate and for this reason its properties have been extensively studied. The variety of results encountered with barium sulphate samples prepared by different methods is an indication of the complex nature of this interesting substance. Intro., p. 8.
- Full Text:
- Date Issued: 1957
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