subject:(Monoamine Oxidase Inhibitors)

University of the Western Cape

1. Foka, Germaine Boulenoue. Synthesis and evaluation of novel coumarin-donepezil derivatives as dual acting monoamine oxidase B and cholinesterase in Alzheimer's disease .

Degree: 2016, University of the Western Cape

URL: http://hdl.handle.net/11394/5549

► Alzheimer's disease is a progressive neurodegenerative disease characterised by low acetylcholine (ACh) levels in the hippocampus and cortex of the brain, causing symptoms like progressive… (more)

▼ Alzheimer's disease is a progressive neurodegenerative disease characterised by low acetylcholine (ACh) levels in the hippocampus and cortex of the brain, causing symptoms like progressive memory loss, decline in language skills and other cognitive impairments to occur. The hallmarks of AD include the presence of extracellular insoluble amyloid beta plaques, intracellular neurofibrillary tangles, and the decrease in ACh concentration. The pathophysiology of AD is not well understood, however, acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and monoamine oxidases (MAO) are conspicuous role players in AD pathogenesis. Based on the cholinergic hypothesis, the AChE inhibitor donepezil was developed and has been used effectively clinically in the management of AD, with minimal side effects. Studies regarding the binding interactions of donepezil with AChE has shown that the benzyl-piperidine moiety of this compound shows substantial binding interactions at the CAS site of AChE where it blocks AChE activity. Coumarin is a compound of natural source that has shown some MAO inhibitory activity. Further studies done to clarify the potential of coumarin as a drug against AD has shown that coumarin has the capacity to bind at the PAS site of AChE, thus giving it the potential to prevent AChE induced amyloid plaque formation. Due to the multifactorial nature of AD, the drugs in the market show limited therapeutic benefits and are mainly for symptomatic relief. In order to address this limitation in AD treatment, researchers are exploring the possibility of designing a multi-target-directed-ligand (MTDL). The aim of this study was to synthesise a series of compounds out of pharmacophoric groups of donepezil and coumarin that will be able to inhibit both cholinesterases and MAO B. Four series of 5 compounds per series were synthesised. The first series of compounds consisted of the coumarin moiety to which a 1,4-dibromo benzene moiety was attached. The second series represented the coumarin moiety to which a piperidine (donepezil moiety shown to confer cholinesterase inhibitory property) was attached. The third series represented the coumarin moiety to which bromobenzyl-piperazine was attached and in the last series were compounds similar in structure to series 1 with an unsubstituted benzyl moiety as opposed to the dibromobenzyl moiety. Prior to the synthesis, molecular modelling was conducted in order to have an idea of the binding capacity of the compounds to MAO A and B and cholinesterases. In vitro biological evaluation of the compounds was done and used to determine the IC₅₀ values of the compounds. Nineteen compounds were synthesised and purified successfully as shown by their NMR, MS and IR spectra. The compounds to which dual inhibitory activity was conferred were those in series 2 and 3, of which series 2 showed the best overall inhibitory activity with IC₅₀ values within the low μM range. The compound with the best overall activity was Cp 9. Molecular modelling of Cp 9 showed that the coumarin core was… Advisors/Committee Members: Joubert, J (advisor), Malan, S. F (advisor), Kapp, E (advisor).

Subjects/Keywords: Alzheimer's disease; Acetylcholinesterase; Butyrylcholinesterase; Monoamine oxidase; Monoamine oxidase inhibitors

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APA (6^th Edition):

Foka, G. B. (2016). Synthesis and evaluation of novel coumarin-donepezil derivatives as dual acting monoamine oxidase B and cholinesterase in Alzheimer's disease . (Thesis). University of the Western Cape. Retrieved from http://hdl.handle.net/11394/5549

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Foka, Germaine Boulenoue. “Synthesis and evaluation of novel coumarin-donepezil derivatives as dual acting monoamine oxidase B and cholinesterase in Alzheimer's disease .” 2016. Thesis, University of the Western Cape. Accessed March 07, 2021. http://hdl.handle.net/11394/5549.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Foka, Germaine Boulenoue. “Synthesis and evaluation of novel coumarin-donepezil derivatives as dual acting monoamine oxidase B and cholinesterase in Alzheimer's disease .” 2016. Web. 07 Mar 2021.

Vancouver:

Foka GB. Synthesis and evaluation of novel coumarin-donepezil derivatives as dual acting monoamine oxidase B and cholinesterase in Alzheimer's disease . [Internet] [Thesis]. University of the Western Cape; 2016. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/11394/5549.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Foka GB. Synthesis and evaluation of novel coumarin-donepezil derivatives as dual acting monoamine oxidase B and cholinesterase in Alzheimer's disease . [Thesis]. University of the Western Cape; 2016. Available from: http://hdl.handle.net/11394/5549

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

North-West University

2. Mpitimpiti, Annah Nyasha. Synthesis and evaluation of chromone derivatives as inhibitors of monoamine oxidase / Annah Nyasha Mpitimpiti .

Degree: 2014, North-West University

URL: http://hdl.handle.net/10394/15449

► BACKGROUND AND RATIONALE Parkinson’s disease (PD) is a chronic, progressive neurodegenerative disorder affecting the central nervous system, primarily, the substantia nigra. It is characterized by… (more)

▼ BACKGROUND AND RATIONALE Parkinson’s disease (PD) is a chronic, progressive neurodegenerative disorder affecting the central nervous system, primarily, the substantia nigra. It is characterized by loss of dopaminergic neurons in the nigro-striatal pathway, and ultimately patients with Parkinson’s disease may lose up to 80% of their dopamine-producing cells in the brain. Symptoms include bradykinesia, muscle rigidity, resting tremor and impaired postural balance. Symptomatic relief is obtained by using levodopa and various adjunct therapy including dopamine agonists, catechol-O-methyltransferase inhibitors and monoamine oxidase B inhibitors. Levodopa is used as the gold-standard for treatment of this disease. It effectively controls motor symptoms, however, motor complications that impair the quality of life develop with continued levodopa use. No treatments currently available can halt disease progression, therefore novel drugs that can slow down or stop disease progression are urgently required. The monoamine oxidase (MAO) A and B enzymes are flavoenzymes that play an important role in the oxidative degradation of amine neurotransmitters such as dopamine, serotonin and epinephrine. Early attempts to block dopamine metabolism in the brain using nonselective MAO inhibitors was effective but led to side effects such as hypertensive crisis, thus they lost favor. The MAO-B enzyme is of particular importance in Parkinson’s disease because it is more active than MAO-A in the basal ganglia, and is thus primarily responsible for the catabolism of dopamine in the brain. Selegiline and rasagiline, both irreversible, selective MAO-B inhibitors have proven efficacy in symptomatic treatment of Parkinson’s disease, but due to the irreversible nature of their binding, it can take several weeks after treatment termination for the enzyme to recover. Use of reversible inhibitors such as lazabemide and safinamide do not have this disadvantage, and have safer side effect profiles. Unfortunately, clinical trials for lazabemide use in Parkinson’s disease have been discontinued. Therefore, due to the lack of disease modifying agents for Parkinson’s disease, as well as safety concerns of current PD therapy, an urgent need exists for novel, safe and efficient MAO inhibitors. Current research is thus aimed at designing selective or non-selective reversible inhibitors that bind competitively to the enzyme. The MAO inhibitory potential of chromone derivatives has been illustrated previously. Evaluation of C6- and C7-alkyloxy substituted chromones, for example revealed that these compounds were potent, selective and reversible MAO-B inhibitors. It has further been shown that chromone 3-carboxylic acid is a potent selective, irreversible MAO-B inhibitor. Phenylcarboxamide substitution in position 3 of chromone 3-carboxylic acid also results in potent, selective MAO-B inhibitory activity. Therefore, further evaluation of the effect of substitution with flexible side chains in the 3-position to evaluate MAO-B…

Subjects/Keywords: Chromones; Monoamine oxidase inhibitors; Parkinson’s disease

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Mpitimpiti, A. N. (2014). Synthesis and evaluation of chromone derivatives as inhibitors of monoamine oxidase / Annah Nyasha Mpitimpiti . (Thesis). North-West University. Retrieved from http://hdl.handle.net/10394/15449

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Mpitimpiti, Annah Nyasha. “Synthesis and evaluation of chromone derivatives as inhibitors of monoamine oxidase / Annah Nyasha Mpitimpiti .” 2014. Thesis, North-West University. Accessed March 07, 2021. http://hdl.handle.net/10394/15449.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Mpitimpiti, Annah Nyasha. “Synthesis and evaluation of chromone derivatives as inhibitors of monoamine oxidase / Annah Nyasha Mpitimpiti .” 2014. Web. 07 Mar 2021.

Vancouver:

Mpitimpiti AN. Synthesis and evaluation of chromone derivatives as inhibitors of monoamine oxidase / Annah Nyasha Mpitimpiti . [Internet] [Thesis]. North-West University; 2014. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10394/15449.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Mpitimpiti AN. Synthesis and evaluation of chromone derivatives as inhibitors of monoamine oxidase / Annah Nyasha Mpitimpiti . [Thesis]. North-West University; 2014. Available from: http://hdl.handle.net/10394/15449

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Victoria University of Wellington

3. Crowther, Alex John. Contribution of Harman and Norharman to the Reinforcing Efficacy of Aqueous Tobacco Smoke Extract Self-Administered by Rats.

Degree: 2012, Victoria University of Wellington

URL: http://hdl.handle.net/10063/2337

► Background: Animal models of drug abuse treat nicotine as the primary reinforcing agent that promotes tobacco addiction. However, rodents demonstrate poor self-administration of nicotine despite… (more)

▼ Background: Animal models of drug abuse treat nicotine as the primary reinforcing agent that promotes tobacco addiction. However, rodents demonstrate poor self-administration of nicotine despite evidence of tobacco's high abuse potential in humans. This discrepancy has been attributed to other constituents of tobacco smoke that facilitate the development of nicotine dependence. Objectives: This study aimed to determine whether rats would self-administer intravenous an aqueous tobacco smoke extract (TPM) to find evidence if it was more reinforcing than nicotine alone. The study also evaluated the role of tobacco smoke constituent’s harman and norharman in any differences observed. Methods: Firstly, male Sprague-Dawley rats (n=29) were assigned to treatment groups: nicotine (30.0μg/kg/infusion), TPM (containing 30.0μg/kg/infusion nicotine) or saline vehicle. Ability for each treatment to support intravenous self-administration was assessed using spontaneous acquisition of responding on gradually increasing fixed ratio schedules (FR1, FR2, FR5). Subsequent progressive ratio (PR) testing was employed to determine reinforcing efficacy of each treatment. Then a second group of rats (N = 56) were assigned to treatment groups: nicotine alone (30.0 or 75.0μg/kg/infusion) or nicotine combined with norharman (0, 0.4, 2.5 or 6.25μg/kg/infusion) and harman (0.0, 1.6 or 10.0μg/kg, IP), and tested using a similar protocol. Results: Animals readily acquired self-administration responding for TPM and produced higher PR breakpoints (BP) than rats treated with nicotine alone or vehicle. Rats trained to respond for a larger dose of nicotine demonstrated significantly greater response rates than those receiving the lower dose of nicotine. Finally, the addition of harman and norharman to nicotine significantly reduced BP at the lower unit dose of nicotine tested. Conclusions: These findings support the hypothesis that TPM is more reinforcing than nicotine alone. However, the increased reinforcing efficacy of TPM cannot be attributed to the actions of harman and norharman. The potential role of serotonin inhibition in tobacco reward processes is discussed. Advisors/Committee Members: Brennan, Katie, Harper, David.

Subjects/Keywords: Self-administration; Nicotine; Monoamine oxidase inhibitors

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Crowther, A. J. (2012). Contribution of Harman and Norharman to the Reinforcing Efficacy of Aqueous Tobacco Smoke Extract Self-Administered by Rats. (Masters Thesis). Victoria University of Wellington. Retrieved from http://hdl.handle.net/10063/2337

Chicago Manual of Style (16^th Edition):

Crowther, Alex John. “Contribution of Harman and Norharman to the Reinforcing Efficacy of Aqueous Tobacco Smoke Extract Self-Administered by Rats.” 2012. Masters Thesis, Victoria University of Wellington. Accessed March 07, 2021. http://hdl.handle.net/10063/2337.

MLA Handbook (7^th Edition):

Crowther, Alex John. “Contribution of Harman and Norharman to the Reinforcing Efficacy of Aqueous Tobacco Smoke Extract Self-Administered by Rats.” 2012. Web. 07 Mar 2021.

Vancouver:

Crowther AJ. Contribution of Harman and Norharman to the Reinforcing Efficacy of Aqueous Tobacco Smoke Extract Self-Administered by Rats. [Internet] [Masters thesis]. Victoria University of Wellington; 2012. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10063/2337.

Council of Science Editors:

Crowther AJ. Contribution of Harman and Norharman to the Reinforcing Efficacy of Aqueous Tobacco Smoke Extract Self-Administered by Rats. [Masters Thesis]. Victoria University of Wellington; 2012. Available from: http://hdl.handle.net/10063/2337

University of Toronto

4. Chiuccariello, Lina. Monoamine Oxidase A in Relation to Subtypes and Treatment of Major Depressive Disorder.

Degree: PhD, 2015, University of Toronto

URL: http://hdl.handle.net/1807/77749

►

Identification of central biomarkers related to subtypes of major depressive episodes (MDEs) can contribute to a more personalized treatment approach of major depressive disorder (MDD).… (more)

Subjects/Keywords: Major Depressive Disorder; Monoamine Oxidase A; Monoamine Oxidase Inhibitors; Positron Emission Tomography; 0419

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Chiuccariello, L. (2015). Monoamine Oxidase A in Relation to Subtypes and Treatment of Major Depressive Disorder. (Doctoral Dissertation). University of Toronto. Retrieved from http://hdl.handle.net/1807/77749

Chicago Manual of Style (16^th Edition):

Chiuccariello, Lina. “Monoamine Oxidase A in Relation to Subtypes and Treatment of Major Depressive Disorder.” 2015. Doctoral Dissertation, University of Toronto. Accessed March 07, 2021. http://hdl.handle.net/1807/77749.

MLA Handbook (7^th Edition):

Chiuccariello, Lina. “Monoamine Oxidase A in Relation to Subtypes and Treatment of Major Depressive Disorder.” 2015. Web. 07 Mar 2021.

Vancouver:

Chiuccariello L. Monoamine Oxidase A in Relation to Subtypes and Treatment of Major Depressive Disorder. [Internet] [Doctoral dissertation]. University of Toronto; 2015. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/1807/77749.

Council of Science Editors:

Chiuccariello L. Monoamine Oxidase A in Relation to Subtypes and Treatment of Major Depressive Disorder. [Doctoral Dissertation]. University of Toronto; 2015. Available from: http://hdl.handle.net/1807/77749

University of Alberta

5. Kumpula, David J. The Antidepressant/Antipanic/Neuroprotective Drug Phenelzine: Neuropharmacological and Drug Metabolism Studies.

Degree: MS, Department of Psychiatry, 2013, University of Alberta

URL: https://era.library.ualberta.ca/files/w9505154d

► Phenelzine (PLZ) is a monoamine oxidase (MAO)-inhibiting antidepressant with anxiolytic and neuroprotective properties. Metabolites of PLZ were investigated in rat brain. Levels of phenylacetic acid… (more)

Subjects/Keywords: phenylethylidenehydrazine; phenelzine; monoamine oxidase inhibitors; gamma-aminobutyric acid; phenylacetic acid; monoamine oxidase; phenylethylamine; drug metabolism; alanine

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Kumpula, D. J. (2013). The Antidepressant/Antipanic/Neuroprotective Drug Phenelzine: Neuropharmacological and Drug Metabolism Studies. (Masters Thesis). University of Alberta. Retrieved from https://era.library.ualberta.ca/files/w9505154d

Chicago Manual of Style (16^th Edition):

Kumpula, David J. “The Antidepressant/Antipanic/Neuroprotective Drug Phenelzine: Neuropharmacological and Drug Metabolism Studies.” 2013. Masters Thesis, University of Alberta. Accessed March 07, 2021. https://era.library.ualberta.ca/files/w9505154d.

MLA Handbook (7^th Edition):

Kumpula, David J. “The Antidepressant/Antipanic/Neuroprotective Drug Phenelzine: Neuropharmacological and Drug Metabolism Studies.” 2013. Web. 07 Mar 2021.

Vancouver:

Kumpula DJ. The Antidepressant/Antipanic/Neuroprotective Drug Phenelzine: Neuropharmacological and Drug Metabolism Studies. [Internet] [Masters thesis]. University of Alberta; 2013. [cited 2021 Mar 07]. Available from: https://era.library.ualberta.ca/files/w9505154d.

Council of Science Editors:

Kumpula DJ. The Antidepressant/Antipanic/Neuroprotective Drug Phenelzine: Neuropharmacological and Drug Metabolism Studies. [Masters Thesis]. University of Alberta; 2013. Available from: https://era.library.ualberta.ca/files/w9505154d

Universidade do Rio Grande do Sul

6. Recalde Gil, Maria Angélica. Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase).

Degree: 2015, Universidade do Rio Grande do Sul

URL: http://hdl.handle.net/10183/149485

►

The plant Garcinia gardneriana (Planch. & Triana) Zappi, popularly known in Brazil as "bacupari" has traditionally been used for various types of inflammatory diseases and… (more)

▼

The plant Garcinia gardneriana (Planch. & Triana) Zappi, popularly known in Brazil as "bacupari" has traditionally been used for various types of inflammatory diseases and the evaluation of their chemical composition, mainly of leaves, has resulted in biflavonoids as major compounds. These phenolic compounds have shown anti-inflammatory activity validating the popular use of the plant. In this work was isolated from dried branches of Garcinia gardneriana the biflavonoids: morelloflavone, that is an naringenin covalently linked to luteolin, Gb-2a which is an naringenin linked to eriodictyol and Gb-2a- 7-O-glucose. These compounds have been previously evaluated in various activities such as anti-inflammatory and anti-antioxidants but there is no report of its activity as enzymatic inhibitors. However, the monomers that form it, have been evaluated in the inhibition of aromatase and antidepressant activity with positive outcome, which commonly are used MAO-A inhibitors. In the isolation process were also founded terpenoid compounds as lupeol and friedelin The isolated and purified biflavonoids were used to evaluate enzyme inhibition "in vitro" in monoamine oxidases (MAO-A MAO-B) and aromatase. The compounds showed a positive response even of IC50 5,47 μM and 1,35 μM for MAO-A inhibition of and aromatase enzyme respectively; discovering a way for a new proposal to link both enzymes for treatment of hormone-dependent cancers and anxiety and depression disorders.

La planta Garcinia gardneriana (Planch. & Triana) Zappi, popularmente conocida en Brasil como "bacupari" ha sido tradicionalmente usada para varios tipos de enfermedades inflamatorias y la evaluación de su composición química, principalmente de las hojas, ha resultado en biflavonoides como compuestos mayoritarios. Estos compuestos fenólicos han demostrado actividad anti-inflamatória validando el uso popular de la planta. En este trabajo se asilaron a partir de tallos secos de la Garcinia gardneriana los biflavonoides: moreloflavona, que consiste en una naringenina unida covalentemente a luteolina, Gb-2a que es un compuesto que consiste en una naringenina unida a un eriodictyol y Gb-2a-7-O-glucose. Estos compuestos ya han sido previamente evaluados en diversas actividades como anti inflamatorios y anti antioxidantes pero no se tiene reporte de su actividad como inhibidores enzimáticos. Sin embargo, los monomeros que los conforman han sido evaluados en la inhibición de la aromatasa y con resultados positivos como en la actividad antidepresiva, para la cual comúnmente son usados los inibidores de MAO-A. En el proceso de aislamiento también fueron encontrados compuestos terpenoides como lupeol y friedelina. Los biflavonoides aislados y purificados se usaron para evaluar la inhibición enzimática “in vitro” en monoaminooxidasas (MAO-A, MAO-B) y aromatasa. Los compuestos presentaron una respuesta positiva calculada con IC50 de hasta 5,47 μM y 1,35 μM para la inhibición de las enzimas MAO-A y aromatasa respectivamente, abriendo el camino a una nueva propuesta de…

Advisors/Committee Members: Henriques, Amelia Teresinha.

Subjects/Keywords: Garcinia gardneriana; Farmácia; Biflavonoids; Aromatase; Monoamine oxidase inhibitors; Biflavonoides; Aromatasa; Monoaminooxidasa; Inhibidores

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Recalde Gil, M. A. (2015). Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase). (Thesis). Universidade do Rio Grande do Sul. Retrieved from http://hdl.handle.net/10183/149485

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Recalde Gil, Maria Angélica. “Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase).” 2015. Thesis, Universidade do Rio Grande do Sul. Accessed March 07, 2021. http://hdl.handle.net/10183/149485.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Recalde Gil, Maria Angélica. “Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase).” 2015. Web. 07 Mar 2021.

Vancouver:

Recalde Gil MA. Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase). [Internet] [Thesis]. Universidade do Rio Grande do Sul; 2015. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10183/149485.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Recalde Gil MA. Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase). [Thesis]. Universidade do Rio Grande do Sul; 2015. Available from: http://hdl.handle.net/10183/149485

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

North-West University

7. Minders, Corné. Monoamine oxidase inhibitory activities of heterocyclic chalcones / Corné Minders .

Degree: 2013, North-West University

URL: http://hdl.handle.net/10394/12251

► Parkinson’s disease is the second most common age-related neurodegenerative disease after Alzheimer’s disease. The characteristic pathological feature of Parkinson’s disease is the loss of neurons… (more)

▼ Parkinson’s disease is the second most common age-related neurodegenerative disease after Alzheimer’s disease. The characteristic pathological feature of Parkinson’s disease is the loss of neurons in the substantia nigra pars compacta (SNpc), which leads to a striatal dopamine deficiency responsible for the major symptoms of Parkinson’s disease. These symptoms include tremor at rest, postural instability, bradykinesia and in the later stages of Parkinson’s disease, even psychosis. Presently, there is still no cure for Parkinson’s disease and all treatments are only symptomatic. Current research is therefore directed towards the prevention of further dopaminergic neurodegeneration, while the ultimate aim is the reversal of neurodegeneration. Monoamine oxidase (MAO) enzymes are responsible for the regulation and metabolism of monoamine neurotransmitters, such as dopamine. There are two MAO isoforms, MAO-A and MAO-B. Since MAO-B has greater activity in the basal ganglia, it is of particular importance in movement disorders, which include Parkinson’s disease. The selective inhibition of MAO-B, increases dopamine available for binding, and thus reduces Parkinson’s disease symptoms. MAO inhibitors also have neuroprotective potential and thus may slow down, halt and even reverse neurodegeneration in Parkinson’s disease. It is still unclear exactly how MAO inhibitors protect neurons, but one theory suggests that MAO inhibition decreases oxidative stress by reducing the formation of hydrogen peroxide, a metabolic by-product of MAO oxidation of monoamines. Normally, hydrogen peroxide is inactivated by glutathione (GSH), however, in Parkinson’s disease, GSH levels are low, resulting in the accumulation of hydrogen peroxide, which then becomes available for the Fenton reaction. In the Fenton reaction, Fe2+ reacts with hydrogen peroxide and generates an active free radical, the hydroxyl radical. This radical depletes cellular anti-oxidants, damage lipids, proteins and DNA. MAO inhibitors reduce the formation of hydrogen peroxide thus decreasing the formation of hydroxyl radicals and oxidative stress. The MAO inhibitory potential of natural and synthetic chalcones have been illustrated. For example, in 1987, Tanaka and co-workers determined that natural chalcones, such as isoliquiritigenin, have MAO inhibitory activity in rat mitochondria. In 2009, Chimenti and co-workers synthesized a series of 1,3-diphenyl-2-propen-1-ones which exhibited human MAO-B (hMAO-B) selective inhibitory activity. On the other hand, Robinson and co-workers (2013), synthesized novel furanochalcones which also had hMAO-B selective inhibitory activity. A reversible, competitive mode of binding was demonstrated by these compounds. Since the effect of heterocyclic substitution, other than furan on the MAO inhibitory properties of the chalcone scaffold remains unexplored, the aim of this study was to synthesize and evaluate further heterocyclic chalcone analogues as inhibitors of hMAO. RESULTS Design and synthesis:…

Subjects/Keywords: Chalcones; Monoamine oxidase inhibitors; Parkinson’s disease; Chalkone; Monoamienoksidase-inhibeerders; Parkinson se siekte

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Minders, C. (2013). Monoamine oxidase inhibitory activities of heterocyclic chalcones / Corné Minders . (Thesis). North-West University. Retrieved from http://hdl.handle.net/10394/12251

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Minders, Corné. “Monoamine oxidase inhibitory activities of heterocyclic chalcones / Corné Minders .” 2013. Thesis, North-West University. Accessed March 07, 2021. http://hdl.handle.net/10394/12251.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Minders, Corné. “Monoamine oxidase inhibitory activities of heterocyclic chalcones / Corné Minders .” 2013. Web. 07 Mar 2021.

Vancouver:

Minders C. Monoamine oxidase inhibitory activities of heterocyclic chalcones / Corné Minders . [Internet] [Thesis]. North-West University; 2013. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10394/12251.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Minders C. Monoamine oxidase inhibitory activities of heterocyclic chalcones / Corné Minders . [Thesis]. North-West University; 2013. Available from: http://hdl.handle.net/10394/12251

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

North-West University

8. Fourie, Petrus Michiel. Neuroprotective effects of amantadine–flavonoid conjugates / Fourie P.M.

Degree: 2011, North-West University

URL: http://hdl.handle.net/10394/7339

► Neurodegenerative disorders like Parkinson’s and Alzheimer’s disease affect millions of people around the world. Oxidative stress has been implicated in the pathogenesis of a number… (more)

▼ Neurodegenerative disorders like Parkinson’s and Alzheimer’s disease affect millions of people around the world. Oxidative stress has been implicated in the pathogenesis of a number of neurodegenerative disorders, cancer and ischemia. The brain is particularly vulnerable to oxidative damage because of its high utilisation of oxygen, high levels of polyunsaturated fatty acids, relatively high levels of redox transition metal ions and low levels of antioxidants. Oxidative stress occurs due to an imbalance in the pro–oxidant and antioxidant levels. Reactive oxygen/nitrogen species (ROS/RNS) is a collective term used for free radicals and related molecules, promoting oxidative stress within cells and ultimately leading to neurodegeneration. Antioxidants counteract the excess in ROS/RNS, and is therefore of interest in the treatment and prevention of neurodegenerative disorders. Monoamine oxidases, especially monoamine oxidase B (MAO–B), also play an important role in neurodegenerative disorders. MAO–B is the main enzyme responsible for the oxidative deamination of dopamine in the substantia nigra of the brain. By inhibiting MAO–B, dopamine is increased in the brain providing symptomatic relief in Parkinson’s disease. The focus of the current study was to synthesise multifunctional compounds that could be used in the treatment and/or prevention of neurodegenerative diseases. In this study flavonoids were selected because of their wide spectrum of biological activities, including antioxidant activity and its monoamine oxidase inhibition. Flavones and chalcones are both classified under flavonoids and both structures were included. The amantadine moiety was included because of its known ability to inhibit calcium flux through the N–methyl–D–aspartate (NMDA) receptor channel. Six amantadine–flavonoid derivatives were synthesised using standard laboratory procedures and structures were determined with standard methods such as NMR, IR and mass spectrometry. The synthesised compounds were tested in a selection of biological assays, to establish the relative antioxidant properties and MAO inhibitory activity. The biological assays employed to test antioxidant properties were the thiobarbituric acid (TBA) and nitro–blue tetrazolium (NBT) assays. The TBA assay relies on the assessment of lipid peroxidation, induced via hydroxyl anions (OH), generating a pink colour with the complex formation between malondialdehyde (MDA) and TBA, which is measured spectrophotometrically at 532 nm. The principal of the NBT assay is the reduction of NBT to nitro–blue diformazan (NBD), producing a purple colour in the presence of superoxide anions (O2 –). The synthesised compounds were also evaluated for their MAO inhibitory activity toward recombinant human MAO–A and -B and inhibition values were expressed as IC50 values. The experimental data obtained in the NBT and TBA assay indicated a weak but a significant ability to scavenge O2 – and OH. In the NBT assay N–(adamantan–1–yl)–2–{3–hydroxy–4–[(2E)– …

Subjects/Keywords: Antioxidant; Monoamine oxidase inhibitors; Amantadine; Flavonoids; Neuroprotective; Anti-oksidant; Monoamienoksidase inhibeerder; Flavonoïed; Amantadien; Neurobeskermd

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APA (6^th Edition):

Fourie, P. M. (2011). Neuroprotective effects of amantadine–flavonoid conjugates / Fourie P.M. (Thesis). North-West University. Retrieved from http://hdl.handle.net/10394/7339

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Fourie, Petrus Michiel. “Neuroprotective effects of amantadine–flavonoid conjugates / Fourie P.M. ” 2011. Thesis, North-West University. Accessed March 07, 2021. http://hdl.handle.net/10394/7339.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Fourie, Petrus Michiel. “Neuroprotective effects of amantadine–flavonoid conjugates / Fourie P.M. ” 2011. Web. 07 Mar 2021.

Vancouver:

Fourie PM. Neuroprotective effects of amantadine–flavonoid conjugates / Fourie P.M. [Internet] [Thesis]. North-West University; 2011. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10394/7339.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Fourie PM. Neuroprotective effects of amantadine–flavonoid conjugates / Fourie P.M. [Thesis]. North-West University; 2011. Available from: http://hdl.handle.net/10394/7339

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

North-West University

9. Harmse, Rozanne. Syntheses of 8-(phenoxymethyl)caffeine analogues and their evaluation as inhibitors of monoamine oxidase and as antagonists of the adenosine A2A receptor / Rozanne Harmse.

Degree: 2013, North-West University

URL: http://hdl.handle.net/10394/9663

► Background and rationale: Parkinson’s disease (PD) is a progressive, degenerative disorder of the central nervous system and is characterized by the loss of dopaminergic neurons… (more)

▼ Background and rationale: Parkinson’s disease (PD) is a progressive, degenerative disorder of the central nervous system and is characterized by the loss of dopaminergic neurons in the substantia nigra pars compacta. The loss of functional dopamine in the striatum is thought to be responsible for the typical symptoms of PD. Cardinal features of PD include bradykinesia, muscular rigidity, resting tremor and impairment of postural balance. This study focuses on the inhibition of monoamine oxidase B (MAO-B) and antagonism of A2A receptors as therapeutic strategies for PD. Monoamine oxidase (MAO) is a flavin adenine dinucleotide (FAD)-containing mitochondrial bound isoenzyme which consists of two isoforms namely MAO-A and MAO-B. The primary function of MAO is to catalyze the oxidative deamination of dietary amines, monoamine neurotransmitters and hormones. MAO-A is responsible for the oxidative deamination of serotonin (5-HT) and norepinephrine (NE), while MAO-B is responsible for the oxidative deamination of dopamine (DA). The formation of DA takes place in the presynaptic neuron where it is stored in vesicles and released into the presynaptic cleft. The released DA then either binds to D1 and D2 receptors which results in an effector response. The excess DA in the presynaptic cleft is metabolized by MAO-B which may result in the formation of free radicals and a decrease in DA concentrations. Under normal physiological conditions free radicals are removed from the body via normal physiological processes, but in PD these normal physiological processes are thought to be unable to remove the radicals and this may lead to oxidative stress. Oxidative stress is believed to be one of the leading causes of neurodegeneration in PD. The rationale for the use of MAO-B inhibitors in PD would be to increase the natural DA levels in the brain and also diminish the likelihood of free radicals to be formed. Adenosine is an endogenous purine nucleoside and yields a variety of physiological effects. Four adenosine receptor subtypes have been characterized: A1, A2A, A2B and A3. They are all part of the G-protein-coupled receptor family and have seven transmembrane domains. The A2A receptor is highly concentrated in the striatum. There are two important pathways in the basal ganglia (BG) through which striatal information reaches the globus pallidus, namely the direct pathway containing A1 and D1 receptors and the indirect pathway containing A2A and D2 receptors. The direct pathway facilitates willed movement and the indirect pathway inhibits willed movement. A balance of the two pathways is necessary for normal movement. In PD, there is a decrease in DA in the striatum, thus leading to unopposed A2A receptor signaling and ultimately resulting in overactivity of the indirect pathway. Overactivity of the indirect pathway results in the locomotor symptoms associated with PD. Treatment with an A2A antagonist will block the A2A receptor, resulting in the restoration of balance between the indirect and direct pathways, thus leading to a…

Subjects/Keywords: Parkinson’s disease; monoamine oxidase inhibitors; adenosine A2A antagonists; dual-targeted compounds; 8-(phenoxymethyl)caffeine

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APA (6^th Edition):

Harmse, R. (2013). Syntheses of 8-(phenoxymethyl)caffeine analogues and their evaluation as inhibitors of monoamine oxidase and as antagonists of the adenosine A2A receptor / Rozanne Harmse. (Thesis). North-West University. Retrieved from http://hdl.handle.net/10394/9663

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Harmse, Rozanne. “Syntheses of 8-(phenoxymethyl)caffeine analogues and their evaluation as inhibitors of monoamine oxidase and as antagonists of the adenosine A2A receptor / Rozanne Harmse. ” 2013. Thesis, North-West University. Accessed March 07, 2021. http://hdl.handle.net/10394/9663.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Harmse, Rozanne. “Syntheses of 8-(phenoxymethyl)caffeine analogues and their evaluation as inhibitors of monoamine oxidase and as antagonists of the adenosine A2A receptor / Rozanne Harmse. ” 2013. Web. 07 Mar 2021.

Vancouver:

Harmse R. Syntheses of 8-(phenoxymethyl)caffeine analogues and their evaluation as inhibitors of monoamine oxidase and as antagonists of the adenosine A2A receptor / Rozanne Harmse. [Internet] [Thesis]. North-West University; 2013. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10394/9663.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Harmse R. Syntheses of 8-(phenoxymethyl)caffeine analogues and their evaluation as inhibitors of monoamine oxidase and as antagonists of the adenosine A2A receptor / Rozanne Harmse. [Thesis]. North-West University; 2013. Available from: http://hdl.handle.net/10394/9663

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

10. Gogineni, Vedanjali. Phytochemical Investigation of Psychoactive Medicinal Plants for the Treatment of Neurological Disorders.

Degree: PhD, Biomolecular Sciences, 2017, University of Mississippi

URL: https://egrove.olemiss.edu/etd/1455

► Neurological disorders include disorders such as migraine, tension-type headaches, Parkinson’s disease (PD), epilepsy, dementia, and Alzheimer’s disease (AD). Globally, PD is the second most common… (more)

▼ Neurological disorders include disorders such as migraine, tension-type headaches, Parkinson’s disease (PD), epilepsy, dementia, and Alzheimer’s disease (AD). Globally, PD is the second most common neurodegenerative disorder following AD. In developed countries, PD affects 1% of all population over 60 years of age. The prevalence of PD is increasing over the years and is expected to double by 2030. It is proposed that combination of dopaminergic drugs with monoamine oxidase B (MAO-B) inhibitors, anticholinergics, catechol-O-methyl transferase inhibitors, and other non-dopaminergic drugs can better alleviate levodopa-induced motor complications along with better control of motor symptoms. MAO-B inhibitors play a significant role in dopamine (DA) metabolism and can be used as monotherapy in the early stages of PD, or in combination with levodopa. Currently, there are only three MAO-B inhibitors that are approved by Food and Drug Administration (FDA): selegiline, rasagiline, and safinamide. Hence, there is the need to discover potent and selective MAO-B inhibitors for effective treatment of PD. About 60% of the marketed drugs today are either natural products or derivatives that are inspired from natural products. We studied plants with extensive traditional use in CNS-related disorders, in which the chloroform extract of C. urticifolia exhibited potent inhibition of MAO-A and -B. Calea urticifolia (Asteraceae) commonly known as “Juanislama” is native to the Central America. Bioassay-guided fractionation has been implemented for the isolation of the secondary metabolites from C. urticifolia. From the bioactive fraction, acacetin and a series of sesquiterpenes were isolated; acacetin was found to be the bioactive compound. A series of acacetin analogs were designed with the aid of computational docking studies, to improve their selectivity towards MAO-B. The structures of the isolated compounds were determined on the basis of HR-MS and 1D- and 2D-NMR studies; configurations were partly established by ECD calculations. Monoamine oxidase assays were performed on the extracts, fractions, and purified compounds. Molecular modeling and molecular dynamic studies were used to predict the binding modes on the active sites of the MAO isoenzymes. Advisors/Committee Members: John M. Rimoldi, Samir A. Ross, David A. Colby.

Subjects/Keywords: Acacetin; Calea; Flavonoids; Monoamine Oxidase Inhibitors; Parkinson's Disease; Sesquiterpenes; Pharmacy and Pharmaceutical Sciences

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Gogineni, V. (2017). Phytochemical Investigation of Psychoactive Medicinal Plants for the Treatment of Neurological Disorders. (Doctoral Dissertation). University of Mississippi. Retrieved from https://egrove.olemiss.edu/etd/1455

Chicago Manual of Style (16^th Edition):

Gogineni, Vedanjali. “Phytochemical Investigation of Psychoactive Medicinal Plants for the Treatment of Neurological Disorders.” 2017. Doctoral Dissertation, University of Mississippi. Accessed March 07, 2021. https://egrove.olemiss.edu/etd/1455.

MLA Handbook (7^th Edition):

Gogineni, Vedanjali. “Phytochemical Investigation of Psychoactive Medicinal Plants for the Treatment of Neurological Disorders.” 2017. Web. 07 Mar 2021.

Vancouver:

Gogineni V. Phytochemical Investigation of Psychoactive Medicinal Plants for the Treatment of Neurological Disorders. [Internet] [Doctoral dissertation]. University of Mississippi; 2017. [cited 2021 Mar 07]. Available from: https://egrove.olemiss.edu/etd/1455.

Council of Science Editors:

Gogineni V. Phytochemical Investigation of Psychoactive Medicinal Plants for the Treatment of Neurological Disorders. [Doctoral Dissertation]. University of Mississippi; 2017. Available from: https://egrove.olemiss.edu/etd/1455

University of Alberta

11. Sherry-McKenna, Rhonda Lynn. Neurochemical studies of tranylcypromine and ring-substituted analogues.

Degree: PhD, Faculty of Pharmacy and Pharmaceutical Sciences, 1996, University of Alberta

URL: https://era.library.ualberta.ca/files/tb09j752q

Subjects/Keywords: Antidepressants – Physiological effect.; Monoamine oxidase – Inhibitors – Metabolism.

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Sherry-McKenna, R. L. (1996). Neurochemical studies of tranylcypromine and ring-substituted analogues. (Doctoral Dissertation). University of Alberta. Retrieved from https://era.library.ualberta.ca/files/tb09j752q

Chicago Manual of Style (16^th Edition):

Sherry-McKenna, Rhonda Lynn. “Neurochemical studies of tranylcypromine and ring-substituted analogues.” 1996. Doctoral Dissertation, University of Alberta. Accessed March 07, 2021. https://era.library.ualberta.ca/files/tb09j752q.

MLA Handbook (7^th Edition):

Sherry-McKenna, Rhonda Lynn. “Neurochemical studies of tranylcypromine and ring-substituted analogues.” 1996. Web. 07 Mar 2021.

Vancouver:

Sherry-McKenna RL. Neurochemical studies of tranylcypromine and ring-substituted analogues. [Internet] [Doctoral dissertation]. University of Alberta; 1996. [cited 2021 Mar 07]. Available from: https://era.library.ualberta.ca/files/tb09j752q.

Council of Science Editors:

Sherry-McKenna RL. Neurochemical studies of tranylcypromine and ring-substituted analogues. [Doctoral Dissertation]. University of Alberta; 1996. Available from: https://era.library.ualberta.ca/files/tb09j752q

Virginia Commonwealth University

12. Zhang, Zhenxian. ASSESSMENT OF THE FEASIBILITY OF CO-ADMINISTRATION OF PHENOLIC DIETARY COMPOUNDS WITH PHENYLEPHRINE TO INCREASE ITS BIOAVAILABILITY.

Degree: PhD, Pharmaceutical Sciences, 2013, Virginia Commonwealth University

URL: https://doi.org/10.25772/ZNNS-G983 ; https://scholarscompass.vcu.edu/etd/539

► R-(-)-Phenylephrine (PE) is the most commonly used nonprescription oral nasal decongestant in the United States. It is a selective α1-adrenergic receptor agonist and has… (more)

▼ R-(-)-Phenylephrine (PE) is the most commonly used nonprescription oral nasal decongestant in the United States. It is a selective α1-adrenergic receptor agonist and has many years of safe usage. However, the efficacy of PE is controversial, due to its extensive pre-systemic metabolism, which leads to low and variable oral bioavailability (38 ± 9%, mean ± SD). Sulfation plays a very important role in pre-systemic metabolism of PE. The sulfation of PE occurs at its phenolic group, which is the preferred structural feature of many sulfotransferase (SULT) substrates. Compounds with phenolic groups have similar structures to PE, which may share the same SULT isoforms with PE and have the potential to inhibit PE sulfation. Co-administration of the phenolic compounds from the Food and Drug Administration’s (FDA) “Generally Recognized as Safe” (GRAS) list, Everything Added to Food in the United States (EAFUS), or dietary supplements along with PE could be an effective strategy to inhibit the pre-systemic sulfation of PE. The primary side effect of PE is hypertension. Since monoamine oxidase (MAO) inhibitors may increase the risk of hypertension, they should not be taken with PE. In order to increase the oral bioavailability and eventually improve the efficacy of PE, this research project aimed to investigate the feasibility of inhibiting the pre-systemic sulfation of PE with phenolic dietary compounds. Considering the safety issue, this research project also aimed to investigate whether these phenolic dietary compounds have inhibitory effects on MAO-A/B. A human colon adenocarcinoma epithelial cell line (LS180), which shows sulfation activity, was used as a model to test the effect of these phenolic compounds on the sulfation of PE. The extent of disappearance of PE was significantly (p < 0.05) decreased to the following (mean ± SEM, as % of control) when incubated with phenolic dietary compounds in LS180 cells for 14 - 19 hrs: curcumin 24.5 ± 14.0%, guaiacol 51.3 ± 8.0%, isoeugenol 73.9 ± 4.3%, pterostilbene 70.6 ± 4.2%, resveratrol 14.2 ± 28.0%, zingerone 52.4 ± 14.6%, and the combinations eugenol + propylparaben 42.6 ± 8.4%, vanillin + propylparaben 37.0 ± 11.2%, eugenol + propylparaben + vanillin + ascorbic acid 31.1 ± 10.9%, eugenol + vanillin 57.5 ± 20.6%, and pterostilbene + zingerone 36.5 ± 7.0%. The combinations of curcumin + resveratrol and curcumin + pterostilbene + resveratrol + zingerone almost completely inhibited PE disappearance. PE sulfate formation was inhibited 67.0 ± 4.2% (mean ± SEM, as % of control) by guaiacol and 71.7 ± 2.6% by pterostilbene + zingerone. The combinations of curcumin + resveratrol and curcumin + pterostilbene + resveratrol + zingerone inhibited ≥ 99% of PE sulfate formation. These results were consistent with those from analysis of the disappearance of PE in LS180 cells. These phenolic inhibitors for sulfation were also tested to see whether they have any inhibitory effects on MAO-A or B. Significant inhibition was found with curcumin, guaiacol, isoeugenol, pterostilbene,… Advisors/Committee Members: Phillip Gerk.

Subjects/Keywords: Phenylephrine; Bioavailability; Sulfation; Phenolic dietary compounds; Monoamine oxidase inhibitors; Medicine and Health Sciences; Pharmacy and Pharmaceutical Sciences

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Zhang, Z. (2013). ASSESSMENT OF THE FEASIBILITY OF CO-ADMINISTRATION OF PHENOLIC DIETARY COMPOUNDS WITH PHENYLEPHRINE TO INCREASE ITS BIOAVAILABILITY. (Doctoral Dissertation). Virginia Commonwealth University. Retrieved from https://doi.org/10.25772/ZNNS-G983 ; https://scholarscompass.vcu.edu/etd/539

Chicago Manual of Style (16^th Edition):

Zhang, Zhenxian. “ASSESSMENT OF THE FEASIBILITY OF CO-ADMINISTRATION OF PHENOLIC DIETARY COMPOUNDS WITH PHENYLEPHRINE TO INCREASE ITS BIOAVAILABILITY.” 2013. Doctoral Dissertation, Virginia Commonwealth University. Accessed March 07, 2021. https://doi.org/10.25772/ZNNS-G983 ; https://scholarscompass.vcu.edu/etd/539.

MLA Handbook (7^th Edition):

Zhang, Zhenxian. “ASSESSMENT OF THE FEASIBILITY OF CO-ADMINISTRATION OF PHENOLIC DIETARY COMPOUNDS WITH PHENYLEPHRINE TO INCREASE ITS BIOAVAILABILITY.” 2013. Web. 07 Mar 2021.

Vancouver:

Zhang Z. ASSESSMENT OF THE FEASIBILITY OF CO-ADMINISTRATION OF PHENOLIC DIETARY COMPOUNDS WITH PHENYLEPHRINE TO INCREASE ITS BIOAVAILABILITY. [Internet] [Doctoral dissertation]. Virginia Commonwealth University; 2013. [cited 2021 Mar 07]. Available from: https://doi.org/10.25772/ZNNS-G983 ; https://scholarscompass.vcu.edu/etd/539.

Council of Science Editors:

Zhang Z. ASSESSMENT OF THE FEASIBILITY OF CO-ADMINISTRATION OF PHENOLIC DIETARY COMPOUNDS WITH PHENYLEPHRINE TO INCREASE ITS BIOAVAILABILITY. [Doctoral Dissertation]. Virginia Commonwealth University; 2013. Available from: https://doi.org/10.25772/ZNNS-G983 ; https://scholarscompass.vcu.edu/etd/539

North-West University

13. Van Dyk, Adriaan Sarel. Synthesis and biological evaluation of 6-substituted coumaranone derivatives and related compounds as monoamine oxidase inhibitors / Adriaan Sarel van Dyk .

Degree: 2014, North-West University

URL: http://hdl.handle.net/10394/16548

► Parkinson’s disease (PD) is an age related neurodegenerative disorder that presents with both motor and non-motor symptoms. The most common pathological characteristic of PD is… (more)

▼ Parkinson’s disease (PD) is an age related neurodegenerative disorder that presents with both motor and non-motor symptoms. The most common pathological characteristic of PD is the loss of the pigmented dopaminergic neurons of the substantia nigra pars compacta (SNpc), with the appearance of intracellular inclusions known as Lewy bodies in the affected neurons. The loss of the SNpc neurons results in a deficiency of dopamine in the nigrostriatal pathway of the brain, and it is this deficiency that is responsible for the motor symptoms of PD. Monoamine oxidase B (MAO-B) is predominantly found in the striatum and is responsible for the oxidative metabolism of dopamine. The first-line treatment of PD is dopamine replacement therapy with levodopa, the metabolic precursor of dopamine. Rapid metabolism of levodopa at central and peripheral level, however, hampers its therapeutic potential. MAO-B inhibition enhances striatal dopamine activity by means of inhibiting dopamine metabolism, and MAO-B inhibitors are thus used in the treatment of PD, particularly in combination with levodopa. The aim of this study was to design new potent, reversible MAO inhibitors with selectivity towards MAO-B for the symptomatic treatment of PD. Recent studies have shown that C5-substituted phthalide derivatives are highly potent inhibitors of human MAO-B. Phthalide derivatives were also found to be potent inhibitors of human MAO-A. The structural similarity between phthalide and 3-coumaranone suggests that 3-coumaranone may be a useful scaffold for the design of reversible MAO-B inhibitors. In the present study, 3-coumaranone derivatives were thus synthesised and evaluated as potential MAO-A and MAO-B inhibitors. By reacting 6-hydroxy-3-coumaranone with the appropriate alkylbromide in N,N-dimethylformamide in the presence of potassium carbonate, a series of twenty 3-coumaranone derivatives were synthesised. The structures of the compounds were verified with NMR spectroscopy and mass spectrometry. The purities of the compounds were determined by HPLC analyses. To determine the inhibition potencies, the recombinant human MAO-A and MAO-B enzymes were used, and the inhibition potencies were expressed as IC50 values. The results indicated that the 3-coumaranone derivatives are highly potent MAO-B inhibitors. For example, 9 of the 3-coumaranone derivatives inhibited MAO-B with IC50 values < 0.05 μM, with the most potent inhibitor exhibiting an IC50 value of 0.004 μM. Although the 3-coumaranone derivatives are selective MAO-B inhibitors, some compounds were also potent MAO-A inhibitors with the most potent inhibitor exhibiting an IC50 value of 0.586 μM. The reversibility of MAO-B inhibition by a representative inhibitor was examined by measuring the degree to which the enzyme activity recovers after dialysis of the enzyme-inhibitor complex. Since MAO-B activity was almost completely recovered after dialysis, it may be concluded that the 3-coumaranone derivatives bind reversibly to MAO-B. Lineweaver-Burk plots were constructed to show that the…

Subjects/Keywords: Parkinson’s disease; Monoamine oxidase; Inhibitors; Reversible; 3-Coumaranone; Parkinson se siekte; Monoamienoksidase; Inhibeerders; Omkeerbaar; 3-Kumaranoon

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APA (6^th Edition):

Van Dyk, A. S. (2014). Synthesis and biological evaluation of 6-substituted coumaranone derivatives and related compounds as monoamine oxidase inhibitors / Adriaan Sarel van Dyk . (Thesis). North-West University. Retrieved from http://hdl.handle.net/10394/16548

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Van Dyk, Adriaan Sarel. “Synthesis and biological evaluation of 6-substituted coumaranone derivatives and related compounds as monoamine oxidase inhibitors / Adriaan Sarel van Dyk .” 2014. Thesis, North-West University. Accessed March 07, 2021. http://hdl.handle.net/10394/16548.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Van Dyk, Adriaan Sarel. “Synthesis and biological evaluation of 6-substituted coumaranone derivatives and related compounds as monoamine oxidase inhibitors / Adriaan Sarel van Dyk .” 2014. Web. 07 Mar 2021.

Vancouver:

Van Dyk AS. Synthesis and biological evaluation of 6-substituted coumaranone derivatives and related compounds as monoamine oxidase inhibitors / Adriaan Sarel van Dyk . [Internet] [Thesis]. North-West University; 2014. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10394/16548.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Van Dyk AS. Synthesis and biological evaluation of 6-substituted coumaranone derivatives and related compounds as monoamine oxidase inhibitors / Adriaan Sarel van Dyk . [Thesis]. North-West University; 2014. Available from: http://hdl.handle.net/10394/16548

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

North-West University

14. Robinson, Sarel Johannes. Syntheses of chalcones and 2-aminopyrimidines and their evaluation as monoamine oxidase inhibitors and as adenosine receptor antagonists / Sarel Johannes Robinson .

Degree: 2013, North-West University

URL: http://hdl.handle.net/10394/9534

► Background and rationale - Parkinson’s disease is a neurodegenerative disorder characterised by reduced levels of dopamine in the brain. The cause of Parkinson's disease is… (more)

▼ Background and rationale - Parkinson’s disease is a neurodegenerative disorder characterised by reduced levels of dopamine in the brain. The cause of Parkinson's disease is still unknown; however several theories pertaining to the etiology exist. Current treatment mainly aims at dopamine replacement, with agents such as levodopa and dopamine agonists that provide patients with symptomatic relief. This relief is unfortunately only temporary as the progression of the disease is not halted. Furthermore, these therapies are associated with a range of side effects and novel approaches to the treatment are thus urgently required. Adenosine A2A receptor antagonists recently emerged as a promising non-dopaminergic alternative, not only as symptomatic treatment, but also as potential neuroprotective therapy. Adenosine A2A receptors are co-localised with dopamine D2 receptors in the striatum and other nuclei of the basal ganglia. Adenosine A2A stimulation decreases the affinity of dopamine for the D2 receptor, and increase cyclic AMP (cAMP) levels. The stimulation of dopamine D2 receptors, in contrast, decreases cAMP levels and therefore these receptors (A2A and D2), act in an opposing manner. Adenosine A2A antagonism will thus have similar effects as dopamine D2 agonism and will reduce the postsynaptic effects of dopamine depletion to give symptomatic relief. There are also several mechanisms where by adenosine A2A antagonists may be neuroprotective, for example by preventing glutamate excitotoxicity, that may cause damage to dopaminergic neurons. A number of adenosine A2A antagonists have already reached clinical trials and promising results were obtained, especially when combined with levodopa. Consequently, A2A antagonists are realistic prospects that have therapeutic potential in diseases with dopaminergic hypofunction, like Parkinson's disease. Many of the current A2A antagonists contain an amino-substituted heterocyclic scaffold, such as an aminopyrimidine. The primary aim of this study was the design, synthesis and evaluation of 2-aminopyrimidine derivatives as adenosine A2A receptor antagonists. Monoamine oxidase B (MAO-B) inhibitors are also promising candidates for the symptomatic treatment of Parkinson's disease, since MAO-B is the enzyme primarily responsible for the catabolism of dopamine in the brain. Irreversible inhibitors of MAO-B, such as selegeline and rasagiline, have been used clinically for the treatment of Parkinson's disease. This type of inhibition comes with certain disadvantages as it may take up to several weeks after termination of treatment for the enzyme activity to recover. Reversible inhibitors in contrast will have much better safety profiles seeing that they will not inactivate the enzyme permanently and allow for competition with the substrate. When dopamine is oxidized by MAO, toxic metabolic by-products, such as hydrogen peroxide (H2O2) forms, and this is believed to be a possible cause of Parkinson's disease. MAO-B inhibitors will therefore not only…

Subjects/Keywords: 2-Aminopyrimidines; Adenosine A2A antagonists; Chalcones; Monoamine oxidase inhibitors; 2-Aminopirimidiene; Adenosien A2A antagonisme; Chalkone; Monoamienoksidaseremmers

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APA (6^th Edition):

Robinson, S. J. (2013). Syntheses of chalcones and 2-aminopyrimidines and their evaluation as monoamine oxidase inhibitors and as adenosine receptor antagonists / Sarel Johannes Robinson . (Thesis). North-West University. Retrieved from http://hdl.handle.net/10394/9534

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Robinson, Sarel Johannes. “Syntheses of chalcones and 2-aminopyrimidines and their evaluation as monoamine oxidase inhibitors and as adenosine receptor antagonists / Sarel Johannes Robinson .” 2013. Thesis, North-West University. Accessed March 07, 2021. http://hdl.handle.net/10394/9534.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Robinson, Sarel Johannes. “Syntheses of chalcones and 2-aminopyrimidines and their evaluation as monoamine oxidase inhibitors and as adenosine receptor antagonists / Sarel Johannes Robinson .” 2013. Web. 07 Mar 2021.

Vancouver:

Robinson SJ. Syntheses of chalcones and 2-aminopyrimidines and their evaluation as monoamine oxidase inhibitors and as adenosine receptor antagonists / Sarel Johannes Robinson . [Internet] [Thesis]. North-West University; 2013. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10394/9534.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Robinson SJ. Syntheses of chalcones and 2-aminopyrimidines and their evaluation as monoamine oxidase inhibitors and as adenosine receptor antagonists / Sarel Johannes Robinson . [Thesis]. North-West University; 2013. Available from: http://hdl.handle.net/10394/9534

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

North-West University

15. Mentz, Wayne. Novel sulfanyl- and sulfinylcaffeine analogues as inhibitors of monoamine oxidase / Wayne Mentz .

Degree: 2013, North-West University

URL: http://hdl.handle.net/10394/9521

► Parkinson’s disease (PD) is a neurodegenerative disorder, which is progressive in nature and usually associated with the elderly. It is the second most common age-related… (more)

▼ Parkinson’s disease (PD) is a neurodegenerative disorder, which is progressive in nature and usually associated with the elderly. It is the second most common age-related neurodegenerative disorder after Alzheimer’s disease (AD). PD occurs when there is a dramatic loss of dopamine (DA) in the striatum, a substructure of the basal ganglia, of the brain due to the degeneration of the nigrostriatal pathway that contains the dopaminergic neurons. Motor symptoms of PD include bradykinesia, muscular rigidity and resting tremors. Non-motor symptoms include speech and sleep problems, hallucinations and depression. Diverse treatment options are available to treat the symptoms of PD, including levodopa (L-Dopa), DA agonists and monoamine oxidase B (MAO-B) inhibitors. The MAOs are flavoproteins that are bound to the outer membrane of the mitochondria and catalyze the oxidative deamination of neurotransmitters such as serotonin (5-HT), noradrenaline (NA) and DA. Two isoforms occur, namely MAO-A and –B, which share a 70% sequence identity. MAO-A catalyzes the oxidation of 5-HT and MAO-B has a substrate specificity towards benzylamine and 2-phenylethylamine. DA, NA, adrenaline and tryptamine are oxidized by both forms. MAO-A plays an important role in depression while MAO-B plays an important role in PD. The two isoforms are not evenly distributed in the brain. Of particular relevance to PD is the observation that, in the basal ganglia, MAO-B is the predominant form and the oxidation of DA in this region is largely due to MAO-B activity. Also, with an increase in age, there is an up to fourfold increase in MAO-B activity in the brain. In the aged parkinsonian brain, MAO-B is therefore a major DA metabolizing enzyme and MAO-B inhibitors have an important role in the therapy of PD. MAO-B inhibitors may potentially reduce the metabolic destruction of DA and thereby provide relief from the symptoms of PD. MAO-B inhibitors may also exert a neuroprotective effect in PD. In the catalytic cycle of MAO-B, one mole each of an aldehyde, hydrogen peroxide and ammonia are formed for each mole of primary amine substrate oxidized. Ferrous iron, which is abundant in the basal ganglia, may react with the hydrogen peroxide to form hydroxyl radicals in the Fenton reaction. The hydroxyl radical damages virtually all types of biomolecules including proteins, DNA, lipids, carbohydrates and amino acids. The aldehyde, in turn, may react with amino groups of proteins, and thus lead to cell injury. Inhibitors of MAO-B may reduce the MAO-catalyzed formation of hydrogen peroxide and aldehydes in the basal ganglia, and thus act as neuroprotective agents. MAO-B inhibitors that are currently being used in the treatment of PD are selegiline and rasagiline. Both are irreversible inhibitors of MAO-B. While irreversible inhibitors of MAO have been used extensively as drugs, irreversible inhibition has a number of disadvantages. These include the loss of selectivity as a result of repeated drug administration and a slow and variable …

Subjects/Keywords: 8-Sulfanylcaffeine analogues; 8-sulfinylcaffeine analogues; Caffeine; Monoamine oxidase inhibitors; Parkinson’s disease; 8-sulfanielkafeïen-analoë; 8-sulfinielkafeïen-analoë; Kafeïen; Monoamien oksidase inhibeerders; Parkinson se siekte

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Mentz, W. (2013). Novel sulfanyl- and sulfinylcaffeine analogues as inhibitors of monoamine oxidase / Wayne Mentz . (Thesis). North-West University. Retrieved from http://hdl.handle.net/10394/9521

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Mentz, Wayne. “Novel sulfanyl- and sulfinylcaffeine analogues as inhibitors of monoamine oxidase / Wayne Mentz .” 2013. Thesis, North-West University. Accessed March 07, 2021. http://hdl.handle.net/10394/9521.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Mentz, Wayne. “Novel sulfanyl- and sulfinylcaffeine analogues as inhibitors of monoamine oxidase / Wayne Mentz .” 2013. Web. 07 Mar 2021.

Vancouver:

Mentz W. Novel sulfanyl- and sulfinylcaffeine analogues as inhibitors of monoamine oxidase / Wayne Mentz . [Internet] [Thesis]. North-West University; 2013. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10394/9521.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Mentz W. Novel sulfanyl- and sulfinylcaffeine analogues as inhibitors of monoamine oxidase / Wayne Mentz . [Thesis]. North-West University; 2013. Available from: http://hdl.handle.net/10394/9521

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

University of Alberta

16. Kwan, Eva. A novel deprenyl analogue, N-methyl, N-propargyl-2-phenylethylamine (MPPE), increases neuronal cell survival in thiamine deficiency encephalopathy.

Degree: MSin Psychiatry, Department of Psychiatry, 2002, University of Alberta

URL: https://era.library.ualberta.ca/files/kk91fp06v

Subjects/Keywords: Cell death – Prevention.; Brain chemistry.; Wernicke's encephalopathy – Chemotherapy.; Brain – Cytopathology.; Monoamine oxidase – Inhibitors – Therapeutic use.

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Kwan, E. (2002). A novel deprenyl analogue, N-methyl, N-propargyl-2-phenylethylamine (MPPE), increases neuronal cell survival in thiamine deficiency encephalopathy. (Masters Thesis). University of Alberta. Retrieved from https://era.library.ualberta.ca/files/kk91fp06v

Chicago Manual of Style (16^th Edition):

Kwan, Eva. “A novel deprenyl analogue, N-methyl, N-propargyl-2-phenylethylamine (MPPE), increases neuronal cell survival in thiamine deficiency encephalopathy.” 2002. Masters Thesis, University of Alberta. Accessed March 07, 2021. https://era.library.ualberta.ca/files/kk91fp06v.

MLA Handbook (7^th Edition):

Kwan, Eva. “A novel deprenyl analogue, N-methyl, N-propargyl-2-phenylethylamine (MPPE), increases neuronal cell survival in thiamine deficiency encephalopathy.” 2002. Web. 07 Mar 2021.

Vancouver:

Kwan E. A novel deprenyl analogue, N-methyl, N-propargyl-2-phenylethylamine (MPPE), increases neuronal cell survival in thiamine deficiency encephalopathy. [Internet] [Masters thesis]. University of Alberta; 2002. [cited 2021 Mar 07]. Available from: https://era.library.ualberta.ca/files/kk91fp06v.

Council of Science Editors:

Kwan E. A novel deprenyl analogue, N-methyl, N-propargyl-2-phenylethylamine (MPPE), increases neuronal cell survival in thiamine deficiency encephalopathy. [Masters Thesis]. University of Alberta; 2002. Available from: https://era.library.ualberta.ca/files/kk91fp06v

North-West University

17. Engelbrecht, Idalet. Synthesis and evaluation of sesamol derivatives as inhibitors of monoamine oxidase / Idalet Engelbrecht .

Degree: 2014, North-West University

URL: http://hdl.handle.net/10394/15218

► Parkinson’s disease is an age-related neurodegenerative disorder. The major symptoms of Parkinson’s disease are closely linked to the pathology of the disease. The main pathology… (more)

▼ Parkinson’s disease is an age-related neurodegenerative disorder. The major symptoms of Parkinson’s disease are closely linked to the pathology of the disease. The main pathology of Parkinson’s disease consists of the degeneration of neurons of the substantia nigra pars compacta (SNpc), which leads to reduced amounts of dopamine in the brain. One of the treatment strategies in Parkinson’s disease is to conserve dopamine by inhibiting the enzymes responsible for its catabolism. The monoamine oxidase (MAO) B isoform catalyses the oxidation of dopamine in the central nervous system and is therefore an important target for Parkinson’s disease treatment. Inhibition of MAO-B provides symptomatic relief for Parkinson’s disease patients by increasing endogenous dopamine levels as well as enhancing the levels of dopamine after administration of levodopa (L-dopa), the metabolic precursor of dopamine. Recent studies have shown that phthalide can be used as a scaffold for the design of reversible MAO inhibitors. Although phthalide is a weak MAO-B inhibitor, substitution on the C5 position of phthalide yields highly potent reversible MAO-B inhibitors. In the present study, sesamol and benzodioxane were used as scaffolds for the design of MAO inhibitors. The structures of sesamol and benzodioxane closely resemble that of phthalide, which suggests that these moieties may be useful for the design of MAO inhibitors. This study may be viewed as an exploratory study to discover new scaffolds for MAO inhibition. Since substitution at C5 of phthalide with a benzyloxy side chain yielded particularly potent MAO inhibitors, the sesamol and benzodioxane derivatives possessed the benzyloxy substituent in the analogous positions to C5 of phthalide. These were the C5 and C6 positions of sesamol and benzodioxane, respectively. The sesamol and benzodioxane derivatives were synthesised by reacting sesamol and 6- hydroxy-1,4-benzodioxane, respectively, with an appropriate alkyl bromide in the presence of potassium carbonate (K2CO3) in N,N-dimethylformamide (DMF). 6-Hydroxy-1,4- benzodioxane, in turn, was synthesised from 1,4-benzodioxan-6-carboxaldehyde. The structures of the compounds were verified with nuclear magnetic resonance (NMR) and mass spectrometry (MS) analyses, while the purities were estimated by high-pressure liquid chromatography (HPLC). Sixteen sesamol and benzodioxane derivatives were synthesised. To determine the inhibition potencies of the synthesised compounds the recombinant human MAO-A and MAO-B enzymes were used. The inhibition potencies were expressed as the corresponding IC50 values. The results showed that the sesamol and benzodioxane derivatives are highly potent and selective inhibitors of MAO-B and to a lesser extent MAOA. The most potent MAO-B inhibitor was 6-(3-bromobenzyloxy)-1,4-benzodioxane with an IC50 value of 0.045 μM. All compounds examined displayed selectivity for the MAO-B isoform over MAO-A. Generally the benzodioxane derivatives were found to be more potent inhibitors of…

Subjects/Keywords: Parkinson’s disease; Substantia nigra pars compacta (SNpc); Dopamine; Monoamine oxidase (MAO); MAO-A; MAO-B; Levodopa (L-dopa); Phthalide; Sesamol; Benzodioxane; MAO-B inhibitors; Inhibition potencies; IC50 values; Dialysis; Reversibility; Lineweaver-Burk plots; Competitive mode of inhibition

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Engelbrecht, I. (2014). Synthesis and evaluation of sesamol derivatives as inhibitors of monoamine oxidase / Idalet Engelbrecht . (Thesis). North-West University. Retrieved from http://hdl.handle.net/10394/15218

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Engelbrecht, Idalet. “Synthesis and evaluation of sesamol derivatives as inhibitors of monoamine oxidase / Idalet Engelbrecht .” 2014. Thesis, North-West University. Accessed March 07, 2021. http://hdl.handle.net/10394/15218.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Engelbrecht, Idalet. “Synthesis and evaluation of sesamol derivatives as inhibitors of monoamine oxidase / Idalet Engelbrecht .” 2014. Web. 07 Mar 2021.

Vancouver:

Engelbrecht I. Synthesis and evaluation of sesamol derivatives as inhibitors of monoamine oxidase / Idalet Engelbrecht . [Internet] [Thesis]. North-West University; 2014. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10394/15218.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Engelbrecht I. Synthesis and evaluation of sesamol derivatives as inhibitors of monoamine oxidase / Idalet Engelbrecht . [Thesis]. North-West University; 2014. Available from: http://hdl.handle.net/10394/15218

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Michigan State University

18. Xu, Zhen. Preparation of thioalkyl substituted small ring nitrogen heterocycles and 5-disubstituted-ethyl-2-oxazolidinones for antibacterial and antiviral candidacy.

Degree: MS, Department of Chemistry, 2004, Michigan State University

URL: http://etd.lib.msu.edu/islandora/object/etd:33296

Subjects/Keywords: Drug resistance; Bacteria – Effect of drugs on; Bacterial diseases – Effect of drugs on; Monoamine oxidase; Enzyme inhibitors

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Xu, Z. (2004). Preparation of thioalkyl substituted small ring nitrogen heterocycles and 5-disubstituted-ethyl-2-oxazolidinones for antibacterial and antiviral candidacy. (Masters Thesis). Michigan State University. Retrieved from http://etd.lib.msu.edu/islandora/object/etd:33296

Chicago Manual of Style (16^th Edition):

Xu, Zhen. “Preparation of thioalkyl substituted small ring nitrogen heterocycles and 5-disubstituted-ethyl-2-oxazolidinones for antibacterial and antiviral candidacy.” 2004. Masters Thesis, Michigan State University. Accessed March 07, 2021. http://etd.lib.msu.edu/islandora/object/etd:33296.

MLA Handbook (7^th Edition):

Xu, Zhen. “Preparation of thioalkyl substituted small ring nitrogen heterocycles and 5-disubstituted-ethyl-2-oxazolidinones for antibacterial and antiviral candidacy.” 2004. Web. 07 Mar 2021.

Vancouver:

Xu Z. Preparation of thioalkyl substituted small ring nitrogen heterocycles and 5-disubstituted-ethyl-2-oxazolidinones for antibacterial and antiviral candidacy. [Internet] [Masters thesis]. Michigan State University; 2004. [cited 2021 Mar 07]. Available from: http://etd.lib.msu.edu/islandora/object/etd:33296.

Council of Science Editors:

Xu Z. Preparation of thioalkyl substituted small ring nitrogen heterocycles and 5-disubstituted-ethyl-2-oxazolidinones for antibacterial and antiviral candidacy. [Masters Thesis]. Michigan State University; 2004. Available from: http://etd.lib.msu.edu/islandora/object/etd:33296

19. 山本, 梓司. Protective and therapeutic role of 2-carba-cyclic phosphatidic acid in demyelinating disease. : 脱髄性疾患における環状ホスファチジン酸誘導体の脱髄抑制及び治療効果.

Degree: 博士(医学), 2018, Saitama Medical University / 埼玉医科大学

URL: http://id.nii.ac.jp/1386/00000615/

►

Multiple sclerosis is a neuroinflammatory demyelinating and neurodegenerative disease of the central nervous system characterized by recurrent and progressive demyelination/remyelination cycles, neuroinflammation, oligodendrocyte loss, demyelination,… (more)

▼

Multiple sclerosis is a neuroinflammatory demyelinating and neurodegenerative disease of the central nervous system characterized by recurrent and progressive demyelination/remyelination cycles, neuroinflammation, oligodendrocyte loss, demyelination, and axonal degeneration. Cyclic phosphatidic acid (cPA) is a natural phospholipid mediator with a unique cyclic phosphate ring structure at the sn-2 and sn-3 positions of the glycerol backbone. We reported earlier that cPA elicits a neurotrophin-like action and protects hippocampal neurons from ischemia-induced delayed neuronal death. We designed, chemically synthesized, and metabolically stabilized derivatives of cPA: 2-carba-cPA (2ccPA), a synthesized compound in which one of the phosphate oxygen molecules is replaced with a methylene group at the sn-2 position. In the present study, we investigated whether 2ccPA exerts protective effects in oligodendrocytes and suppresses pathology in the two most common mouse models of multiple sclerosis.

To evaluate whether 2ccPA has potential beneficial effects on the pathology of multiple sclerosis, we investigated the effects of 2ccPA on oligodendrocyte cell death in vitro and administrated 2ccPA to mouse models of experimental autoimmune encephalomyelitis (EAE) and cuprizone-induced demyelination.

We demonstrated that 2ccPA suppressed the CoCl

-induced increase in the Bax/Bcl-2 protein expression ratio and phosphorylation levels of p38MAPK and JNK protein. 2ccPA treatment reduced cuprizone-induced demyelination, microglial activation, NLRP3 inflammasome, and motor dysfunction. Furthermore, 2ccPA treatment reduced autoreactive T cells and macrophages, spinal cord injury, and pathological scores in EAE, the autoimmune multiple sclerosis mouse model.

We demonstrated that 2ccPA protected oligodendrocytes via suppression of the mitochondrial apoptosis pathway. Also, we found beneficial effects of 2ccPA in the multiperiod of cuprizone-induced demyelination and the pathology of EAE. These data indicate that 2ccPA may be a promising compound for the development of new drugs to treat demyelinating disease and ameliorate the symptoms of multiple sclerosis.

平成29年度

Subjects/Keywords: Animals; Anti-Inflammatory Agents; Apoptosis; Cell Differentiation; Cell Line, Transformed; Cuprizone; Demyelinating Diseases; Disease Models, Animal; Female; Gene Expression Regulation; Humans; MAP Kinase Signaling System; Male; Mice; Mice, Inbred C57BL; Monoamine Oxidase Inhibitors; Myelin Sheath; NLR Family, Pyrin Domain-Containing 3 Protein; Phosphatidic Acids; Proto-Oncogene Proteins c-bcl-2; p38 Mitogen-Activated Protein Kinases

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APA (6^th Edition):

山本, �. (2018). Protective and therapeutic role of 2-carba-cyclic phosphatidic acid in demyelinating disease. : 脱髄性疾患における環状ホスファチジン酸誘導体の脱髄抑制及び治療効果. (Thesis). Saitama Medical University / 埼玉医科大学. Retrieved from http://id.nii.ac.jp/1386/00000615/

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

山本, 梓司. “Protective and therapeutic role of 2-carba-cyclic phosphatidic acid in demyelinating disease. : 脱髄性疾患における環状ホスファチジン酸誘導体の脱髄抑制及び治療効果.” 2018. Thesis, Saitama Medical University / 埼玉医科大学. Accessed March 07, 2021. http://id.nii.ac.jp/1386/00000615/.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

山本, 梓司. “Protective and therapeutic role of 2-carba-cyclic phosphatidic acid in demyelinating disease. : 脱髄性疾患における環状ホスファチジン酸誘導体の脱髄抑制及び治療効果.” 2018. Web. 07 Mar 2021.

Vancouver:

山本 �. Protective and therapeutic role of 2-carba-cyclic phosphatidic acid in demyelinating disease. : 脱髄性疾患における環状ホスファチジン酸誘導体の脱髄抑制及び治療効果. [Internet] [Thesis]. Saitama Medical University / 埼玉医科大学; 2018. [cited 2021 Mar 07]. Available from: http://id.nii.ac.jp/1386/00000615/.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

山本 �. Protective and therapeutic role of 2-carba-cyclic phosphatidic acid in demyelinating disease. : 脱髄性疾患における環状ホスファチジン酸誘導体の脱髄抑制及び治療効果. [Thesis]. Saitama Medical University / 埼玉医科大学; 2018. Available from: http://id.nii.ac.jp/1386/00000615/

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

University of Debrecen

20. Mohammad ali, Bahmaei. Pharmacotherapy of Parkinson`s disease .

Degree: DE – Általános Orvostudományi Kar, University of Debrecen

URL: http://hdl.handle.net/2437/233607

► There are several drugs which are effective in symptomatic management of Parkinson`s disease However there is no definitive pharmaceutical therapy for Parkinson`s disease. Drugs used… (more)

Subjects/Keywords: Pharmacotherapy; Parkinson`s disease; dopaminergic agents; monoamine oxidase type B inhibitors; catecholo-methyltransferase; Freezing of gait; wearing-off; dystonias; dyskinesias; nonmotor complications

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APA (6^th Edition):

Mohammad ali, B. (n.d.). Pharmacotherapy of Parkinson`s disease . (Thesis). University of Debrecen. Retrieved from http://hdl.handle.net/2437/233607

Note: this citation may be lacking information needed for this citation format:
No year of publication.
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Mohammad ali, Bahmaei. “Pharmacotherapy of Parkinson`s disease .” Thesis, University of Debrecen. Accessed March 07, 2021. http://hdl.handle.net/2437/233607.

Note: this citation may be lacking information needed for this citation format:
No year of publication.
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Mohammad ali, Bahmaei. “Pharmacotherapy of Parkinson`s disease .” Web. 07 Mar 2021.

Note: this citation may be lacking information needed for this citation format:
No year of publication.

Vancouver:

Mohammad ali B. Pharmacotherapy of Parkinson`s disease . [Internet] [Thesis]. University of Debrecen; [cited 2021 Mar 07]. Available from: http://hdl.handle.net/2437/233607.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation
No year of publication.

Council of Science Editors:

Mohammad ali B. Pharmacotherapy of Parkinson`s disease . [Thesis]. University of Debrecen; Available from: http://hdl.handle.net/2437/233607

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation
No year of publication.

North-West University

21. Ogunrombi, Modupe Olufunmilayo. The synthesis and evaluation of 1-methyl-3-pyrrolines and 1-methylpyrroles as substrates and inhibitors of monoamine oxidase B / Modupe O. Ogunrombi .

Degree: 2007, North-West University

URL: http://hdl.handle.net/10394/1837

► Very little is known about why and how the Parkinson's disease (PD) neurodegenerative process begins and progresses. In the course of developments for treatment of… (more)

Subjects/Keywords: Monoamine oxidase B; MPTP; 1-methyl-3-phenyl-3-pyrroline; 1-methyl-3-phenyl-3-pyrrole; Neurotoxicity; Dopamine; Striata; Reversible inhibitors; Competitive inhibition; Structure-activity relationship

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APA (6^th Edition):

Ogunrombi, M. O. (2007). The synthesis and evaluation of 1-methyl-3-pyrrolines and 1-methylpyrroles as substrates and inhibitors of monoamine oxidase B / Modupe O. Ogunrombi . (Thesis). North-West University. Retrieved from http://hdl.handle.net/10394/1837

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Ogunrombi, Modupe Olufunmilayo. “The synthesis and evaluation of 1-methyl-3-pyrrolines and 1-methylpyrroles as substrates and inhibitors of monoamine oxidase B / Modupe O. Ogunrombi .” 2007. Thesis, North-West University. Accessed March 07, 2021. http://hdl.handle.net/10394/1837.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Ogunrombi, Modupe Olufunmilayo. “The synthesis and evaluation of 1-methyl-3-pyrrolines and 1-methylpyrroles as substrates and inhibitors of monoamine oxidase B / Modupe O. Ogunrombi .” 2007. Web. 07 Mar 2021.

Vancouver:

Ogunrombi MO. The synthesis and evaluation of 1-methyl-3-pyrrolines and 1-methylpyrroles as substrates and inhibitors of monoamine oxidase B / Modupe O. Ogunrombi . [Internet] [Thesis]. North-West University; 2007. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/10394/1837.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Ogunrombi MO. The synthesis and evaluation of 1-methyl-3-pyrrolines and 1-methylpyrroles as substrates and inhibitors of monoamine oxidase B / Modupe O. Ogunrombi . [Thesis]. North-West University; 2007. Available from: http://hdl.handle.net/10394/1837

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

ETH Zürich

22. Bürgi, Sibylle Carmen. Antidepressiva-induzierte β-Adrenozeptor-Downregulation: Biochemische, molekularbiologische und konfokalmikroskopische Untersuchungen.

Degree: 2001, ETH Zürich

URL: http://hdl.handle.net/20.500.11850/145391

Subjects/Keywords: BETA-ADRENERGE REZEPTOREN (NEUROLOGIE); GENREGULATION, REGULATION DER GENEXPRESSION (MOLEKULARBIOLOGIE); ANTIDEPRESSIVA + MONOAMIN-OXIDASE HEMMER (PHARMAZIE); PHOSPHOLIPASEN (ENZYME); ZELLMEMBRAN (CYTOLOGIE); BETA ADRENERGIC RECEPTORS (NEUROLOGY); GENE REGULATION, REGULATION OF GENE-EXPRESSION (MOLECULAR BIOLOGY); ANTIDEPRESSIVES + MONOAMINE-OXYDASE INHIBITORS (PHARMACY); PHOSPHOLIPASES (ENZYMES); CELL MEMBRANE (CYTOLOGY); info:eu-repo/classification/ddc/570; Life sciences

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APA (6^th Edition):

Bürgi, S. C. (2001). Antidepressiva-induzierte β-Adrenozeptor-Downregulation: Biochemische, molekularbiologische und konfokalmikroskopische Untersuchungen. (Doctoral Dissertation). ETH Zürich. Retrieved from http://hdl.handle.net/20.500.11850/145391

Chicago Manual of Style (16^th Edition):

Bürgi, Sibylle Carmen. “Antidepressiva-induzierte β-Adrenozeptor-Downregulation: Biochemische, molekularbiologische und konfokalmikroskopische Untersuchungen.” 2001. Doctoral Dissertation, ETH Zürich. Accessed March 07, 2021. http://hdl.handle.net/20.500.11850/145391.

MLA Handbook (7^th Edition):

Bürgi, Sibylle Carmen. “Antidepressiva-induzierte β-Adrenozeptor-Downregulation: Biochemische, molekularbiologische und konfokalmikroskopische Untersuchungen.” 2001. Web. 07 Mar 2021.

Vancouver:

Bürgi SC. Antidepressiva-induzierte β-Adrenozeptor-Downregulation: Biochemische, molekularbiologische und konfokalmikroskopische Untersuchungen. [Internet] [Doctoral dissertation]. ETH Zürich; 2001. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/20.500.11850/145391.

Council of Science Editors:

Bürgi SC. Antidepressiva-induzierte β-Adrenozeptor-Downregulation: Biochemische, molekularbiologische und konfokalmikroskopische Untersuchungen. [Doctoral Dissertation]. ETH Zürich; 2001. Available from: http://hdl.handle.net/20.500.11850/145391

ETH Zürich

23. Scheidegger, Milan. Exploring the antidepressant effects of ketamine: Insights from multimodal neuroimaging.

Degree: 2015, ETH Zürich

URL: http://hdl.handle.net/20.500.11850/109942

Subjects/Keywords: SCHLAFMITTEL + HYPNOTIKA (PHARMAZIE); ANALGESICS + ANTIPYRETRICS (PHARMACY); ANALGETIKA + ANTIPYRETIKA (PHARMAZIE); EXPERIMENTS ON HUMAN BEINGS AND CLINICAL TRIALS (MEDICINE); SOPORIFICS + HYPNOTICS (PHARMACY); PHARMAKODYNAMIK + ARZNEIMITTELWIRKUNG (PHARMAKOLOGIE); ANTIDEPRESSIVA + MONOAMIN-OXIDASE HEMMER (PHARMAZIE); VERSUCHE AN MENSCHEN UND KLINISCHE STUDIEN (MEDIZIN); PHARMACODYNAMICS + DRUG ACTION (PHARMACOLOGY); ANTIDEPRESSIVES + MONOAMINE-OXYDASE INHIBITORS (PHARMACY); info:eu-repo/classification/ddc/610; Medical sciences, medicine

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Scheidegger, M. (2015). Exploring the antidepressant effects of ketamine: Insights from multimodal neuroimaging. (Doctoral Dissertation). ETH Zürich. Retrieved from http://hdl.handle.net/20.500.11850/109942

Chicago Manual of Style (16^th Edition):

Scheidegger, Milan. “Exploring the antidepressant effects of ketamine: Insights from multimodal neuroimaging.” 2015. Doctoral Dissertation, ETH Zürich. Accessed March 07, 2021. http://hdl.handle.net/20.500.11850/109942.

MLA Handbook (7^th Edition):

Scheidegger, Milan. “Exploring the antidepressant effects of ketamine: Insights from multimodal neuroimaging.” 2015. Web. 07 Mar 2021.

Vancouver:

Scheidegger M. Exploring the antidepressant effects of ketamine: Insights from multimodal neuroimaging. [Internet] [Doctoral dissertation]. ETH Zürich; 2015. [cited 2021 Mar 07]. Available from: http://hdl.handle.net/20.500.11850/109942.

Council of Science Editors:

Scheidegger M. Exploring the antidepressant effects of ketamine: Insights from multimodal neuroimaging. [Doctoral Dissertation]. ETH Zürich; 2015. Available from: http://hdl.handle.net/20.500.11850/109942

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