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https://www.readbyqxmd.com/read/28342849/comparative-effects-of-etoh-consumption-and-thiamine-deficiency-on-cognitive-impairment-oxidative-damage-and-%C3%AE-amyloid-peptide-overproduction-in-the-brain
#1
Yu-Shi Gong, Kun Hu, Lu-Qi Yang, Juan Guo, Yong-Qing Gao, Feng-Lin Song, Fang-Li Hou, Cui-Yi Liang
The effects of chronic EtOH consumption, associated or not with thiamine deficiency (TD), on cognitive impairment, oxidative damage, and β-amyloid (Aβ) peptide accumulation in the brain were investigated in male C57BL/6 mice. We established an alcoholic mouse model by feeding an EtOH liquid diet, a TD mouse model by feeding a thiamine-depleted liquid diet, and an EtOH treatment associated with TD mouse model by feeding a thiamine-depleted EtOH liquid diet for 7 weeks. The learning and memory functions of the mice were detected through the Y-maze test...
March 22, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28332824/indole-substituted-benzothiazoles-and-benzoxazoles-as-selective-and-reversible-mao-b-inhibitors-for-treatment-of-parkinson-s-disease
#2
Min-Ho Nam, Moosung Park, Hyeri Park, Youngjae Kim, Seulki Yoon, Vikram Shahaji Sawant, Ji Won Choi, Jong-Hyun Park, Ki Duk Park, Sun-Joon Min, Changjoon Justin Lee, Hyunah Choo
To develop a novel, selective, and reversible MAO-B inhibitors for safer treatment of Parkinson's disease, benzothiazole and benzoxazole derivatives with indole moiety were designed and synthesized. Most of the synthesized compounds showed inhibitory activities against MAO-B and selectivity over MAO-A. The most active compound was Compound 5b, 6-fluoro-2-(1-methyl-1H-indol-5-yl)benzo[d]thiazole with an IC50 value of 29 nM with no apparent effect on MAO-A activity at 10 M. Based on the reversibility assay, Compound 5b turned out to be a fully reversible with over 95% of recovery of enzyme activity after washout of the compound...
March 23, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28320274/brain-mitochondrial-subproteome-of-rpn10-binding-proteins-and-its-changes-induced-by-the-neurotoxin-mptp-and-the-neuroprotector-isatin
#3
A E Medvedev, O A Buneeva, A T Kopylov, O V Tikhonova, M V Medvedeva, L N Nerobkova, I G Kapitsa, V G Zgoda
Mitochondria play an important role in molecular mechanisms of neuroplasticity, adaptive changes of the brain that occur in the structure and function of its cells in response to altered physiological conditions or development of pathological disorders. Mitochondria are a crucial target for actions of neurotoxins, causing symptoms of Parkinson's disease in various experimental animal models, and also neuroprotectors. Good evidence exists in the literature that mitochondrial dysfunction induced by the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) influences functioning of the ubiquitin-proteasomal system (UPS) responsible for selective proteolytic degradation of proteins from various intracellular compartments (including mitochondria), and neuroprotective effects of certain antiparkinsonian agents (monoamine oxidase inhibitors) may be associated with their effects on UPS...
March 2017: Biochemistry. Biokhimii︠a︡
https://www.readbyqxmd.com/read/28320234/gelidiella-acerosa-protects-against-a%C3%AE-25-35-induced-toxicity-and-memory-impairment-in-swiss-albino-mice-an-in-vivo-report
#4
Syad Arif Nisha, Kasi Pandima Devi
CONTEXT: Alzheimer's disease (AD) is believed to develop due to deposition of β-amyloid (Aβ) peptide. Hence, efforts are being made to develop potent drug that target amyloid hypothesis. OBJECTIVE: The present study explores the effect of the seaweed Gelidiella acerosa (Forsskål) Feldmann & Hamel (Gelidiellaceae) against Aβ 25-35 peptide in Swiss albino mice. MATERIALS AND METHODS: The animals were administered through intracerebroventricular (ICV) injection with the Aβ 25-35 peptide (10 μg/10 μL/ICV site) on 21st day of the pretreatment of G...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28302559/in-vitro-monoamine-oxidase-inhibition-potential-of-alpha-methyltryptamine-analog-new-psychoactive-substances-for-assessing-possible-toxic-risks
#5
Lea Wagmann, Simon D Brandt, Pierce V Kavanagh, Hans H Maurer, Markus R Meyer
Tryptamines have emerged as new psychoactive substances (NPS), which are distributed and consumed recreationally without preclinical studies or safety tests. Within the alpha-methylated tryptamines, some of the psychoactive effects of the prototypical alpha-methyltryptamine (AMT) have been described decades ago and a contributing factor of its acute toxicity appears to involve the inhibition of monoamine oxidase (MAO). However, detailed information about analogs is scarce. Therefore, thirteen AMT analogs were investigated for their potential to inhibit MAO...
March 13, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28299453/simultaneous-determination-of-mao-a-and-b-activity-following-first-time-intake-of-an-irreversible-mao-b-inhibitor-in-patients-with-parkinson-s-disease
#6
Thomas Müller, Peter Riederer, Edna Grünblatt
We determined monoamine oxidase-A (plasma) and -B (platelets) enzyme activity in chronic levodopa treated patients with Parkinson's disease after first time intake of an irreversible monoamine oxidase-B inhibitor. One patient received 10 mg selegiline and eleven patients took 1 mg rasagiline. A significant decrease of monoamine oxidase-B activity appeared 2 and 4 h following monoamine oxidase-B inhibitor intake in comparison to baseline. We confirm with this design, that rasagiline and selegiline inhibit monoamine oxidase-B but not monoamine oxidase-A after single dosing...
March 15, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28294055/therapeutic-molecular-and-computational-aspects-of-novel-monoamine-oxidase-mao-inhibitors
#7
M Ramesh, Yussif M Dokurugu, Michael D Thompson, Mahmoud Soliman
Due to the limited number of MAOs inhibitors in the clinic and several research efforts are aimed at the discovery of novel MAOs inhibitors. At present, high specificity and a reversible mode of inhibition of MAO-A/B are cited as desirable traits in drug discovery process. This will help to reduce the probability of causing target disruption and may increase the duration of action. Most of the existing MAO inhibitors lead to side effects due to lack of affinity and selectivity. Therefore, there is an urgent need to design novel, potent, reversible and selective inhibitors for MAO-A/B...
March 10, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28291352/understanding-the-molecular-determinant-of-reversible-human-monoamine-oxidase-b-inhibitors-containing-2h-chromen-2-one-core-structure-based-and-ligand-based-derived-3-d-qsar-predictive-models
#8
Milan Mladenovic, Alexandros Patsilinakos, Adele Pirolli, Manuela Sabatino, Rino Ragno
Monoamine oxidase B (MAO B) catalyzes the oxidative deamination of aryalkylamines neurotransmitters with concomitant reduction of oxygen to hydrogen peroxide. Consequently, the enzyme's malfunction can induce oxidative damage to mitochondrial DNA and mediates development of Parkinson's disease. Thus, MAO B emerges as a promising target for developing pharmaceuticals potentially useful to treat this vicious neurodegenerative condition. Aiming to contribute to the development of drugs with the reversible mechanism of MAO B inhibition only, herein, an extended in silico-in vitro procedure for the selection of novel MAO B inhibitors is demonstrated, including: (1) definition of optimized and validated structure-based (SB) 3-D QSAR models derived from available co-crystallized inhibitor-MAO B complexes; (2) elaboration of structure-activity relationships (SAR) features for either irreversible or reversible MAO B inhibitors to characterize and improve coumarin-based inhibitor activity (Protein Data Bank ID: 2V61) as the most potent reversible lead compound; (3) definition of structure-based (SB) and ligand-based (LB) alignment rules assessments by which virtually any untested potential MAO B inhibitor might be evaluated; (4) predictive ability validation of the best 3-D QSAR model through SB/LB modeling of four coumarin-based external test sets (267 compounds); (5) design and SB/LB alignment of novel coumarin-based scaffolds experimentally validated through synthesis and biological evaluation in vitro...
March 14, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28289795/-pharmacological-treatment-of-motor-symptoms-in-parkinson-s-diseases
#9
W H Jost
Since the 1960s many substance classes have been introduced for treatment of idiopathic Parkinson's disease. The most important and effective medication is levodopa (L-dopa) always in combination with a decarboxylase inhibitor. In addition, dopamine agonists, monoamine oxidase B (MAO-B) inhibitors, catechol-o-methyltransferase (COMT) inhibitors, N‑methyl-D-aspartate (NMDA) antagonists and very rarely anticholinergics are administered depending on the motor symptoms, age and a multitude of other factors. Fortunately, within the substance classes there are various preparations, which also have different effects...
March 13, 2017: Der Nervenarzt
https://www.readbyqxmd.com/read/28279509/-medical-and-surgical-treatment-of-parkinson-s-disease
#10
Luc Defebvre, Caroline Moreau
The treatment of Parkinson's disease is symptomatic with the use of dopaminergic medications: levodopa, dopaminergic agonists and enzymatic inhibitors. At the initial stage, the main goals are to improve the quality of life of patients and delay the onset of motor complications, using a combination of these therapies taking into account both clinical disability and tolerance of different treatments. At the stage of motor and non-motor fluctuations inhibitors of MAO-B and COMT are proposed; amantadine may limit moderate dyskinesias...
March 6, 2017: La Presse Médicale
https://www.readbyqxmd.com/read/28273563/discovery-of-highly-selective-and-potent-monoamine-oxidase-b-inhibitors-contribution-of-additional-phenyl-rings-introduced-into%C3%A2-2-aryl-1-3-4-oxadiazin-5-6h-one
#11
Jungeun Lee, Yeongcheol Lee, So Jung Park, Joohee Lee, Yeong Shik Kim, Young-Ger Suh, Jeeyeon Lee
Monoamine oxidase B (MAO-B) is a flavin adenine dinucleotide (FAD)-containing enzyme that plays a major role in the oxidative deamination of biogenic amines and neurotransmitters. Inhibiting MAO-B activity is a promising approach in the treatment of neurological disorders. Here, we report a series of 2-aryl-1,3,4-oxadiazin-5(6H)-one derivatives as highly selective and potent MAO-B inhibitors. Analysis of the binding sites of hMAO-A and hMAO-B led to design of linear analogs of 2-aryl-1,3,4-oxadiazin-5(6H)-one with an additional phenyl ring...
April 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28267984/pyridoxine-resveratrol-hybrids-mannich-base-derivatives-as-novel-dual-inhibitors-of-ache-and-mao-b-with-antioxidant-and-metal-chelating-properties-for-the-treatment-of-alzheimer-s-disease
#12
Xia Yang, Xiaoming Qiang, Yan Li, Li Luo, Rui Xu, Yunxiaozhu Zheng, Zhongcheng Cao, Zhenghuai Tan, Yong Deng
A series of pyridoxine-resveratrol hybrids Mannich base derivatives as multifunctional agents have been designed, synthesized and evaluated for cholinesterase (ChE) and monoamine oxidase (MAO) inhibitory activity. To further explore the multifunctional properties of the new derivatives, their antioxidant activities and metal-chelating properties were also tested. The results showed that most of these compounds could selectively inhibit acetylcholinesterase (AChE) and MAO-B. Among them, compounds 7d and 8b exhibited the highest potency for AChE inhibition with IC50 values of 2...
February 28, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28251489/evaluation-of-the-inhibitory-effects-of-eckol-and-dieckol-isolated-from-edible-brown-alga-eisenia-bicyclis-on-human-monoamine-oxidases-a-and-b
#13
Hyun Ah Jung, Anupom Roy, Jee H Jung, Jae Sue Choi
Eckol and dieckol are important phlorotannins found in edible brown algae including Eisenia bicyclis, Ecklonia stolonifera, and others. Inhibition of monoamine oxidase (MAO) play an important role in the early management of Parkinson's disease (PD). The aim of this study was to determine the effectiveness of eckol and dieckol isolated from the methanolic extract of E. bicyclis against PD by the inhibition of human MAO-A and MAO-B (hMAO-A and hMAO-B). A sensitive enzyme-based chemiluminescent assay and kinetics methods were used to investigate enzyme inhibition and mode of inhibition...
March 1, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28251298/perseveration-in-a-spatial-discrimination-serial-reversal-learning-task-is-differentially-affected-by-mao-a-and-mao-b-inhibition-and-associated-with-reduced-anxiety-and-peripheral-serotonin-levels
#14
Peter Zhukovsky, Johan Alsiö, Bianca Jupp, Jing Xia, Chiara Guiliano, Lucy Jenner, Jessica Griffiths, Errin Riley, Sajeed Ali, Angela C Roberts, Trevor W Robbins, Jeffrey W Dalley
RATIONALE: Impairments in behavioral flexibility lie at the core of anxiety and obsessive-compulsive disorders. Few studies, however, have investigated the neural substrates of natural variation in behavioral flexibility and whether inflexible behavior is linked to anxiety and peripheral markers of stress and monoamine function. OBJECTIVE: The objective of the study was to investigate peripheral and central markers associated with perseverative behavior on a spatial-discrimination serial reversal learning task...
March 2, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28245770/structural-exploration-of-synthetic-chromones-as-selective-mao-b-inhibitors-a-mini-review
#15
Bijo Mathew, Githa Elizabeth Mathew, Jacobus P Petzer, Anel Petzer
Specific inhibitors of monoamine oxidase (MAO)-B are considered useful therapeutic agents in targeting of neurological disorders like Alzheimer's and Parkinson's diseases. Due to the academic challenge of designing new hMAO-B inhibitors and the possibility of discovering compounds with improved properties compared to existing MAO-B inhibitors, a number of research groups are searching for new classes of chemical compounds that may act as selective hMAO-B inhibitors. Among these, chromone (4H-1-benzopyran-4-one) derivatives have recently emerged as a chemotype with specific and high potency MAO-B inhibition...
February 27, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28238669/ellagic-acid-exerts-protective-effect-in-intrastriatal-6-hydroxydopamine-rat-model-of-parkinson-s-disease-possible-involvement-of-er%C3%AE-nrf2-ho-1-signaling
#16
Tourandokht Baluchnejadmojarad, Nafiseh Rabiee, Sedigheh Zabihnejad, Mehrdad Roghani
Parkinson's disease (PD) is a prevalent movement disorder in the elderly with progressive loss of mesencephalic dopaminergic neurons and incapacitating motor and non-motor complications. Ellagic acid is a natural phenolic compound with potent antioxidant and anti-inflammatory properties. In this study, we investigated its possible neuroprotective effect in 6-hydroxydopamine (6-OHDA) rat model of PD. Intrastriatal 6-OHDA-lesioned rats were pretreated with ellagic acid at a dose of 50 mg/kg/day for 1 week. Results showed that ellagic acid attenuates apomorphine-induced rotational bias and lowers the latency to initiate and the total time in the narrow beam task and this beneficial effect was partially abrogated following intracerebroventricular microinjection of estrogen receptor β (ERβ) antagonist...
February 23, 2017: Brain Research
https://www.readbyqxmd.com/read/28237559/multifunctional-thioxanthone-derivatives-with-acetylcholinesterase-monoamine-oxidases-and-%C3%AE-amyloid-aggregation-inhibitory-activities-as-potential-agents-against-alzheimer-s-disease
#17
Li Luo, Yan Li, Xiaoming Qiang, Zhongcheng Cao, Rui Xu, Xia Yang, Ganyuan Xiao, Qing Song, Zhenghuai Tan, Yong Deng
A series of 1-hydroxyl-3-aminoalkoxy-thioxanthone derivatives were designed, synthesized and evaluated as potential multifunctional agents against Alzheimer's disease (AD). The results indicated that most of these compounds exhibited good AChE and MAOs inhibitory activities, significant inhibition of self- and Cu(2+)-induced Aβ1-42 aggregation, and moderate to good antioxidant activities. Specifically, compound 9e displayed high inhibitory potency toward AChE (IC50=0.59±0.02μM), MAO-A and MAO-B (IC50=1.01±0...
February 14, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28214749/impairment-in-the-mesohippocampal-dopamine-circuit-following-exposure-to-the-brominated-flame-retardant-hbcdd
#18
Camille Pham-Lake, Elizabeth B Aronoff, Chad R Camp, Aimee Vester, Sam J Peters, W Michael Caudle
Many chemicals have been used to increase the safety of consumer products by reducing their flammability and risk for ignition. Recent focus on brominated flame retardants, such as polybrominated diphenyl ethers (PBDEs) has shown them to contribute to neurobehavioral deficits in children, including learning and memory. As the manufacture and use of PBDEs have been reduced, replacement chemicals, such as hexabromocyclododecane (HBCDD) have been substituted. Our current study evaluated the neurotoxicity of HBCDD, concentrating on dopaminergic innervation to the hippocampus...
March 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28214564/downregulation-of-gna13-erk-network-in-prefrontal-cortex-of-schizophrenia-brain-identified-by-combined-focused-and-targeted-quantitative-proteomics
#19
Mio Hirayama-Kurogi, Yohei Takizawa, Yasuto Kunii, Junya Matsumoto, Akira Wada, Mizuki Hino, Hiroyasu Akatsu, Yoshio Hashizume, Sakon Yamamoto, Takeshi Kondo, Shingo Ito, Masanori Tachikawa, Shin-Ichi Niwa, Hirooki Yabe, Tetsuya Terasaki, Mitsutoshi Setou, Sumio Ohtsuki
Schizophrenia is a disabling mental illness associated with dysfunction of the prefrontal cortex, which affects cognition and emotion. The purpose of the present study was to identify altered molecular networks in the prefrontal cortex of schizophrenia patients by comparing protein expression levels in autopsied brains of patients and controls, using a combination of targeted and focused quantitative proteomics. We selected 125 molecules possibly related to schizophrenia for quantification by knowledge-based targeted proteomics...
February 16, 2017: Journal of Proteomics
https://www.readbyqxmd.com/read/28188065/selective-inhibition-of-monoamine-oxidase-a-by-purpurin-an-anthraquinone
#20
Hyun Woo Lee, Hyung Won Ryu, Myung-Gyun Kang, Daeui Park, Sei-Ryang Oh, Hoon Kim
Monoamine oxidase (MAO) catalyzes the oxidation of monoamines that act as neurotransmitters. During a target-based screening of natural products using two isoforms of recombinant human MAO-A and MAO-B, purpurin (an anthraquinone derivative) was found to potently and selectively inhibit MAO-A, with an IC50 value of 2.50μM, and not to inhibit MAO-B. Alizarin (also an anthraquinone) inhibited MAO-A less potently with an IC50 value of 30.1μM. Furthermore, purpurin was a reversible and competitive inhibitor of MAO-A with a Ki value of 0...
January 31, 2017: Bioorganic & Medicinal Chemistry Letters
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