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https://www.readbyqxmd.com/read/28228728/perivascular-adipose-tissue-s-impact-on-norepinephrine-induced-contraction-of-mesenteric-resistance-arteries
#1
Nadia Ayala-Lopez, Janice M Thompson, Stephanie W Watts
Background: Perivascular adipose tissue (PVAT) can decrease vascular contraction to NE. We tested the hypothesis that metabolism and/or uptake of vasoactive amines by mesenteric PVAT (MPVAT) could affect NE-induced contraction of the mesenteric resistance arteries. Methods: Mesenteric resistance vessels (MRV) and MPVAT from male Sprague-Dawley rats were used. RT-PCR and Western blots were performed to detect amine metabolizing enzymes. The Amplex® Red Assay was used to quantify oxidase activity by detecting the oxidase reaction product H2O2 and the contribution of PVAT on the mesenteric arteries' contraction to NE was measured by myography...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28219215/-natural-history-of-breast-cancer-a-systematic-review-of-worldwide-randomized-controlled-trials-of-mammography-screening
#2
X P Yue, J F Shi, A Y Mao, L Wang, H M Ma, L L Chen, J Zhu, X Cheng, M Dai
Objective: To parameterize the 1-year transition probabilities between different health status of the natural history of breast cancer based on the data of randomized controlled trial of X-ray mammography screening worldwide. Methods: Based on the breast cancer screening randomized controlled trials defined by a mammography screening review from the Cochrane 2013 and the International Agency for Research on Cancer, a systematic review was initiated in PubMed by searching names of the key investigators of the trials, combined with the diseases, screening intervention and outcome indicators...
February 23, 2017: Zhonghua Zhong Liu za Zhi [Chinese Journal of Oncology]
https://www.readbyqxmd.com/read/28205135/apium-graveolens-extract-influences-mood-and-cognition-in-healthy-mice
#3
Phetcharat Boonruamkaew, Wanida Sukketsiri, Pharkphoom Panichayupakaranant, Wijittra Kaewnam, Supita Tanasawet, Varomyalin Tipmanee, Pilaiwanwadee Hutamekalin, Pennapa Chonpathompikunlert
Apium graveolens is a food flavoring which possesses various health promoting effects. This study investigates the effect of a sub-acute administration of A. graveolens on cognition and anti-depression behaviors via antioxidant and related neurotransmitter systems in mice brains. Cognition and depression was assessed by various models of behavior. The antioxidant system of glutathione peroxidase (GPx), % inhibition of superoxide anion (O2(-)), and lipid peroxidation were studied. In addition, neurochemical parameters including acetylcholinesterase (AChE) and monoamine oxidase-type A (MAO-A) were also evaluated...
February 15, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/28188065/selective-inhibition-of-monoamine-oxidase-a-by-purpurin-an-anthraquinone
#4
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
https://www.readbyqxmd.com/read/28185143/characterization-of-1-aminobenzotriazole-and-ketoconazole-as-novel-inhibitors-of-monoamine-oxidase-mao-an-in-vitro-investigation
#5
Abdul Naveed Shaik, Barbara W LeDuc, Ansar A Khan
BACKGROUND AND OBJECTIVES: 1-Aminobenzotriazole, a known time-dependent inhibitor of cytochrome P450 (CYP) enzymes, and ketoconazole, a strong inhibitor of the human CYP3A4 isozyme, are used as standard probe inhibitors to characterize the CYP and/or non-CYP-mediated metabolism of xenobiotics. In the present investigation, 1-Aminobenzotriazole and ketoconazole are characterized as potent monoamine oxidase (MAO) inhibitors in vitro using mouse, rat and human liver microsomes and S9 fractions...
February 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28158205/structure-activity-relationship-and-modeling-studies-of-inhibitors-of-lysine-specific-demethylase-1
#6
Chao Zhou, Fangrui Wu, Lianghao Lu, Liping Wei, Eric Pai, Yuan Yao, Yongcheng Song
Post-translational modifications of histone play important roles in gene transcription. Aberrant methylation of histone lysine sidechains have been often found in cancer. Lysine specific demethylase 1 (LSD1), which can demethylate histone H3 lysine 4 (H3K4) and other proteins, has recently been found to be a drug target for acute myeloid leukemia. To understand structure activity/selectivity relationships of LSD1 inhibitors, several series of cyclopropylamine and related compounds were synthesized and tested for their activities against LSD1 and related monoamine oxidase (MAO) A and B...
2017: PloS One
https://www.readbyqxmd.com/read/28151561/monoamine-oxidase-a-and-b-activities-in-the-cerebellum-and-frontal-cortex-of-children-and-young-adults-with-autism
#7
Feng Gu, Ved Chauhan, Abha Chauhan
Monoamine oxidases (MAOs) catalyze the metabolism of monoamine neurotransmitters, such as serotonin, dopamine, and norepinephrine, and are key regulators for brain function. In this study, we analyzed the activities of MAO-A and MAO-B in the cerebellum and frontal cortex from subjects with autism and age-matched control subjects. In the cerebellum, MAO-A activity in subjects with autism (aged 4-38 years) was significantly lower by 20.6% than in controls. When the subjects were divided into children (aged 4-12 years) and young adults (aged 13-38 years) subgroups, a significant decrease by 27...
February 2, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28131710/dl-3-n-butylphthalide-edaravone-hybrids-as-novel-dual-inhibitors-of-amyloid-%C3%AE-aggregation-and-monoamine-oxidases-with-high-antioxidant-potency-for-alzheimer-s-therapy
#8
Xiaoming Qiang, Yan Li, Xia Yang, Li Luo, Rui Xu, Yunxiaozhu Zheng, Zhongcheng Cao, Zhenghuai Tan, Yong Deng
Considering the complex etiology of Alzheimer's disease (AD), multifunctional agents may be beneficial for the treatment of this disease. A series of DL-3-n-butylphthalide-Edaravone hybrids were designed, synthesized and evaluated as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases. Among them, compounds 9a-d exhibited good inhibition of self-induced Aβ1-42 aggregation with inhibition ratio 57.7-71.5%. For MAO, these new hybrids exhibited good balance of inhibition for MAO-A and MAO-B...
January 17, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28109809/potent-inhibition-of-monoamine-oxidase-a-by-decursin-from-angelica-gigas-nakai-and-by-wogonin-from-scutellaria-baicalensis-georgi
#9
Hyun Woo Lee, Hyung Won Ryu, Myung-Gyun Kang, Daeui Park, Hanna Lee, Heung Mook Shin, Sei-Ryang Oh, Hoon Kim
During the ongoing search for new monoamine oxidase (MAO) inhibitors, five coumarin derivatives and eight flavonoids were isolated from the roots of Angelica gigas Nakai and Scutellaria baicalensis Georgi, respectively. Of the phytochemicals, decursin (4) was found to potently and selectively inhibit human MAO-A (IC50=1.89μM). The IC50 value of 4 for MAO-A belonged to the lowest group in herbal sources and was similar to that of toloxatone (1.78μM), a marketed drug. Wogonin (11) effectively inhibited MAO-A and MAO-B (IC50=6...
April 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28107736/crystal-structures-binding-interactions-and-adme-evaluation-of-brain-penetrant-n-substituted-indazole-5-carboxamides-as-subnanomolar-selective-monoamine-oxidase-b-and-dual-mao-a-b-inhibitors
#10
Nikolay T Tzvetkov, Hans-Georg Stammler, Beate Neumann, Silvia Hristova, Liudmil Antonov, Marcus Gastreich
The pharmacological and physicochemical analysis of structurally optimized N-alkyl-substituted indazole-5-carboxamides, developed as potential drug and radioligand candidates for the treatment and diagnosis of Parkinson's disease (PD) and other neurological disorders, is reported. Recent efforts have been focused on the development of subnanomolar potent, selective MAO-B (N1-alkyl-substituted compounds 12a-14a and 15) and dual active MAO-A/B (N2-methylated compounds 12b-14b) inhibitors with nanomolar potency towards MAO-B and moderately active against MAO-A enzyme, respectively...
January 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28097890/novel-1-2-pyrimidin-2-yl-piperazine-derivatives-as-selective-monoamine-oxidase-mao-a-inhibitors
#11
Betül Kaya, Leyla Yurttaş, Begüm Nurpelin Sağlik, Serkan Levent, Yusuf Özkay, Zafer Asim Kaplancikli
In the present study, a new series of 2-[4-(pyrimidin-2-yl)piperazin-1-yl]-2-oxoethyl 4-substituted piperazine-1-carbodithioate derivatives (2a-n) were synthesized and screened for their monoamine oxidase A and B inhibitory activity. The structures of compounds were elucidated using spectroscopic methods and some physicochemical properties of new compounds were predicted using Molinspiration and MolSoft programs. Compounds 2-[4-(pyrimidin-2-yl)piperazin-1-yl]-2-oxoethyl 4-(4-nitrophenyl)piperazine-1-carbodithioate (2j) and 2-[4-(pyrimidin-2-yl)piperazin-1-yl]-2-oxoethyl 4-benzhydrylpiperazine-1-carbodithioate (2m) exhibited selective MAO-A inhibitory activity with IC50 = 23...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097874/through-scaffold-modification-to-3-5-diaryl-4-5-dihydroisoxazoles-new-potent-and-selective-inhibitors-of-monoamine-oxidase-b
#12
Rita Meleddu, Simona Distinto, Roberto Cirilli, Stefano Alcaro, Matilde Yanez, Maria Luisa Sanna, Angela Corona, Claudia Melis, Giulia Bianco, Peter Matyus, Filippo Cottiglia, Elias Maccioni
3,5-Diaryl-4,5-dihydroisoxazoles were synthesized and evaluated as monoamine oxidase (MAO) enzyme inhibitors and iron chelators. All compounds exhibited selective inhibitory activity towards the B isoform of MAO in the nanomolar concentration range. The best performing compound was preliminarily evaluated for its ability to bind iron II and III cations, indicating that neither iron II nor iron III is coordinated. The best compounds racemic mixtures were separated and single enantiomers inhibitory activity evaluated...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28069007/the-benzopyrone-biochanin-a-as-a-reversible-competitive-and-selective-monoamine-oxidase-b-inhibitor
#13
Najla O Zarmouh, Suresh K Eyunni, Karam F A Soliman
BACKGROUND: Monoamine oxidase-B (MAO-B) inhibitors are widely used in the treatment of Parkinson's disease. They increase vital monoamine neurotransmitters in the brain. However, there is a need for safer natural reversible MAO inhibitors with MAO-B selectivity. Our previous studies showed that Psoralea corylifolia seeds (PCS) extract contains compounds that inhibit monoamine oxidase-B. METHODS: In this study, six of PCS constituents sharing a benzopyrone structure were investigated...
January 10, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28068665/potent-inhibition-of-monoamine-oxidase-b-by-a-piloquinone-from-a-marine-derived-streptomyces-sp-cnq-027
#14
Hyun Woo Lee, Hansol Choi, Sang-Jip Nam, William Fenical, Hoon Kim
Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an IC₅₀ value of 1.21 µM; in addition, it was found to be highly effective against MAO-A, with an IC₅₀ value of 6.47 µM. Compound 1 was selective, but not extremely so, for MAO-B compared to MAO-A, with a selectivity index value of 5...
January 9, 2017: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28057462/monoamine-oxidase-inhibitory-activity-in-tobacco-particulate-matter-are-harman-and-norharman-the-only-physiologically-relevant-inhibitors
#15
Penelope Truman, Peter Grounds, Katharine A Brennan
Monoamine oxidase inhibition is significant in smokers, but it is still unclear how the inhibition that is seen in the brains and bodies of smokers is brought about. Our aim was to test the contribution of the harman and norharman in tobacco smoke to MAO-A inhibition from tobacco smoke preparations, as part of a re-examination of harman and norharman as the cause of the inhibition of MAO-A inhibition in the brain. Tobacco smoke particulate matter and cigarette smoke particulate matter were prepared and the amounts of harman and norharman measured...
January 3, 2017: Neurotoxicology
https://www.readbyqxmd.com/read/28052533/what-a-difference-a-methyl-group-makes-the-selectivity-of-monoamine-oxidase%C3%A2-b-towards-histamine-and-n-methylhistamine
#16
Aleksandra Maršavelski, Robert Vianello
Monoamine oxidase (MAO) enzymes catalyze the degradation of a very broad range of biogenic and dietary amines including many neurotransmitters in the brain, whose imbalance is extensively linked with the biochemical pathology of various neurological disorders. Although sharing around 70 % sequence identity, both MAO A and B isoforms differ in substrate affinities and inhibitor sensitivities. Inhibitors that act on MAO A are used to treat depression, due to their ability to raise serotonin concentrations, whereas MAO B inhibitors decrease dopamine degradation and improve motor control in patients with Parkinson disease...
January 3, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28034283/in-silico-studies-revealed-multiple-neurological-targets-for-the-antidepressant-molecule-ursolic-acid
#17
Rajeev K Singla, Luciana Scotti, Ashok K Dubey
BACKGROUND: Ursolic acid, a bioactive pentacyclic triterpenoid had been evaluated for its interaction with the neurological targets associated with antidepressant drugs. Current study was to mechanistically analyze the probable site of action for ursolic acid on the target proteins. METHODS: Ursolic acid has been docked with monoamine oxidase isoforms: MAO-A and MAO-B, LeuT (homologue of SERT, NET, DAT) and Human C-terminal CAP1 using GRIP docking methodology. RESULTS: Results revealed its non-selective antidepressant action with strong binding affinity towards LeuT and MAO-A proteins, which was found to be comparable with the reference ligands like chlorgyline, clomipramine, sertraline and deprenyl / selegiline...
December 29, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/28012831/selective-inhibition-of-mao-a-activity-results-in-an-antidepressant-like-action-of-2-benzoyl-4-iodoselenophene-in-mice
#18
Daniela Velasquez, Caroline Quines, Renan Pistóia, Gilson Zeni, Cristina W Nogueira
Depression is a leading cause of disability worldwide. For this reason, the aim of this study was to investigate the possible antidepressant-like activity of 2-benzoyl-4-iodoselenophene (C17H11IOSe), a selenophene compound, in two well-consolidated behavioral assays for screening antidepressant activity (forced swimming test and tail suspension test) in mice. In order to investigate the mechanism of action of C17H11IOSe, it was investigated the activities of cerebral enzymes: monoamine oxidase MAO A and B and Na(+), K(+) ATPase, and if an inhibitor of serotonin synthesis, p-chlorophenylalanine (pCPA) (100mg/kg) blocks the antidepressant-like effect of C17H11IOSe...
December 21, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/28012396/antidepressant-like-effects-of-hydrolysable-tannins-of-terminalia-catappa-leaf-extract-via-modulation-of-hippocampal-plasticity-and-regulation-of-monoamine-neurotransmitters-subjected-to-chronic-mild-stress-cms
#19
Y Chandrasekhar, E M Ramya, K Navya, G Phani Kumar, K R Anilakumar
Terminalia catappa L. belonging to Combretaceae family is a folk medicine, known for its multiple pharmacological properties, but the neuro-modulatory effect of TC against chronic mild stress was seldom explored. The present study was designed to elucidate potential antidepressant-like effect of Terminalia cattapa (leaf) hydro-alcoholic extract (TC) by using CMS model for a period of 7 weeks. Identification of hydrolysable tannins was done by using LC-MS. After the CMS exposure, mice groups were administered with imipramine (IMP, 10mg/kg, i...
February 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27998471/-economic-burden-of-cancer-in-china-during-1996-2014-a-systematic-review
#20
J F Shi, C L Shi, X P Yue, H Y Huang, L Wang, J Li, P A Lou, A Y Mao, M Dai
Objective: To explore the current status of research on economic burden of cancer in China from 1996 to 2014. Methods: The key words including cancer, economic burden, expenditure, cost were used to retrieve the literatures published in CNKI and Wanfang (the two most commonly used databases for literature in Chinese) and PubMed during 1996-2014. A total of 91 studies were included after several exclusionary procedures. Information on subjects and data source, methodology, main results were structurally abstracted...
December 23, 2016: Zhonghua Zhong Liu za Zhi [Chinese Journal of Oncology]
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