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https://www.readbyqxmd.com/read/28923922/trkb-neurotrophic-activities-are-blocked-by-%C3%AE-synuclein-triggering-dopaminergic-cell-death-in-parkinson-s-disease
#1
Seong Su Kang, Zhentao Zhang, Xia Liu, Fredric P Manfredsson, Matthew J Benskey, Xuebing Cao, Jun Xu, Yi E Sun, Keqiang Ye
BDNF/TrkB neurotrophic signaling is essential for dopaminergic neuronal survival, and the activities are reduced in the substantial nigra (SN) of Parkinson's disease (PD). However, whether α-Syn (alpha-synuclein) aggregation, a hallmark in the remaining SN neurons in PD, accounts for the neurotrophic inhibition remains elusive. Here we show that α-Syn selectively interacts with TrkB receptors and inhibits BDNF/TrkB signaling, leading to dopaminergic neuronal death. α-Syn binds to the kinase domain on TrkB, which is negatively regulated by BDNF or Fyn tyrosine kinase...
September 18, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28890698/multi-target-screening-and-experimental-validation-of-natural-products-from-selaginella-plants-against-alzheimer-s-disease
#2
Yin-Hua Deng, Ning-Ning Wang, Zhen-Xing Zou, Lin Zhang, Kang-Ping Xu, Alex F Chen, Dong-Sheng Cao, Gui-Shan Tan
Alzheimer's disease (AD) is a progressive and irreversible neurodegenerative disorder which is considered to be the most common cause of dementia. It has a greater impact not only on the learning and memory disturbances but also on social and economy. Currently, there are mainly single-target drugs for AD treatment but the complexity and multiple etiologies of AD make them difficult to obtain desirable therapeutic effects. Therefore, the choice of multi-target drugs will be a potential effective strategy inAD treatment...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28864633/correlations-of-18-f-thk5351-pet-with-post-mortem-burden-of-tau-and-astrogliosis-in-alzheimer-s-disease
#3
Ryuichi Harada, Aiko Ishiki, Hideaki Kai, Naomi Sato, Katsutoshi Furukawa, Shozo Furumoto, Tetsuro Tago, Naoki Tomita, Shoichi Watanuki, Kotaro Hiraoka, Yoichi Ishikawa, Yoshihito Funaki, Tadaho Nakamura, Takeo Yoshikawa, Ren Iwata, Manabu Tashiro, Hironobu Sasano, Tetsuyuki Kitamoto, Kazuhiko Yanai, Hiroyuki Arai, Yukitsuka Kudo, Nobuyuki Okamura
Clinical PET studies using (18)F-THK5351 have demonstrated significant tracer retention in sites susceptible to tau burden in Alzheimer's disease (AD). However, the in vivo PET signal to reflect tau aggregates remains controversial. Methods: We examined the spatial pattern of tracer binding, amyloid-β, tau and gliosis in an autopsy-confirmed AD case who underwent (18)F-THK5351 and (11)C-PiB PET before death. Results: Regional in vivo (18)F-THK5351 retention was significantly correlated with the density of tau aggregates in the neocortex and monoamine oxidase-B (MAO-B) in the whole brain, but not correlated with that of insoluble amyloid-β...
September 1, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28862601/-comparative-analysis-of-expression-of-genes-encoding-enzymes-of-catecholamine-catabolism-and-renalase-in-tissues-of-normotensive-and-hypertensive-rats
#4
V I Fedchenko, A E Medvedev
Comparative analysis of expression of genes encoding enzymes of catecholamine catabolism (monoaminbe oxidases A and B (MAO A and MAO B) and catechol-O-methyl transferase (COMT)) and renalase has been carried out in tissues of normotensive Wistar-Kyoto (WKY) rats and spontaneously hypertensive rats (SHR). Among investigated tissues the highest level of mRNA of genes encoding key enzymes of catecholamine catabolism (MAO A, MAO B, COMT) was found in the heart of WKY rats. In SHR the mRNA levels of these genes were lower (p<0...
July 2017: Biomedit︠s︡inskai︠a︡ Khimii︠a︡
https://www.readbyqxmd.com/read/28857544/identification-of-5-1-methyl-5-trifluoromethyl-1h-pyrazol-3-yl-thiophene-2-carboxamides-as-novel-and-selective-monoamine-oxidase-b-inhibitors-used-to-improve-memory-and-cognition
#5
Alan P Kaplan, Terence Keenan, Roderick Scott, Xianbo Zhou, Rusiko Bourchouladze, Andrew J McRiner, Mark E Wilson, Darlene Romashko, Regina Miller, Matthew Bletsch, Gary Anderson, Jennifer Stanley, Adia Zhang, Dong Lee, John Nikpur
Initial work in Drosophila and mice demonstrated that the transcription factor cyclic adenosine monophosphate (cAMP) response element binding protein (CREB) is a master control gene for memory formation. The relationship between CREB and memory has also been found to be true in other species, including aplysia and rats. It is thus well-established that CREB activation plays a central role in memory enhancement and that CREB is activated during memory formation. On the basis of these findings, a phenotypic high-throughput screening campaign utilizing a CRE-luciferase (CRE-Luci) SK-N-MC cell line was performed to identify compounds that enhance transcriptional activation of the CRE promoter with a suboptimal dose of forskolin...
September 20, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28840582/n-acetylcysteine-prevents-the-increase-in-spontaneous-oxidation-of-dopamine-during-monoamine-oxidase-inhibition-in-pc12-cells
#6
David S Goldstein, Yunden Jinsmaa, Patti Sullivan, Yehonatan Sharabi
The catecholaldehyde hypothesis for the pathogenesis of Parkinson's disease proposes that the deaminated dopamine metabolite 3,4-dihydroxyphenylacetaldehyde (DOPAL) is toxic to nigrostriatal dopaminergic neurons. Inhibiting monoamine oxidase (MAO) should therefore slow the disease progression; however, MAO inhibition increases spontaneous oxidation of dopamine, as indicated by increased 5-S-cysteinyl-dopamine (Cys-DA) levels, and the oxidation products may also be toxic. This study examined whether N-acetylcysteine (NAC), a precursor of the anti-oxidant glutathione, attenuates the increase in Cys-DA production during MAO inhibition...
August 24, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28839357/using-molecular-docking-analysis-to-discovery-dregea-sinensis-hemsl-potential-mechanism-of-anticancer-antidepression-and-immunoregulation
#7
Xiujie Liu, Yu Shi, Yulin Deng, Rongji Dai
BACKGROUND: Dregea sinensis Hemsl. plant of the genus Dregea volubilis (Asclepiadaceae), plays a vital role in anticancer, antidepression, and immunoregulation. Steroidal glycosides are the main constituents of this herb, which were significant biological active ingredients. OBJECTIVE: The objective of this study is to recognize the mechanism of anticancer, antidepression, and immunoregulation of D. sinensis Hemsl. MATERIALS AND METHODS: Seventy-two steroidal glycosides of D...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28836294/how-fast-monoamine-oxidases-decompose-adrenaline-kinetics-of-isoenzymes-a-and-b-evaluated-by-empirical-valence-bond-simulation
#8
Gabriel Oanca, Jernej Stare, Janez Mavri
This work scrutinizes kinetics of decomposition of adrenaline catalyzed by monoamine oxidase (MAO) A and B enzymes, a process controlling the levels of adrenaline in the central nervous system and other tissues. Experimental kinetic data for MAO A and B catalyzed decomposition of adrenaline are reported only in the form of the maximum reaction rate. Therefore we estimated the experimental free energy barriers form the kinetic data of closely related systems using regression method, as was done in our previous study...
August 24, 2017: Proteins
https://www.readbyqxmd.com/read/28825626/pharmacological-and-toxicological-screening-of-novel-benzimidazole-morpholine-derivatives-as-dual-acting-inhibitors
#9
Nafiz Öncü Can, Ulviye Acar Çevik, Begüm Nurpelin Sağlık, Yusuf Özkay, Özlem Atlı, Merve Baysal, Ümide Demir Özkay, Özgür Devrim Can
The aim of this study was to investigate acetylcholinesterase (AChE), monoamine oxidase A (MAO-A), monoamine oxidase B (MAO-B), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzyme inhibitory, and antimicrobial activities of a new series of 2-(4-substituted phenyl)-1-[2-(morpholin-4-yl)ethyl]-1H-benzimidazole derivatives, for their possible use as multi-action therapeutic agents. Target compounds (n = 15) were synthesized under microwave irradiation conditions in two steps, and their structures were elucidated by FT-IR, ¹H-NMR, (13)C-NMR and high resolution mass spectroscopic analyses...
August 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28807675/substantial-protection-against-mptp-associated-parkinson-s-neurotoxicity-in%C3%A2-vitro-and-in%C3%A2-vivo-by-anti-cancer-agent-su4312-via-activation-of-mef2d-and-inhibition-of-mao-b
#10
Baojian Guo, Shengquan Hu, Chengyou Zheng, Hongyu Wang, Fangcheng Luo, Haitao Li, Wei Cui, Xifei Yang, Guozhen Cui, Shinghung Mak, Tony Chung-Lit Choi, Edmond Dik-Lung Ma, Yuqiang Wang, Simon Ming Yuen Lee, Zaijun Zhang, Yifan Han
We have previously demonstrated the unexpected neuroprotection of the anti-cancer agent SU4312 in cellular models associated with Parkinson's disease (PD). However, the precise mechanisms underlying its neuroprotection are still unknown, and the effects of SU4312 on rodent models of PD have not been characterized. In the current study, we found that the protection of SU4312 against 1-methyl-4-phenylpyridinium ion (MPP(+))-induced neurotoxicity in PC12 cells was achieved through the activation of transcription factor myocyte enhancer factor 2D (MEF2D), as evidenced by the fact that SU4312 stimulated myocyte enhancer factor 2 (MEF2) transcriptional activity and prevented the inhibition of MEF2D protein expression caused by MPP(+), and that short hairpin RNA (ShRNA)-mediated knockdown of MEF2D significantly abolished the neuroprotection of SU4312...
August 12, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28806057/rational-design-and-multi-biological-profiling-of-novel-donepezil-trolox-hybrids-against-alzheimer-s-disease-with-cholinergic-antioxidant-neuroprotective-and-cognition-enhancing-properties
#11
Pei Cai, Si-Qiang Fang, Xue-Lian Yang, Jia-Jia Wu, Qiao-Hong Liu, Hao Hong, Xiao-Bing Wang, Lingyi Kong
A novel series of donepezil-trolox hybrids were designed, synthesized and evaluated as multifunctional ligands against Alzheimer's disease (AD). Biological assays showed that these derivatives possessed moderate to good inhibitory activities against acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) as well as remarkable antioxidant effects. The optimal compound 6d exhibited balanced functions with good inhibition against hAChE (IC50 = 0.54 μM) and hMAO-B (IC50 = 4.3 μM), significant antioxidant activity (41...
August 14, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28797883/design-synthesis-and-biological-evaluation-of-novel-coumarin-n-benzyl-pyridinium-hybrids-as-multi-target-agents-for-the-treatment-of-alzheimer-s-disease
#12
Jin-Shuai Lan, Yue Ding, Yun Liu, Ping Kang, Jian-Wei Hou, Xin-Yu Zhang, Sai-Sai Xie, Tong Zhang
Combining N-benzyl pyridinium moiety and coumarin into in a single molecule, novel hybrids with ChE and MAO-B inhibitory activities were designed and synthesized. The biological screening results indicated that most of compounds displayed potent inhibitory activity for ChE and Aβ (1-42) self-aggregation, and clearly selective inhibition to MAO-B over MAO-A. Of these compounds, compound 7f was the most potent inhibitor for hMAO-B, and it was also a good and balanced inhibitor to ChEs and hMAO-B (0.0373 μM for eeAChE; 2...
July 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28797881/synthesis-and-structure-activity-relationship-study-of-novel-3-heteroarylcoumarins-based-on-pyridazine-scaffold-as-selective-mao-b-inhibitors
#13
María Carmen Costas-Lago, Pedro Besada, Fernanda Rodríguez-Enríquez, Dolores Viña, Santiago Vilar, Eugenio Uriarte, Fernanda Borges, Carmen Terán
Compounds of hybrid structure pyridazine-coumarin were discovered as potent, selective and reversible inhibitors of monoamine oxidase B (MAO-B). These compounds were synthesized in good yield following a multistep approach based on Knoevenagel reaction and using as key intermediate pyridazinone 16, which was obtained from maleic anhydride and furan. Compounds 9b and 9d are the most active compounds of these series, with IC50 values in the sub-micromolar range, and lack of cytotoxic effects. Theoretical calculation of ADME properties also suggested a good pharmacokinetic profile for both compounds...
July 25, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28777756/long-term-effects-of-safinamide-on-mood-fluctuations-in-parkinson-s-disease
#14
Carlo Cattaneo, Thomas Müller, Erminio Bonizzoni, Gabriele Lazzeri, Ioannis Kottakis, Charlotte Keywood
BACKGROUND: Mood disorders are very frequent in Parkinson's Disease (PD), and their effective treatment is still a major unresolved issue: growing evidence suggests that glutamatergic system dysfunction is directly involved. Safinamide is a drug with an innovative mechanism of action, dopaminergic and non-dopaminergic, that includes the reversible inhibition of the monoamine oxidase-B (MAO-B) enzyme and the modulation of excessive glutamate release through the use- and state-dependent blockade of the sodium channels...
August 4, 2017: Journal of Parkinson's Disease
https://www.readbyqxmd.com/read/28764767/monoamine-oxidase-b-is-elevated-in-alzheimer-disease-neurons-is-associated-with-%C3%AE-secretase-and-regulates-neuronal-amyloid-%C3%AE-peptide-levels
#15
Sophia Schedin-Weiss, Mitsuhiro Inoue, Lenka Hromadkova, Yasuhiro Teranishi, Natsuko Goto Yamamoto, Birgitta Wiehager, Nenad Bogdanovic, Bengt Winblad, Anna Sandebring-Matton, Susanne Frykman, Lars O Tjernberg
BACKGROUND: Increased levels of the pathogenic amyloid β-peptide (Aβ), released from its precursor by the transmembrane protease γ-secretase, are found in Alzheimer disease (AD) brains. Interestingly, monoamine oxidase B (MAO-B) activity is also increased in AD brain, but its role in AD pathogenesis is not known. Recent neuroimaging studies have shown that the increased MAO-B expression in AD brain starts several years before the onset of the disease. Here, we show a potential connection between MAO-B, γ-secretase and Aβ in neurons...
August 1, 2017: Alzheimer's Research & Therapy
https://www.readbyqxmd.com/read/28753408/contribution-of-monoamine-oxidases-to-vascular-oxidative-stress-in-patients-with-end-stage-renal-disease-requiring-hemodialysis
#16
Diana Utu, Stelian Pantea, Oana M Duicu, Danina M Muntean, Adrian Sturza
Arteriovenous fistula (AVF) is the 'life line' for patients with end-stage renal disease (ESRD) undergoing hemodialysis. AVF maturation failure is a poorly understood process, one of the contributors being endothelial dysfunction due to oxidative stress. Monoamine oxidases (MAOs) A and B were recently identified as novel sources of vascular oxidative stress. The aim of the present study was to assess the contribution of MAOs to the endothelial dysfunction in patients with ESDR with indication of hemodialysis...
July 28, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28751116/monoamine-oxidase-b-oxidizes-a-novel-multikinase-inhibitor-kw-2449-to-its-iminium-ion-and-aldehyde-oxidase-further-converts-it-to-the-oxo-piperazine-form-in-human
#17
Jun Hosogi, Rui Ohashi, Hiroshi Maeda, Satoshi Tashiro, Eiichi Fuse, Yorihiro Yamamoto, Takashi Kuwabara
(E)-1-{4-[2-(1H-Indazol-3-yl)vinyl]benzoyl}piperazine (KW-2449) is a novel multikinase inhibitor. During our clinical study, we found that KW-2449 is mainly metabolized to its oxo-piperazine form (M1). An inhibition study suggested that monoamine oxidase-B (MAO-B) oxidizes KW-2449 to an iminium (intermediate) and aldehyde oxidase (AO) then metabolizes the intermediate to M1. The conversion of KW-2449 to the iminium (intermediate) by MAO-B was confirmed by the formation of its cyanide adduct. This cooperative metabolic pathway by MAO-B and AO was newly identified in the metabolism of piperazine...
June 22, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28744755/resveratrol-protects-against-vacuous-chewing-movements-induced-by-chronic-treatment-with-fluphenazine
#18
Alcindo Busanello, Caroline Queiroz Leal, Luis Ricardo Peroza, Jivago Röpke, Elizete de Moraes Reis, Catiuscia Molz de Freitas, Milena Libardoni, Nilda Berenice de Vargas Barbosa, Roselei Fachinetto
Typical antipsychotics, which are commonly used to treat schizophrenia, cause motor disorders such as tardive dyskinesia (TD) in humans and orofacial dyskinesia (OD) in rodents. The disease mechanisms as well as treatment effectiveness are still unknown. In this study, we investigated the effect of resveratrol, a polyphenol with neuroprotective properties, on behavioral changes induced by chronic treatment with fluphenazine in rats and the possible relationship between monoamine oxidase (MAO) activity and vacuous chewing movements (VCMs)...
July 25, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28728104/design-synthesis-and-evaluation-of-coumarin-pargyline-hybrids-as-novel-dual-inhibitors-of-monoamine-oxidases-and-amyloid-%C3%AE-aggregation-for-the-treatment-of-alzheimer-s-disease
#19
Hua-Li Yang, Pei Cai, Qiao-Hong Liu, Xue-Lian Yang, Fan Li, Jin Wang, Jia-Jia Wu, Xiao-Bing Wang, Ling-Yi Kong
A series of coumarin-pargyline hybrids (4a-x) have been designed, synthesized and evaluated as novel dual inhibitors of Alzheimer's disease (AD). Most of the compounds exhibited a potent ability to inhibit amyloid-β (Aβ) aggregation and monoamine oxidases. In particular, compound 4x exhibited remarkable inhibitory activities against monoamine oxidases (IC50, 0.027 ± 0.004 μM for MAO-B; 3.275 ± 0.040 μM for MAO-A) and Aβ1-42 aggregation (54.0 ± 1.1%, 25 μM). Moreover, compound 4x showed low toxicity according to in vitro cell toxicity test...
July 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28726524/subnanomolar-indazole-5-carboxamide-inhibitors-of-monoamine-oxidase-b-mao-b-continued-indications-of-iron-binding-experimental-evidence-for-optimised-solubility-and-brain-penetration
#20
Nikolay T Tzvetkov, Liudmil Antonov
Pharmacological and physicochemical studies of N-unsubstituted indazole-5-carboxamides (subclass I) and their structurally optimised N1-methylated analogues (subclass II), initially developed as drug and radioligand candidates for the treatment and diagnosis of Parkinson's disease (PD), are presented. The compounds are highly brain permeable, selective, reversible, and competitive monoamine oxidase B (MAO-B) inhibitors with improved water-solubility and subnanomolar potency (pIC50 >8.8). Using a well-validated, combined X-ray/modelling technology platform, we performed a semi-quantitative analysis of the binding modes of all compounds and investigated the role of the indazole N1 position for their MAO-B inhibitory activity...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
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