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Parham Taslimi, Cuneyt Caglayan, Vagif Farzaliyev, Oruj Nabiyev, Afsun Sujayev, Fikret Turkan, Ruya Kaya, İlhami Gulçin
During this investigation, N,N'-bis-azidomethylamines, N,N'-bis-cyanomethylamine, new alkoxymethylamine and chiral derivatives, which are considered to be a new generation of multifunctional compounds, were synthesized, functional properties were investigated, and anticholinergic and antidiabetic properties of those compounds were studied through the laboratory tests, and it was approved that they contain physiologically active compounds rather than analogues. Novel N-bis-cyanomethylamine and alkoxymethylamine derivatives were effective inhibitors of the α-glycosidase, cytosolic carbonic anhydrase I and II isoforms, butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with Ki values in the range of 0...
February 19, 2018: Journal of Biochemical and Molecular Toxicology
Shu-Ying Liu, Daryl J Wile, Jessie Fanglu Fu, Jason Valerio, Elham Shahinfard, Siobhan McCormick, Rostom Mabrouk, Nasim Vafai, Jess McKenzie, Nicole Neilson, Alexandra Perez-Soriano, Julieta E Arena, Mariya Cherkasova, Piu Chan, Jing Zhang, Cyrus P Zabetian, Jan O Aasly, Zbigniew K Wszolek, Martin J McKeown, Michael J Adam, Thomas J Ruth, Michael Schulzer, Vesna Sossi, A Jon Stoessl
BACKGROUND: Markers of neuroinflammation are increased in some patients with LRRK2 Parkinson's disease compared with individuals with idiopathic Parkinson's disease, suggesting possible differences in disease pathogenesis. Previous PET studies have suggested amplified dopamine turnover and preserved serotonergic innervation in LRRK2 mutation carriers. We postulated that patients with LRRK2 mutations might show abnormalities of central cholinergic activity, even before the diagnosis of Parkinson's disease...
February 15, 2018: Lancet Neurology
Esther E Nwanna, Adeniyi A Adebayo, Ganiyu Oboh, Opeyemi B Ogunsuyi, Ayokunle O Ademosun
Most alkaloids are produced by plants as a defense mechanism against herbivores. Since alkaloids are known to possess pharmacological effects, this study sought to investigate the in vitro modulatory effect of alkaloid obtained from two commonly consumed vegetables in southern Nigeria, Lasianthera africana (editan) and Gongronema latifolium (utazi), on some enzyme activities relevant to neurodegeneration. Effects of the alkaloids on cholinesterases (acetylcholinesterase [AChE] and butyrylcholinesterase [BChE]) and monoamine oxidase (MAO) activities were determined in vitro...
February 16, 2018: Journal of Dietary Supplements
Minsu Kim, Kangwon Lee, Ji Eon Kwon, Won Gun Koh
In this study, we developed an enzyme-based miniaturized fluorescence biosensor to detect paraoxon, one of the most well-known neurotoxic organophosphorus compounds (OPs). The biosensor was fabricated with poly(ethylene glycol) (PEG) hydrogel microarrays that entrapped acetylcholinesterase (AChE) and quantum dots (QDs) as fluorescence reporters. Metal-enhanced fluorescence (MEF) was utilized to amplify the fluorescence signal, which was achieved by decorating QDs on the surface of silica-coated silver nanoparticles (Ag@Silica)...
February 16, 2018: Biofabrication
Jiali Jin, Tomofumi Kurobe, Wilson F Ramírez-Duarte, Melissa B Bolotaolo, Chelsea H Lam, Pramod K Pandey, Tien-Chieh Hung, Marie E Stillway, Leanna Zweig, Jeffrey Caudill, Li Lin, Swee J Teh
Concerns regarding non-target toxicity of new herbicides used to control invasive aquatic weeds in the San Francisco Estuary led us to compare sub-lethal toxicity of four herbicides (penoxsulam, imazamox, fluridone, and glyphosate) on an endangered fish species Delta Smelt (Hypomesus transpacificus). We measured 17β-estradiol (E2) and glutathione (GSH) concentrations in liver, and acetylcholinesterase (AChE) activity in brain of female and male fish after 6 h of exposure to each of the four herbicides. Our results indicate that fluridone and glyphosate disrupted the E2 concentration and decreased glutathione concentration in liver, whereas penoxsulam, imazamox, and fluridone inhibited brain AChE activity...
February 1, 2018: Aquatic Toxicology
Aline Rocha de Melo, Israel J Pereira Garcia, José Eduardo Serrão, Hérica Lima Santos, Luciana A Rodrigues Dos Santos Lima, Stênio Nunes Alves
The Culex quinquefasciatus mosquito is a vector of several diseases, and its control has been performed with synthetic insecticides, which may have human and environmental side effects. Thus, the use of new and safe molecules are important, and this study evaluated the toxicity of active substances against this mosquito. The oleic, linoleic, linolenic, palmitic and stearic acids and their respective methyl esters were tested against fourth instar C. quinquefasciatus larvae. Oleic, linoleic and linolenic acids had LC50 values of 8...
February 12, 2018: Ecotoxicology and Environmental Safety
Xiaohui Gao, Jingjing Tang, Haoran Liu, Linbo Liu, Lu Kang, Wen Chen
In the present investigation, 48 new tertiary amine derivatives of cinnamic acid, phenylpropionic acid, sorbic acid and hexanoic acid (4d-6g, 10d-12g, 16d-18g and 22d-24g) were designed, synthesized and evaluated for the effect on AChE and BChE in vitro. The results revealed that the alteration of aminoalkyl types and substituted positions markedly influences the effects in inhibiting AChE. Almost of all cinnamic acid derivatives had the most potent inhibitory activity than that of other acid derivatives with the same aminoalkyl side chain...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Balaji Govindan, Anil John Johnson, Gayathri Viswanathan, Venkataraman Ramaswamy, Konnath Chacko Koshy, Sabulal Baby
Phytochemistry of fruits and leaves of the unique bamboo Melocanna baccifera resulted in the isolation of 27 secondary metabolites, including 4-Oxabicyclo[3.2.2]nona-1(7),5,8-triene and Verbacine. Biological activity studies of Verbacine revealed it as an inhibitor of acetylcholinesterase and as cytotoxic against C6 cancer cells.
February 15, 2018: Natural Product Research
Hongxia Li, Xu Yan, Shanpeng Qiao, Geyu Lu, Xingguang Su
Carbon dots (CDs) attract increasing interest in bioimaging and sensing recently. Herein, we present a simple synthetic strategy to prepare yellow-emission CDs (λem = 535 nm) by one-pot hydrothermal treatment of p-phenylenediamine and aspartic acid. The as-prepared CDs possess outstanding optical features, excellent biocompatibility and low cytotoxicity, especially for fluorescence cellular imaging. Interestingly, by combining the quenching and recognition ability of AgNPs with the optical capacity of CDs, a label-free strategy for specifically monitoring H2O2-generated biocatalytic processes was proposed, such as glucose oxidase-induced conversion of glucose, cholesterol oxidase-catalyzed oxidization of cholesterol, bi-enzyme of acetylcholinesterase and choline oxidase-mediated reaction of acetylcholine...
February 14, 2018: ACS Applied Materials & Interfaces
Corina O Bondi, Narayana K Yelleswarapu, Julian Day-Cooney, Kimiya Memarzadeh, Kaitlin A Folweiler, Carine E Bou-Abboud, Jacob B Leary, Jeffrey P Cheng, Roya Tehranian-DePasquale, Anthony E Kline
BACKGROUND: The acetylcholinesterase inhibitor (AChEI) donepezil (DON) is recommended as a potential treatment for cognition after clinical traumatic brain injury (TBI) and therefore may be prescribed as an adjunct therapy during rehabilitation. However, a dose-response study evaluating DON after a controlled cortical impact (CCI) injury in rats did not reveal cognitive benefits. OBJECTIVE: The aim of this study was to determine the effect of DON on behavioral and histological outcome when combined with environmental enrichment (EE), a preclinical model of neurorehabilitation...
2018: Restorative Neurology and Neuroscience
Núbia Fernanda Marinho Rodrigues, Sakae Yotsumoto Neto, Rita de Cássia Silva Luz, Flávio Santos Damos, Hideko Yamanaka
A renewable, disposable, low cost, and sensitive sensor for the detection of organophosphorus pesticides was constructed by immobilizing the acetylcholinesterase enzyme (AChE), via glutaraldehyde, on magnetic iron nanoparticles (Fe₃O₄) previously synthesized and functionalized with chitosan (CS). The sensor was denoted AChE/CS/Fe₃O₄. The magnetic nanoparticles were characterized by Fourier transform infrared spectroscopy and transmission electron microscopy. Acetylthiocholine (ATCh) was incubated with AChE/CS/Fe₃O₄ and attached to a screen-printed electrode using a magnet...
February 13, 2018: Biosensors
Ganiyu Oboh, Sunday I Oyeleye, Omoyemi A Akintemi, Tosin A Olasehinde
There are strong correlations between diabetes mellitus and cognitive dysfunction. This study sought to investigate the modulatory effects of Moringa oleifera leaf (ML) and seed (MS) inclusive diets on biomolecules [acetylcholinesterase (AChE), butyrylcholinesterase (BChE)] angiotensin-I converting enzyme (ACE), arginase, catalase, glutathione transferase (GST) and glutathione peroxidase (GSH-Px) activities, glutathione (GSH) and nitric oxide (NO) levels] associated with cognitive function in the brain of streptozotocin (STZ)-induced diabetic rats treated with acarbose (ACA)...
February 12, 2018: Metabolic Brain Disease
Youngmi Koo, Brian T Hawkins, Yeoheung Yun
Organophosphate-based compounds (OPs) represent a significant threat to warfighters (nerve agents) and civilian populations (pesticides). There is a pressing need to develop in vitro brain models that correlate to the in vivo brain to rapidly study OPs for neurotoxicity. Here we report on a microfluidic-based three-dimensional, four-cell tissue construct consisting of 1) a blood-brain barrier that has dynamic flow and membrane-free culture of the endothelial layer, and 2) an extracellular matrix (ECM)-embedded tissue construct with neuroblastoma, microglia, and astrocytes...
February 12, 2018: Scientific Reports
Javier E Ortiz, Adriana Garro, Natalia B Pigni, María Belén Agüero, German Roitman, Alberto Slanis, Ricardo D Enriz, Gabriela E Feresin, Jaume Bastida, Alejandro Tapia
BACKGROUND: In Argentina, the Amaryllidaceae family (59 species) comprises a wide variety of genera, only a few species have been investigated as a potential source of cholinesterases inhibitors to treat Alzheimer disease (AD). PURPOSE: To study the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the basic dichloromethane extracts (E) from Hieronymiella aurea, H. caletensis, H. clidanthoides, H. marginata, and H. speciosa species, as well as the isolated compounds from these plant extracts...
January 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Baiping Ren, Yonglan Liu, Yanxian Zhang, Yongqing Cai, Xiong Gong, Yung Chang, Lijian Xu, Jie Zheng
Abnormal misfolding and aggregation of amyloid peptides into amyloid fibrils are a common and critical pathological event in many neurodegenerative diseases. Most of inhibitors or drugs have been developed to prevent amyloid aggregation of a specific peptide, exhibiting sequence-dependent inhibition mechanisms. It is more challenging to develop or discover inhibitors capable of preventing the aggregation of two or more different amyloid peptides. Genistein, a major phytoestrogen in soybean, has been widely used as anti-inflammation and cerebrovascular drugs due to their anti-oxidation and anti-acetylcholinesterase effects...
February 12, 2018: ACS Chemical Neuroscience
Elsa Brito, André Silva, Pedro Luis Vieira Falé, Rita Pacheco, António Serralheiro, Parvez I Haris, Lia Ascensão, Maria Luísa Serralheiro
Rosmarinic acid (RA) is a phenolic compound with biological activity. The objective of the present study was to investigate whether this compound kept its biological activity in the presence of proteins. For this purpose, bovine serum albumin (BSA) was used as a model protein, and the capacity of the RA to inhibit acetylcholinesterase (AChE) and affect antioxidant activity was evaluated in the absence and presence of BSA. A mixture of phenolic compounds containing RA, obtained from a medicinal plant was added to this study...
February 12, 2018: Journal of Medicinal Food
Yusuke Hirasawa, Chiho Mitsui, Nahoko Uchiyama, Takashi Hakamatsuka, Hiroshi Morita
A novel class of C38N4 Lycopodium alkaloid, hupercumine A (1), consisting of two octahydroquinolines, a decahydroquinoline, and a piperidine, and a new C27N3-type alkaloid, hupercumine B (2), were isolated from Huperzia cunninghamioides (Hayata) Holub. The structures and absolute configurations of 1 and 2 were elucidated on the basis of spectroscopic data, chemical means, and biogenetic point of view. Hupercumines A (1) and B (2) showed moderate inhibitory activity against acetylcholinesterase.
February 12, 2018: Organic Letters
Y Li, Y H Li, X Zhou, B Wu, J P Chen, Z K Wang, X Wang, H J Shi, R S Li
The relationship of altered DNA 5'-hydroxymethylation in human spermatozoa with seminal parameters remains unclear. The aim of the study was to investigate the association between the 5'-hydroxymethylcytosine (5hmC) rate in the promoters of acetylcholinesterase (AChE) and homeobox C4 (HoxC4) genes and human sperm concentration/motility. The study population consisted of three groups: asthenozoospermia (AZ), oligoasthenozoospermia (OAZ) and normozoospermia (NZ). The 5hmC rate in the promoter was measured by CCGG loci-dependent MspI/HpaII restriction mapping of glycosylation-modified sperm DNA combined with a hydroxymethylation-specific real-time polymerase chain reaction assay...
February 11, 2018: Andrologia
Sandra Gonçalves, Joana Medronho, Elsa Moreira, Clara Grosso, Paula B Andrade, Patrícia Valentão, Anabela Romano
In this work we evaluated methanolic extracts from different parts (leaves, seeds, fruit peel and pulp) of Chamaerops humilis L. for antioxidant activity and the ability to inhibit enzymes linked with neurodegenerative diseases: acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase (TYR). The total content of phenolics, flavonoids and condensed tannins was also determined. The antioxidant and inhibitory activities of the extracts varied significantly according to the tissue. Seed extracts showed the greatest ability to scavenge DPPH (IC50 = 81...
February 2018: 3 Biotech
Florencia Aguirre, Andres M Villa
BACKGROUND: We investigated the prognosis of patients with myasthenia gravis (MG) initially presenting with only ocular symptoms in an Argentinian population. SUMMARY: We performed a retrospective analysis of 61 patients with MG with pure ocular involvement at onset. Generalized MG (gMG) developed in 73.7% of patients, while the rest only exhibited ocular symptoms throughout the course of the disease (ocular MG [oMG]). The AChR antibody (AChR-ab) was found in 81...
February 9, 2018: European Neurology
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