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acetylcholinesterase

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https://www.readbyqxmd.com/read/28822269/correlation-of-cholinergic-drug-induced-quenching-of-acetylcholinesterase-bound-thioflavin-t-fluorescence-with-their-inhibition-activity
#1
Mullah Muhaiminul Islam, Mostofa Ataur Rohman, Arun Bahadur Gurung, Atanu Bhattacharjee, Kripamoy Aguan, Sivaprasad Mitra
The development of new acetylcholinesterase inhibitors (AChEIs) and subsequent assay of their inhibition efficiency is considered to be a key step for AD treatment. The fluorescence intensity of thioflavin-T (ThT) bound in the active site of acetylcholinesterase (AChE) quenches substantially in presence of standard AChEI drugs due to the dynamic replacement of the fluorophore from the AChE active site as confirmed from steady state emission as well as time-resolved fluorescence anisotropy measurement and molecular dynamics simulation in conjunction with docking calculation...
August 5, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28821921/anti-nociceptive-effect-of-stigmasterol-in-mouse-models-of-acute-and-chronic-pain
#2
Cristiani Isabel Banderó Walker, Sara Marchesan Oliveira, Raquel Tonello, Mateus Fortes Rossato, Evelyne da Silva Brum, Juliano Ferreira, Gabriela Trevisan
Stigmasterol is a common sterol found in plants, but the anti-nociceptive effect of this compound and its mechanism of action are not fully explored. Thus, in the present study, the anti-nociceptive effect of stigmasterol was investigated in acute and chronic models of pain and its mechanism of action. We used adult male albino Swiss mice (25-35 g) to observe the anti-nociceptive effect of stigmasterol in acetic-acid writhing test or in complete Freund's adjuvant injection, surgical incision in hind paw, or partial sciatic nerve ligation...
August 18, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28821158/synthesis-characterization-bioactivity-and-potential-application-of-phenolic-acid-grafted-chitosan-a-review
#3
REVIEW
Jun Liu, Huimin Pu, Shuang Liu, Juan Kan, Changhai Jin
In recent years, increasing attention has been paid to the grafting of phenolic acid onto chitosan in order to enhance the bioactivity and widen the application of chitosan. Here, we present a comprehensive overview on the recent advances of phenolic acid grafted chitosan (phenolic acid-g-chitosan) in many aspects, including the synthetic method, structural characterization, biological activity, physicochemical property and potential application. In general, four kinds of techniques including carbodiimide based coupling, enzyme catalyzed grafting, free radical mediated grafting and electrochemical methods are frequently used for the synthesis of phenolic acid-g-chitosan...
October 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28819811/circulating-extracellular-vesicles-in-the-aging-process-impact-of-aerobic-exercise
#4
Karine Bertoldi, Laura Reck Cechinel, Bruna Schallenberger, Giana Blume Corssac, Samuel Davies, Irene Clemes Külkamp Guerreiro, Adriane Belló-Klein, Alex Sander R Araujo, Ionara Rodrigues Siqueira
Our aim was to investigate transitory and delayed exercise effects on serum extracellular vesicles (EVs) in aging process. Male Wistar rats of 3-, 21-, and 26-month old were allocated into exercised and sedentary groups. The exercise protocol consisted in a daily moderate treadmill exercise (20 min daily during 2 weeks). Trunk blood was collected 1 and 18 h after the last exercise session, and circulating EVs were obtained. CD63 levels and acetylcholinesterase (AChE) activity were used as markers of exosome, a subtype of EVs...
August 17, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28818531/the-position-of-fluorine-in-cp-118-954-affects-ache-inhibition-potency-and-pet-imaging-quantification-for-ache-expression-in-the-rat-brain
#5
Byung Chul Lee, Byung Seok Moon, Hyun Soo Park, Jae Ho Jung, Hyun Sik Park, Do Dam Park, Modesto de Candia, Nunzio Denora, Cosimo D Altomare, Sang Eun Kim
The in vitro inhibition potency against acetylcholinesterase (AChE) of fluorinated derivatives of CP-118,954 (1) has been shown to depend upon the position of aromatic fluorine (F) substitution on the N-benzyl moiety. Indeed, the meta-F-substituted compound 3 (IC50=1.4nM) shows similar potency with the parent compound 1 (IC50=1.2nM), whereas the ortho-F derivative 2 (IC50=3.2nM) and para-F derivative 4 (IC50=10.8nM) were found to be less potent AChE inhibitors. A comparative in vivo microdialysis study in rats showed that 3 has the strongest effect on the neuropharmacological properties as AChE inhibitor...
August 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28818332/antimicrobial-activity-and-acetylcholinesterase-inhibition-by-extracts-from-chromatin-modulated-fungi
#6
Matheus Thomaz Nogueira Silva Lima, Larissa Batista Dos Santos, Rafael Wesley Bastos, Jacques Robert Nicoli, Jacqueline Aparecida Takahashi
Major health challenges as the increasing number of cases of infections by antibiotic multiresistant microorganisms and cases of Alzheimer's disease have led to searching new control drugs. The present study aims to verify a new way of obtaining bioactive extracts from filamentous fungi with potential antimicrobial and acetylcholinesterase inhibitory activities, using epigenetic modulation to promote the expression of genes commonly silenced. For such finality, five filamentous fungal species (Talaromyces funiculosus, Talaromyces islandicus, Talaromyces minioluteus, Talaromyces pinophilus, Penicillium janthinellum) were grown or not with DNA methyltransferases inhibitors (procainamide or hydralazine) and/or a histone deacetylase inhibitor (suberohydroxamic acid)...
August 1, 2017: Brazilian Journal of Microbiology: [publication of the Brazilian Society for Microbiology]
https://www.readbyqxmd.com/read/28817076/spirulina-maxima-extract-prevents-neurotoxicity-via-promoting-activation-of-bdnf-creb-signaling-pathways-in-neuronal-cells-and-mice
#7
Eun-Jeong Koh, Young-Jin Seo, Jia Choi, Hyeon Yong Lee, Do-Hyung Kang, Kui-Jin Kim, Boo-Yong Lee
Spirulina maxima is a microalgae which contains flavonoids and other polyphenols. Although Spirulina maxima 70% ethanol extract (SM70EE) has diverse beneficial effects, its effects on neurotoxicity have not been fully understood. In this study, we investigated the neuroprotective effects of SM70EE against trimethyltin (TMT)-induced neurotoxicity in HT-22 cells. SM70EE inhibited the cleavage of poly-ADP ribose polymerase (PARP). Besides, ROS production was decreased by down-regulating oxidative stress-associated enzymes...
August 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28816008/lactuca-capensis-reverses-memory-deficits-in-a%C3%AE-1-42-induced-an-animal-model-of-alzheimer-s-disease
#8
Paula Alexandra Postu, Jaures A K Noumedem, Oana Cioanca, Monica Hancianu, Marius Mihasan, Mitica Ciorpac, Dragos Lucian Gorgan, Brindusa Alina Petre, Lucian Hritcu
We investigated the neuropharmacological effects of the methanolic extract from Lactuca capensis Thunb. leaves (100 and 200 mg/kg) for 21 days on memory impairment in an Alzheimer's disease (AD) rat model produced by direct intraventricular delivery of amyloid-β1-42 (Aβ1-42). Behavioural assays such as Y-maze and radial arm maze test were used for assessing memory performance. Aβ1-42 decreased cognitive performance in the behavioural tests which were ameliorated by pre-treatment with the methanolic extract...
August 16, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/28814961/compound-schisandra-ginseng-notoginseng-lycium-extract-ameliorates-scopolamine-induced-learning-and-memory-disorders-in-mice
#9
Ning Li, Cong Liu, Shu Jing, Mengyang Wang, Han Wang, Jinghui Sun, Chunmei Wang, Jianguang Chen, He Li
Schisandra, Ginseng, Notoginseng, and Lycium barbarum are traditional Chinese medicinal plants sharing cognitive-enhancing properties. To design a functional food to improve memory, we prepared a compound Schisandra-Ginseng-Notoginseng-Lycium (CSGNL) extract and investigated its effect on scopolamine-induced learning and memory loss in mice. To optimize the dose ratios of the four herbal extracts in CSGNL, orthogonal experiments were performed. Mice were administered CSGNL by gavage once a day for 30 days and then mouse learning and memory were evaluated by Morris water maze and step-through tests...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28811187/chiral-resolution-absolute-configuration-and-bioactivity-of-a-new-racemic-asarone-derivative-from-the-rhizome-of-acorus-tatarinowii
#10
En Gao, Fei-Fei Ren, Jian Zou, Yang Yu, Hong-Xia Fan, Zheng-Qun Zhou, Guo-Dong Chen, Rong-Rong He, Xin-Sheng Yao, Hao Gao
A new asarone-derived racemate (1) was isolated from the rhizome of Acorus tatarinowii. The structure of 1 was established by comprehensive spectroscopic analyses, and it was successfully resolved by chiral HPLC, demonstrating that it is racemic. The absolute configurations of 1a [(-)-acortatarone A] and 1b [(+)-acortatarone A] were determined using quantum chemical calculations. Compounds 1a and 1b were the first cases of asarone derivatives with the 5,7-dialkyl-6-aryl-8-oxabicyclo[3.2.1]oct-3-en-2-one core...
August 12, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28810519/the-beneficial-role-of-naringin-a-citrus-bioflavonoid-against-oxidative-stress-induced-neurobehavioral-disorders-and-cognitive-dysfunction-in-rodents-a-systematic-review-and-meta-analysis
#11
REVIEW
Gollapalle Lakshminarayanashastry Viswanatha, H Shylaja, Yogananda Moolemath
OBJECTIVES: Naringin is a bioflavonoid, very abundantly found in citrus species. In literature, naringin has been scientifically well documented for its beneficial effects in various neurological disorders. In this systematic review and meta-analysis, we have made an attempt to correlate the protective role of naringin against oxidative stress-induced neurological disorders in rodents. METHODS: The systematic search was performed using electronic databases; the search was mainly focused on the role of naringin in oxidative stress-induced neuropathological conditions in rodents...
August 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28810188/novel-tacrine-derivatives-exhibiting-improved-acetylcholinesterase-inhibition-design-synthesis-and-biological-evaluation
#12
Eeda Koti Reddy, Chandran Remya, Kumar Mantosh, Ayyiliath M Sajith, R V Omkumar, C Sadasivan, Shaik Anwar
A novel series of twenty four tacrine derivatives were designed and synthesised. Among these, thirteen were taken for the acetylcholinesterase (AChE) inhibition studies. Three compounds such as 4c, 6c and 6f were found to possess significant AChE inhibitory properties with IC50 values 12.97 ± 0.47 nM, 5.17 ± 0.24 nM and 7.14 ± 0.78 nM respectively. In silico docking studies revealed that these compounds can bind strongly in the active site of the enzyme and prevent enzyme-substrate interactions...
August 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28809439/in-silico-profiling-of-the-biological-activities-of-amaryllidaceae-alkaloids
#13
Eman Shawky
OBJECTIVES: The large number of publications about Amaryllidaceae alkaloids reflects the abundance and variety in biological activity of these alkaloids. An in-silico approach was implemented in this work to rationalize the individual alkaloids to molecular biological activity. METHODS: A database was generated containing 313 Amaryllidaceae alkaloids which were then subjected to in-silico-validated structure-based virtual screening using extra precision (XP) approach of Glide docking program...
August 15, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28806470/efficacy-and-safety-of-sugammadex-versus-neostigmine-in-reversing-neuromuscular-blockade-in-adults
#14
REVIEW
Ana-Marija Hristovska, Patricia Duch, Mikkel Allingstrup, Arash Afshari
BACKGROUND: Acetylcholinesterase inhibitors, such as neostigmine, have traditionally been used for reversal of non-depolarizing neuromuscular blocking agents. However, these drugs have significant limitations, such as indirect mechanisms of reversal, limited and unpredictable efficacy, and undesirable autonomic responses. Sugammadex is a selective relaxant-binding agent specifically developed for rapid reversal of non-depolarizing neuromuscular blockade induced by rocuronium. Its potential clinical benefits include fast and predictable reversal of any degree of block, increased patient safety, reduced incidence of residual block on recovery, and more efficient use of healthcare resources...
August 14, 2017: Cochrane Database of Systematic Reviews
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
#15
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/28805453/colletotrichine-a-a-new-sesquiterpenoid-from-colletotrichum-gloeosporioides-gt-7-a-fungal-endophyte-of-uncaria-rhynchophylla
#16
Xiao-Wei Chen, Zhong-Duo Yang, Jian-Hui Sun, Tong-Tong Song, Bao-Ying Zhu, Jun-Wen Zhao
One new compound, Colletotrichine A (1), was produced by the fungal Colletotrichum gloeosporioides GT-7. The structure was established by 1D and 2D NMR spectra. Monoamine oxidase (MAO) and acetylcholinesterase (AChE) inhibitory activity of 1 was also evaluated. Compound 1 showed AChE-inhibiting activity with IC50 value of 28 μg/mL.
August 14, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28802958/interaction-of-erythromycin-and-ketoconazole-on-the-neurological-biochemical-and-behavioral-responses-in-crucian-carp
#17
Jianchao Liu, Yuanfei Cai, Guanghua Lu, Xiaoxiang Dan, Donghai Wu, Zhenhua Yan
The presence of pharmaceuticals in the aquatic environment has received great attention due to their potential impacts on public health. The single, as well as the combined toxicities of erythromycin (ERY) and ketoconazole (KCZ) on the bioaccumulation, biochemical and behavioral responses, were examined in crucian carp. This study focused on the uptake of contaminants, acetylcholinesterase (AChE) activity in the brain, swimming and shoaling behavior of fish. After 14days of binary exposure, the addition of KCZ at nominal concentrations of 0...
August 7, 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28802122/piperlongumine-b-and-analogs-are-promising-and-selective-inhibitors-for-acetylcholinesterase
#18
Jana Wiemann, Julia Karasch, Anne Loesche, Lucie Heller, Wolfgang Brandt, René Csuk
Piperlongumine B (19), an alkaloid previously isolated from long pepper (Piper longum) has been synthesized for the first time in a short sequence and in good yield together with 19 analogs. Screening of these compounds in Ellman's assays showed several of them to be good inhibitors of acetylcholinesterase while being less active for butyrylcholinesterase. Activity of the compounds increased with the ring size of the heterocycle, and a maximum of activity was observed for an analog holding 12 methylene groups in the aliphatic side chain...
August 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28800181/synephrine-and-phenylephrine-act-as-%C3%AE-amylase-%C3%AE-glycosidase-acetylcholinesterase-butyrylcholinesterase-and-carbonic-anhydrase-enzymes-inhibitors
#19
Parham Taslimi, Hülya Akıncıoglu, İlhami Gülçin
In this paper, synephrine and phenylephrine compounds showed excellent inhibitory effects against human carbonic anhydrase (hCA) isoforms I and II, α-amylase, α-glycosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). Synephrine and phenylephrine had Ki values of 199.02 ± 16.01 and 65.01 ± 5.00 μM against hCA I and 336.02 ± 74.01 and 92.04  ±  18.03 μM against hCA II, respectively. On the other hand, their Ki values were found to be 169.10  ±  80.03 and 88.03  ±  5...
August 11, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28797788/novel-dehydroabietylamine-derivatives-as-potent-inhibitors-of-acetylcholinesterase
#20
Jana Wiemann, Anne Loesche, René Csuk
Nowadays, the inhibition of acetylcholinesterase is one of the main pharmacological strategies for the treatment of Alzheimer's disease. Therefore, a set of thirty-four derivatives of the diterpenoid dehydroabietylamine has been synthesized and screened in colorimetric Ellman's assays to determine their ability to inhibit the enzymes acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine serum). A systematic variation of the substitution of dehydroabietylamides enabled an approach to analogs showing a remarkable inhibition potency for AChE...
August 1, 2017: Bioorganic Chemistry
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