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Acetylcholinesterase inhibition
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Currently, nearly 36.5 million people live with Alzheimer’s disease worldwide, and acetylcholinesterase inhibition is considered the main treatment strategy against it. Seaweeds (or macroalgae) are a natural source of high-value bioactive compounds and have great potential in the production of health foods/foods, pharmaceuticals, cosmetics, animal feeds, biofertilizers, and biofuels.
13p
vicaptainmarvel
21-04-2023
2
2
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In this study, anticholinergic, antidiabetic, antioxidant and cytotoxic activities of Reseda lutea L. (R. lutea) were determined. Ethanol extracts of R. lutea (EERL) and water extract of R. lutea (WERL) were prepared for biochemical analysis. The antioxidant capacities of EERL and WERL were evaluated with 6 different methods. In addition, acetylcholinesterase (AChE), α-amylase and α-glycosidase enzyme inhibition by EERL were measured.
16p
lyhuyenthu
31-01-2023
3
2
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Alzheimer’s disease (AD) is a progressive neurodegenerative disorder and the main cause of dementia in the elderly population. Since the treatment of AD has been associated with the activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), their inhibitors remain the main focus of AD investigations. In this study we evaluated cholinesterase inhibitory activity of 14 bicyclo[3.2.1]octene/octadiene derivatives and naturally occurring sesquiterpene alcohol cedrol.
21p
tudichquannguyet
29-11-2021
3
0
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Coordination compounds containing dicyanoargentate(I) have remarkable biological potential due to their therapeutic antibacterial, antifungal, antibiofilm, and anticancer properties. In this study, a new dicyanoargentate(I)- based complex was synthesized and characterized by various procedures (elemental, thermal, FT-IR for complex) involving crystal analysis of the complex. In addition, the biological activity of this new compound on the acetylcholinesterase (AChE) enzyme, an important enzyme for the nervous system, was investigated.
12p
tudichquannguyet
29-11-2021
9
2
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N-(1-(4-Methoxyphenyl)-3-oxo-3-((4-(N-(substituted)sulfamoyl)phenyl)amino)prop-1-en-1-yl)benzamides 3a – g were designed since sulfonamide and benzamide pharmacophores draw great attention in novel drug design due to their wide range of bioactivities including acetylcholinesterase (AChE) and human carbonic anhydrase I and II (hCA I and hCA II) inhibitory potencies. Structure elucidation of the compounds was carried out by 1 H NMR, 13C NMR, and HRMS spectra.
28p
tudichquannguyet
29-11-2021
13
1
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In this study, hydroxy benzoin (1-7), benzil (8-14), and benzoin/benzil-O-β-D-glucosides (15-25) were synthesized to investigate their biological activities. An efficient method for synthesizing hydroxy benzoin compounds (1-7) was prepared from four different benzaldehydes using an ultrasonic bath. Then, antioxidant (FRAP, CUPRAC, and DPPH), antimicrobial (3 Gram (-), 4/6 Gram (+), one tuberculosis and one fungus), and enzyme inhibition (acetylcholinesterase, butyrylcholine esterase, tyrosinase, α-amylase, and α- glucosidase) for the all synthesized compounds (1-25) were evaluated.
17p
tudichquannguyet
29-11-2021
13
1
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In this study, a new series of Mannich bases, 3-(aminomethyl)-6-{3-[4-(trifluoromethyl)phenyl]acryloyl}-2(3H)- benzoxazolones (1a–g), were synthesized by the Mannich reaction. Inhibitory effects of the newly synthesized compounds towards carbonic anhydrases (CAs) and acetylcholinesterase (AChE) enzymes were evaluated to find out new potential drug candidate compounds. According to the inhibitory activity results, Ki values of the compounds 1 and 1a–g were in the range of 12.3 ± 1.2 to 154.0 ± 9.3 nM against hCA I, and they were in the range of 8.6 ± 1.9 to 41.0 ± 5.5 nM against hCA II.
14p
tudichquannguyet
29-11-2021
6
1
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In this study, the synthesis of new monostyryl (BDPY-2) and distyryl BODIPY dyes (BDPY-4, BDPY-5) containing pyridine groups has been reported for the first time. The acetylcholinesterase from Electrophorus electricus (AChE), butyrylcholinesterase from equine serum (BuChE), α-glucosidase from Saccharomyces cerevisiae and DNA hydrolytic cleavage actions of BDPY-2, BDPY-4, BDPY5 were investigated using various techniques. The results indicated that the compounds had varying inhibition properties against AChE, BuChE, and α-glucosidase.
14p
tudichquannguyet
29-11-2021
4
1
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Objectives of the dissertation: Research and synthesize and determine the hybrid compound structure containing Quinazoline frame. Research on carcinogenic activity and inhibition of acetylcholinesterase enzyme of synthetic compounds..
26p
extraenglish
24-05-2021
19
3
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Hippeastrum reticulatum (L.Hér.) Herb is a species of the Hippeastrum Herb. genus. Screening studies have shown that this species has the ability to inhibit the enzyme acetylcholinesterase. So far, research on this species is still very limited. The purpose of this study is to provide some more informations about the chemical composition and bioactive of isolated compounds from this species.
5p
cothumenhmong11
06-05-2021
21
2
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Synthesis and structural determination of some 4-aminoquinazoline derivatives containing prop-2-yn-1-yloxy substituents at C-6 position; research and synthesize and determine the hybrid compound structure containing Quinazoline frame; research on carcinogenic activity and inhibition of acetylcholinesterase enzyme of synthetic compounds; studying protein docking and predicting the pharmacokinetic properties of some compounds that inhibit the enzyme acetylcholinesterase.
26p
capheviahe27
23-02-2021
34
3
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Based on in vitro and in vivo rat experiments, the newly developed acetylcholinesterase (AChE) reactivator, K203, appears to be much more effective in the treatment of tabun poisonings than currently fielded oximes.
10p
vimax2711
30-03-2020
9
2
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Synthesis and bioactivity testing of some novel N-(adamantan-1-yl)-1-arylmethanimines derivatives. Methods: The novel of N-(adamantan-1-yl)-1-aryl-methanimines were synthesized by the condensation of 1-aminoadamantane with aromatic aldehydes in absolute ethanol under the catalyzation of acetic acid. Synthesized compounds were bioactivity tested as inhibition of acetylcholinesterase, antimicrobial, anticancer in vitro.
7p
caygaolon
01-11-2019
31
1
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The antioxidant and acetylcholinesterase inhibitory potential of methanol extract from Arnica montana cultivated in Bulgaria was evaluated. For the determination of antioxidant activity 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) di-ammonium salt (ABTS) free radicals, and ferric reducing antioxidant power (FRAP) assay were used.
6p
vivant2711
01-02-2019
35
0
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Arnebia densiflora Ledeb. (Boraginaceae), a medicinal plant growing in Turkey, has been reported to contain a well-known red pigment, shikonin, a naphthoquinone derivative. In the current study, the acetylcholinesterase (AChE) inhibitory and antioxidant activities of the chloroform, ethyl acetate, methanol, and water extracts of the root, stem, and flowers of the plant, as well as shikonin, were investigated.
5p
vivant2711
01-02-2019
30
1
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This report presents the results of ternary alloy quantum dots (TQDs) manufacturing and its superior optical properties to fabricate the biosensor for pesticide detection. The explanation for the changes in PL intensity based on the change of electronic charges that alters the pH value of the surrounding environment, and the types of interaction on the surface of CdZnSe/ZnS TQDs were discussed.
7p
thuyliebe
09-10-2018
29
0
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Acetylcholine hydrolysis by acetylcholinesterase is inhi-bited at high substrate concentrations. To determine the residues involved in this phenomenon, we have mutated most of the residues lining the active-site gorge but mutating these did not completely eliminate hydrolysis. Thus, we analyzed the effect of a nonhydrolysable sub-strate analogue on substrate hydrolysis and on reactiva-tion of an analogue of the acetylenzyme.
8p
dell39
03-04-2013
22
3
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The hydrolysis of acetylthiocholine by acetylcholinesterase fromElectro-phorus electricuswas investigated in the presence of the inhibitors tacrine, gallamine and compound1. The interaction of the enzyme with the sub-strate and the inhibitors was characterized by the parametersKI , a¢, borb, Kmand Vmax, which were determined directly and simultaneously from nonlinear Michaelis–Menten plots.
16p
viettel02
22-02-2013
22
2
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Such pesticides are widely used agricultural inputs, and they are esters of the phosphoric acid and the derivates thereof, and they share in common as a pharmacological characteristic, the action of inhibiting enzymes having esteracic activities, and more specifically, the inhibition of the acetylcholinesterase. They are easily hydrolyze and they have a low capacity of remaining in the environment (Palacios and Moreno, 2004), (Chakraborty, 2009), (Ntow et al, 2009). Other pesticides under study are the organochlorated, which are persistent, lypophilic and very steady.
428p
conquynho32
18-09-2012
73
11
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