Abstract：
:A new series of substituted tacrine/acridine and tacrine/tacrine dimers with aliphatic or alkylene-thiourea linkers was synthesized and the potential of these compounds as novel human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE) inhibitors with nanomolar inhibition activity was evaluated. The most potent AChE inhibitor was found to be homodimeric tacrine derivative 14a, which demonstrated an IC50 value of 2 nM; this value indicates an activity rate which is 250-times higher than that of tacrine 1 and 7500-times higher than 7-MEOTA 15, the compounds which were used as standards in the study. IC50 values of derivatives 1, 9, 10, 14b and 15 were compared with the dissociation constants of the enzyme-inhibitor complex, Ki1, and the enzyme-substrate-inhibitor complex, Ki2, for. A dual binding site is presumed for the synthesized compounds which possess two tacrines or tacrine and acridine as terminal moieties show evidence of dual site binding. DFT calculations of theoretical desolvation free energies, ΔΔGtheor, and docking studies elucidate these suggestions in more detail.
journal_name
Int J Biol Macromoljournal_title
International journal of biological macromoleculesauthors
Hamulakova S,Imrich J,Janovec L,Kristian P,Danihel I,Holas O,Pohanka M,Böhm S,Kozurkova M,Kuca Kdoi
10.1016/j.ijbiomac.2014.06.064subject
Has Abstractpub_date
2014-09-01 00:00:00pages
435-9eissn
0141-8130issn
1879-0003pii
S0141-8130(14)00482-6journal_volume
70pub_type
杂志文章abstract：:Until now, there is a lack of knowledge about the presence of chitin in numerous representatives of corals (Cnidaria). However, investigations concerning the chitin-based skeletal organization in different coral taxa are significant from biochemical, structural, developmental, ecological and evolutionary points of vie...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
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abstract：:Dental caries and trauma, particularly in childhood, are among the most prevalent teeth problems, which result in the creation of cavities and probably tooth loss. Thus, novel regenerative approaches with high efficiency and less toxicity are required. Stem cell therapy along with the implementation of scaffolds has p...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章,评审
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abstract：:Starch retrogradation during freeze drying is a contributor to an undesirable decrease in the viscosity of soup prepared from instant soup with high starch content. Monitoring starch retrogradation during drying is therefore of importance if such a process is to be optimized. Here, cream mushroom soup was used as an e...
journal_title：International journal of biological macromolecules
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abstract：:The in vitro digestive and fermentation properties of Sargassum pallidum polysaccharide (SPP) after ultrasound degradation were investigated. The results showed that SPP and its degraded fractions were not affected by human saliva, but slightly degraded by breaking glycosidic bonds under simulated gastrointestinal dig...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
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更新日期：2020-12-01 00:00:00
abstract：:Wound healing is a complex, dynamic and difficult process. Much effort and attempt has been made to accelerate this process. The purpose of this study is to prepare nanoparticles loaded with vaccarin (VAC-NPS)hydrogel and evaluate its effect on promoting wound healing. In the present study, the physicochemical propert...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
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abstract：:Snake venoms contain various proteins, especially phospholipases A2 (PLA2s), which present potential applications in diverse areas of health and medicine. In this study, a new basic PLA2 from Bothrops marajoensis with parasiticidal activity was purified and characterized biochemically and biologically. B. marajoensis ...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
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abstract：:The effects of cinnamon essential oil (CEO) and Tween 80 addition on the structural, physical, antioxidant and antimicrobial properties of the pullulan-based edible films were investigated in this study. The results demonstrated that the incorporation of CEO in pullulan-based composite films decreased their tensile st...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
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abstract：:The current study involves development of novel tamarind seed gum - alginate complex microspheres for sustained release of dalfampridine by using Central Composite design in combination with response surface methodology. Polymer ratio (A), agitation speed (B) and concentration of CaCl2 (C) were selected as independent...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2019.11.203
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abstract：:Lamellar single crystals of amylose V glycerol were grown at 100 degrees C by evaporating water from solutions of amylose in aqueous glycerol. The crystals which were square, with lateral dimensions of several micrometers, gave sharp electron diffraction patterns presenting an orthorhombic symmetry with a probable spa...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
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更新日期：1996-02-01 00:00:00
abstract：:The aims of this work were designed to investigate the hepatoprotective and antioxidant effects of acidic- and alkali-extractable mycelia zinc polysaccharides (AcMZPS, AlMZPS) from Pleurotus eryngii var. tuoliensis on high-fat-high-cholesterol emulsion-induced hyperlipidemic mice. The in vivo experiments demonstrated ...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2016.11.060
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abstract：:One popular and relevant proposed function for cyanobacterial hemoglobin (Synechocystis Hb) is anaerobic nitrite reductase in vivo. During such reduction reactions, the hexacoordinated heme iron atom of SynHb is oxidized from the ferrous (Fe+2) to ferric (Fe+3) state and prevent damage by limiting the concentration of...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
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更新日期：2020-11-01 00:00:00
abstract：:Various materials, both biological and alloplastic, have been used for mastoid obliteration after canal wall-down mastoidectomy in chronic otitis media. The purpose of this study is to investigate the osteoinductive potential of PCL scaffolds in mastoid obliteration, and to test that osteoinductivity can be enhanced b...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2013.10.011
更新日期：2013-11-01 00:00:00
abstract：:It is well accepted that porphyrins related to heme, are effectively able to act as pharmaceutical. For instance, they were found to interfere with the aggregation of beta-amyloid peptide. In present study, the influence of heme concentration on the amyloid-type aggregation of ovalbumin was investigated. We provided e...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2008.10.011
更新日期：2009-01-01 00:00:00
abstract：:Wider plastic applications of poly(vinyl chloride) (PVC) has raised serious problem to the environment. Since (PVC) waste products resist biodegradation and persist in the environment for longer time. The object of this study is to blend (PVC) with biodegradable cellulose acetate to thermally support the polymer durin...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2014.06.033
更新日期：2014-09-01 00:00:00
abstract：:Halymenia durvillei is a red seaweed with a great potential as sulphated galactan producer collected in the coastal waters of small island of Madagascar (Nosy-be in Indian Ocean). To elucidate the structure of its polysaccharide, NMR (1H and 13C), FTIR, HPAEC and different colorimetric methods were carried out. It has...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2009.04.015
更新日期：2009-08-01 00:00:00
abstract：:3-Methyl-1-(4-sulfonylbutyl) imidazolium hydrogensulfate, [HO3S(CH2)4mim]HSO4, was applied as an extractant in an ultrasound-microwave synergistic extraction approach to substitute conventional solvent for the extraction of pectin from the albedo part of pomelo peels. The analysis of variance (ANOVA) test and response...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2016.10.028
更新日期：2017-01-01 00:00:00
abstract：:In this study, the kraft lignin/cubic boron nitride hybrid materials have been obtained and characterized for the first time. The effectiveness of the combination of lignin and boron nitride was evaluated on the basis of Fourier transform infrared spectroscopy. Furthermore, it was confirmed that the addition of cubic ...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2018.10.163
更新日期：2019-02-01 00:00:00
abstract：:Hot water extraction technique was employed to extract the hydrocolloid from Cordia myxa leaf (PCM). The optimal conditions for extraction of PCM were determined using response surface methodology. A Box-Behnken design (BBD) was applied to evaluate the effects of three independent variables (extraction time (X1: 1-4 h...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2014.01.047
更新日期：2014-04-01 00:00:00
abstract：:Accumulation of advanced glycation end products (AGEs) in tissues and serum plays important roles in diabetes-associated complications. Therefore, the identification of antiglycating compounds is attracting considerable interest. In this study, the structural changes associated with the glycation of superoxide dismuta...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2014.06.003
更新日期：2014-08-01 00:00:00
abstract：:As iron supplement, the antioxidant activities of APS-iron (III) complex were comprehensively evaluated by 5-axe cobweb charts, which indicated the APS-iron (III) complex had a certain antioxidant activity and been weaker than that of APS. The results of immunological activity experiments indicated the stimulation ind...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
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更新日期：2019-07-01 00:00:00
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journal_title：International journal of biological macromolecules
pub_type： 杂志文章
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更新日期：2015-05-01 00:00:00
abstract：:A threefold helical crystal structure of Bombyx mori silk fibroin has been observed in films prepared from aqueous silk fibroin solutions using the Langmuir Blodgett (LB) technique. The films were studied using a combination of transmission electron microscopy and electron diffraction techniques. Films prepared at a s...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/s0141-8130(99)00002-1
更新日期：1999-03-01 00:00:00
abstract：:In this study, three different carboxymethyl chitosans (CMCs), namely O-carboxymethyl chitosan (OC), N-carboxymethyl chitosan (NC) and N,O-carboxymethyl chitosan (NOC), were prepared as nano-carriers for an anti-tumor drug, docetaxel (DCT). Three CMCs were fabricated into drug-loading nanoparticles under different pre...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
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更新日期：2017-08-01 00:00:00
abstract：:Entamoeba histolytica D-phosphoglycerate dehydrogenase (EhPGDH) exists as a functionally active homodimer at pH 7. Our earlier studies have shown that ionic interactions are essentially required for the oligomeric status and activity of the protein. Present study focuses on pH associated structural modulations of EhPG...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2015.04.058
更新日期：2015-08-01 00:00:00
abstract：:A new hoop shaped three dimensional chitin was obtained successfully from the body segment of a diplopod species (Ommatoiulus sabulosus) by following the procedure decolorization, demineralization and deproteinization. Purity of the hoop shaped three-dimensional chitin was proved by FT-IR analysis and chitinase digest...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2016.09.103
更新日期：2017-01-01 00:00:00
abstract：:Composites based on combination of biopolymers (chitosan, hyaluronic acid and bovine serum albumin or gelatin), calcium phosphates (CP) and magnetic nanoparticles have been prepared by a biomimetic co-precipitation method. The biomimetic strategy is inspired by natural mineralization processes, where the synthesized m...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2018.12.083
更新日期：2019-03-15 00:00:00
abstract：:An acetylcholinesterase (AChE) purified from rat brain was immobilized onto gold nanoparticles (AuNPs) assembled on the surface of porous calcium carbonate (CaCO(3)) microsphere. The resulting AChE-AuNPs-CaCO(3) bioconjugate was mounted on the surface of Au electrode with the help of silica sol-gel matrix to prepare t...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2011.08.006
更新日期：2011-12-01 00:00:00
abstract：:Plant glycoproteins, especially allergenic glycoproteins such as pollen allergens, often carry antigenic N-glycans with α1-3 fucose and/or β1-2 xylose residue(s) on the trimannosyl core structure. We previously reported that one of such antigenic free-form N-glycans, Man3Xyl1Fuc1GlcNAc2 (M3FX) suppressed IL-4 producti...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2019.10.231
更新日期：2020-06-15 00:00:00
abstract：:Hyaluronan is an extremely important polysaccharide from both the biological and commercial points of view. This review summarizes the present state of the art concerning the polymer and our understanding of the molecular mechanisms of its synthesis with emphasis on the implications of this understanding for polysacch...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章,评审
doi：10.1016/0141-8130(94)90056-6
更新日期：1994-12-01 00:00:00
abstract：:Normal corn starch was treated with acidic ethanol solution with various concentrations of ethanol (0, 10, 30, 50 and 95%) and acid (0.0026, 0.0053 and 0.0079M) and then subjected to a dry heating treatment for 1, 2 and 4h at 130°C to prepare starch nanoparticles. Size of nanoparticles was determined using DLS (dynami...
journal_title：International journal of biological macromolecules
pub_type： 杂志文章
doi：10.1016/j.ijbiomac.2018.11.072
更新日期：2019-02-15 00:00:00
