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Journal ArticleDOI: 10.1080/13813455.2019.1618341

Investigation of the toxicological and inhibitory effects of some benzimidazole agents on acetylcholinesterase and butyrylcholinesterase enzymes.

04 Mar 2021-Archives of Physiology and Biochemistry (Arch Physiol Biochem)-Vol. 127, Iss: 2, pp 97-101
Abstract: Benzimidazole, an anthelmintic used in the manufacture of human and veterinary drugs, is an important heterocyclic compound. In this work, I investigated the effect of drugs such as ricobendazole, ...

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Topics: Benzimidazole (62%), Veterinary Drugs (50%)
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14 results found


Journal ArticleDOI: 10.1016/J.BIOORG.2020.103647
Abstract: In this study, using the Cu(OTf)2 catalyst, 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivative molecules were carried out in one step and with high yield (86–91%). The previously synthesized 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivatives, carbonic anhydrase I and II isozymes (hCA I and II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and α-glycosidase (α-Gly) enzymes with Ki values in the range of 4.88–15.94 nM for hCA I, 7.04–20.83 nM for hCA II, 68.25–158.27 for AChE, 60.17–91.27 for BChE and 0.36–2.36 nM for α-Gly, respectively. In silico studies were performed on the molecules inhibiting hCA I, hCA II, AChE, BChE and α-Gly receptors. When we evaluated the data obtained in this work, we determined the inhibition type of the 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivatives at the receptors. Reference inhibitors were used for all enzymes.

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27 Citations


Journal ArticleDOI: 10.1007/S11164-019-03949-3
Kenan Buldurun1, Nevin Turan1, Ercan Bursal1, Asim Mantarcı1  +3 moreInstitutions (4)
Abstract: Considering the importance of metal complexes in the development of medical science, two different Schiff base Fe(II) and Co(II) metal complex compounds were synthesized with Schiff base obtained through the condensation of 1-(4-aminophenyl)ethanone with 2-hydroxy-3-methoxybenzaldehyde. The reactions of the ligand with Co(II) and Fe(II) metal ions enabled six coordination compounds with octahedral geometries. The novel metal complexes were characterized by IR, elemental analyses, magnetic susceptibility, mass spectra, UV–Vis, thermogravimetry–differential thermal analysis (TGA–DTA) and X-ray diffraction analysis. The antioxidant properties of the new compounds were investigated using different in vitro assays. Moreover, enzyme inhibition of derivatives complexes against carbonic anhydrase I and II isoenzymes (CA I and II) and acetylcholinesterase (AChE) was evaluated. The best inhibitor complex for CA I and II isoenzymes was the Fe(II) complex with Ki values of 52.83 ± 11.52 and 63.34 ± 8.88, respectively.

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Topics: Schiff base (55%), Coordination complex (53%), Ligand (52%)

21 Citations


Journal ArticleDOI: 10.1080/07391102.2020.1768901
Abstract: Inhibitory effect of the complexes on some metabolic enzyme results demonstrated that the enzymes inhibited by ligand and it’s complex molecules at the micromolar level. The best inhibition effect ...

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Topics: Enzyme (54%), Butyrylcholinesterase (51%), Ligand (biochemistry) (50%)

16 Citations


Journal ArticleDOI: 10.1016/J.COMPBIOLCHEM.2020.107355
Vinay Kumar1, Achintya Saha2, Kunal Roy1Institutions (2)
Abstract: In this research, we have implemented two-dimensional quantitative structure-activity relationship (2D-QSAR) modeling using two different datasets, namely, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzyme inhibitors. A third dataset has been derived based on their selectivity and used for the development of partial least squares (PLS) based regression models. The developed models were extensively validated using various internal and external validation parameters. The features appearing in the model against AChE enzyme suggest that a small ring size, higher number of −CH2- groups, higher number of secondary aromatic amines and higher number of aromatic ketone groups may contribute to the inhibitory activity. The features obtained from the model against BuChE enzyme suggest that the sum of topological distances between two nitrogen atoms, higher number of fragments X-C(=X)-X, higher number of secondary aromatic amides, fragment R--CR-X may be more favorable for inhibition. The features obtained from selectivity based model suggest that the number of aromatic ethers, unsaturation content relative to the molecular size and molecular shape may be more specific for the inhibition of the AChE enzyme in comparison to the BuChE enzyme. Moreover, we have implemented the molecular docking studies using the most and least active molecules from the datasets in order to identify the binding pattern between ligand and target enzyme. The obtained information is then correlated with the essential structural features associated with the 2D-QSAR models.

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8 Citations


Journal ArticleDOI: 10.1016/J.JPBA.2019.113048
Abstract: Benzimidazoles are antiparasitic drugs having an extensive application field like agriculture, medicine, and especially in veterinary medicine. In this study, we report the effect of some benzimidazole drugs such as ricobendazole (RBZ), thiabendazole (TBZ), albendazole (ALBA) and oxfendazole (OFZ) on glutathione s-transferase (GST) enzyme activity. The kinetics studies, IC50 and Ki values of the tested drugs on GSTs enzyme activity were investigated. The obtained ranking of IC50 values were found to be approximately RBZ (53.31 μM, r2: 0.9778)

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Topics: Oxfendazole (51%)

4 Citations


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42 results found


Journal ArticleDOI: 10.1016/0006-2952(61)90145-9
Abstract: A photometric method for determining acetylcholinesterase activity of tissue extracts, homogenates, cell suspensions, etc., has been described. The enzyme activity is measured by following the increase of yellow color produced from thiocholine when it reacts with dithiobisnitrobenzoate ion. It is based on coupling of these reactions: The latter reaction is rapid and the assay is sensitive (i.e. a 10 μ1 sample of blood is adequate). The use of a recorder has been most helpful, but is not essential. The method has been used to study the enzyme in human erythrocytes and homogenates of rat brain, kidney, lungs, liver and muscle tissue. Kinetic constants determined by this system for erythrocyte eholinesterase are presented. The data obtained with acetylthiocholine as substrate are similar to those with acetylcholine.

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Topics: Aryl-acylamidase activity (54%), Thiocholine (53%), Acetylthiocholine (53%) ... show more

20,867 Citations


Journal ArticleDOI: 10.1021/JA908293N
Ming-Hua Zeng1, Qiang-Xin Wang1, Yan-Xi Tan1, Sheng Hu1  +3 moreInstitutions (1)
Abstract: A highly stable pillared and double-walled zinc(II) metal-organic framework with regular nanochannels displays single-crystal to single-crystal transformation upon desolvation and a large quantity of iodine uptake, controlled release, and electrical conductivity elevation due to synergy between the iodine guests and the host framework.

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Topics: Single crystal (50%)

545 Citations


Journal ArticleDOI: 10.1016/0169-4758(90)90227-U
Ernest Lacey1Institutions (1)
01 Apr 1990-Parasitology Today
Abstract: Benzimidazoles represent the only class of truly broad-spectrum anthelmintics, however, they also show activity against fungi and mammalian cells. This raises the question as to why benzimidazoles can selectively kill helminths and yet exhibit little or no mammalian toxicity. In this paper, Ernest Lacey examines this example of selectivity of drug action to the ubiquitous target of these drugs, the structural protein, tubulin.

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465 Citations


Journal ArticleDOI: 10.1016/J.JNUTBIO.2004.05.002
Abstract: Tea consumption is varying its status from a mere ancient beverage and a lifestyle habit, to a nutrient endowed with possible prospective neurobiological-pharmacological actions beneficial to human health. Accumulating evidence suggest that oxidative stress resulting in reactive oxygen species generation and inflammation play a pivotal role in neurodegenerative diseases, supporting the implementation of radical scavengers, transition metal (e.g., iron and copper) chelators, and nonvitamin natural antioxidant polyphenols in the clinic. These observations are in line with the current view that polyphenolic dietary supplementation may have an impact on cognitive deficits in individuals of advanced age. As a consequence, green tea polyphenols are now being considered as therapeutic agents in well controlled epidemiological studies, aimed to alter brain aging processes and to serve as possible neuroprotective agents in progressive neurodegenerative disorders such as Parkinson's and Alzheimer's diseases. In particular, literature on the putative novel neuroprotective mechanism of the major green tea polyphenol, (-)-epigallocatechin-3-gallate, are examined and discussed in this review.

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431 Citations


Journal ArticleDOI: 10.1021/JA808444Z
Abstract: The 3D metal−organic framework (MOF) 3∞{[Ni3(μ3-btc)2(μ4-btre)2(μ-H2O)2]·∼22H2O} is found to be a reversibly dehydratable−hydratable water-stable MOF material with a large loading spread of 210 g/kg as a candidate for solid adsorbents in heat transformation cycles for refrigeration, heat pumping, and heat storage.

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Topics: Refrigeration (56%), Thermal energy storage (51%)

373 Citations