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1.
Methamidophos (Met) is a weak inhibitor of housefly head AChE but at the same time it is highly toxic to the common housefly. The lethality of Met is believed to be due to AChE inhibition. An extensive QSAR study may help in determining the mode of action of Met in vivo and in vitro and provide a rational for its high insecticidal toxicity. Acephate (Ace), like Met, is a poor inhibitor of AChE in vitro and has a comparable to Met insect toxicity in vivo. Contrary to Met, though, Ace has much lower mammalian toxicity. Understanding the structural properties which make insecticides toxic to insects but not to mammals is of great importance, since mammals (including humans) are inadvertently exposed to these compounds. Our results were consistent with the model in which both the in vitro and in vivo toxicity of Met depends on the inhibition of the active center of AChE by the unchanged Met. An optimal susceptibility to hydrolysis is needed for Met and its analogs to have high insecticidal activity since in order to phosphorylate AChE they need to be hydrolyzed and at the same time their stability is of great importance in vivo for accumulating at the site of action. The insecticidal activity of Ace analogs may be due to direct interaction with the active center of the AChE. The mammalian toxicity of Ace analogs may be due to interaction with an 'allosteric' reaction center in the AChE. 相似文献
2.
Acetylcholinesterase based assay of eleven organophosphorus pesticides: finding of assay limitations
Miroslav Pohanka Lucie Drtinova Kamil Kuca 《International journal of environmental analytical chemistry》2013,93(1):125-132
The study includes findings about limitations of acetylcholinesterase (AChE) based assay. Eleven organophosphorus pesticides: chlorpyrifos ethyl, chlorpyrifos methyl, DFP, dichlorvos, dimethoate, fenthion, paraoxon ethyl, paraoxon methyl, phosalone, pirimiphos methyl and pirimiphos ethyl were photometrically assayed using AChE as a recognition element. The study was carried out in order to find approachability of AChE based assay. In the first round, common organic solvents were tested for interfering in assay, since samples collection and extraction is a necessary part in samples processing. Isopropanol was found as the most convenient due to minimal inhibition not exceeding 5%. Though all analysed pesticides inhibit AChE in vivo, some of them are toxic after metabolisation. We found AChE based assay approachable for assay of DFP, paraoxons, and dichlorvos. These are oxoforms of organophosphorus pesticides. From thioforms of assayed pesticides, only fenthion was able significantly inhibit AChE in vitro. Electrochemical biosensor with AChE attached on platinum electrode was used for confirmation of interaction pesticide – AChE and complex stability estimation. DFP, paraoxons and dichlorvos were allowed to interact with AChE in biosensor. These pesticides were settled firmly in AChE active site as no spontaneous recovery of AChE activity was observed. 相似文献
3.
《Arabian Journal of Chemistry》2021,14(12):103449
In this study, we aimed to (i) synthesize new 2-methylindole analogs containing various amino structures, pyrrolidine, piperidine, morpholine, and substituted phenyl groups through structural and molecular modifications, (ii) evaluate the pharmaceutical potential of 2-methylindole analogs via assessing enzyme inhibitory activity against glutathione S-transferase (GST), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE), (iii) predict ADMET and pharmacokinetic properties of the synthesized 2-methylindole analogs, (iv) reveal the possible interactions between the synthesized 2-methylindole analogs with GST, AChE, and BChE enzymes using several molecular docking software. In vitro enzyme inhibition assays showed that the synthesized indole analogs exhibited moderate to good inhibitory activities against GST, AChE, and BChE enzymes. Briefly, the inhibitory activities of the analogs 4b and 4i against AChE, 4a and 4b against BChE, and analogs 1 and 4i against GST were detected to be higher or close to the standard inhibitor compounds. The analog 4b was detected to have the best inhibitory activity against both AChE and BChE enzymes with the lowest IC50 values as 0.648 µM for AChE and 0.745 µM for BChE. The analyses of enzyme inhibition relationship with the synthesized analogs could help to design new analogs for the inhibitors of cholinergic and glutathione pathways based on the indole derivatives. 相似文献
4.
Green and one‐pot surface coating of iron oxide magnetic nanoparticles with natural amino acids and biocompatibility investigation
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Hamed Nosrati Marziyeh Salehiabar Elahe Attari Soodabeh Davaran Hossein Danafar Hamidreza Kheiri Manjili 《应用有机金属化学》2018,32(2)
We report the synthesis of iron oxide magnetic nanoparticles (IONPs) coated with various natural amino acids (AAs) using a one‐pot reaction in an aqueous medium. Several AAs, which contained hydrophilic and hydrophobic groups, were selected to study their effects on size, morphology and toxicity of IONPs. Functionalized IONPs were characterized using X‐ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared spectroscopy, and scanning and transmission electron microscopies. Furthermore, vibrating sample magnetometry analysis shows these nanoparticles have excellent magnetic properties. Cellular toxicity of IONPs was also investigated on HFF2 cell lines. The AA‐coated IONPs are non‐toxic and biocompatible. Natural AA‐coated IONPs show a potential for their development in in vitro and in vivo biomedical fields due to their non‐toxicity, good ζ‐potential and related small size and narrow size distribution. 相似文献
5.
Jatuporn Phaopongthai Jureeporn Noiphrom Supat Phaopongthai Narumol Pakmanee Jirapast Sichaem 《Natural product research》2016,30(6):697-699
This study evaluates the in vitro anti-snake venom potential of Peristrophe bivalvis (PB) extracts against Naja kaouthia (NK) and Trimeresurus albolabris (TA) venoms, including inhibition of cytotoxic effects and enzymatic activities, and the binding-precipitation of extracts and venom proteins analysis. In addition, the antioxidant, cytotoxic and in vivo acute oral toxic activities of PB extracts are also reported. The in vitro cytotoxic and enzymatic analysis reveals that the ethanol extracts of stems and leaves of PB showed good anti-snake venom activity against NK and TA venoms. In addition, the antioxidant result indicated that only the ethanol extract of leaves exhibited weak DPPH radical-scavenging activity. The ethanol whole-plant extract of PB also showed no cytotoxicity against four cell lines. Moreover, the in vivo acute oral toxicity result of the ethanol whole-plant extract showed that all treated rats did not exhibit abnormal toxic signs or deaths. 相似文献
6.
Tetsuo Okada Teruji Tsuji Tadahiko Tsushima Kiyoshi Ezumi Tadashi Yoshida Shinzo Matsuura 《Journal of heterocyclic chemistry》1991,28(4):1067-1074
Several analogs 4 and 5 of Ofloxacin ( 1 ) which contain the oxazine and thiazine rings fused with a quinolone carboxylic acid moiety, respectively, were prepared and their in vitro and in vivo antibacterial activities were compared with those of 1 and its previously prepared 3-exo-methylene analogs 2 and 3 . Unlike 1, 2 , and 3 , analogs 4 and 5 possess an antiaromatic oxazine and thiazine moiety and show markedly lower antibacterial activities. Alteration of their C-10 amino-substituent groups from piperazine to azetidine significantly improved the in vitro antibacterial activities, particularly in the case of the thiazine derivative 5 , but not the in vivo ones. The antibacterial activities of these three types of tricyclic quinolonecarboxylic acids are briefly discussed on the basis of the molecular properties revealed by molecular orbital calculation. The molecular dipole moment was suggested to be one possible factor controlling the binding affinity of these compounds with DNA gyrase. 相似文献
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J. Gailer 《应用有机金属化学》2002,16(12):701-707
Human activities have been contaminating the environment with toxic heavy metal and metalloid compounds. Since the toxicity of one metal or metalloid can be dramatically modulated by the simultaneous ingestion of another, studies addressing the molecular basis of chemical interactions between toxic and essential elements are increasingly important. The intravenous injection of rabbits with selenite and arsenite or with selenite and mercuric mercury resulted in the in vivo formation of the seleno‐bis (S‐glutathionyl) arsinium ion, [(GS)2AsSe]?, or a glutathione‐coated mercuric selenide, (GS)5(HgSe)core, in blood. The formation of these species (and the formation of a cadmium–selenium species in blood after the exposure of rats to selenite and cadmium) critically involves reactive selenite metabolites, such as GS–Se? and/or HSe?, which indicates that these physiologically important metabolites are molecular targets of ingested toxic metals and metalloids. The fate and stability of [(GS)2AsSe]? and (GS)5(HgSe)core in vivo imply that the chronic exposure of mammals to inorganic arsenic and mercury will cumulatively affect the bioavailability of selenium, which could lead to selenium deficiency. Since selenium deficiency is significantly associated with the etiology of cancer in humans, the GSH‐driven in vivo formation of selenium‐containing metal and metalloid species provides a likely molecular mechanism for the chronic toxicity of environmentally persistent inorganic arsenic, mercury and cadmium. Copyright © 2002 John Wiley & Sons, Ltd. 相似文献
9.
E. U. Weil J. G. Colson P. E. Hoch R. H. Gruber 《Journal of heterocyclic chemistry》1969,6(5):643-649
Upon treatment with alcoholic base, 1,4,5,6,7,7-hexachloro-5-norbornene-endo-cis-2,3-dimethanol (1) yields a tricyclic ether (111) which is converted by sulfuric acid to two epimeric 4,6,7,8,8-pentachloro-octahydro-4,7-methanoisobenzofuran-5-ones (111 A & B). These relatively nontoxic isomers, upon introduction of two chlorine atoms α and α′ to the ether oxygen, yield two epimeric products of high toxicity to insects and mammals. These 1,3,4,6,7,8,8-heptachloro-octahydro-4,7-methanoisobenzofuran-5-ones (IV A & B) upon transannular dehydrochlorination yield a toxic tetracyclic ketone (VI A). Reduction of this ketone by lithium aluminum hydride affords an alcohol (VII) of similarly high insecticidal toxicity. Nuclear magnetic resonance and infrared spectra are presented as evidence for the indicated structures. Results of this study are interpreted as indicative of the regions of the molecule which are critical in regard to toxicity. 相似文献
10.
Chuan‐wen Sun Ting Fang Zhi‐bing Hao Chun‐cheng Pang Xiao Xu Hua‐jia Xin 《Journal of heterocyclic chemistry》2013,50(5):1025-1030
Two series of novel (Z)‐nitenpyram analogs 2a , 2b , 2c , 2d , 2e , 2f , 2g , 2h , 3a , 3b , 3c , 3d were synthesized by introducing various amino acids benzyl ester or amino acids tetrahydrofurfur‐2‐yl ester into nitenpyram and forming a tetrahydropyrimidine ring to fix (Z)‐configuration. The structures of the target compounds were characterized by 1HNMR, MS, IR, and elemental analysis. Preliminary bioassays against Nilaparvata lugens indicated that all the nitenpyram analogs exhibited good insecticidal activity at 100 mg/L, whereas the compounds 3b and 3d afforded the best in vitro inhibitory activities that had ≥ 90% mortality at 20 mg/L. 相似文献
11.
Qian-sheng Yu Chi Liu Margareth Brzostowska Linda Chrisey Arnold Brossi Nigel H. Greig John R. Atack Timothy T. Soncrant Stanley I. Rapoport Hans-Eckart Radunz 《Helvetica chimica acta》1991,74(4):761-766
Column chromatography of easy available (±)-physovenine ( 2 ) on cellulose triacetate afforded (?)- and (+)-physovenine ( 2a and 2b , resp.). Alkaloids 2a , b required for pharmacological testing were prepared from eserolincs ( 3a , b ) by an improved procedure. Natural (?)-physovenine ( 2a ) was equally potent in inhibiting AChE and BChE in vitro as natural physostigmine (1a), and twice as potent as the unnatural antipode 2b against AChE and 14 times as potent against BChE. Several carbamate analogs of 2a were at least as potent as the former compound in these assays. None of the compounds tested did bind to different opiate receptor or serotonine receptor preparations. Most of the compounds tested had considerable analgesic activity in the Writhing test. 相似文献
12.
Boris Pejin Ana Ciric Dejan Markovic Giuseppina Tommonaro Marina Sokovic 《Natural product research》2016,30(17):1956-1960
This work extends in vitro screening of antimicrobial activity of avarol, the marine natural product firstly isolated from the Mediterranean sponge Dysidea avara. Its anticandidial activity was evaluated by microdilution method against eight Candida strains, two ATCC and six clinical ones. At a different extent this compound was proven to be active against all the strains tested (MIC 0.8–6.0 μg/mL and MFC 1.6–12.0 μg/mL, respectively). According to the best of our knowledge, this is the first report on avarol activity towards any yeast strain which may be of relevance for Alzheimer’s disease. Indeed, avarol derivatives showing moderate AChE activity should be screened for anticandidial activity both in vitro and in vivo. 相似文献
13.
Chuan‐Wen Sun Hai‐Feng Wang Jun Zhu Ding‐Rong Yang Jia Jin Jia‐Hua Xing 《Journal of heterocyclic chemistry》2011,48(4):829-835
A series of novel neonicotinoids analogs were designed by modifying the pharmacophore of imidacloprid to 1,3,5‐hexahydrotriazine conjugated to nitroimine (?NNO2) and introducing the phenyl or arylmethyl at the 5‐position, and their insecticidal activities were evaluated. Introducing a heterocyclic methyl at 5‐position increased the insecticidal activities, whereas other phenyl, phenylmethyl or phenylethyl substituents were unfavorable to activities. Molecular docking study was also performed to clarify the interactions of the most potent analog 1‐((6‐chloropyridin‐3‐yl)methyl)‐5‐(3‐pyridylmethyl)‐1,3,5‐hexahydrotriazine‐2‐(N‐nitro) imine ( 7s ) with the target nicotinic acetylcholine receptor, which explained the structure‐activity relationships observed in vitro, and revealed further possibilities for insecticide development. J. Heterocyclic Chem., (2011). 相似文献
14.
Rat exposed to toxic cadmium chronically and acutely are diagnosed byin vivo promt gamma-ray activation andin vitro neutron activation using nuclear reactor neutron beam. Linear correlation of bothin vivo andin vitro methods is established, damage level of 1.7 mg/g Cd in kidneys and 0.16 mg/g Cd in liver are confirmed by biochemical diagnosis. Features ofin vivo andin vitro nuclear medical diagnoses of cadmium contamination, serving as the basis for future research and correletion to human beings, are discussed. 相似文献
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The review summarizes the results of studies aimed at developing the fundamentals for the design of a new class of nitric
oxide donors, viz., iron nitrosyl complexes with functionalized sulfur-containing ligands, which are structural analogs of the active sites
of non-heme nitrosyl iron-sulfur proteins. The structures, reactivities, and pharmacological activity in vitro and in vivo of these complexes are considered. 相似文献
18.
A kinetic model employing calculated atom and bond localization energies to approximate relative activation energies of reaction is used to analyse previously obtained experimental results for in vitro and in vivo chemical binding of polycyclic aromatic hydrocarbons to nucleic acids. It is found that in vitro linkage of hydrocarbons to DNA induced by a microsomal hydroxylating system is compatible with mechanisms involving either attack at the most reactive hydrocarbon center or attack at the most reactive hydrocarbon bond. Independent evidence leads us to favor the former mechanism. Further, the limited experimental data for in vivo linkage of hydrocarbons to DNA is found to be consistent with a model involving attack at the most reactive bond of the molecule: the “K region”. This model is supported by a close parallelism found between extent of hydrocarbons bound to DNA in vivo and the experimentally determined relative reactivities of their K regions. 相似文献
19.
Xiao-Qian Chi Bo Hou Liu Yang Cheng-Ting Zi Yong-Feng Lv Jin-Yu Li 《Natural product research》2020,34(10):1380-1388
Abstractα-mangostin, a polyphenol xanthone derivative, was mainly isolated from pericarps of the mangosteen fruit (Garcinia mangostana L.). In present investigation, a series of derivatives were designed, synthesised and evaluated in vitro for their inhibitory activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among the synthesised xanthones, compounds 1, 9, 13 and 16 showed AChE selective inhibitory activity, 15 was a BuChE selective inhibitor while 2, 3, 5, 6, 7, 12 and 14 were dual inhibitors. The most potent inhibitor of AChE was 16 while 5 was the most potent inhibitor of BuChE with IC50 values of 5.26?μM and 7.55?μM respectively. 相似文献
20.
Courtney R LaValle Karla Bravo-Altamirano Karthik V Giridhar Jun Chen Elizabeth Sharlow John S Lazo Peter Wipf Q Jane Wang 《BMC chemical biology》2010,10(1):5