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Sample records for insensitive acetylcholinesterase insecticide

  1. Costs of insensitive acetylcholinesterase insecticide resistance for the malaria vector Anopheles gambiae homozygous for the G119S mutation

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    Noel Valérie

    2010-01-01

    Full Text Available Abstract Background The G119S mutation responsible for insensitive acetylcholinesterase resistance to organophosphate and carbamate insecticides has recently been reported from natural populations of Anopheles gambiae in West Africa. These reports suggest there are costs of resistance associated with this mutation for An. gambiae, especially for homozygous individuals, and these costs could be influential in determining the frequency of carbamate resistance in these populations. Methods Life-history traits of the AcerKis and Kisumu strains of An. gambiae were compared following the manipulation of larval food availability in three separate experiments conducted in an insecticide-free laboratory environment. These two strains share the same genetic background, but differ in being homozygous for the presence or absence of the G119S mutation at the ace-1 locus, respectively. Results Pupae of the resistant strain were significantly more likely to die during pupation than those of the susceptible strain. Ages at pupation were significantly earlier for the resistant strain and their dry starved weights were significantly lighter; this difference in weight remained when the two strains were matched for ages at pupation. Conclusions The main cost of resistance found for An. gambiae mosquitoes homozygous for the G119S mutation was that they were significantly more likely to die during pupation than their susceptible counterparts, and they did so across a range of larval food conditions. Comparing the frequency of G119S in fourth instar larvae and adults emerging from the same populations would provide a way to test whether this cost of resistance is being expressed in natural populations of An. gambiae and influencing the dynamics of this resistance mutation.

  2. Identification and characterization of mutations in housefly (Musca domestica) acetylcholinesterase involved in insecticide resistance

    DEFF Research Database (Denmark)

    Walsh, Sinead B.; Dolden, Tracey A.; Moores, Graham D.

    2001-01-01

    Acetylcholinesterase (AChE) insensitive to organophosphate and carbamate insecticides has been identified as a major resistance mechanism in numerous arthropod species. However, the associated genetic changes have been reported in the AChE genes from only three insect species; their role in confe...... of the AChE protein from Torpedo californica and D. melanogaster....

  3. Salivary gland proteome analysis reveals modulation of anopheline unique proteins in insensitive acetylcholinesterase resistant Anopheles gambiae mosquitoes.

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    Sylvie Cornelie

    Full Text Available Insensitive acetylcholinesterase resistance due to a mutation in the acetylcholinesterase (ace encoding ace-1 gene confers cross-resistance to organophosphate and carbamate insecticides in Anopheles gambiae populations from Central and West Africa. This mutation is associated with a strong genetic cost revealed through alterations of some life history traits but little is known about the physiological and behavioural changes in insects bearing the ace-1(R allele. Comparative analysis of the salivary gland contents between An. gambiae susceptible and ace-1(R resistant strains was carried out to charaterize factors that could be involved in modifications of blood meal process, trophic behaviour or pathogen interaction in the insecticide-resistant mosquitoes. Differential analysis of the salivary gland protein profiles revealed differences in abundance for several proteins, two of them showing major differences between the two strains. These two proteins identified as saglin and TRIO are salivary gland-1 related proteins, a family unique to anopheline mosquitoes, one of them playing a crucial role in salivary gland invasion by Plasmodium falciparum sporozoites. Differential expression of two other proteins previously identified in the Anopheles sialome was also observed. The differentially regulated proteins are involved in pathogen invasion, blood feeding process, and protection against oxidation, relevant steps in the outcome of malaria infection. Further functional studies and insect behaviour experiments would confirm the impact of the modification of the sialome composition on blood feeding and pathogen transmission abilities of the resistant mosquitoes. The data supports the hypothesis of alterations linked to insecticide resistance in the biology of the primary vector of human malaria in Africa.

  4. Novel and viable acetylcholinesterase target site for developing effective and environmentally safe insecticides.

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    Pang, Yuan-Ping; Brimijoin, Stephen; Ragsdale, David W; Zhu, Kun Yan; Suranyi, Robert

    2012-04-01

    Insect pests are responsible for human suffering and financial losses worldwide. New and environmentally safe insecticides are urgently needed to cope with these serious problems. Resistance to current insecticides has resulted in a resurgence of insect pests, and growing concerns about insecticide toxicity to humans discourage the use of insecticides for pest control. The small market for insecticides has hampered insecticide development; however, advances in genomics and structural genomics offer new opportunities to develop insecticides that are less dependent on the insecticide market. This review summarizes the literature data that support the hypothesis that an insect-specific cysteine residue located at the opening of the acetylcholinesterase active site is a promising target site for developing new insecticides with reduced off-target toxicity and low propensity for insect resistance. These data are used to discuss the differences between targeting the insect-specific cysteine residue and targeting the ubiquitous catalytic serine residue of acetylcholinesterase from the perspective of reducing off-target toxicity and insect resistance. Also discussed is the prospect of developing cysteine-targeting anticholinesterases as effective and environmentally safe insecticides for control of disease vectors, crop damage, and residential insect pests within the financial confines of the present insecticide market.

  5. Multiple insecticide resistance mechanisms involving metabolic changes and insensitive target sites selected in anopheline vectors of malaria in Sri Lanka

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    Karunaratne SHP Parakrama

    2008-08-01

    Full Text Available Abstract Background The current status of insecticide resistance and the underlying resistance mechanisms were studied in the major vector of malaria, Anopheles culicifacies, and the secondary vector, Anopheles subpictus in five districts (Anuradhapura, Kurunegala, Moneragala, Puttalam and Trincomalee of Sri Lanka. Eight other anophelines, Anopheles annularis, Anopheles barbirostris, Anopheles jamesii, Anopheles nigerrimus, Anopheles peditaeniatus, Anopheles tessellatus, Anopheles vagus and Anopheles varuna from Anuradhapura district were also tested. Methods Adult females were exposed to the WHO discriminating dosages of DDT, malathion, fenitrothion, propoxur, λ-cyhalothrin, cyfluthrin, cypermethrin, deltamethrin, permethrin and etofenprox. The presence of metabolic resistance by esterase, glutathione S-transferase (GST and monooxygenase-based mechanisms, and the sensitivity of the acetylcholinesterase target site were assessed using synergists, and biochemical, and metabolic techniques. Results All the anopheline species had high DDT resistance. All An. culicifacies and An. subpictus populations were resistant to malathion, except An. culicifacies from Kurunegala, where there was no malathion carboxylesterase activity. Kurunegala and Puttalam populations of An. culicifacies were susceptible to fenitrothion. All the An. culicifacies populations were susceptible to carbamates. Both species were susceptible to the discriminating dosages of cypermethrin and cyfluthrin, but had different levels of resistance to other pyrethroids. Of the 8 other anophelines, only An. nigerrimus and An. peditaeniatus were resistant to all the insecticides tested, probably due to their high exposure to the insecticides used in agriculture. An. vagus showed some resistance to permethrin. Esterases, GSTs and monooxygenases were elevated in both An. culicifacies and An. subpictus. AChE was most sensitive to insecticides in Kurunegala and Trincomalee An. culicifacies

  6. Detection of the acetylcholinesterase insecticide resistance mutation (G328A) in natural populations of Ceratitis capitata

    International Nuclear Information System (INIS)

    Elfekih, Samia; Haran, Julien; Shannon, Matthew; Vogler, Alfried P.

    2015-01-01

    Wild Mediterranean fruit fly specimens collected from various regions worldwide were screened for the glycine to alanine (Gly->Ala) point mutation (G328A) in the acetylcholinesterase enzyme, presumably causing resistance to organophosphates. We found that the single nucleotide polymorphism (SNP) responsible for this amino acid change is located at the beginning of exon 6 of the Ccace2 gene. The identification of the exact location of the SNP permitted PCR primer design around this site and direct sequencing of the corresponding genomic region. We detected the resistance allele in natural Mediterranean fruit fly populations from Brazil and Spain, but not from other sites in four continents. The known treatment history of sites suggests that the resistance build up is linked to organophosphate application in the held. The PCR-based detection provides a screening method useful for monitoring Mediterranean fruit fly insecticide resistance in local populations and improving pest management strategies accordingly. (author)

  7. Sublethal Effects of Insecticide Exposure on Megacopta cribraria (Fabricius) Nymphs: Key Biological Traits and Acetylcholinesterase Activity.

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    Miao, Jin; Reisig, Dominic D; Li, Guoping; Wu, Yuqing

    2016-01-01

    Megacopta cribraria F. (Hemiptera: Plataspidae), the kudzu bug, is an invasive insect pest of U.S. soybean. At present, insecticide application is the primary and most effective control option for M. cribraria In this study, the potential effects of sublethal and low-lethal concentrations (LC10 and LC40) of three common insecticides on key biological traits and acetylcholinesterase (AChE) activity of the treated nymphal stage of insect were assessed. The results show that the sublethal concentration of imidacloprid significantly reduced adult emergence rate of M. cribraria A low-lethal concentration of imidacloprid significantly increased nymphal development time, but significantly decreased adult emergence rate and adult longevity. Both sublethal and low-lethal concentrations of acephate caused an increase in nymphal development time and a reduction in adult emergence rate and adult longevity. Fecundity of females was significantly reduced only by exposure to low-lethal concentrations of acephate. Sublethal and low-lethal concentrations of bifenthrin increased nymphal development time, but significantly decreased adult emergence rate. In addition, we found that the AChE activity of M. cribraria was significantly increased only by LC40 imidacloprid, but strongly inhibited by acephate. © The Author 2016. Published by Oxford University Press on behalf of the Entomological Society of America.

  8. Identification of two acetylcholinesterases in Pardosa pseudoannulata and the sensitivity to insecticides.

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    Zhang, Yixi; Shao, Ying; Jiang, Feng; Li, Jian; Liu, Zewen

    2014-03-01

    Pardosa pseudoannulata is an important predatory enemy against insect pests, such as rice planthoppers and leafhoppers. In order to understand the insecticide selectivity between P. pseudoannulata and insect pests, two acetylcholinesterase genes, Pp-ace1 and Pp-ace2, were cloned from this natural enemy. The putative proteins encoded by Pp-ace1 and Pp-ace2 showed high similarities to insect AChE1 (63% to Liposcelis entomophila AChE1) and AChE2 (36% to Culex quinquefasciatus AChE2) with specific functional motifs, which indicated that two genes might encode AChE1 and AChE2 proteins respectively. The recombinant proteins by expressing Pp-ace1 and Pp-ace2 genes in insect sf9 cells showed high AChE activities. The kinetic parameters, Vmax and Km, of two recombinant AChE proteins were significantly different. The sensitivities to six insecticides were determined in two recombinant AChEs. Pp-AChE1 was more sensitive to all tested insecticides than Pp-AChE2, such as fenobucarb (54 times in Ki ratios), isoprocarb (31 times), carbaryl (13 times) and omethoate (6 times). These results indicated that Pp-AChE1 might be the major synaptic enzyme in the spider. By sequence comparison of P. pseudoannulata and insect AChEs, the key amino acid differences at or close to the functional sites were found. The locations of some key amino acid differences were consistent with the point mutation sites in insect AChEs that were associated with insecticide resistance, such as Phe331 in Pp-AChE2 corresponding to Ser331Phe mutation in Myzus persicae and Aphis gossypii AChE2, which might play important roles in insecticide selectivity between P. pseudoannulata and insect pests. Of course, the direct evidences are needed through further studies. Copyright © 2014 Elsevier Ltd. All rights reserved.

  9. Effect of carbaryl (carbamate insecticide) on acetylcholinesterase activity of two strains of Daphnia magna (Crustacea, Cladocera).

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    Toumi, Hela; Bejaoui, Mustapha; Touaylia, Samir; Burga Perez, Karen F; Ferard, Jean François

    2016-11-01

    The present study was designed to investigate the effect of carbaryl (carbamate insecticide) on the acetylcholinesterase activity in two strains (same clone A) of the crustacean cladoceran Daphnia magna. Four carbaryl concentrations (0.4, 0.9, 1.8 and 3.7 µg L(-1)) were compared against control AChE activity. Our results showed that after 48 h of carbaryl exposure, all treatments induced a significant decrease of AChE activities whatever the two considered strains. However, different responses were registered in terms of lowest observed effect concentrations (LOEC: 0.4 µg L(-1) for strain 1 and 0.9 µg L(-1) for strains 2) revealing differences in sensitivity among the two tested strains of D. magna. These results suggest that after carbaryl exposure, the AChE activity responses can be also used as a biomarker of susceptibility. Moreover, our results show that strain1 is less sensitive than strain 2 in terms of IC50-48 h of AChE activity. Comparing the EC50-48 h of standard ecotoxicity test and IC50-48 h of AChE inhibition, there is the same order of sensitivity with both strains.

  10. Assessing joint toxicity of four organophosphate and carbamate insecticides in common carp (Cyprinus carpio) using acetylcholinesterase activity as an endpoint.

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    Wang, Yanhua; Chen, Chen; Zhao, Xueping; Wang, Qiang; Qian, Yongzhong

    2015-07-01

    Mixtures of organophosphate (OP) and carbamate (CB) pesticides are commonly detected in freshwater ecosystems. These pesticides inhibit the activity of acetylcholinesterase (AChE) and have potential to interfere with behaviors that may be essential for the survival of species. Although the effects of individual anticholinesterase insecticides on aquatic species have been studied for decades, the neurotoxicity of mixtures is still poorly understood. In the present study, brain AChE inhibition in carp (Cyprinus carpio) exposed to a series of concentrations of the organophosphates (malathion and triazophos) as well as the carbamates (fenobucarb and carbosulfan) was measured. In equitoxic mixtures, the observed AChE activity inhibition of the malathion plus triazophos, and triazophos plus carbosulfan mixtures, was synergism. In equivalent concentration mixtures, the combination of malathion plus fenobucarb mixture conformed to synergism, while the observed AChE activity inhibition of the remaining pairings was less than additive. Single pesticide risk assessments are likely to underestimate the impacts of these insecticides on carps in aquatic environment where mixtures occur. Moreover, mixtures of pesticides that have been commonly reported in aquatic ecosystems may pose a more important challenge than previously anticipated. Copyright © 2014 Elsevier Inc. All rights reserved.

  11. Chromogenic platform based on recombinant Drosophila melanogaster acetylcholinesterase for visible unidirectional assay of organophosphate and carbamate insecticide residues

    Energy Technology Data Exchange (ETDEWEB)

    Han Zheng [Institute for Agri-food Standards and Testing Technology, Shanghai Academy of Agricultural Sciences, 1018 Jinqi Road, Shanghai 201403 (China); Chi Chensen [School of Life Science and Biotechnology, Bor Luh Food Safety Center, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240 (China); Bai Bing; Liu Gang; Rao Qinxiong [Institute for Agri-food Standards and Testing Technology, Shanghai Academy of Agricultural Sciences, 1018 Jinqi Road, Shanghai 201403 (China); Peng Shaojie [Institute of Shanghai Food and Drug Supervision, 615 Liuzhou Road, Shanghai 200233 (China); Liu Hong [Shanghai Municipal Center for Disease Control and Prevention, 1380 Zhongshan West Road, Shanghai 200336 (China); Zhao Zhihui [Institute for Agri-food Standards and Testing Technology, Shanghai Academy of Agricultural Sciences, 1018 Jinqi Road, Shanghai 201403 (China); Zhang Dabing [School of Life Science and Biotechnology, Bor Luh Food Safety Center, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240 (China); Wu Aibo, E-mail: wuaibo@saas.sh.cn [Institute for Agri-food Standards and Testing Technology, Shanghai Academy of Agricultural Sciences, 1018 Jinqi Road, Shanghai 201403 (China)

    2012-03-30

    Highlight: Black-Right-Pointing-Pointer A visible chromogenic platform for rapid analysis of OP and CM insecticide residues was developed. Black-Right-Pointing-Pointer The assay has the capabilities of both qualitative measurement and quantitative analysis. Black-Right-Pointing-Pointer The sensitivity, capabilities of resisting interferences and storage stability were desirable. Black-Right-Pointing-Pointer Matrix effects were acceptable and detection performance was satisfactory in real application. - Abstract: In this study we propose a chromogenic platform for rapid analysis of organophosphate (OP) and carbamate (CM) insecticide residues, based on recombinant Drosophila melanogaster acetylcholinesterase (R-DmAChE) as enzyme and indoxyl acetate as substrate. The visible chromogenic strip had the advantages identical to those of commonly used lateral flow assays (LFAs) with utmost simplicity in sample loading and result observation. After optimization, depending on the color intensity (CI) values, the well-established assay has the capabilities of both qualitative measurement via naked eyes and quantitative analysis by colorimetric reader with the desirable IC{sub 50} values against the tested six insecticides (0.06 {mu}g mL{sup -1} of carbofuran, 0.28 {mu}g mL{sup -1} of methomyl, 0.03 {mu}g mL{sup -1} of dichlorvos, 31.6 {mu}g mL{sup -1} of methamidophos, 2.0 {mu}g mL{sup -1} of monocrotophos, 6.3 {mu}g mL{sup -1} of omethoate). Acceptable matrix effects and satisfactory detection performance were confirmed by in-parallel LC-MS/MS analysis in different vegetable varieties at various spiked levels of 10{sup -3} to 10{sup 1} {mu}g g{sup -1}. Overall, the testified suitability and applicability of this novel platform meet the requirements for practical use in food safety management and environmental monitoring, especially in the developing world.

  12. Chromogenic platform based on recombinant Drosophila melanogaster acetylcholinesterase for visible unidirectional assay of organophosphate and carbamate insecticide residues

    International Nuclear Information System (INIS)

    Han Zheng; Chi Chensen; Bai Bing; Liu Gang; Rao Qinxiong; Peng Shaojie; Liu Hong; Zhao Zhihui; Zhang Dabing; Wu Aibo

    2012-01-01

    Highlight: ► A visible chromogenic platform for rapid analysis of OP and CM insecticide residues was developed. ► The assay has the capabilities of both qualitative measurement and quantitative analysis. ► The sensitivity, capabilities of resisting interferences and storage stability were desirable. ► Matrix effects were acceptable and detection performance was satisfactory in real application. - Abstract: In this study we propose a chromogenic platform for rapid analysis of organophosphate (OP) and carbamate (CM) insecticide residues, based on recombinant Drosophila melanogaster acetylcholinesterase (R-DmAChE) as enzyme and indoxyl acetate as substrate. The visible chromogenic strip had the advantages identical to those of commonly used lateral flow assays (LFAs) with utmost simplicity in sample loading and result observation. After optimization, depending on the color intensity (CI) values, the well-established assay has the capabilities of both qualitative measurement via naked eyes and quantitative analysis by colorimetric reader with the desirable IC 50 values against the tested six insecticides (0.06 μg mL −1 of carbofuran, 0.28 μg mL −1 of methomyl, 0.03 μg mL −1 of dichlorvos, 31.6 μg mL −1 of methamidophos, 2.0 μg mL −1 of monocrotophos, 6.3 μg mL −1 of omethoate). Acceptable matrix effects and satisfactory detection performance were confirmed by in-parallel LC–MS/MS analysis in different vegetable varieties at various spiked levels of 10 −3 to 10 1 μg g −1 . Overall, the testified suitability and applicability of this novel platform meet the requirements for practical use in food safety management and environmental monitoring, especially in the developing world.

  13. RNA interference of acetylcholinesterase in the Asian citrus psyllid, Diaphorina citri, increases its susceptibility to carbamate and organophosphate insecticides.

    Science.gov (United States)

    Kishk, Abdelaziz; Hijaz, Faraj; Anber, Helmy A I; AbdEl-Raof, Tsamoh K; El-Sherbeni, AbdEl-Hakeem D; Hamed, Sobhy; Killiny, Nabil

    2017-11-01

    The Asian citrus psyllid, Diaphorina citri Kuwayama (Hemiptera: Lividae) transmits the Candidatus Liberibacter asiaticus, which causes citrus greening disease or Huanglongbing, (HLB). To date, there is no efficient cure for HLB disease and the control of D. citri using insecticides became the most important tools for the management of HLB. However, the extensive use of insecticides could increase D. citri resistance to these insecticides. The objective of this study was to investigate the effect of RNA interference of acetylcholinesterase (AChE) on the mortality and susceptibility of D. citri to the four major insecticides used in Florida. In this study, we used a consensus sequence derived from the two AChE genes and cholinesterase 2-like (ChE-2-like) gene to target all of the three genes. Treatment with dsRNA-AChE increased the mortality percentages of both nymphs and adults of D. citri. The mortality percentage increased with the increase in the concentration of applied dsRNA-AChE, and the highest mortality (> 60%) was observed at the highest applied concentration (125ng/μl). Treatments of nymphs or adults with dsRNA-AChE down-regulated the expression of the three targeted genes of D. citri. Silencing of AChE and ChE in D. citri nymphs increased the susceptibility of emerged adults to chlorpyrifos and carbaryl, which act as AChE inhibitors. However, treatment with dsRNA-AChE did not increase the susceptibility of emerged adults to imidacloprid, which acts as an agonist of nicotinic acetylcholine receptors. In the same manner, treatment of adults with dsRNA-AChE increased their susceptibility to chlorpyrifos and carbaryl, but did not affect their susceptibility to imidacloprid. The ANOVA did not show any significant increase in susceptibility of D. citri adults to fenpropathrin after treatment with dsRNA-AChE, either as nymphs or as adults. However, simple linear regression showed that treatment with dsRNA-AChE increased D. citri susceptibility to fenpropathrin

  14. Highly Sensitive Detection of Organophosphate Insecticides Using Biosensors Based on Genetically Engineered Acetylcholinesterase and Poly(3,4-Ethylenedioxythiophene

    Directory of Open Access Journals (Sweden)

    Tomasz Sikora

    2011-01-01

    Full Text Available A poly(3,4-ethylenedioxythiophene (PEDOT conducting ink is presented as a new electroactive material to be incorporated in acetylcholinesterase-(AChE- based screen printed biosensors, acting not only as a conducting template but also as an electrochemical mediator for thiocholine oxidation. Two different strategies have been studied for the chemical synthesis of PEDOT: (a a classical oxidative polymerisation and (b a more innovative enzymatic polymerisation, giving a water-soluble PEDOT. The use of this water-soluble conducting polymer as mediator in screen-printed biosensors enables its deposition by printing like the rest of the layers. Highly sensitive acetylcholinesterase-(AChE- based screen-printed biosensors have been constructed using both classical and enzymatic PEDOT, in combination with genetically modified AChE. These electrodes allow the measurement of thiocholine oxidation at potentials of 100 mV versus Ag/AgCl reference electrode through the mediation of PEDOT. Inhibition of thiocholine production in presence of CPO allow for detection of this pesticide in concentrations as low as 1·10−10 M.

  15. Investigation of insecticide-resistance status of Cydia pomonella in Chinese populations.

    Science.gov (United States)

    Yang, X-Q; Zhang, Y-L

    2015-06-01

    The codling moth Cydia pomonella (L.) is an economically important fruit pest and it has been directly targeted by insecticides worldwide. Serious resistance to insecticides has been reported in many countries. As one of the most serious invasive pest, the codling moth has populated several areas in China. However, resistance to insecticides has not been reported in China. We investigated the insecticide-resistance status of four field populations from Northwestern China by applying bioassays, enzyme activities, and mutation detections. Diagnostic concentrations of lambda-cyhalothrin, chlorpyrifos-ethyl, carbaryl, and imidacloprid were determined and used in bioassays. Field populations were less susceptible to chlorpyrifos-ethyl and carbaryl than laboratory strain. Insensitive populations displayed an elevated glutathione S-transferases (GSTs) activity. Reduced carboxylesterase (CarE) activity was observed in some insecticide insensitive populations and reduced acetylcholinesterase activity was observed only in the Wuw population. The cytochrome P450 polysubstrate monooxygenases activities in four field populations were not found to be different from susceptible strains. Neither the known-resistance mutation F399V in the acetylcholinesterase (AChE) gene, ace1, nor mutations in CarE gene CpCE-1 were found in adult individuals from our field populations. Native-PAGE revealed that various CarE isozymes and AChE insensitivity were occurring among Chinese populations. Our results indicate that codling moth populations from Northwestern China were insensitivity to chlorpyrifos-ethyl and carbaryl. Increased GST activity was responsible for insecticides insensitivity. Decreased CarE activity, as well as the presence of CarE and AChE polymorphisms might also be involved in insecticides insensitivity. New management strategies for managing this pest are discussed.

  16. Transmembrane potential polarization, calcium influx, and receptor conformational state modulate the sensitivity of the imidacloprid-insensitive neuronal insect nicotinic acetylcholine receptor to neonicotinoid insecticides.

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    Bodereau-Dubois, Béatrice; List, Olivier; Calas-List, Delphine; Marques, Olivier; Communal, Pierre-Yves; Thany, Steeve H; Lapied, Bruno

    2012-05-01

    Neonicotinoid insecticides act selectively on insect nicotinic acetylcholine receptors (nAChRs). Recent studies revealed that their efficiency was altered by the phosphorylation/dephosphorylation process and the intracellular signaling pathway involved in the regulation of nAChRs. Using whole-cell patch-clamp electrophysiology adapted for dissociated cockroach dorsal unpaired median (DUM) neurons, we demonstrated that intracellular factors involved in the regulation of nAChR function modulated neonicotinoid sensitivity. DUM neurons were known to express two α-bungarotoxin-insensitive nAChR subtypes: nAChR1 and nAChR2. Whereas nAChR1 was sensitive to imidacloprid, nAChR2 was insensitive to this insecticide. Here, we demonstrated that, like nicotine, acetamiprid and clothianidin, other types of neonicotinoid insecticides, acted as agonists on the nAChR2 subtype. Using acetamiprid, we revealed that both steady-state depolarization and hyperpolarization affected nAChR2 sensitivity. The measurement of the input membrane resistance indicated that change in the acetamiprid-induced agonist activity was related to the receptor conformational state. Using cadmium chloride, ω-conotoxin GVIA, and (R,S)-(3,4-dihydro-6,7-dimethoxy-isoquinoline-1-yl)-2-phenyl-N,N-di-acetamide (LOE 908), we found that inhibition of calcium influx through high voltage-activated calcium channels and transient receptor potential γ (TRPγ) activated by both depolarization and hyperpolarization increased nAChR2 sensitivity to acetamiprid. Finally, using N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide hydrochloride (W7), forskolin, and cAMP, we demonstrated that adenylyl cyclase sensitive to the calcium/calmodulin complex regulated internal cAMP concentration, which in turn modulated TRPγ function and nAChR2 sensitivity to acetamiprid. Similar TRPγ-induced modulatory effects were also obtained when clothianidin was tested. These findings bring insights into the signaling pathway modulating

  17. An amperometric biosensor based on acetylcholinesterase immobilized onto iron oxide nanoparticles/multi-walled carbon nanotubes modified gold electrode for measurement of organophosphorus insecticides

    Energy Technology Data Exchange (ETDEWEB)

    Chauhan, Nidhi [Department of Biochemistry, M.D. University, Rohtak 124001, Haryana (India); Pundir, Chandra Shekhar, E-mail: pundircs@rediffmail.com [Department of Biochemistry, M.D. University, Rohtak 124001, Haryana (India)

    2011-09-02

    Graphical abstract: The stepwise amperometric biosensor fabrication process and immobilized acetylcholinesterase inhibition in pesticide solution. Highlights: {center_dot} Constructed a novel composite material using Fe{sub 3}O{sub 4}NP and c-MWCNT at Au electrode for electrocatalysis. {center_dot} The properties of nanoparticles modified electrodes were studied by SEM, FTIR, CVs and EIS. {center_dot} The biosensor exhibited good sensitivity (0.475 mA {mu}M{sup -1}) {center_dot} The half life of electrode was 2 months. {center_dot} The sensor was suitable for trace detection of OP pesticide residues in milk and water. - Abstract: An acetylcholinesterase (AChE) purified from maize seedlings was immobilized covalently onto iron oxide nanoparticles (Fe{sub 3}O{sub 4}NP) and carboxylated multi walled carbon nanotubes (c-MWCNT) modified Au electrode. An organophosphorus (OP) biosensor was fabricated using this AChE/Fe{sub 3}O{sub 4}/c-MWCNT/Au electrode as a working electrode, Ag/AgCl as standard and Pt wire as an auxiliary electrode connected through a potentiostat. The biosensor was based on inhibition of AChE by OP compounds/insecticides. The properties of nanoparticles modified electrodes were studied by scanning electron microscopy (SEM), Fourier transform infrared (FTIR), cyclic voltammograms (CVs) and electrochemical impedance spectroscopy (EIS). The synergistic action of Fe{sub 3}O{sub 4}NP and c-MWCNT showed excellent electrocatalytic activity at low potential (+0.4 V). The optimum working conditions for the sensor were pH 7.5, 35 deg. C, 600 {mu}M substrate concentration and 10 min for inhibition by pesticide. Under optimum conditions, the inhibition rates of OP pesticides were proportional to their concentrations in the range of 0.1-40 nM, 0.1-50 nM, 1-50 nM and 10-100 nM for malathion, chlorpyrifos, monocrotophos and endosulfan respectively. The detection limits were 0.1 nM for malathion and chlorpyrifos, 1 nM for monocrotophos and 10 nM for endosulfan. The

  18. The P450 CYP6Z1 confers carbamate/pyrethroid cross-resistance in a major African malaria vector beside a novel carbamate-insensitive N485I acetylcholinesterase-1 mutation.

    Science.gov (United States)

    Ibrahim, Sulaiman S; Ndula, Miranda; Riveron, Jacob M; Irving, Helen; Wondji, Charles S

    2016-07-01

    Carbamates are increasingly used for vector control notably in areas with pyrethroid resistance. However, a cross-resistance between these insecticides in major malaria vectors such as Anopheles funestus could severely limit available resistance management options. Unfortunately, the molecular basis of such cross-resistance remains uncharacterized in An. funestus, preventing effective resistance management. Here, using a genomewide transcription profiling, we revealed that metabolic resistance through upregulation of cytochrome P450 genes is driving carbamate resistance. The P450s CYP6P9a, CYP6P9b and CYP6Z1 were the most upregulated detoxification genes in the multiple resistant mosquitoes. However, in silico docking simulations predicted CYP6Z1 to metabolize both pyrethroids and carbamates, whereas CYP6P9a and CYP6P9b were predicted to metabolize only the pyrethroids. Using recombinant enzyme metabolism and inhibition assays, we demonstrated that CYP6Z1 metabolizes bendiocarb and pyrethroids, whereas CYP6P9a and CYP6P9b metabolize only the pyrethroids. Other upregulated gene families in resistant mosquitoes included several cuticular protein genes suggesting a possible reduced penetration resistance mechanism. Investigation of the target-site resistance in acetylcholinesterase 1 (ace-1) gene detected and established the association between the new N485I mutation and bendiocarb resistance (odds ratio 7.3; P resistance and improve the design of effective resistance management strategies to control this malaria vector. © 2016 The Authors. Molecular Ecology Published by John Wiley & Sons Ltd.

  19. Point mutations in acetylcholinesterase 1 associated with chlorpyrifos resistance in the brown planthopper, Nilaparvata lugens Stål.

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    Zhang, Y; Yang, B; Li, J; Liu, M; Liu, Z

    2017-08-01

    Insecticide resistance frequently results from target-site insensitivity, such as point mutations in acetylcholinesterases (AChEs) for resistance to organophosphates and carbamates. From a field-originated population of Nilaparvata lugens, a major rice pest, a resistant population (R9) was obtained by nine-generation continuous selection with chlorpyrifos. From the same field population, a relatively susceptible population (S9) was also constructed through rearing without any insecticides. Compared to the susceptible strain, Sus [medium lethal dose (LC 50 ) = 0.012 mg/l], R9 had a resistance ratio (RR) of 253.08-fold, whereas the RR of S9 was only 2.25-fold. Piperonyl butoxide and triphenyl phosphate synergized chlorpyrifos in R9 less than three-fold, indicating other important mechanisms for high resistance. The target-site insensitivity was supported by the key property differences of crude AChEs between R9 and S9. Compared to S9, three mutations (G119S, F331C and I332L) were detected in NlAChE1 from individuals of the R9 and field populations, but no mutation was detected in NlAChE2. G119S and F331C could decreased insecticide sensitivities in recombinant NlAChE1, whereas I332L took effect through increasing the influence of F331C on target insensitivity. F331C might be deleterious because of its influence on the catalytic efficiency of NlAChE1, whereas I332L would decrease these adverse effects and maintain the normal functions of AChEs. © 2017 The Royal Entomological Society.

  20. Buprofezin inhibits acetylcholinesterase activity in B-biotype Bemisia tabaci.

    Science.gov (United States)

    Cottage, Emma L A; Gunning, Robin V

    2006-01-01

    B-biotype Bemisia tabaci is a severe insect pest worldwide in many ornamental, agricultural, and horticultural industries. Control of this insect is hampered by resistance to many acetylcholinesterase (AChE)-inhibiting insecticides, such as organophosphates and carbamates. Consequently, insect growth regulators such as buprofezin, which act by inhibiting chitin synthesis, are being investigated for use against B-biotype B. tabaci in Australia. This study discusses the effects of buprofezin on B. tabaciAChE.

  1. Insensitive Munitions Testing

    Data.gov (United States)

    Federal Laboratory Consortium — Insensitive Munitions Testing at RTC is conducted (IAW MILSTD-2105) at Test Area 4. Our engineers and technicians obtain data for hazards classification and safety...

  2. Malaria transmission and insecticide resistance of Anopheles gambiae in Libreville and Port-Gentil, Gabon

    Directory of Open Access Journals (Sweden)

    Kombila Maryvonne

    2010-11-01

    Full Text Available Abstract Background Urban malaria is a major health priority for civilian and militaries populations. A preliminary entomologic study has been conducted in 2006-2007, in the French military camps of the two mains towns of Gabon: Libreville and Port-Gentil. The aim was to assess the malaria transmission risk for troops. Methods Mosquitoes sampled by human landing collection were identified morphologically and by molecular methods. The Plasmodium falciparum circumsporozoïte (CSP indexes were measured by ELISA, and the entomological inoculation rates (EIR were calculated for both areas. Molecular assessments of pyrethroid knock down (kdr resistance and of insensitive acetylcholinesterase resistance were conducted. Results In Libreville, Anopheles gambiae s.s. S form was the only specie of the An. gambiae complex present and was responsible of 9.4 bites per person per night. The circumsporozoïte index was 0.15% and the entomological inoculation rate estimated to be 1.23 infective bites during the four months period. In Port-Gentil, Anopheles melas (75.5% of catches and An. gambiae s.s. S form (24.5% were responsible of 58.7 bites per person per night. The CSP indexes were of 1.67% for An. gambiae s.s and 0.28% for An. melas and the EIRs were respectively of 1.8 infective bites per week and of 0.8 infective bites per week. Both kdr-w and kdr-e mutations in An. gambiae S form were found in Libreville and in Port-Gentil. Insensitive acetylcholinesterase has been detected for the first time in Gabon in Libreville. Conclusion Malaria transmission exists in both town, but with high difference in the level of risk. The co-occurrence of molecular resistances to the main families of insecticide has implications for the effectiveness of the current vector control programmes that are based on pyrethroid-impregnated bed nets.

  3. Anticholinesterase insecticide retrospective.

    Science.gov (United States)

    Casida, John E; Durkin, Kathleen A

    2013-03-25

    The anticholinesterase (antiChE) organophosphorus (OP) and methylcarbamate (MC) insecticides have been used very effectively as contact and systemic plant protectants for seven decades. About 90 of these compounds are still in use - the largest number for any insecticide chemotype or mode of action. In both insects and mammals, AChE inhibition and acetylcholine accumulation leads to excitation and death. The cholinergic system of insects is located centrally (where it is protected from ionized OPs and MCs) but not at the neuromuscular junction. Structural differences between insect and mammalian AChE are also evident in their genomics, amino acid sequences and active site conformations. Species selectivity is determined in part by inhibitor and target site specificity. Pest population selection with OPs and MCs has resulted in a multitude of modified AChEs of altered inhibitor specificity some conferring insecticide resistance and others enhancing sensitivity. Much of the success of antiChE insecticides results from a suitable balance of bioactivation and detoxification by families of CYP450 oxidases, hydrolases, glutathione S-transferases and others. Known inhibitors for these enzymes block detoxification and enhance potency which is particularly important in resistant strains. The current market for OPs and MCs of 19% of worldwide insecticide sales is only half of that of 10 years ago for several reasons: there have been no major new compounds for 30 years; resistance has eroded their effectiveness; human toxicity problems are still encountered; the patents have expired reducing the incentive to update registration packages; alternative chemotypes or control methods have been developed. Despite this decline, they still play a major role in pest control and the increasing knowledge on their target sites and metabolism may make it possible to redesign the inhibitors for insensitive AChEs and to target new sites in the cholinergic system. The OPs and MCs are down

  4. Decrease of insecticide resistance over generations without exposure to insecticides in Nilaparvata lugens (Hemipteran: Delphacidae).

    Science.gov (United States)

    Yang, Yajun; Dong, Biqin; Xu, Hongxing; Zheng, Xusong; Tian, Junce; Heong, Kongleun; Lu, Zhongxian

    2014-08-01

    The brown planthopper, Nilaparvata lugens (Stål), is one of the most important insect pests on paddy rice in tropical and temperate Asia. Overuse and misuse of insecticides have resulted in the development of high resistance to many different insecticides in this pest. Studies were conducted to evaluate the change of resistance level to four insecticides over 15 generations without any exposure to insecticides in brown planthopper. After 15 generations' rearing without exposure to insecticide, brown planthopper could reverse the resistance to imidacloprid, chlorpyrifos, fipronil, and fenobucarb. The range and style of resistance reversal of brown planthopper differed when treated with four different insecticides. To monitor potential changes in insect physiological responses, we measured the activity of each of the three selected enzymes, including acetylcholinesterases (AChE), general esterases (EST), and glutathione S-transferases. After multiple generations' rearing without exposure to insecticide, AChE and EST activities of brown planthopper declined with the increased generations, suggesting that the brown planthopper population adjusted activities of EST and AChE to adapt to the non-insecticide environment. These findings suggest that the reducing, temporary stop, or rotation of insecticide application could be incorporated into the brown planthopper management.

  5. Inheritance and stability of mevinphos-resistance in Plutella xylostella (L.), with special reference to mutations of acetylcholinesterase 1.

    Science.gov (United States)

    Lin, Chia-Li; Yeh, Shih-Chia; Feng, Hai-Tung; Dai, Shu-Mei

    2017-09-01

    Diamondback moth (Plutella xylostella L.) causes enormous damage on cruciferous vegetables and can rapidly develop resistance to all kinds of insecticides. To effectively manage the insecticide resistance of P. xylostella, an understanding of its inheritance and stability is essential. Here we investigated the phenotypic and genotypic basis of mevinphos resistance by crossing two genetically pure lines of P. xylostella, an SH ggt wild-type strain and an SHM TCN resistant strain carrying 892T/T, 971C/C, and 1156T/G (TCN) mutations of the acetylcholinesterase 1 gene (Pxace1). Similar median lethal concentrations and degrees of dominance in the reciprocal cross progeny, and no plateau on the log concentration-probit line of F1 backcross and self-cross progeny, suggest that the mevinphos-resistance in P. xylostella is inherited as an autosomal and incomplete dominant trait governed by more than one gene. In the absence of mevinphos exposure, the resistance ratio and Pxace1 mutation frequency declined concomitantly in the SHM TCN strain. After 20-generation relaxation, the mevinphos resistance decreased from 52- to 6-fold and the Pxace1 mutation frequency of the TCN haplotype pair decreased from 100% to 0%. A good correlation was found between the resistance ratio and TCN frequency within the range of 12.5- to 25-fold resistance. Since there was no TCN haplotype pair detected below a resistance level of 12.5-fold, we speculate that resistance mechanisms other than target site insensitivity may exist. These observations are important for the prediction and management of mevinphos and related organophosphate resistance in field populations of P. xylostella. Copyright © 2016. Published by Elsevier Inc.

  6. Insensitive Enough Semantics

    Directory of Open Access Journals (Sweden)

    Richard Vallée

    2006-06-01

    Full Text Available According to some philosophers, sentences like (1 “It is raining” and (2 “John is ready” are context sensitive sentences even if they do not contain indexicals or demonstratives. That view initiated a context sensitivity frenzy. Cappelen and Lepore (2005 summarize the frenzy by the slogan “Every sentence is context sensitive” (Insensitive Semantics, p. 6, note 5. They suggest a view they call Minimalism according to which the truth conditions of utterances of sentences like (1/(2 are exactly what Convention T gives you. I will distinguish different propositions, and refocus semantics on sentences. As distinct from what the protagonists in the ongoing debate think, I argue that the content or truth conditions of utterances of both context sensitive sentences and sentences like (1/(2 are not interesting from a semantic point of view, and that the problem sentences like (1/(2 raises is not about context sensitivity or context insensitivity of sentences, but relevance of the content of utterances.

  7. Acetylcholinesterase of Rhipicephalus (Boophilus) microplus and Phlebotomus papatasi: Gene identification, expression, and biochemical properties of recombinant proteins

    Science.gov (United States)

    Rhipicephalus (Boophilus) microplus (Bm) ticks are vectors of bovine babesiosis and anaplasmosis. Tick resistance to organophosphate (OP) acaricide involves acetylcholinesterase (AChE) insensitivity to OP and metabolic detoxification. Sequencing and in vitro expression of Bm genes encoding AChE allo...

  8. Acetylcholinesterases of Rhipicephalus (Boophilus) microplus and Phlebotomus papatasi: Gene identification, expression and biochemical properties of recombinant proteins

    Science.gov (United States)

    Rhipicephalus (Boophilus) microplus (Bm) is a vector of bovine babesiosis and anaplasmosis. Tick resistance to organophosphate (OP) acaricide involves acetylcholinesterase (AChE) insensitivity to OP and metabolic detoxification. In vitro expression of Bm genes encoding AChE allowed biochemical chara...

  9. Concentration-dependent interactions of the organophosphates chlorpyrifos oxon and methyl paraoxon with human recombinant acetylcholinesterase

    International Nuclear Information System (INIS)

    Kaushik, R.; Rosenfeld, Clint A.; Sultatos, L.G.

    2007-01-01

    For many decades it has been thought that oxygen analogs (oxons) of organophosphorus insecticides phosphorylate the catalytic site of acetylcholinesterase by a mechanism that follows simple Michaelis-Menten kinetics. More recently, the interactions of at least some oxons have been shown to be far more complex and likely involve binding of oxons to a second site on acetylcholinesterase that modulates the inhibitory capacity of other oxon molecules at the catalytic site. The current study has investigated the interactions of chlorpyrifos oxon and methyl paraoxon with human recombinant acetylcholinesterase. Both chlorpyrifos oxon and methyl paraoxon were found to have k i 's that change as a function of oxon concentration. Furthermore, 10 nM chlorpyrifos oxon resulted in a transient increase in acetylthiocholine hydrolysis, followed by inhibition. Moreover, in the presence of 100 nM chlorpyrifos oxon, acetylthiocholine was found to influence both the K d (binding affinity) and k 2 (phosphorylation constant) of this oxon. Collectively, these results demonstrate that the interactions of chlorpyrifos oxon and methyl paraoxon with acetylcholinesterase cannot be described by simple Michaelis-Menten kinetics but instead support the hypothesis that these oxons bind to a secondary site on acetylcholinesterase, leading to activation/inhibition of the catalytic site, depending on the nature of the substrate and inhibitor. Additionally, these data raise questions regarding the adequacy of estimating risk of low levels of insecticide exposure from direct extrapolation of insecticide dose-response curves since the capacity of individual oxon molecules at low oxon levels could be greater than individual oxon molecules in vivo associated with the dose-response curve

  10. Experimental hut evaluation of bednets treated with an organophosphate (chlorpyrifos-methyl or a pyrethroid (lambdacyhalothrin alone and in combination against insecticide-resistant Anopheles gambiae and Culex quinquefasciatus mosquitoes

    Directory of Open Access Journals (Sweden)

    Corbel Vincent

    2005-05-01

    Full Text Available Abstract Background Pyrethroid resistant mosquitoes are becoming increasingly common in parts of Africa. It is important to identify alternative insecticides which, if necessary, could be used to replace or supplement the pyrethroids for use on treated nets. Certain compounds of an earlier generation of insecticides, the organophosphates may have potential as net treatments. Methods Comparative studies of chlorpyrifos-methyl (CM, an organophosphate with low mammalian toxicity, and lambdacyhalothrin (L, a pyrethroid, were conducted in experimental huts in Côte d'Ivoire, West Africa. Anopheles gambiae and Culex quinquefasciatus mosquitoes from the area are resistant to pyrethroids and organophosphates (kdr and insensitive acetylcholinesterase Ace.1R. Several treatments and application rates on intact or holed nets were evaluated, including single treatments, mixtures, and differential wall/ceiling treatments. Results and Conclusion All of the treatments were effective in reducing blood feeding from sleepers under the nets and in killing both species of mosquito, despite the presence of the kdr and Ace.1R genes at high frequency. In most cases, the effects of the various treatments did not differ significantly. Five washes of the nets in soap solution did not reduce the impact of the insecticides on A. gambiae mortality, but did lead to an increase in blood feeding. The three combinations performed no differently from the single insecticide treatments, but the low dose mixture performed encouragingly well indicating that such combinations might be used for controlling insecticide resistant mosquitoes. Mortality of mosquitoes that carried both Ace.1R and Ace.1S genes did not differ significantly from mosquitoes that carried only Ace.1S genes on any of the treated nets, indicating that the Ace.1R allele does not confer effective resistance to chlorpyrifos-methyl under the realistic conditions of an experimental hut.

  11. Tissue distribution of human acetylcholinesterase and butyrylcholinesterase messenger RNA

    Energy Technology Data Exchange (ETDEWEB)

    Jbilo, O.; Barteles, C.F.; Chatonnet, A.; Toutant, J.P.; Lockridge, O.

    1994-12-31

    Tissue distribution of human acetyicholinesterase and butyryicholinesterase messenger RNA. 1 Cholinesterase inhibitors occur naturally in the calabar bean (eserine), green potatoes (solanine), insect-resistant crab apples, the coca plant (cocaine) and snake venom (fasciculin). There are also synthetic cholinesterase inhibitors, for example man-made insecticides. These inhibitors inactivate acetyicholinesterase and butyrylcholinesterase as well as other targets. From a study of the tissue distribution of acetylcholinesterase and butyrylcholinesterase mRNA by Northern blot analysis, we have found the highest levels of butyrylcholinesterase mRNA in the liver and lungs, tissues known as the principal detoxication sites of the human body. These results indicate that butyrylcholinesterase may be a first line of defense against poisons that are eaten or inhaled.

  12. Acetylcholinesterase Inhibitory Activity of Green Tea Polyphenols ...

    African Journals Online (AJOL)

    Inhibition of acetylcholinesterase activity is one of the most popular approaches for treatment of neurological disorders such as Alzheimer's disease and others. In the present study, we evaluated inhibition of acetylcholinesterase activity by different concentrations of green tea (Camellia sinensis L.) extract using ...

  13. Variation of Musca domestica L. acetylcholinesterase in Danish housefly populations

    DEFF Research Database (Denmark)

    Kristensen, Michael; Huang, Jing; Qiao, Chuan-Ling

    2006-01-01

    Anti-cholinesterase resistance is in many cases caused by modified acetylcholinesterase (MACE). A comparison was made of toxicological data and AChE activity gathered from 21 field populations and nine laboratory strains of houseflies, Musca domestica L., to elucidate the best way of generating...... data to provide advice for management strategies and gathering information for resistance risk assessment on the organophosphates azamethiphos and dimethoate and the carbamate methomyl, which have been the primary insecticides used against adult houseflies in Denmark. Cluster analysis was performed...... and > 2000 houseflies were assigned to one of three phenotypes based on total acetylcholinesterase activity as well as inhibition by azamethiphos, methomyl or omethoate. A cluster, i.e. a phenotype, with high total AChE activity and high sensitivity to azamethiphos and less sensitivity to inhibition...

  14. Insecticide resistance in the western flower thrips, Frankliniella occidentalis

    DEFF Research Database (Denmark)

    Jensen, Sten Erik

    of acetylcholinesterase, the target site enzyme for methiocarb. The results from bioassays with synergists included indicated involvement of cytochrome P450- monooxygenases and esterases in methiocarb resistance in the most resistant populations. Selection with methiocarb on one of the populations to increase the level......The western flower thrips, Frankliniella occidentalis (Pergande) is a serious pest on a wide range of crops throughout the world. In Denmark F. occidentalis is a pest in greenhouses. F. occidentalis is difficult to control with insecticides because of its thigmokinetic behaviour and resistance...... to insecticides. Since F. occidentulis spread to become a worldwide pest in 1980’es, resistance to a number of different insecticides has been shown in many populations of F. occidentalis. This flower thrips has the potential of fast development of resistance owing to the short generation time, high fecundity...

  15. Molecular basis of androgen insensitivity

    NARCIS (Netherlands)

    Brinkmann, A.; Jenster, G.; Ris-Stalpers, C.; van der Korput, H.; Brüggenwirth, H.; Boehmer, A.; Trapman, J.

    1996-01-01

    Male sexual differentiation and development proceed under direct control of androgens. Androgen action is mediated by the intracellular androgen receptor, which belongs to the superfamily of ligand-dependent transcription factors. In the X-linked androgen insensitivity syndrome, defects in the

  16. Insecticide resistance and, efficacy of space spraying and larviciding in the control of dengue vectors Aedes aegypti and Aedes albopictus in Sri Lanka.

    Science.gov (United States)

    Karunaratne, S H P P; Weeraratne, T C; Perera, M D B; Surendran, S N

    2013-09-01

    Unprecedented incidence of dengue has been recorded in Sri Lanka in recent times. Source reduction and use of insecticides in space spraying/fogging and larviciding, are the primary means of controlling the vector mosquitoes Aedes aegypti and Ae. albopictus in the island nation. A study was carried out to understand insecticide cross-resistance spectra and mechanisms of insecticide resistance of both these vectors from six administrative districts, i.e. Kandy, Kurunegala, Puttalam, Gampaha, Ratnapura and Jaffna, of Sri Lanka. Efficacy of the recommended dosages of frequently used insecticides in space spraying and larviciding in dengue vector control programmes was also tested. Insecticide bioassay results revealed that, in general, both mosquito species were highly resistant to DDT but susceptible to propoxur and malathion except Jaffna Ae. aegypti population. Moderate resistance to malathion shown by Jaffna Ae. aegypti population correlated with esterase and malathion carboxylesterase activities of the population. High levels of acetylcholinesterase (AChE) insensitivity in the absence of malathion and propoxur resistance may be due to non-synaptic forms of AChE proteins. Moderate pyrethroid resistance in the absence of high monooxygenase levels indicated the possible involvement of 'kdr' type resistance mechanism in Sri Lankan dengue vectors. Results of the space spraying experiments revealed that 100% mortality at a 10 m distance and >50% mortality at a 50 m distance can be achieved with malathion, pesguard and deltacide even in a ground with dense vegetation. Pesguard and deltacide spraying gave 100% mortality up to 50 m distance in open area and areas with little vegetation. Both species gave >50% mortalities for deltacide at a distance of 75 m in a dense vegetation area. Larval bioassays conducted in the laboratory showed that a 1 ppm temephos solution can maintain a larval mortality rate of 100% for ten months, and the mortality rate declined to 0% in the

  17. Genetics Home Reference: androgen insensitivity syndrome

    Science.gov (United States)

    ... Androgen insensitivity syndrome is a condition that affects sexual development before birth and during puberty. People with this ... characteristics or signs of both male and female sexual development. Complete androgen insensitivity syndrome occurs when the body ...

  18. Male patients with partial androgen insensitivity syndrome

    DEFF Research Database (Denmark)

    Hellmann, Philip; Christiansen, Peter; Johannsen, Trine Holm

    2012-01-01

    To describe the natural history of phenotype, growth and gonadal function in patients with partial androgen insensitivity syndrome.......To describe the natural history of phenotype, growth and gonadal function in patients with partial androgen insensitivity syndrome....

  19. Phytochemical screening and in vitro acetylcholinesterase inhibitory ...

    African Journals Online (AJOL)

    Phytochemical screening and in vitro acetylcholinesterase inhibitory activity of seven plant extracts. Titilayo Johnson, Oduje A. Akinsanmi, Enoch J. Banbilbwa, Tijani A. Yahaya, Karima Abdulaziz, Kolade Omole ...

  20. Insecticide solvents: interference with insecticidal action.

    Science.gov (United States)

    Brattsten, L B; Wilkinson, C F

    1977-06-10

    Several commercial solvent mixtures commonly used as insecticide carriers in spray formulations increase by more than threefold the microsomal N-demethylation of p-chloro N-methylaniline in midgut preparations of southern army-worm (Spodoptera eridania) larvae exposed orally to the test solvents. Under laboratory conditions, the same solvent mixtures exhibit a protective action against the in vivo toxicity of the insecticide carbaryl to the larvae. The data are discussed with respect to possible solvent-insecticide interactions occurring under field conditions and, more broadly, to potential toxicological hazards of these solvents to humans.

  1. Insecticidal and Nematicidal Activities of Novel Mimosine Derivatives

    Directory of Open Access Journals (Sweden)

    Binh Cao Quan Nguyen

    2015-09-01

    Full Text Available Mimosine, a non-protein amino acid, is found in several tropical and subtropical plants, which has high value for medicine and agricultural chemicals. Here, in continuation of works aimed to development of natural product-based pesticidal agents, we present the first significant findings for insecticidal and nematicidal activities of novel mimosine derivatives. Interestingly, mimosinol and deuterated mimosinol (D-mimosinol from mimosine had strong insecticidal activity which could be a result of tyrosinase inhibition (IC50 = 31.4 and 46.1 μM, respectively. Of synthesized phosphoramidothionate derivatives from two these amino alcohols, two compounds (1a and 1b showed high insecticidal activity (LD50 = 0.5 and 0.7 μg/insect, respectively with 50%–60% mortality at 50 μg/mL which may be attributed to acetylcholinesterase inhibition. Compounds 1a and 1b also had strong nematicidal activity with IC50 = 31.8 and 50.2 μM, respectively. Our results suggest that the length of the alkyl chain and the functional group at the C5-position of phosphoramidothionates derived from mimosinol and d-mimosinol are essential for the insecticidal and nematicidal activities. These results reveal an unexplored scaffold as new insecticide and nematicide.

  2. Surface display of recombinant Drosophila melanogaster acetylcholinesterase for detection of organic phosphorus and carbamate pesticides.

    Directory of Open Access Journals (Sweden)

    Jingquan Li

    Full Text Available Acetylcholinesterase (AChE is commonly used for the detection of organophosphate (OP and carbamate (CB insecticides. However, the cost of this commercially available enzyme is high, making high-throughput insecticide detection improbable. In this study we constructed a new AChE yeast expression system in Saccharomyces cerevisiae for the expression of a highly reactive recombinant AChE originating from Drosophila melanogaster (DmAChE. Specifically, the coding sequence of DmAChE was fused with the 3'-terminal half of an α-agglutinin anchor region, along with an antigen tag for the detection of the recombinant protein. The target sequence was cloned into the yeast expression vector pYes-DEST52, and the signal peptide sequence was replaced with a glucoamylase secretion region for induced expression. The resultant engineered vector was transformed into S. cerevisiae. DmAChE was expressed and displayed on the cell surface after galactose induction. Our results showed that the recombinant protein displayed activity comparable to the commercial enzyme. We also detected different types of OP and CB insecticides through enzyme inhibition assays, with the expressed DmAChE showing high sensitivity. These results show the construction of a new yeast expression system for DmAChE, which can subsequently be used for detecting OP and CB insecticides with reduced economic costs.

  3. Synthesis of Novel Chalcones as Acetylcholinesterase Inhibitors

    Directory of Open Access Journals (Sweden)

    Thanh-Dao Tran

    2016-07-01

    Full Text Available A new series of benzylaminochalcone derivatives with different substituents on ring B were synthesized and evaluated as inhibitors of acetylcholinesterase. The study is aimed at identification of novel benzylaminochalcones capable of blocking acetylcholinesterase activity for further development of an approach to Alzheimer’s disease treatment. These compounds were produced in moderate to good yields via Claisen-Schmidt condensation and subjected to an in vitro acetylcholinesterase inhibition assay, using Ellman’s method. The in silico docking procedure was also employed to identify molecular interactions between the chalcone compounds and the enzyme. Compounds with ring B bearing pyridin-4-yl, 4-nitrophenyl, 4-chlorophenyl and 3,4-dimethoxyphenyl moieties were discovered to exhibit significant inhibitory activities against acetylcholinesterase, with IC50 values ranging from 23 to 39 µM. The molecular modeling studies are consistent with the hypothesis that benzylaminochalcones could exert their effects as dual-binding-site acetylcholinesterase inhibitors, which might simultaneously enhance cholinergic neurotransmission and inhibit β-amyloid aggregation through binding to both catalytic and peripheral sites of the enzyme. These derivatives could be further developed to provide novel leads for the discovery of new anti-Alzheimer drugs in the future.

  4. Myrtenal inhibits acetylcholinesterase, a known Alzheimer target.

    Science.gov (United States)

    Kaufmann, Dorothea; Dogra, Anudeep Kaur; Wink, Michael

    2011-10-01

    Inhibition of acetylcholinesterase (AChE) is a common treatment for early stages of the most general form of dementia, Alzheimer's disease. In this study selected components of essential oils, which carry a variety of important functional groups, were tested for their in-vitro anti-acetylcholinesterase activity. In-vitro anti-acetylcholinesterase activity was measured by an adapted version of Ellman's colorimetric assay. 1,8-cineole, carvacrol, myrtenal and verbenone apparently inhibited AChE; the highest inhibitory activity was observed for myrtenal (IC50 = 0.17 mm). This is the first study showing the AChE inhibitory activity of myrtenal. Our investigations provided evidence for the efficacy of monoterpenes as inhibitors of AChE. © 2011 The Authors. JPP © 2011 Royal Pharmaceutical Society.

  5. Anionic subsites of the acetylcholinesterase from Torpedo californica: affinity labelling with the cationic reagent N,N-dimethyl-2-phenyl-aziridinium.

    OpenAIRE

    Weise, C; Kreienkamp, H J; Raba, R; Pedak, A; Aaviksaar, A; Hucho, F

    1990-01-01

    Several peptides of acetylcholinesterase of Torpedo californica labelled with the alkylating reagent [3H]N,N-dimethyl-2-phenyl-aziridinium (DPA) were localized within the primary structure. One peptide had the sequence KPQELIDVE (positions 270-278); the incorporation of DPA into this peptide could be specifically suppressed by propidium, which suggests that it is part of the peripheral anionic site. The incorporation of DPA into two other peptides was insensitive to propidium but could be pre...

  6. A small-volume bioassay for quantification of the esterase inhibiting potency of mixtures of organophosphate and carbamate insecticides in rainwater : development and optimization

    NARCIS (Netherlands)

    Hamers, T.; Molin, K.R.J.; Koeman, J.H.; Murk, A.J.

    2000-01-01

    The goal of this study was to develop a sensitive in vitro bioassay for quantification of the total esterase inhibiting potency of low concentrations of organophosphate and carbamate insecticides in relatively small rainwater samples. Purified acetylcholinesterase (AChE) from electric eel

  7. Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon

    Czech Academy of Sciences Publication Activity Database

    Kuča, K.; Musilová, L.; Paleček, J.; Církva, Vladimír; Paar, M.; Musílek, K.; Hrabinová, M.; Pohanka, M.; Zdarová Karasová, J.; Jun, D.

    2009-01-01

    Roč. 14, č. 12 (2009), s. 4915-4921 ISSN 1420-3049 Grant - others:MO0(CZ) FZV0000604 Institutional research plan: CEZ:AV0Z40720504 Keywords : acetylcholinesterase * reactivator * oxime Subject RIV: CC - Organic Chemistry Impact factor: 1.738, year: 2009

  8. The Pragmatics of Insensitive Assessments

    Directory of Open Access Journals (Sweden)

    Alexander Almér

    2010-12-01

    Full Text Available In assessing the veridicality of utterances, we normally seem to assess the satisfaction of conditions that the speaker had been concerned to get right in making the utterance. However, the debate about assessor-relativism about epistemic modals, predicates of taste, gradable adjectives and conditionals has been largely driven by cases in which seemingly felicitous assessments of utterances are insensitive to aspects of the context of utterance that were highly relevant to the speaker’s choice of words.In this paper, we offer an explanation of why certain locutions invite insensitive assessments, focusing primarily on ’tasty’ and ’might’. We spell out some reasons why felicitous insensitive assessments are puzzling and argue briefly that recent attempts to accommodate such assessments (including attempts by John MacFarlane, Kai von Fintel and Anthony Gillies all fail to provide more than hints at a solution to the puzzle. In the main part of the paper, we develop an account of felicitous insensitive assessments by identifying a number of pragmatic factors that influence the felicity of assessments. Before closing, we argue that the role of these factors extends beyond cases considered in the debate about assessor-relativism and fits comfortably with standard contextualist analyses of the relevant locutions.ReferencesAlmér, A. & Björnsson, G. 2009. ‘Relativism, Contextualism and Insensitive Assessments’. Logique et Analyse 52: 363–372.Bach, K. 2011. ‘Perspectives on possibilities: Contextualism, Relativism, or what?’Bennett, J. 2003. A Philosophical Guide to Conditionals. Oxford U. P.http://dx.doi.org/10.1093/0199258872.001.0001Björnsson, G. 2011. ‘Towards a Radically Pragmatic Theory of If-Conditionals’. Forthcoming in Making Semantics Pragmatic, (ed Ken Turner, in Current Research in the Semantics/Pragmatics Interface, Vol 24, Emerald.Björnsson, G. ms. ‘Do “Objectivist” Features of Moral Discourse and Thinking

  9. Differences between organophosphorus insecticides in human self-poisoning: a prospective cohort study.

    Science.gov (United States)

    Eddleston, Michael; Eyer, Peter; Worek, Franz; Mohamed, Fahim; Senarathna, Lalith; von Meyer, Ludwig; Juszczak, Edmund; Hittarage, Ariyasena; Azhar, Shifa; Dissanayake, Wasantha; Sheriff, M H Rezvi; Szinicz, Ladislaus; Dawson, Andrew H; Buckley, Nick A

    Although more than 100 organophosphorus insecticides exist, organophosphorus poisoning is usually regarded as a single entity, distinguished only by the compound's lethal dose in animals. We aimed to determine whether the three most common organophosphorus insecticides used for self-poisoning in Sri Lanka differ in the clinical features and severity of poisoning they cause. We prospectively studied 802 patients with chlorpyrifos, dimethoate, or fenthion self-poisoning admitted to three hospitals. Blood cholinesterase activity and insecticide concentration were measured to determine the compound and the patients' response to insecticide and therapy. We recorded clinical outcomes for each patient. Compared with chlorpyrifos (35 of 439, 8.0%), the proportion dying was significantly higher with dimethoate (61 of 264, 23.1%, odds ratio [OR] 3.5, 95% CI 2.2-5.4) or fenthion (16 of 99, 16.2%, OR 2.2, 1.2-4.2), as was the proportion requiring endotracheal intubation (66 of 439 for chlorpyrifos, 15.0%; 93 of 264 for dimethoate, 35.2%, OR 3.1, 2.1-4.4; 31 of 99 for fenthion, 31.3%, 2.6, 1.6-4.2). Dimethoate-poisoned patients died sooner than those ingesting other pesticides and often from hypotensive shock. Fenthion poisoning initially caused few symptoms but many patients subsequently required intubation. Acetylcholinesterase inhibited by fenthion or dimethoate responded poorly to pralidoxime treatment compared with chlorpyrifos-inhibited acetylcholinesterase. Organophosphorus insecticide poisoning is not a single entity, with substantial variability in clinical course, response to oximes, and outcome. Animal toxicity does not predict human toxicity since, although chlorpyrifos is generally the most toxic in rats, it is least toxic in people. Each organophosphorus insecticide should be considered as an individual poison and, consequently, patients might benefit from management protocols developed for particular organophosphorus insecticides.

  10. Acetylcholinesterase immobilized capillary reactors coupled to protein coated magnetic beads: A new tool for plant extract ligand screening

    OpenAIRE

    Vanzolini, Kenia Lourenço; Jiang, Zhengjin; Zhang, Xiaoqi; Vieira, Lucas Campos Curcino; Corrêa, Arlene Gonçalvez; Cardoso, Carmen Lucia; Cass, Quezia Bezerra; Moaddel, Ruin

    2013-01-01

    The use of immobilized capillary enzyme reactors (ICERs) and enzymes coated to magnetic beads ((NT or CT)-MB) for ligand screening has been adopted as a new technique of high throughput screening (HTS). In this work the selected target was the enzyme acetylcholinesterase (AChE), which acts on the central nervous system and is a validated target for the treatment of Alzheimer’s disease, as well as for new insecticides. A new approach for the screening of plant extracts was developed based on t...

  11. Insecticide Exposure in Parkinsonism

    National Research Council Canada - National Science Library

    Bloomquist, Jeffrey

    2002-01-01

    Behavioral, neurochemical, and immunocytochemical studies characterized the possible role of insecticide exposure in the etiology of Parkinson's disease as it may relate to Gulf War Syndrome. Chlorpyrifos (CP) and permethrin (PM...

  12. Insecticide Exposure in Parkinsonism

    National Research Council Canada - National Science Library

    Bloomquist, Jeffrey

    2001-01-01

    Behavioral, neurochemical, and immunocytochemical studies characterized the possible role of insecticide exposure in the etiology of Parkinson's disease as it may relate to Gulf War Syndrome. Chlorpyrifos (CP) and permethrin (PM...

  13. Insecticide Exposure in Parkinsonism

    National Research Council Canada - National Science Library

    Bloomquist, Jeffrey

    2003-01-01

    Behavioral, neurochemical, and immunocytochemical studies are characterizing the possible role of insecticide exposure in the etiology of Parkinson's disease as it may relate to Gulf War Syndrome. Chlorpyrifos (CP) and/or permethrin (PM...

  14. 3 Insecticide Use Practice

    African Journals Online (AJOL)

    Administrator

    500,000 metric tonnes in the 1964/1965 season. Problems ... insecticides on the open market. ... effective in the management of insect pests of cocoa. .... Effectiveness and profitability of pest ... Youth in Agriculture; Programme Policy, Strategy.

  15. Insecticides and Biological Control

    Science.gov (United States)

    Furness, G. O.

    1972-01-01

    Use of insecticides has been questioned due to their harmful effects on edible items. Biological control of insects along with other effective practices for checking spread of parasites on crops are discussed. (PS)

  16. Intermediate Syndrome Following Organophosphate Insecticide Poisoning

    Directory of Open Access Journals (Sweden)

    Chen-Chang Yang

    2007-11-01

    Full Text Available Acute organophosphate insecticide poisoning can manifest 3 different phases of toxic effects, namely, acute cholinergic crisis, intermediate syndrome (IMS, and delayed neuropathy. Among them, IMS has been considered as a major contributing factor of organophosphate-related morbidity and mortality because of its frequent occurrence and probable consequence of respiratory failure. Despite a high incidence, the pathophysiology that underlies IMS remains unclear. Previously proposed mechanisms of IMS include different susceptibility of various cholinergic receptors, muscle necrosis, prolonged acetylcholinesterase inhibition, inadequate oxime therapy, downregulation or desensitization of postsynaptic acetylcholine receptors, failure of postsynaptic acetylcholine release, and oxidative stress-related myopathy. The clinical manifestations of IMS typically occur within 24 to 96 hours, affecting conscious patients without cholinergic signs, and involve the muscles of respiration, proximal limb muscles, neck flexors, and muscles innervated by motor cranial nerves. With appropriate therapy that commonly includes artificial respiration, complete recovery develops 5–18 days later. Patients with atypical manifestations of IMS, especially a relapse or a continuum of acute cholinergic crisis, however, were frequently reported in clinical studies of IMS. The treatment of IMS is mainly supportive. Nevertheless, because IMS generally concurs with severe organophosphate toxicity and persistent inhibition of acetylcholinesterase, early aggressive decontamination, appropriate antidotal therapy, and prompt institution of ventilatory support should be helpful in ameliorating the magnitude and/or the incidence of IMS. Although IMS is well recognized as a disorder of neuromuscular junctions, its exact etiology, incidence, and risk factors are not clearly defined because existing studies are largely small-scale case series and do not employ a consistent and rigorous

  17. Three siblings with complete androgen insensitivity syndrome

    African Journals Online (AJOL)

    2013-01-13

    Jan 13, 2013 ... male reference range. A diagnosis of complete androgen insensitivity syndrome was made, based on this clinical ... Laboratory test. Value Normal ..... scenario, incomplete resistance may lead to virilisation during puberty.24, ...

  18. Syndrome of achalasia, ACTH insensitivity and alacrima

    Energy Technology Data Exchange (ETDEWEB)

    Ambrosino, M.M.; Genieser, N.B.; Becker, M.H.; Bangaru, B.S.; Sklar, C.

    1986-05-01

    An unusual multisystem disorder characterized by the triad of selective ACTH insensitivity, achalasia and alacrima has recently been described. The following case fulfills the criteria for this syndrome which has not been previously reported in the radiographic literature.

  19. Climate change, agricultural insecticide exposure, and risk for freshwater communities.

    Science.gov (United States)

    Kattwinkel, Mira; Kühne, Jan-Valentin; Foit, Kaarina; Liess, Matthias

    2011-09-01

    Climate change exerts direct effects on ecosystems but has additional indirect effects due to changes in agricultural practice. These include the increased use of pesticides, changes in the areas that are cultivated, and changes in the crops cultivated. It is well known that pesticides, and in particular insecticides, affect aquatic ecosystems adversely. To implement effective mitigation measures it is necessary to identify areas that are affected currently and those that will be affected in the future. As a consequence, we predicted potential exposure to insecticide (insecticide runoff potential, RP) under current conditions (1990) and under a model scenario of future climate and land use (2090) using a spatially explicit model on a continental scale, with a focus on Europe. Space-for-time substitution was used to predict future levels of insecticide application, intensity of agricultural land use, and cultivated crops. To assess the indirect effects of climate change, evaluation of the risk of insecticide exposure was based on a trait-based, climate-insensitive indicator system (SPEAR, SPEcies At Risk). To this end, RP and landscape characteristics that are relevant for the recovery of affected populations were combined to estimate the ecological risk (ER) of insecticides for freshwater communities. We predicted a strong increase in the application of, and aquatic exposure to, insecticides under the future scenario, especially in central and northern Europe. This, in turn, will result in a severe increase in ER in these regions. Hence, the proportion of stream sites adjacent to arable land that do not meet the requirements for good ecological status as defined by the EU Water Framework Directive will increase (from 33% to 39% for the EU-25 countries), in particular in the Scandinavian and Baltic countries (from 6% to 19%). Such spatially explicit mapping of risk enables the planning of adaptation and mitigation strategies including vegetated buffer strips and

  20. Toxicological effect of herbicides (diuron and bentazon) on snake venom and electric eel acetylcholinesterase.

    Science.gov (United States)

    Ahmed, Mushtaq; Latif, Nadia; Khan, Rehmat Ali; Ahmad, Akhlaq

    2012-08-01

    The toxicological effects of the active ingredients of the herbicides diuron and bentazon on the activity of acetylcholinesterase (AChE) of krait (Bungarus sindanus) venom and electric eel (Electrophorus electricus) were studied. The diuron and entazon caused non-competitive inhibition of AChE from both species. For the venom AChE, the calculated IC50 for diuron and bentazon were found to be 3.25 and 0.14 μM, while for eel AChE, the respective IC50 values were 3.6 and 0.135 μM. In comparison, bentazon was a more potent inhibitor than diuron of AChE from both species. The insecticide lindane did not have any inhibitory effect on AChE activity in either species, even when tested at high concentrations (200-800 μM).

  1. Acetylcholinesterase Inhibitory Activities of Flavonoids from the Leaves of Ginkgo biloba against Brown Planthopper

    Directory of Open Access Journals (Sweden)

    Xiao Ding

    2013-01-01

    Full Text Available Ginkgo biloba is a traditional Chinese medicinal plant which has potent insecticidal activity against brown planthopper. The MeOH extract was tested in the acetylcholinesterase (AChE inhibitory assay with IC50 values of 252.1 μg/mL. Two ginkgolides and thirteen flavonoids were isolated from the leaves of Ginkgo biloba. Their structures were established on the basis of spectroscopic data interpretation. It revealed that the 13 isolated flavonoids were found to inhibit AChE with IC50 values ranging from 57.8 to 133.1 μg/mL in the inhibitory assay. AChE was inhibited dose dependently by all tested flavonoids, and compound 6 displayed the highest inhibitory effect against AChE with IC50 values of 57.8 μg/mL.

  2. Insecticide resistance and resistance mechanisms in bed bugs, Cimex spp. (Hemiptera: Cimicidae).

    Science.gov (United States)

    Dang, Kai; Doggett, Stephen L; Veera Singham, G; Lee, Chow-Yang

    2017-06-29

    The worldwide resurgence of bed bugs [both Cimex lectularius L. and Cimex hemipterus (F.)] over the past two decades is believed in large part to be due to the development of insecticide resistance. The transcriptomic and genomic studies since 2010, as well as morphological, biochemical and behavioral studies, have helped insecticide resistance research on bed bugs. Multiple resistance mechanisms, including penetration resistance through thickening or remodelling of the cuticle, metabolic resistance by increased activities of detoxification enzymes (e.g. cytochrome P450 monooxygenases and esterases), and knockdown resistance by kdr mutations, have been experimentally identified as conferring insecticide resistance in bed bugs. Other candidate resistance mechanisms, including behavioral resistance, some types of physiological resistance (e.g. increasing activities of esterases by point mutations, glutathione S-transferase, target site insensitivity including altered AChEs, GABA receptor insensitivity and altered nAChRs), symbiont-mediated resistance and other potential, yet undiscovered mechanisms may exist. This article reviews recent studies of resistance mechanisms and the genes governing insecticide resistance, potential candidate resistance mechanisms, and methods of monitoring insecticide resistance in bed bugs. This article provides an insight into the knowledge essential for the development of both insecticide resistance management (IRM) and integrated pest management (IPM) strategies for successful bed bug management.

  3. Is acetylcholinesterase a biomarker of susceptibility in Daphnia magna (Crustacea, Cladocera) after deltamethrin exposure?

    Science.gov (United States)

    Toumi, Héla; Boumaiza, Moncef; Millet, Maurice; Radetski, Claudemir Marcos; Felten, Vincent; Férard, Jean François

    2015-02-01

    In the present study, we explored the possibility of using the acetylcholinesterase (AChE) as a biomarker after deltamethrin (pyrethroid insecticide) exposure with three strains of the cladoceran Daphnia magna. Four calculated time-weighted deltamethrin concentrations (20.1, 40.3, 80.6 and 161.3 ng L(-1)) were compared against control acetylcholinesterase activity. Our results showed that after 48 h of deltamethrin exposure, all treatments induced a significant decrease of AChE activities whatever the three considered strains. However, diverse responses were registered in terms of lowest observed effect concentrations (LOEC: 80.6 ng L(-1) for strain 1 and 20.1 ng L(-1) for strains 2 and 3) revealing differences in sensitivity among the three tested strains of D. magna. Our results suggest that after deltamethrin exposure, the AChE activity responses can be also used as a biomarker of susceptibility (i.e., variation of strain specific response). Moreover, our results show that strain 1 is the less sensitive in terms of IC50-48 h of AChE, whereas it became the most sensitive when considering the EC50-48 h estimated in the standard ecotoxicity test. Copyright © 2014 Elsevier Ltd. All rights reserved.

  4. THE ROLES OF DETOXIFYING ENZYMES AND AChE INSENSITIVITY IN METHAMIDOPHOS RESISTANCE DEVELOPMENT AND DECLINE IN NILAPARVATA LUGENS

    Institute of Scientific and Technical Information of China (English)

    Ze-wenLiu; Zhao-junHan; Ling-chunZhang

    2003-01-01

    Methamidophos resistance of brown planthopper (Nilaparvata lugens Stal, BPH) was selected in laboratory. After successive selection for 9 generations, the selection was ceased by rearing BPH without contact with any insecticide for 9 generations. In the full course, the successive changes of esterase activity, MFO activity, GSTs activity and AChE insensitivity were analyzed. The results showed that the change of esterase activity was high correlated with that of methamidophos in the full course, which indicated that esterase played very important role both in the resistance development and in the resistance decline. However, the change of AChE insensitivity only significantly correlated with that of resistance in the development stage, and the change of MFO activity or GSTs activity only significantly correlated with that of the resistance in the decline stage, which indicated the changes of AChE insensitivity, MFO activity or GSTs activity only played some roles in different stages of the resistance change.

  5. Botanical Insecticides in Plant Protection

    OpenAIRE

    Grdiša, Martina; Gršić, Kristina

    2013-01-01

    Botanical insecticides are natural compounds with insecticidal properties and their use in crop protection is as old as agricultural practice. Although they have been in use for over one hundred years, the advent of synthetic insecticides has unfortunately displaced their use today. Due to fast action, low cost, easy application and efficiency against a wide range of harmful species, synthetic insecticides have become an important part of pest management in modern agricultural systems....

  6. A simple radiometric in vitro assay for acetylcholinesterase inhibitors

    International Nuclear Information System (INIS)

    Guilarte, T.R.; Burns, H.D.; Dannals, R.F.; Wagner, H.N. Jr.

    1983-01-01

    A radiometric method for screening acetylcholinesterase inhibitors has been described. The method is based on the production of [ 14 C]carbon dioxide from the hydrolysis of acetylcholine. The inhibitory concentration at 50% (IC50) values for several known acetylcholinesterase inhibitors were in agreement with literature values. The new radiometric method is simple, inexpensive, and has the potential for automation

  7. Acetylcholinesterase Inhibitory and Antioxidant Properties of Euphorbiacharacias Latex

    Directory of Open Access Journals (Sweden)

    Francesca Pintus

    2013-03-01

    Full Text Available The aim of the present study was to evaluate the acetylcholinesterase inhibitory capacity and the antioxidant properties of extracts of Euphorbia characias latex, a Mediterranean shrub. We performed a new extraction method involving the use of the trichloroacetic acid. The extract showed high antioxidant activity, was rich in total polyphenolic and flavonoid content and exhibited substantial inhibition of acetylcholinesterase activity.

  8. Acetyl-cholinesterase Enzyme Inhibitory Effect of Calophyllum species

    African Journals Online (AJOL)

    Purpose: To search for new acetylcholinesterase enzyme inhibitors from Calopyllum species. Methods: Six stem bark extracts of Calophyllum inophyllum, C. soulattri, C. teysmannii, C. lowii, C. benjaminum and C. javanicum were subjected to anti-cholinesterase analysis against acetylcholinesterase (AChE) enzyme using ...

  9. Evaluative Conditioning is Insensitive to Blocking

    Directory of Open Access Journals (Sweden)

    Tom Beckers

    2009-01-01

    Full Text Available Evaluative conditioning has been claimed to have a number of functional characteristics that set it apart from other forms of associative learning in humans, such as insensitivity to extinction and contingency, independence of contingency awareness, and insensitivity to modulation. Despite its potential theoretical importance, until now few data are available concerning the susceptibility of evaluative conditioning to cue competition effects such as blocking. In the present study, we assessed the susceptibility of acquired preferences and evaluations to blocking in a candy game. Results suggest that evaluative conditioning is not susceptible to blocking. We discuss this observation in the light of theoretical accounts of evaluative conditioning and associative learning in humans.

  10. Monitoring the operational impact of insecticide usage for malaria control on Anopheles funestus from Mozambique

    Directory of Open Access Journals (Sweden)

    Sharp Brian L

    2007-10-01

    Full Text Available Abstract Background Indoor residual spraying (IRS has again become popular for malaria control in Africa. This combined with the affirmation by WHO that DDT is appropriate for use in the absence of longer lasting insecticide formulations in some malaria endemic settings, has resulted in an increase in IRS with DDT as a major malaria vector control intervention in Africa. DDT was re-introduced into Mozambique's IRS programme in 2005 and is increasingly becoming the main insecticide used for malaria vector control in Mozambique. The selection of DDT as the insecticide of choice in Mozambique is evidence-based, taking account of the susceptibility of Anopheles funestus to all available insecticide choices, as well as operational costs of spraying. Previously lambda cyhalothrin had replaced DDT in Mozambique in 1993. However, resistance appeared quickly to this insecticide and, in 2000, the pyrethroid was phased out and the carbamate bendiocarb introduced. Low level resistance was detected by biochemical assay to bendiocarb in 1999 in both An. funestus and Anopheles arabiensis, although this was not evident in WHO bioassays of the same population. Methods Sentinel sites were established and monitored for insecticide resistance using WHO bioassays. These assays were conducted on 1–3 day old F1 offspring of field collected adult caught An. funestus females to determine levels of insecticide resistance in the malaria vector population. WHO biochemical assays were carried out to determine the frequency of insecticide resistance genes within the same population. Results In surveys conducted between 2002 and 2006, low levels of bendiocarb resistance were detected in An. funestus, populations using WHO bioassays. This is probably due to significantly elevated levels of Acetylcholinesterase levels found in the same populations. Pyrethroid resistance was also detected in populations and linked to elevated levels of p450 monooxygenase activity. One site had

  11. Developmental neurotoxicity of the organophosphorus insecticide chlorpyrifos: from clinical findings to preclinical models and potential mechanisms.

    Science.gov (United States)

    Burke, Richard D; Todd, Spencer W; Lumsden, Eric; Mullins, Roger J; Mamczarz, Jacek; Fawcett, William P; Gullapalli, Rao P; Randall, William R; Pereira, Edna F R; Albuquerque, Edson X

    2017-08-01

    Organophosphorus (OP) insecticides are pest-control agents heavily used worldwide. Unfortunately, they are also well known for the toxic effects that they can trigger in humans. Clinical manifestations of an acute exposure of humans to OP insecticides include a well-defined cholinergic crisis that develops as a result of the irreversible inhibition of acetylcholinesterase (AChE), the enzyme that hydrolyzes the neurotransmitter acetylcholine (ACh). Prolonged exposures to levels of OP insecticides that are insufficient to trigger signs of acute intoxication, which are hereafter referred to as subacute exposures, have also been associated with neurological deficits. In particular, epidemiological studies have reported statistically significant correlations between prenatal subacute exposures to OP insecticides, including chlorpyrifos, and neurological deficits that range from cognitive impairments to tremors in childhood. The primary objectives of this article are: (i) to address the short- and long-term neurological issues that have been associated with acute and subacute exposures of humans to OP insecticides, especially early in life (ii) to discuss the translational relevance of animal models of developmental exposure to OP insecticides, and (iii) to review mechanisms that are likely to contribute to the developmental neurotoxicity of OP insecticides. Most of the discussion will be focused on chlorpyrifos, the top-selling OP insecticide in the United States and throughout the world. These points are critical for the identification and development of safe and effective interventions to counter and/or prevent the neurotoxic effects of these chemicals in the developing brain. This is an article for the special issue XVth International Symposium on Cholinergic Mechanisms. © 2017 International Society for Neurochemistry.

  12. Structural characterization of acetylcholinesterase 1 from the sand fly Lutzomyia longipalpis (Diptera: Psychodidae).

    Science.gov (United States)

    Coutinho-Abreu, I V; Balbino, V Q; Valenzuela, J G; Sonoda, I V; Ramalho-Ortigão, J M

    2007-07-01

    Acetylcholinesterase (AChE) plays a key role in cholinergic impulse transmission, and it is the target enzyme for organophosphorus and carbamate insecticides. Two genes, AceI and AceII, have been characterized from different insect species, and point mutations in either gene can lead to significant resistance to these classes of insecticides. In this report, we describe the partial characterization of the AceI gene from Lutzomyia longipalpis (Lutz & Neiva) (Diptera: Psychodidae), and we show that the possibility exists for the development of a resistant phenotype to organophosphates and carbamates in sand flies. Our results point to the presence of a single AceI gene in L. longipalpis (LlAce1) and that AChE activity is inhibited by organophosphorus at a concentration of 5 x 10(-5) M. Regarding insecticide resistance, analysis of the truncated LlAce1 cDNA suggests that a single missense mutation leading to a glycine-to-serine substitution at amino acid position 119 (G119S) may arise in L. longipalpis, similar to what has been detected in Anopheles gambiae s.s. Another missense mutation involved in resistant phenotypes, F331W, detected in Culex tritaeniorhynchus Giles, is less likely to occur in L. longipalpis, because it faces codon constraint in this sand fly species. Comparison of the three-dimensional structures of the deduced amino acid sequence of the truncated LLAChE1 with that of An. gambiae and Cx. tritaeniorhynchus also suggests that similar structural modifications due to the missense amino acid changes in the active site gorge are detected in all three insects.

  13. Neurological symptoms among Sri Lankan farmers occupationally exposed to acetylcholinesterase-inhibiting insecticides

    NARCIS (Netherlands)

    Smit, L.A.M.; Wendel- de Joode, B.N. van; Heederik, D.; Peiris-John, R.J.; Hoek, W. van der

    2003-01-01

    Background: In many agricultural districts in Sri Lanka, pesticide poisoning is a leading cause of death. This study aims to evaluate the impact of pesticide use on Sri Lankan farmers' health. Methods: A total of 260 subjects were surveyed in both a low and a high exposure period.

  14. Biochemical Markers for Exposure to Low Doses of Organophosphorus Insecticides

    National Research Council Canada - National Science Library

    Lockridge, Oksana

    2003-01-01

    Though acetylcholinesterase is the primary target of organophosphorus toxicants, our finding that acetylcholinesterase knockout mice are supersensitive to the lethal effects of VX, DFP, chlorpyrifos...

  15. Biochemical Markers for Exposure to Low Doses of Organophosphorus Insecticides

    National Research Council Canada - National Science Library

    Lockridge, Oksana

    2004-01-01

    Though acetylcholinesterase is the primary target of organophosphorus toxicants, our finding that acetylcholinesterase knockout mice are supersensitive to the lethal effects of VX, DFP, chlorpyrifos...

  16. New Acetylcholinesterase Inhibitors for Alzheimer's Disease

    Directory of Open Access Journals (Sweden)

    Mona Mehta

    2012-01-01

    Full Text Available Acetylcholinesterase (AChE remains a highly viable target for the symptomatic improvement in Alzheimer's disease (AD because cholinergic deficit is a consistent and early finding in AD. The treatment approach of inhibiting peripheral AchE for myasthenia gravis had effectively proven that AchE inhibition was a reachable therapeutic target. Subsequently tacrine, donepezil, rivastigmine, and galantamine were developed and approved for the symptomatic treatment of AD. Since then, multiple cholinesterase inhibitors (ChEI continue to be developed. These include newer ChEIs, naturally derived ChEIs, hybrids, and synthetic analogues. In this paper, we summarize the different types of ChEIs in development and their respective mechanisms of actions. This pharmacological approach continues to be active with many promising compounds.

  17. Photonic crystal based polarization insensitive flat lens

    International Nuclear Information System (INIS)

    Turduev, M; Bor, E; Kurt, H

    2017-01-01

    The paper proposes a new design of an inhomogeneous artificially created photonic crystal lens structure consisting of annular dielectric rods to efficiently focus both transverse electric and transverse magnetic polarizations of light into the same focal point. The locations of each individual cell that contains the annular dielectric rods are determined according to a nonlinear distribution function. The inner and outer radii of the annular photonic dielectric rods are optimized with respect to the polarization insensitive frequency response of the transmission spectrum of the lens structure. The physical background of the polarization insensitive focusing mechanism is investigated in both spatial and frequency domains. Moreover, polarization independent wavefront transformation/focusing has been explored in detail by investigating the dispersion relation of the structure. Corresponding phase index distribution of the lens is attained for polarization insensitive normalized frequency range of a / λ   =  0.280 and a / λ   =  0.300, where a denotes the lattice constant of the designed structure and λ denotes the wavelength of the incident light. We show the wave transformation performance and focal point movement dynamics for both polarizations of the lens structure by specially adjusting the length of the structure. The 3D finite-difference time domain numerical analysis is also performed to verifiy that the proposed design is able to focus the wave regardless of polarization into approximately the same focal point (difference between focal distances of both polarizations stays below 0.25 λ ) with an operating bandwidth of 4.30% between 1476 nm and 1541 nm at telecom wavelengths. The main superiorities of the proposed lens structure are being all dielectric and compact, and having flat front and back surfaces, rendering the proposed lens design more practical in the photonic integration process in various applications such as optical switch

  18. Growth hormone insensitivity syndrome: A sensitive approach

    Directory of Open Access Journals (Sweden)

    Soumik Goswami

    2012-01-01

    Full Text Available Patients with Growth Hormone Insensitivity have characteristic phenotypic features and severe short stature. The underlying basis are mutations in the growth hormone receptor gene which gives rise to a characteristic hormonal profile. Although a scoring system has been devised for the diagnosis of this disorder, it has not been indisputably validated. The massive expense incurred in the diagnosis and treatment of this condition with suboptimal therapeutic response necessitates a judicious approach in this regard in our country.

  19. A short history of insecticides

    Directory of Open Access Journals (Sweden)

    Oberemok Volodymyr Volodymyrovych

    2015-07-01

    Full Text Available This review contains a brief history of the use of insecticides. The peculiarities, main advantages, and disadvantages of some modern insecticides are described. The names of the discoverers of some of the most popular insecticide preparations on the world market, are listed. The tendencies to find new insecticides to control the quantity of phytophagous insects are discussed. Special attention is paid to the perspective of creating preparations based on nucleic acids, in particular DNA insecticides. The use of insect-specific, short single-stranded DNA fragments as DNA insecticides, is paving the way in the field of “intellectual” insecticides that “think” before they act. It is worth noting, though, that in the near future, the quantity of produced insecticides will increase due to the challenges associated with food production for a rapidly growing population. It is concluded, that an agreeable interaction of scientists and manufacturers of insecticides should lead to the selection of the most optimal solutions for insect pest control, which would be safe, affordable, and effective at the same time.

  20. Changes in acetylcholinesterase activities in the developing and ...

    African Journals Online (AJOL)

    Changes in acetylcholinesterase activities in the developing and aging pig brain and hypophyses. ... International Journal of Agriculture and Rural Development. Journal Home · ABOUT ... Open Access DOWNLOAD FULL TEXT Subscription ...

  1. Insecticidal and Repellent Activit ies of Laurinterol from the Okinawan Red Alga Laurencia nidifica

    Directory of Open Access Journals (Sweden)

    Takahiro Ishii

    2017-01-01

    Full Text Available An ethyl acetate (EtOAc extract of Laurencia nidifica was found to have toxic effect against brine shrimp larvae (Artemia salina. Bioassay-guided fractionation of the EtOAc extract resulted in the isolation of four known halogenated sesquiterpenes, laurinterol (1, isolaurinterol (2, aplysin (3, and a -bromocuparene (4. Their structures were established on the basis of spectral analysis and comparison with literature data. Among isolated compounds, only laurinterol showed strong toxicity against A. salina. Further experiments revealed that laurinterol also exhibited repellent activity against the maize weevil Sitophilus zeamais , insecticidal activity against the termite Reticulitermes speratus, and acetylcholinesterase (AChE inhibitory effect . This is the first report of insecticidal and repellent activities of laurinterol.

  2. Two Step Synthesis of a Non-symmetric Acetylcholinesterase Reactivator

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    Vit Koleckar

    2007-08-01

    Full Text Available The newly developed and very promising acetylcholinesterase reactivator (E-1- (2-hydroxyiminomethylpyridinium-4-(4-hydroxyiminomethylpyridinium-but-2-ene dibromide was prepared using two different pathways via a two-step synthesis involving the appropriate (E-1-(4-bromobut-2-enyl-2- or 4-hydroxyiminomethyl-pyridinium bromides. Afterwards, purities and yields of the desired product prepared by both routes were compared. Finally, its potency to reactivate several nerve agent-inhibited acetylcholinesterases was tested.

  3. Spiroindolines identify the vesicular acetylcholine transporter as a novel target for insecticide action.

    Directory of Open Access Journals (Sweden)

    Ann Sluder

    Full Text Available The efficacy of all major insecticide classes continues to be eroded by the development of resistance mediated, in part, by selection of alleles encoding insecticide insensitive target proteins. The discovery of new insecticide classes acting at novel protein binding sites is therefore important for the continued protection of the food supply from insect predators, and of human and animal health from insect borne disease. Here we describe a novel class of insecticides (Spiroindolines encompassing molecules that combine excellent activity against major agricultural pest species with low mammalian toxicity. We confidently assign the vesicular acetylcholine transporter as the molecular target of Spiroindolines through the combination of molecular genetics in model organisms with a pharmacological approach in insect tissues. The vesicular acetylcholine transporter can now be added to the list of validated insecticide targets in the acetylcholine signalling pathway and we anticipate that this will lead to the discovery of novel molecules useful in sustaining agriculture. In addition to their potential as insecticides and nematocides, Spiroindolines represent the only other class of chemical ligands for the vesicular acetylcholine transporter since those based on the discovery of vesamicol over 40 years ago, and as such, have potential to provide more selective tools for PET imaging in the diagnosis of neurodegenerative disease. They also provide novel biochemical tools for studies of the function of this protein family.

  4. Identification and Biochemical Properties of Two New Acetylcholinesterases in the Pond Wolf Spider (Pardosa pseudoannulata.

    Directory of Open Access Journals (Sweden)

    Xiangkun Meng

    Full Text Available Acetylcholinesterase (AChE, an important neurotransmitter hydrolase in both invertebrates and vertebrates, is targeted by organophosphorus and carbamate insecticides. In this study, two new AChEs were identified in the pond wolf spider Pardosa pseudoannulata, an important predatory natural enemy of several insect pests. In total, four AChEs were found in P. pseudoannulata (including two AChEs previously identified in our laboratory. The new putative AChEs PpAChE3 and PpAChE4 contain most of the common features of the AChE family, including cysteine residues, choline binding sites, the conserved sequence 'FGESAG' and conserved aromatic residues but with a catalytic triad of 'SDH' rather than 'SEH'. Recombinant enzymes expressed in Sf9 cells showed significant differences in biochemical properties compared to other AChEs, such as the optimal pH, substrate specificity, and catalytic efficiency. Among three test substrates, PpAChE1, PpAChE3 and PpAChE4 showed the highest catalytic efficiency (Vmax/KM for ATC (acetylthiocholine iodide, with PpAChE3 exhibiting a clear preference for ATC based on the VmaxATC/VmaxBTC ratio. In addition, the four PpAChEs were more sensitive to the AChE-specific inhibitor BW284C51, which acts against ATC hydrolysis, than to the BChE-specific inhibitor ISO-OMPA, which acts against BTC hydrolysis, with at least a 8.5-fold difference in IC50 values for each PpAChE. PpAChE3, PpAChE4, and PpAChE1 were more sensitive than PpAChE2 to the tested Carb insecticides, and PpAChE3 was more sensitive than the other three AChEs to the tested OP insecticides. Based on all the results, two new functional AChEs were identified from P. pseudoannulata. The differences in AChE sequence between this spider and insects enrich our knowledge of invertebrate AChE diversity, and our findings will be helpful for understanding the selectivity of insecticides between insects and natural enemy spiders.

  5. Complete Androgen Insensitivity Syndrome in Three Sisters

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    Levent Verim

    2014-01-01

    Full Text Available Disorders of sexual development (DSD are congenital anomalies due to atypical development of chromosomes, gonads and anatomy. Complete androgen insensitivity syndrome (CAIS, also known as testicular feminization (TF is a rare DSD disease. The majority of CAIS patients apply to hospital with the complaint of primary amenorrhea or infertility. Given that CAIS patients are all phenotypically female while having 46, XY karyotypes, CAIS diagnosis should be disclosed in an age-appropriate manner preferably by a mental health professional. Cases are reported here for three 46XY siblings consistent with CAIS.

  6. Acetylcholinesterase immobilized capillary reactors coupled to protein coated magnetic beads: A new tool for plant extract ligand screening

    Science.gov (United States)

    Vanzolini, Kenia Lourenço; Jiang, Zhengjin; Zhang, Xiaoqi; Vieira, Lucas Campos Curcino; Corrêa, Arlene Gonçalvez; Cardoso, Carmen Lucia; Cass, Quezia Bezerra; Moaddel, Ruin

    2013-01-01

    The use of immobilized capillary enzyme reactors (ICERs) and enzymes coated to magnetic beads ((NT or CT)-MB) for ligand screening has been adopted as a new technique of high throughput screening (HTS). In this work the selected target was the enzyme acetylcholinesterase (AChE), which acts on the central nervous system and is a validated target for the treatment of Alzheimer’s disease, as well as for new insecticides. A new approach for the screening of plant extracts was developed based on the ligand fishing experiments and zonal chromatography. For that, the magnetic beads were used for the ligand fishing experiments and capillary bioreactors for the activity assays. The latter was employed also under non-linear conditions to determine the affinity constants of known ligands, for the first time, as well as for the active fished ligand. PMID:24148457

  7. In silico development of new acetylcholinesterase inhibitors.

    Science.gov (United States)

    Pascoini, A L; Federico, L B; Arêas, A L F; Verde, B A; Freitas, P G; Camps, I

    2018-04-19

    In this work, we made use of fragment-based drug design (FBDD) and de novo design to obtain more powerful acetylcholinesterase (AChE) inhibitors. AChE is associated with Alzheimer's disease (AD). It was found that the cholinergic pathways in the cerebral cortex are compromised in AD and the accompanying cholinergic deficiency contributes to the cognitive deterioration of AD patients. In the FBDD approach, fragments are docked into the active site of the protein. As fragments are molecular groups with a low number of atoms, it is possible to study their interaction with localized amino acids. Once the interactions are measured, the fragments are organized by affinity and then linked together to form new molecules with a high degree of interaction with the active site. In the other approach, we used the de novo design technique starting from reference drugs used in the AD treatment. These drugs were broken into fragments (seeds). In the growing strategy, fragments were added to each seed, growing new molecules. In the linking strategy, two or more separated seeds were linked with different fragments. Both strategies combined produced a library of more than 2 million compounds. This library was filtered using absorption, distribution, metabolism, and excretion properties. The resulting library with around six thousand compounds was filtered again. In this case, structures with Tanimoto coefficients >.85 were discarded. The final library with 1500 compounds was submitted to docking studies. As a result, 10 compounds with better interaction energy than the reference drugs were obtained.

  8. Natural sesquiterpen lactones as acetylcholinesterase inhibitors

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    HOMA HAJIMEHDIPOOR

    2014-06-01

    Full Text Available Background and the purpose of the study: The amount of elder people who suffer from Alzheimer disease is continuously increasing every year. Cholinesterase inhibitors have shown to be effective in alleviating the symptoms of the disease, thus opening a field of research for these treatments. Herbal products, owning a reputation as effective agents in many biological studies are now drawing attention for inhibiting acetylcholinesterase, in other words, Alzheimer disease. In the present study, the ability of three sesquiterpene lactones from Inula oculus-christi and I. aucheriana to inhibit AChE has been evaluated through Ellman assay.Materials and Methods: Gaillardin and pulchellin C were obtained from I. oculus-christi and britannin from I. aucheriana by chromatographic methods. They were dissolved in methanol in concentration of 3 mg/mL and the AChEI activity of the compounds was determined by Ellman method using Acethylthiocholine iodide as the substrate and 5, 5′-dithiobis-2-nitrobenzoic acid as the reagent, in 96-well plates at 405 nm.Results: AChEI activity of the examined compounds was obtained as 67.0, 25.2 and 10.9% in concentration of 300 µg/L for gaillardin, britannin and pulchellin C, respectively.Conclusion: Among the three sesquiterpene lactones, gaillardin with 67% inhibition of AChE could be considered a good candidate for future Alzheimer studies.

  9. SERUM ACETYLCHOLINESTERASE LEVEL IN THE PATIENTS OF OPIOID (BROWN SUGAR) DEPENDENCE

    OpenAIRE

    Shah, Nilesh; Dave, Kirti

    1992-01-01

    The authors compared the serum acetylcholinesterase level in the patients of brown sugar dependence and the normal volunteers. Significantly lower level of serum acetylcholinesterase was found in patients of brown sugar dependence.

  10. Partial Androgen Insensitivity Syndrome Presenting with Gynecomastia

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    Sung Won Lee

    2015-06-01

    Full Text Available Gynecomastia is a benign enlargement of the male breast caused by the proliferation of glandular breast tissue. Determining the various causes of gynecomastia such as physiological causes, drugs, systemic diseases, and endocrine disorders is important. Androgen insensitivity syndrome (AIS is a rare endocrine disorder presenting with gynecomastia and is a disorder of male sexual differentiation caused by mutations within the androgen receptor gene. All individuals with AIS have the 46 XY karyotype, although AIS phenotypes can be classified as mild, partial or complete and can differ among both males and females including ambiguous genitalia or infertility in males. We experienced a case of partial AIS presenting with gynecomastia and identified the androgen receptor gene mutation.

  11. Androgen insensitivity syndrome: gonadal androgen receptor activity

    International Nuclear Information System (INIS)

    Coulam, C.B.; Graham, M.L.; Spelsberg, T.C.

    1984-01-01

    To determine whether abnormalities of the androgen receptor previously observed in skin fibroblasts from patients with androgen insensitivity syndrome also occur in the gonads of affected individuals, androgen receptor activity in the gonads of a patient with testicular feminization syndrome was investigated. Using conditions for optimal recovery of androgen receptor from human testes established by previous studies, we detected the presence of a high-affinity (dissociation constant . 3.2 X 10(-10) mol/L), low-capacity (4.2 X 10(-12) mol/mg DNA), androgen-binding protein when tritium-labeled R1881 was incubated at 4 degrees C with nuclear extracts from the gonads of control patients or from a patient with testicular feminization syndrome but not when incubated at 37 degrees C. Thus this patient has an androgen receptor with a temperature lability similar to that of receptors from normal persons

  12. Altered levels of acetylcholinesterase in Alzheimer plasma.

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    María-Salud García-Ayllón

    Full Text Available BACKGROUND: Many studies have been conducted in an extensive effort to identify alterations in blood cholinesterase levels as a consequence of disease, including the analysis of acetylcholinesterase (AChE in plasma. Conventional assays using selective cholinesterase inhibitors have not been particularly successful as excess amounts of butyrylcholinesterase (BuChE pose a major problem. PRINCIPAL FINDINGS: Here we have estimated the levels of AChE activity in human plasma by first immunoprecipitating BuChE and measuring AChE activity in the immunodepleted plasma. Human plasma AChE activity levels were approximately 20 nmol/min/mL, about 160 times lower than BuChE. The majority of AChE species are the light G(1+G(2 forms and not G(4 tetramers. The levels and pattern of the molecular forms are similar to that observed in individuals with silent BuChE. We have also compared plasma AChE with the enzyme pattern obtained from human liver, red blood cells, cerebrospinal fluid (CSF and brain, by sedimentation analysis, Western blotting and lectin-binding analysis. Finally, a selective increase of AChE activity was detected in plasma from Alzheimer's disease (AD patients compared to age and gender-matched controls. This increase correlates with an increase in the G(1+G(2 forms, the subset of AChE species which are increased in Alzheimer's brain. Western blot analysis demonstrated that a 78 kDa immunoreactive AChE protein band was also increased in Alzheimer's plasma, attributed in part to AChE-T subunits common in brain and CSF. CONCLUSION: Plasma AChE might have potential as an indicator of disease progress and prognosis in AD and warrants further investigation.

  13. Characterization of acetylcholinesterase-inhibition by itopride.

    Science.gov (United States)

    Iwanaga, Y; Kimura, T; Miyashita, N; Morikawa, K; Nagata, O; Itoh, Z; Kondo, Y

    1994-11-01

    Itopride is a gastroprokinetic benzamide derivative. This agent inhibited both electric eel acetylcholinesterase (AChE) and horse serum butyrylcholinesterase (BuChE). The IC50 of itopride with AChE (2.04 +/- 0.27 microM) was, however, 100-fold less than that with BuChE, whereas in the case of neostigmine with AChE (11.3 +/- 3.4 nM), it was 10-fold less. The recovery of AChE activity inhibited by 10(-7) M neostigmine was partial, but that inhibited by up to 3 x 10(-5) M itopride was complete when the reaction mixture was subjected to ultrafiltration. Double reciprocal plots of the experimental data showed that both Km and Vmax were affected by itopride, suggesting that the inhibition is a "mixed" type, although primarily being an uncompetitive one. The inhibitory effect of itopride on cholinesterase (ChE) activity in guinea pig gastrointestine was much weaker than that on pure AChE. However, in the presence of a low dose of diisopropyl fluorophosphate, just enough to inhibit BuChE but not AChE, the IC50s of itopride against ChE activities were found to be about 0.5 microM. In conclusion, itopride exerts reversible and a "mixed" type of inhibition preferably against AChE. The IC50 of itopride for electric eel and guinea pig gastrointestinal AChE inhibition was 200 times and 50 times as large as that of neostigmine, respectively.

  14. Caffeine Inhibits Acetylcholinesterase, But Not Butyrylcholinesterase

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    Petr Dobes

    2013-05-01

    Full Text Available Caffeine is an alkaloid with a stimulant effect in the body. It can interfere in transmissions based on acetylcholine, epinephrine, norepinephrine, serotonin, dopamine and glutamate. Clinical studies indicate that it can be involved in the slowing of Alzheimer disease pathology and some other effects. The effects are not well understood. In the present work, we focused on the question whether caffeine can inhibit acetylcholinesterase (AChE and/or, butyrylcholinesterase (BChE, the two enzymes participating in cholinergic neurotransmission. A standard Ellman test with human AChE and BChE was done for altering concentrations of caffeine. The test was supported by an in silico examination as well. Donepezil and tacrine were used as standards. In compliance with Dixon’s plot, caffeine was proved to be a non-competitive inhibitor of AChE and BChE. However, inhibition of BChE was quite weak, as the inhibition constant, Ki, was 13.9 ± 7.4 mol/L. Inhibition of AChE was more relevant, as Ki was found to be 175 ± 9 µmol/L. The predicted free energy of binding was −6.7 kcal/mol. The proposed binding orientation of caffeine can interact with Trp86, and it can be stabilize by Tyr337 in comparison to the smaller Ala328 in the case of human BChE; thus, it can explain the lower binding affinity of caffeine for BChE with reference to AChE. The biological relevance of the findings is discussed.

  15. Pralidoxime in acute organophosphorus insecticide poisoning--a randomised controlled trial.

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    Michael Eddleston

    2009-06-01

    Full Text Available Poisoning with organophosphorus (OP insecticides is a major global public health problem, causing an estimated 200,000 deaths each year. Although the World Health Organization recommends use of pralidoxime, this antidote's effectiveness remains unclear. We aimed to determine whether the addition of pralidoxime chloride to atropine and supportive care offers benefit.We performed a double-blind randomised placebo-controlled trial of pralidoxime chloride (2 g loading dose over 20 min, followed by a constant infusion of 0.5 g/h for up to 7 d versus saline in patients with organophosphorus insecticide self-poisoning. Mortality was the primary outcome; secondary outcomes included intubation, duration of intubation, and time to death. We measured baseline markers of exposure and pharmacodynamic markers of response to aid interpretation of clinical outcomes. Two hundred thirty-five patients were randomised to receive pralidoxime (121 or saline placebo (114. Pralidoxime produced substantial and moderate red cell acetylcholinesterase reactivation in patients poisoned by diethyl and dimethyl compounds, respectively. Mortality was nonsignificantly higher in patients receiving pralidoxime: 30/121 (24.8% receiving pralidoxime died, compared with 18/114 (15.8% receiving placebo (adjusted hazard ratio [HR] 1.69, 95% confidence interval [CI] 0.88-3.26, p = 0.12. Incorporating the baseline amount of acetylcholinesterase already aged and plasma OP concentration into the analysis increased the HR for patients receiving pralidoxime compared to placebo, further decreasing the likelihood that pralidoxime is beneficial. The need for intubation was similar in both groups (pralidoxime 26/121 [21.5%], placebo 24/114 [21.1%], adjusted HR 1.27 [95% CI 0.71-2.29]. To reduce confounding due to ingestion of different insecticides, we further analysed patients with confirmed chlorpyrifos or dimethoate poisoning alone, finding no evidence of benefit.Despite clear reactivation of

  16. Neurotoxicology of insecticides and pheromones

    National Research Council Canada - National Science Library

    Narahashi, Toshio

    1979-01-01

    The purpose of this symposium was to provide a forum where a variety of scientists who were interested in the interactions of insecticides and pheromones with the nervous system got together to exchange their views...

  17. A renaissance for botanical insecticides?

    Science.gov (United States)

    Isman, Murray B

    2015-12-01

    Botanical insecticides continue to be a subject of keen interest among the international research community, reflected in the steady growth in scientific publications devoted to the subject. Until very recently though, the translation of that theory to practice, i.e. the commercialisation and adoption of new botanical insecticides in the marketplace, has seriously lagged behind. Strict regulatory regimes, long the bane of small pesticide producers, are beginning to relax some of the data requirements for 'low-risk' pesticide products, facilitating movement of more botanicals into the commercial arena. In this paper I discuss some of the jurisdictions where botanicals are increasingly finding favour, some of the newer botanical insecticides in the plant and animal health arsenal and some of the specific sectors where botanicals are most likely to compete effectively with other types of insecticidal product. © 2015 Society of Chemical Industry.

  18. An Acetylcholinesterase-Based Chronoamperometric Biosensor for Fast and Reliable Assay of Nerve Agents

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    Rene Kizek

    2013-08-01

    Full Text Available The enzyme acetylcholinesterase (AChE is an important part of cholinergic nervous system, where it stops neurotransmission by hydrolysis of the neurotransmitter acetylcholine. It is sensitive to inhibition by organophosphate and carbamate insecticides, some Alzheimer disease drugs, secondary metabolites such as aflatoxins and nerve agents used in chemical warfare. When immobilized on a sensor (physico-chemical transducer, it can be used for assay of these inhibitors. In the experiments described herein, an AChE- based electrochemical biosensor using screen printed electrode systems was prepared. The biosensor was used for assay of nerve agents such as sarin, soman, tabun and VX. The limits of detection achieved in a measuring protocol lasting ten minutes were 7.41 × 10−12 mol/L for sarin, 6.31 × 10−12 mol /L for soman, 6.17 × 10−11 mol/L for tabun, and 2.19 × 10−11 mol/L for VX, respectively. The assay was reliable, with minor interferences caused by the organic solvents ethanol, methanol, isopropanol and acetonitrile. Isopropanol was chosen as suitable medium for processing lipophilic samples.

  19. Toxicity of azodrin on the morphology and acetylcholinesterase activity of the earthworm Eisenia foetida

    International Nuclear Information System (INIS)

    Rao, J.V.; Kavitha, P.

    2004-01-01

    The acute toxicity of azodrin (monocrotophos, an organophosphorus insecticide) was determined on a soil organism, Eisenia foetida. The median lethal concentrations (LC 50 ) were derived from a 48-h paper contact test and from artificial soil tests. The LC 50 of azodrin in the paper contact test was 0.46±0.1 μg cm -2 (23±6 mg L -1 ) and those in the 7- and 14-day artificial soil tests were 171±21 and 132±20 mg kg -1 , respectively. The neurotoxic potentiality of azodrin was assessed by using a marker enzyme, acetylcholinesterase (AChE; EC 3.1.1.7) in both in vitro and in vivo experiments. The progressive signs of morphological destruction are correlated with percentage inhibition of AChE in the in vivo experiments. The kinetics of AChE activity in the presence and absence of azodrin indicated that the toxicant is competitive in nature. This study demonstrated that azodrin causes concentration-dependent changes in the morphology and AChE activity of the earthworm E. foetida

  20. Motion-insensitive rapid configuration relaxometry.

    Science.gov (United States)

    Nguyen, Damien; Bieri, Oliver

    2017-08-01

    Triple echo steady state (TESS) uses the lowest steady state configuration modes for rapid relaxometry. Due to its unbalanced gradient scheme, however, TESS is inherently motion-sensitive. The purpose of this work is to merge TESS with a balanced acquisition scheme for motion-insensitive rapid configuration relaxometry, termed MIRACLE. The lowest order steady state free precession (SSFP) configurations are retrieved by Fourier transformation of the frequency response of N frequency-shifted balanced SSFP (bSSFP) scans and subsequently processed for relaxometry, as proposed with TESS. Accuracy of MIRACLE is evaluated from simulations, phantom studies as well as in vivo brain and cartilage imaging at 3T. Simulations and phantom results revealed no conceptual flaw, and artifact-free configuration imaging was achieved in vivo. Overall, relaxometry results were accurate in phantoms and in good agreement for cartilage and for T2 in the brain, but apparent low T1 values were observed for brain white matter; reflecting asymmetries in the bSSFP profile. Rapid T1 and T2 mapping with MIRACLE offers analogous properties as TESS while successfully mitigating its motion-sensitivity. As a result of the Fourier transformation, relaxometry becomes sensitive to the voxel frequency distribution, which may contain useful physiologic information, such as structural brain integrity. © 2016 International Society for Magnetic Resonance in Medicine. Magn Reson Med 78:518-526, 2017. © 2016 International Society for Magnetic Resonance in Medicine. © 2016 International Society for Magnetic Resonance in Medicine.

  1. Amino acid substitutions and intron polymorphism of acetylcholinesterase1 associated with mevinphos resistance in diamondback moth, Plutella xylostella (L.).

    Science.gov (United States)

    Yeh, Shih-Chia; Lin, Chia-Li; Chang, Cheng; Feng, Hai-Tung; Dai, Shu-Mei

    2014-06-01

    The diamondback moth, Plutella xylostella L., is the most destructive insect pest of Brassica crops in the world. It has developed resistance rapidly to almost every insecticide used for its control. Mevinphos, a fast degrading and slow resistance evocating organophosphorus insecticide, has been recommended for controlling P. xylostella in Taiwan for more than 40years. SHM strain of P. xylostella, with ca. 22-fold resistance to this chemical, has been established from a field SH strain by selecting with mevinphos since 1997. Three mutations, i.e., G892T, G971C, and T1156T/G leading to A298S, G324A, and F386F/V amino acid substitutions in acetylcholinesterase1 (AChE1), were identified in these two strains; along with three haplotype pairs and a polymorphic intron in AChE1 gene (ace1). Two genetically pure lines, i.e., an SHggt wild type with intron AS and an SHMTCN mutant carrying G892T, G971C, T1156T/G mutations and intron AR in ace1, were established by single pair mating and haplotype determination. The F1 of SHMTCN strain had 52-fold resistance to mevinphos in comparison with the F1 of SHggt strain. In addition, AChE1 of this SHMTCN population, which exhibited lower maximum velocity (Vmax) and affinity (Km), was less susceptible to the inhibition of mevinphos, with an I50 32-fold higher than that of the SHggt F1 population. These results imply that amino acid substitutions in AChE1 of SHMTCN strain are associated with mevinphos resistance in this insect pest, and this finding is important for insecticide resistance management of P. xylostella in the field. Copyright © 2014 Elsevier Inc. All rights reserved.

  2. Organophosphorus insecticides: Toxic effects and bioanalytical tests for evaluating toxicity during degradation processes

    Directory of Open Access Journals (Sweden)

    Čolović Mirjana B.

    2013-01-01

    Full Text Available Organophosphorus insecticides have been the most applied group of insecticides for the last two decades. Their main toxic effects are related to irreversible inactivation of acetylcholinesterase (AChE. Actually, they covalently bind to serine OH group in the enzyme active site forming phosphorylated enzyme that cannot hydrolyze acetylcholine. Organophosphorus insecticides in the environment undergo the natural degradation pathway including mainly homogeneous and heterogeneous hydrolysis (especially at high pH generating non-inhibiting products. Additionally, thio organophosphates are easily oxidized by naturally present oxidants and UV light, forming more toxic and stable oxons. Thus, oxidative degradation procedures, generally referred as advanced oxidation processes (AOP, have been applied for their efficient removal from contaminated waters. The most applied bioassays to monitor the organophosphate toxicity i.e. the detoxification degree during AOP are Vibrio fischeri and AChE bioassays. Vibrio fischeri toxicity test exploits bioluminescence as the measure of luciferase activity of this marine bacterium, whereas AChE bioassay is based on AChE activity inhibition. Both bioanalytical techniques are rapid (several minutes, simple, sensitive and reproducible. Vibrio fischeri test seems to be a versatile indicator of toxic compounds generated in AOP for organophosphorus insecticides degradation. However, detection of neurotoxic AChE inhibitors, which can be formed in AOP of some organophosphates, requires AChE bioassays. Therefore, AChE toxicity test is more appropriate for monitoring the degradation processes of thio organophosphates, because more toxic oxo organophosphates might be formed and overlooked by Vibrio fischeri bioluminescence inhibition. In addition, during organophosphates removal by AOP, compounds with strong genotoxic potential may be formed, which cannot be detected by standard toxicity tests. For this reason, determination of

  3. Insecticide resistance in the sand fly, Phlebotomus papatasi from Khartoum State, Sudan

    Directory of Open Access Journals (Sweden)

    Hassan Mo'awia

    2012-03-01

    Full Text Available Abstract Background Phlebotomus papatasi the vector of cutaneous leishmaniasis (CL is the most widely spread sand fly in Sudan. No data has previously been collected on insecticide susceptibility and/or resistance of this vector, and a first study to establish a baseline data is reported here. Methods Sand flies were collected from Surogia village, (Khartoum State, Rahad Game Reserve (eastern Sudan and White Nile area (Central Sudan using light traps. Sand flies were reared in the Tropical Medicine Research Institute laboratory. The insecticide susceptibility status of first progeny (F1 of P. papatasi of each population was tested using WHO insecticide kits. Also, P. papatasi specimens from Surogia village and Rahad Game Reserve were assayed for activities of enzyme systems involved in insecticide resistance (acetylcholinesterase (AChE, non-specific carboxylesterases (EST, glutathione-S-transferases (GSTs and cytochrome p450 monooxygenases (Cyt p450. Results Populations of P. papatasi from White Nile and Rahad Game Reserve were sensitive to dichlorodiphenyltrichloroethane (DDT, permethrin, malathion, and propoxur. However, the P. papatasi population from Surogia village was sensitive to DDT and permethrin but highly resistant to malathion and propoxur. Furthermore, P. papatasi of Surogia village had significantly higher insecticide detoxification enzyme activity than of those of Rahad Game Reserve. The sand fly population in Surogia displayed high AChE activity and only three specimens had elevated levels for EST and GST. Conclusions The study provided evidence for malathion and propoxur resistance in the sand fly population of Surogia village, which probably resulted from anti-malarial control activities carried out in the area during the past 50 years.

  4. Insecticide resistance in the sand fly, Phlebotomus papatasi from Khartoum State, Sudan.

    Science.gov (United States)

    Hassan, Mo'awia Mukhtar; Widaa, Sally Osman; Osman, Osman Mohieldin; Numiary, Mona Siddig Mohammed; Ibrahim, Mihad Abdelaal; Abushama, Hind Mohammed

    2012-03-07

    Phlebotomus papatasi the vector of cutaneous leishmaniasis (CL) is the most widely spread sand fly in Sudan. No data has previously been collected on insecticide susceptibility and/or resistance of this vector, and a first study to establish a baseline data is reported here. Sand flies were collected from Surogia village, (Khartoum State), Rahad Game Reserve (eastern Sudan) and White Nile area (Central Sudan) using light traps. Sand flies were reared in the Tropical Medicine Research Institute laboratory. The insecticide susceptibility status of first progeny (F1) of P. papatasi of each population was tested using WHO insecticide kits. Also, P. papatasi specimens from Surogia village and Rahad Game Reserve were assayed for activities of enzyme systems involved in insecticide resistance (acetylcholinesterase (AChE), non-specific carboxylesterases (EST), glutathione-S-transferases (GSTs) and cytochrome p450 monooxygenases (Cyt p450). Populations of P. papatasi from White Nile and Rahad Game Reserve were sensitive to dichlorodiphenyltrichloroethane (DDT), permethrin, malathion, and propoxur. However, the P. papatasi population from Surogia village was sensitive to DDT and permethrin but highly resistant to malathion and propoxur. Furthermore, P. papatasi of Surogia village had significantly higher insecticide detoxification enzyme activity than of those of Rahad Game Reserve. The sand fly population in Surogia displayed high AChE activity and only three specimens had elevated levels for EST and GST. The study provided evidence for malathion and propoxur resistance in the sand fly population of Surogia village, which probably resulted from anti-malarial control activities carried out in the area during the past 50 years.

  5. Acetyl-cholinesterase Enzyme Inhibitory Effect of Calophyllum species

    African Journals Online (AJOL)

    1Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, ... Purpose: To search for new acetylcholinesterase enzyme inhibitors from ... Index Medicus, JournalSeek, Journal Citation Reports/Science Edition, .... The data are expressed as mean ± standard .... The authors acknowledge financial support from.

  6. Introducing Dynamic Combinatorial Chemistry: Probing the Substrate Selectivity of Acetylcholinesterase

    Science.gov (United States)

    Angelin, Marcus; Larsson, Rikard; Vongvilai, Pornrapee; Ramstrom, Olof

    2010-01-01

    In this laboratory experiment, college students are introduced to dynamic combinatorial chemistry (DCC) and apply it to determine the substrate selectivity of acetylcholinesterase (AChE). Initially, the students construct a chemical library of dynamically interchanging thioesters and thiols. Then, AChE is added and allowed to select and hydrolyze…

  7. Inhibition of acetylcholinesterase activity by essential oil from Citrus paradisi.

    Science.gov (United States)

    Miyazawa, M; Tougo, H; Ishihara, M

    2001-01-01

    Inhibition of acetylcholinesterase (AChE) activity by essential oils of Citrus paradisi (grapefruit pink in USA) was studied. Inhibition of AChE was measured by the colorimetric method. Nootkatone and auraptene were isolated from C. paradisi oil and showed 17-24% inhibition of AChE activity at the concentration of 1.62 microg/mL.

  8. Acetylcholinesterase assay for cerebrospinal fluid using bupivacaine to inhibit butyrylcholinesterase

    Directory of Open Access Journals (Sweden)

    Anders Jens

    2001-12-01

    Full Text Available Abstract Background Most test systems for acetylcholinesterase activity (E.C.3.1.1.7. are using toxic inhibitors (BW284c51 and iso-OMPA to distinguish the enzyme from butyrylcholinesterase (E.C.3.1.1.8. which occurs simultaneously in the cerebrospinal fluid. Applying Ellman's colorimetric method, we were looking for a non-toxic inhibitor to restrain butyrylcholinesterase activity. Based on results of previous in vitro studies bupivacaine emerged to be a suitable inhibitor. Results Pharmacokinetic investigations with purified cholinesterases have shown maximum inhibition of butyrylcholinesterase activity and minimal interference with acetylcholinesterase activity at bupivacaine final concentrations between 0.1 and 0.5 mmol/l. Based on detailed analysis of pharmacokinetic data we developed three equations representing enzyme inhibition at bupivacaine concentrations of 0.1, 0.2 and 0.5 mmol/l. These equations allow us to calculate the acetylcholinesterase activity in solutions containing both cholinesterases utilizing the extinction differences measured spectrophotometrically in samples with and without bupivacaine. The accuracy of the bupivacaine-inhibition test could be confirmed by investigations on solutions of both purified cholinesterases and on samples of human cerebrospinal fluid. If butyrylcholinesterase activity has to be assessed simultaneously an independent test using butyrylthiocholine iodide as substrate (final concentration 5 mmol/l has to be conducted. Conclusions The bupivacaine-inhibition test is a reliable method using spectrophotometrical techniques to measure acetylcholinesterase activity in cerebrospinal fluid. It avoids the use of toxic inhibitors for differentiation of acetylcholinesterase from butyrylcholinesterase in fluids containing both enzymes. Our investigations suggest that bupivacaine concentrations of 0.1, 0.2 or 0.5 mmol/l can be applied with the same effect using 1 mmol/l acetylthiocholine iodide as substrate.

  9. Curcumin administration suppress acetylcholinesterase gene expression in cadmium treated rats.

    Science.gov (United States)

    Akinyemi, Ayodele Jacob; Oboh, Ganiyu; Fadaka, Adewale Oluwaseun; Olatunji, Babawale Peter; Akomolafe, Seun

    2017-09-01

    Curcumin, the main polyphenolic component of turmeric (Curcuma longa) rhizomes have been reported to exert anticholinesterase potential with limited information on how they regulate acetylcholinesterase (AChE) gene expression. Hence, this study sought to evaluate the effect of curcumin on cerebral cortex acetylcholinesterase (AChE) activity and their mRNA gene expression level in cadmium (Cd)-treated rats. Furthermore, in vitro effect of different concentrations of curcumin (1-5μg/mL) on rat cerebral cortex AChE activity was assessed. Animals were divided into six groups (n=6): group 1 serve as control (without Cd) and receive saline/vehicle, group 2 receive saline plus curcumin at 25mg/kg, group 3 receive saline plus curcumin 50mg/kg, group 4 receive Cd plus vehicle, group 5 receive Cd plus curcumin at 25mg/kg and group 6 receive Cd plus curcumin at 50mg/kg. Rats received Cd (2.5mg/kg) and curcumin (25 and 50mg/kg, respectively) by oral gavage for 7days. Acetylcholinesterase activity was measured by Ellman's method and AChE expression was carried out by a quantitative reverse transcriptase polymerase chain reaction (RT-qPCR) assay. We observed that acute administration of Cd increased acetylcholinesterase activity and in addition caused a significant (Pcurcumin inhibited AChE activity and alters AChE mRNA levels when compared to Cd-treated group. In addition, curcumin inhibits rat cerebral cortex AChE activity in vitro. In conclusion, curcumin exhibit anti-acetylcholinesterase activity and suppressed AChE mRNA gene expression level in Cd exposed rats, thus providing some biochemical and molecular evidence on the therapeutic effect of this turmeric-derived compound in treating neurological disorders including Alzheimer's disease. Copyright © 2017 Elsevier B.V. All rights reserved.

  10. Insecticide Resistance Reducing Effectiveness of Malaria Control

    Centers for Disease Control (CDC) Podcasts

    Malaria prevention is increasingly insecticide based. Dr. John Gimnig, an entomologist with the Division of Parasitic Diseases, CDC, discusses evidence that mosquito resistance to insecticides, which is measured in the laboratory, could compromise malaria prevention in the field.

  11. Synthesis of new α-amino nitriles with insecticidal action on Aedes aegypti (Diptera: Culicidae

    Directory of Open Access Journals (Sweden)

    Andrés G. Rueda

    2018-04-01

    Full Text Available Aedes aegypti is the principal vector of arboviral pathogens that may cause diseases as dengue fever, chikungunya and zika. The harmful environmental effects of commercial pesticides coalesced with the development of insecticide-resistant populations encourage the discovery and generation of new alternative products as a tool to reduce the incidence of vector-borne diseases. In this work, through the classic three component Strecker reaction of commercial benzaldehydes, cyclic secondary amines and KCN, a new series of nine α-amino nitriles, girgensohnine analogs, has been synthetized and screened for larvicide and adulticide properties against A. aegypti, one of the dominant vectors of dengue, chikungunya and zika in tropical and subtropical areas all over the world. Molecules 3 and 4 were identified as potential larvicidal agents with LC50 values of 50.55 and 69.59 ppm, respectively. Molecule 3 showed 100% of mortality after 2 h of treatment when a concentration of 30 ppm in adulticidal assays was evaluated. Additionally, in order to elucidate the mode of action of these molecules, their acetylcholinesterase (AChE inhibitory properties were evaluated using the Ellman assay. It was found that the molecules possess a weak AChE inhibitory activity with IC50 values between 148.80 and 259.40 μM, indicating that AChE could not be a principal target for insecticide activity. Keywords: Arthropod-borne diseases, Girgensohnine analogs, Strecker reaction, Insecticidal activity, Vector control

  12. Resistance Status to the Insecticides Temephos, Deltamethrin, and Diflubenzuron in Brazilian Aedes aegypti Populations

    Science.gov (United States)

    Viana-Medeiros, Priscila Fernandes; Araújo, Simone Costa; Martins, Ademir J.; Lima, José Bento Pereira

    2016-01-01

    Insecticides are still largely applied in public health to control disease vectors. In Brazil, organophosphates (OP) and pyrethroids (PY) are used against Aedes aegypti for years. Since 2009 Insect Growth Regulators (IGR) are also employed in the control of larvae. We quantified resistance to temephos (OP), deltamethrin (PY), and diflubenzuron (IGR) of A. aegypti samples from 12 municipalities distributed throughout the country, collected between 2010 and 2012. High levels of resistance to neurotoxic insecticides were detected in almost all populations: RR95 to temephos varied between 4.0 and 27.1; the lowest RR95 to deltamethrin was 13.1, and values higher than 70.0 were found. In contrast, all samples were susceptible to diflubenzuron (RR95 < 2.3). Biochemical tests performed with larvae and adults discarded the participation of acetylcholinesterase, the OP target, and confirmed involvement of the detoxifying enzymes esterases, mixed function oxidases, and glutathione-S-transferases. The results obtained were discussed taking into account the public chemical control component and the increase in the domestic use of insecticides during dengue epidemic seasons in the evaluated municipalities. PMID:27419140

  13. The contribution of agricultural insecticide use to increasing insecticide resistance in African malaria vectors

    OpenAIRE

    Reid, Molly C.; McKenzie, F. Ellis

    2016-01-01

    The fight against malaria is increasingly threatened by failures in vector control due to growing insecticide resistance. This review examines the recent primary research that addresses the putative relationship between agricultural insecticide use and trends in insecticide resistance. To do so, descriptive evidence offered by the new research was categorized, and additional factors that impact the relationship between agricultural insecticide use and observed insecticide resistance in malari...

  14. Punishment Insensitivity in Early Childhood: A Developmental, Dimensional Approach.

    Science.gov (United States)

    Nichols, Sara R; Briggs-Gowan, Margaret J; Estabrook, Ryne; Burns, James L; Kestler, Jacqueline; Berman, Grace; Henry, David B; Wakschlag, Lauren S

    2015-08-01

    Impairment in learning from punishment ("punishment insensitivity") is an established feature of severe antisocial behavior in adults and youth but it has not been well studied as a developmental phenomenon. In early childhood, differentiating a normal: abnormal spectrum of punishment insensitivity is key for distinguishing normative misbehavior from atypical manifestations. This study employed a novel measure, the Multidimensional Assessment Profile of Disruptive Behavior (MAP-DB), to examine the distribution, dimensionality, and external validity of punishment insensitivity in a large, demographically diverse community sample of preschoolers (3-5 years) recruited from pediatric clinics (N = 1,855). Caregivers completed surveys from which a seven-item Punishment Insensitivity scale was derived. Findings indicated that Punishment Insensitivity behaviors are relatively common in young children, with at least 50 % of preschoolers exhibiting them sometimes. Item response theory analyses revealed a Punishment Insensitivity spectrum. Items varied along a severity continuum: most items needed to occur "Often" in order to be severe and behaviors that were qualitatively atypical or intense were more severe. Although there were item-level differences across sociodemographic groups, these were small. Construct, convergent, and divergent validity were demonstrated via association to low concern for others and noncompliance, motivational regulation, and a disruptive family context. Incremental clinical utility was demonstrated in relation to impairment. Early childhood punishment insensitivity varies along a severity continuum and is atypical when it predominates. Implications for understanding the phenomenology of emergent disruptive behavior are discussed.

  15. Hepatopancreatic intoxication of lambda cyhalothrin insecticide on albino rats.

    Science.gov (United States)

    Elhalwagy, Manal Ea; Abd-Alrahman, Sherif H; Nahas, A A; Ziada, Reem M; Mohamady, Aziza H

    2015-01-01

    Despite the known adverse effects of lambda cyhalothrin insecticide, little is known about its hepatopancreatic intoxication effects. The present study was carried out to elucidate sub-chronic effect of Karat 2.5% EC formulation of lambda cyhalothrin on male albino rats. To explore the effects of exposure to lambda cyhalothrin on rats and its mechanism, low (1/40 of LD50, 5 mg/kg/day) and high dose (1/4 of LD50, 50 mg/kg/day) lambda cyhalothrin were applied to rats via drinking water for 3 months. Blood samples were collected monthly, and the animals were dissected for liver and pancreas's examination at the end of the experiment. Lambda cyhalothrin administration was associated with the elevation in lipid peroxidation marker, malondialdehyde (MDA), reduction in SH-protein a major marker for antioxidant, as well as basel paraoxonase (PON) in both treated groups throughout the experimental periods. In addition, significant elevations in liver enzymes alanin amino transferase, (ALT), and aspartate amino transferase (AST), as well as plasma acetylcholinesterase (AChE) and glucose level. While, significant reduction in insulin level through the experimental periods. Results of histopathological and histochemical studies showed that lambda cyhalothrin exposure induces liver and pancreatic tissues damage and depletion in glycogen content was pronounced in liver of both treated groups. In conclusion subchronic intoxication with lambda cyhalothrin formulation induced remarkable changes in the examined parameters.

  16. Pyrethrum flowers and pyrethroid insecticides.

    OpenAIRE

    Casida, J E

    1980-01-01

    The natural pyrethrins from the daisy-like flower, Tanacetum or Chrysanthemum cinerariifolium, are nonpersistent insecticides of low toxicity to mammals. Synthetic analogs or pyrethroids, evolved from the natural compounds by successive isosteric modifications, are more potent and stable and are the newest important class of crop protection chemicals. They retain many of the favorable properties of the pyrethrins.

  17. Limonene--A Natural Insecticide.

    Science.gov (United States)

    Beatty, Joseph H.

    1986-01-01

    Describes a high school chemistry student's research project in which limonene was isolated from the oil of lemons and oranges. Outlines the students' tests on the use of this chemical as an insecticide. Discusses possible extensions of the exercises based on questions generated by the students. (TW)

  18. Radioligand Recognition of Insecticide Targets.

    Science.gov (United States)

    Casida, John E

    2018-04-04

    Insecticide radioligands allow the direct recognition and analysis of the targets and mechanisms of toxic action critical to effective and safe pest control. These radioligands are either the insecticides themselves or analogs that bind at the same or coupled sites. Preferred radioligands and their targets, often in both insects and mammals, are trioxabicyclooctanes for the γ-aminobutyric acid (GABA) receptor, avermectin for the glutamate receptor, imidacloprid for the nicotinic receptor, ryanodine and chlorantraniliprole for the ryanodine receptor, and rotenone or pyridaben for NADH + ubiquinone oxidoreductase. Pyrethroids and other Na + channel modulator insecticides are generally poor radioligands due to lipophilicity and high nonspecific binding. For target site validation, the structure-activity relationships competing with the radioligand in the binding assays should be the same as that for insecticidal activity or toxicity except for rapidly detoxified or proinsecticide analogs. Once the radioligand assay is validated for relevance, it will often help define target site modifications on selection of resistant pest strains, selectivity between insects and mammals, and interaction with antidotes and other chemicals at modulator sites. Binding assays also serve for receptor isolation and photoaffinity labeling to characterize the interactions involved.

  19. New Temperature-Insensitive Electronically-Tunable Grounded Capacitor Simulator

    OpenAIRE

    Abuelma'atti, Muhammad Taher; Khan, Muhammad Haroon

    1996-01-01

    A new circuit for simulating a grounded capacitor is presented. The circuit uses one operationalamplifier (OA), three operational-transconductance amplifiers (OTAs), and one capacitor. The realized capacitor is temperature-insensitive and electronically tunable. Experimental results are included.

  20. The Limitations to Delay-Insensitivity in Asynchronous Circuits

    National Research Council Canada - National Science Library

    Martin, Alain J

    1990-01-01

    ... produced are delay-insensitive (DI). A digital circuit is DI when its correct operation is independent of the delays in operators and in the wires connecting the operators, except that the delays are finite and positive...

  1. Insensitive detonator apparatus for initiating large failure diameter explosives

    Science.gov (United States)

    Perry, III, William Leroy

    2015-07-28

    A munition according to a preferred embodiment can include a detonator system having a detonator that is selectively coupled to a microwave source that functions to selectively prime, activate, initiate, and/or sensitize an insensitive explosive material for detonation. The preferred detonator can include an explosive cavity having a barrier within which an insensitive explosive material is disposed and a waveguide coupled to the explosive cavity. The preferred system can further include a microwave source coupled to the waveguide such that microwaves enter the explosive cavity and impinge on the insensitive explosive material to sensitize the explosive material for detonation. In use the preferred embodiments permit the deployment and use of munitions that are maintained in an insensitive state until the actual time of use, thereby substantially preventing unauthorized or unintended detonation thereof.

  2. Internal Diffusion-Controlled Enzyme Reaction: The Acetylcholinesterase Kinetics.

    Science.gov (United States)

    Lee, Sangyun; Kim, Ji-Hyun; Lee, Sangyoub

    2012-02-14

    Acetylcholinesterase is an enzyme with a very high turnover rate; it quenches the neurotransmitter, acetylcholine, at the synapse. We have investigated the kinetics of the enzyme reaction by calculating the diffusion rate of the substrate molecule along an active site channel inside the enzyme from atomic-level molecular dynamics simulations. In contrast to the previous works, we have found that the internal substrate diffusion is the determinant of the acetylcholinesterase kinetics in the low substrate concentration limit. Our estimate of the overall bimolecular reaction rate constant for the enzyme is in good agreement with the experimental data. In addition, the present calculation provides a reasonable explanation for the effects of the ionic strength of solution and the mutation of surface residues of the enzyme. The study suggests that internal diffusion of the substrate could be a key factor in understanding the kinetics of enzymes of similar characteristics.

  3. Enzymatic and biochemical characterization of Bungarus sindanus snake venom acetylcholinesterase

    Directory of Open Access Journals (Sweden)

    M Ahmed

    2012-01-01

    Full Text Available This study analyses venom from the elapid krait snake Bungarus sindanus, which contains a high level of acetylcholinesterase (AChE activity. The enzyme showed optimum activity at alkaline pH (8.5 and 45ºC. Krait venom AChE was inhibited by substrate. Inhibition was significantly reduced by using a high ionic strength buffer; low ionic strength buffer (10 mM PO4 pH 7.5 inhibited the enzyme by 1. 5mM AcSCh, while high ionic strength buffer (62 mM PO4 pH 7.5 inhibited it by 1 mM AcSCh. Venom acetylcholinesterase was also found to be thermally stable at 45ºC; it only lost 5% of its activity after incubation at 45ºC for 40 minutes. The Michaelis-Menten constant (Km for acetylthiocholine iodide hydrolysis was found to be 0.068 mM. Krait venom acetylcholinesterase was also inhibited by ZnCl2, CdCl2, and HgCl2 in a concentrationdependent manner. Due to the elevated levels of AChE with high catalytic activity and because it is more stable than any other sources, Bungarus sindanus venom is highly valuable for biochemical studies of this enzyme.

  4. The contribution of agricultural insecticide use to increasing insecticide resistance in African malaria vectors.

    Science.gov (United States)

    Reid, Molly C; McKenzie, F Ellis

    2016-02-19

    The fight against malaria is increasingly threatened by failures in vector control due to growing insecticide resistance. This review examines the recent primary research that addresses the putative relationship between agricultural insecticide use and trends in insecticide resistance. To do so, descriptive evidence offered by the new research was categorized, and additional factors that impact the relationship between agricultural insecticide use and observed insecticide resistance in malaria vectors were identified. In 23 of the 25 relevant recent publications from across Africa, higher resistance in mosquito populations was associated with agricultural insecticide use. This association appears to be affected by crop type, farm pest management strategy and urban development.

  5. The effect of stress on the acute neurotoxicity of the organophosphate insecticide chlorpyrifos

    International Nuclear Information System (INIS)

    Hancock, Sandra; Ehrich, Marion; Hinckley, Jonathan; Pung, Thitiya; Jortner, Bernard S.

    2007-01-01

    A study was conducted to determine if multiple exposures to several stress paradigms might affect the anticholinesterase effect of subsequently administered organophosphate insecticide chlorpyrifos. Male Sprague-Dawley rats were subject to daily periods of restraint, swimming, a combination of the two, or neither of the two (controls) (n = 8/group) for 5 days per week over a six-week period. The most profound stress, as measured by reduced body weight gain and elevated levels of plasma corticosterone, was swimming. On day 39 of the study, shortly after the daily stress episode, one half of the rats in each group was dosed with 60 mg/kg chlorpyrifos subcutaneously. This had no effect on subsequent levels of plasma corticosterone. There were no stress-related differences in the degree of chlorpyrifos-induced inhibition of brain acetylcholinesterase in animals sacrificed on day 43

  6. Calcium pathways such as cAMP modulate clothianidin action through activation of α-bungarotoxin-sensitive and -insensitive nicotinic acetylcholine receptors.

    Science.gov (United States)

    Calas-List, Delphine; List, Olivier; Quinchard, Sophie; Thany, Steeve H

    2013-07-01

    Clothianidin is a neonicotinoid insecticide developed in the early 2000s. We have recently demonstrated that it was a full agonist of α-bungarotoxin-sensitive and -insensitive nicotinic acetylcholine receptors expressed in the cockroach dorsal unpaired median neurons. Clothianidin was able to act as an agonist of imidacloprid-insensitive nAChR2 receptor and internal regulation of cAMP concentration modulated nAChR2 sensitivity to clothianidin. In the present study, we demonstrated that cAMP modulated the agonist action of clothianidin via α-bungarotoxin-sensitive and insensitive receptors. Clothianidin-induced current-voltage curves were dependent to clothianidin concentrations. At 10 μM clothianidin, increasing cAMP concentration induced a linear current-voltage curve. Clothianidin effects were blocked by 0.5 μM α-bungarotoxin suggesting that cAMP modulation occurred through α-bungarotoxin-sensitive receptors. At 1 mM clothianidin, cAMP effects were associated to α-bungarotoxin-insensitive receptors because clothianidin-induced currents were blocked by 5 μM mecamylamine and 20 μM d-tubocurarine. In addition, we found that application of 1mM clothianidin induced a strong increase of intracellular calcium concentration. These data reinforced the finding that calcium pathways including cAMP modulated clothianidin action on insect nicotinic acetylcholine receptors. We proposed that intracellular calcium pathways such as cAMP could be a target to modulate the mode of action of neonicotinoid insecticides. Copyright © 2013 Elsevier Inc. All rights reserved.

  7. Molecular cloning and characterization of an acetylcholinesterase cDNA in the brown planthopper, Nilaparvata lugens.

    Science.gov (United States)

    Yang, Zhifan; Chen, Jun; Chen, Yongqin; Jiang, Sijing

    2010-01-01

    A full cDNA encoding an acetylcholinesterase (AChE, EC 3.1.1.7) was cloned and characterized from the brown planthopper, Nilaparvata lugens Stål (Hemiptera: Delphacidae). The complete cDNA (2467 bp) contains a 1938-bp open reading frame encoding 646 amino acid residues. The amino acid sequence of the AChE deduced from the cDNA consists of 30 residues for a putative signal peptide and 616 residues for the mature protein with a predicted molecular weight of 69,418. The three residues (Ser242, Glu371, and His485) that putatively form the catalytic triad and the six Cys that form intra-subunit disulfide bonds are completely conserved, and 10 out of the 14 aromatic residues lining the active site gorge of the AChE are also conserved. Northern blot analysis of poly(A)+ RNA showed an approximately 2.6-kb transcript, and Southern blot analysis revealed there likely was just a single copy of this gene in N. lugens. The deduced protein sequence is most similar to AChE of Nephotettix cincticeps with 83% amino acid identity. Phylogenetic analysis constructed with 45 AChEs from 30 species showed that the deduced N. lugens AChE formed a cluster with the other 8 insect AChE2s. Additionally, the hypervariable region and amino acids specific to insect AChE2 also existed in the AChE of N. lugens. The results revealed that the AChE cDNA cloned in this work belongs to insect AChE2 subgroup, which is orthologous to Drosophila AChE. Comparison of the AChEs between the susceptible and resistant strains revealed a point mutation, Gly185Ser, is likely responsible for the insensitivity of the AChE to methamidopho in the resistant strain.

  8. Susceptibility of Anopheles gambiae to insecticides used for malaria vector control in Rwanda.

    Science.gov (United States)

    Hakizimana, Emmanuel; Karema, Corine; Munyakanage, Dunia; Iranzi, Gad; Githure, John; Tongren, Jon Eric; Takken, Willem; Binagwaho, Agnes; Koenraadt, Constantianus J M

    2016-12-01

    -cyhalothrin, deltamethrin, permethrin) and organochlorines (DDT) and the large presence of target site insensitivity. The results demonstrate the need for Rwanda to expand monitoring for insecticide resistance including further metabolic resistance testing and implement an insecticide resistance management strategy to sustain the gains made in malaria control.

  9. Recent developments in bend-insensitive and ultra-bend-insensitive fibers

    Science.gov (United States)

    Boivin, David; de Montmorillon, Louis-Anne; Provost, Lionel; Montaigne, Nelly; Gooijer, Frans; Aldea, Eugen; Jensma, Jaap; Sillard, Pierre

    2010-02-01

    Designed to overcome the limitations in case of extreme bending conditions, Bend- and Ultra-Bend-Insensitive Fibers (BIFs and UBIFs) appear as ideal solutions for use in FTTH networks and in components, pigtails or patch-cords for ever demanding applications such as military or sensing. Recently, however, questions have been raised concerning the Multi-Path-Interference (MPI) levels in these fibers. Indeed, they are potentially subject to interferences between the fundamental mode and the higher-order mode that is also bend resistant. This MPI is generated because of discrete discontinuities such as staples, bends and splices/connections that occur on distance scales that become comparable to the laser coherent length. In this paper, we will demonstrate the high MPI tolerance of all-solid single-trench-assisted BIFs and UBIFs. We will present the first comprehensive study combining theoretical and experimental points of view to quantify the impact of fusion splices on coherent MPI. To be complete, results for mechanical splices will also be reported. Finally, we will show how the single-trench- assisted concept combined with the versatile PCVD process allows to tightly control the distributions of fibers characteristics. Such controls are needed to massively produce BIFs and to meet the more stringent specifications of the UBIFs.

  10. Insecticide resistance in Bemisia tabaci Gennadius (Homoptera: Aleyrodidae) and Anopheles gambiae Giles (Diptera: Culicidae) could compromise the sustainability of malaria vector control strategies in West Africa.

    Science.gov (United States)

    Gnankiné, Olivier; Bassolé, Imael H N; Chandre, Fabrice; Glitho, Isabelle; Akogbeto, Martin; Dabiré, Roch K; Martin, Thibaud

    2013-10-01

    Insecticides from the organophosphate (OP) and pyrethroid (PY) chemical families, have respectively, been in use for 50 and 30 years in West Africa, mainly against agricultural pests, but also against vectors of human disease. The selection pressure, with practically the same molecules year after year (mainly on cotton), has caused insecticide resistance in pest populations such as Bemisia tabaci, vector of harmful phytoviruses on vegetables. The evolution toward insecticide resistance in malaria vectors such as Anopheles gambiae sensus lato (s.l.) is probably related to the current use of these insecticides in agriculture. Thus, successful pest and vector control in West Africa requires an investigation of insect susceptibility, in relation to the identification of species and sub species, such as molecular forms or biotypes. Identification of knock down resistance (kdr) and acetylcholinesterase gene (Ace1) mutations modifying insecticide targets in individual insects and measure of enzymes activity typically involved in insecticide metabolism (oxidase, esterase and glutathion-S-transferase) are indispensable in understanding the mechanisms of resistance. Insecticide resistance is a good example in which genotype-phenotype links have been made successfully. Insecticides used in agriculture continue to select new resistant populations of B. tabaci that could be from different biotype vectors of plant viruses. As well, the evolution of insecticide resistance in An. gambiae threatens the management of malaria vectors in West Africa. It raises the question of priority in the use of insecticides in health and/or agriculture, and more generally, the question of sustainability of crop protection and vector control strategies in the region. Here, we review the susceptibility tests, biochemical and molecular assays data for B. tabaci, a major pest in cotton and vegetable crops, and An. gambiae, main vector of malaria. The data reviewed was collected in Benin and Burkina

  11. A polarization-insensitive plasmonic photoconductive terahertz emitter

    KAUST Repository

    Li, Xurong

    2017-11-16

    We present a polarization-insensitive plasmonic photoconductive terahertz emitter that uses a two-dimensional array of nanoscale cross-shaped apertures as the plasmonic contact electrodes. The geometry of the cross-shaped apertures is set to maximize optical pump absorption in close proximity to the contact electrodes. The two-dimensional symmetry of the cross-shaped apertures offers a polarization-insensitive interaction between the plasmonic contact electrodes and optical pump beam. We experimentally demonstrate a polarization-insensitive terahertz radiation from the presented emitter in response to a femtosecond optical pump beam and similar terahertz radiation powers compared to previously demonstrated polarization-sensitive photoconductive emitters with plasmonic contact electrode gratings at the optimum optical pump polarization.

  12. Surface display and bioactivity of Bombyx mori acetylcholinesterase on Pichia pastoris

    Science.gov (United States)

    To construct the Pichia pastoris (P. pastoris) cell surface display system of Bombyx mori acetylcholinesterase (BmAChE), the gene for the anchor protein (AGa1) was obtained from Saccharomyces cerevisiae and was fused with the modified Bombyx mori acetylcholinesterase gene (bmace) and transformed int...

  13. Congenital insensitivity to pain: Case report of a rare entity

    Directory of Open Access Journals (Sweden)

    Swati Dahiya

    2018-01-01

    Full Text Available Hereditary sensory and autonomic neuropathies (HSANs are a group of disorders characterized by insensitivity to noxious stimuli and autonomic dysfunction, associated with pathological abnormalities of the peripheral nerves. Five types of HSAN have been reported in literature, out of which Type V known as congenital insensitivity to pain (CIP is a rare autosomal recessive condition. Self-mutilation is an invariable feature of this disorder, involving the teeth and orofacial structures. This case report describes a case of a 6-year-old girl with CIP brought by her parents for prostheses to replace her self-extracted primary teeth.

  14. Acetylcholinesterase activity in the terrestrial snail Xeropicta derbentina transplanted in apple orchards with different pesticide management strategies

    Energy Technology Data Exchange (ETDEWEB)

    Mazzia, Christophe, E-mail: christophe.mazzia@univ-avignon.f [Universite d' Avignon et des Pays de Vaucluse, Laboratoire de Toxicologie Environnementale, UMR 406 UAPV/INRA, ' Abeilles et Environnement' , Domaine St Paul, Site Agroparc, 84914 Avignon Cedex 9 France (France); Capowiez, Yvan [INRA, UR 1115 ' Plante et Systemes Horticoles' , Domaine St Paul, Site Agroparc, 84914 Avignon Cedex 9 France (France); Sanchez-Hernandez, Juan C. [Laboratory of Ecotoxicology, Faculty of Environmental Science, University of Castilla-La Mancha, Avda. Carlos III s/n, 45071 Toledo (Spain); Koehler, Heinz-R. [Animal Physiological Ecology, Institute for Evolution and Ecology, University of Tuebingen, Konrad-Adenauer-Str. 20, D-72072 Tuebingen (Germany); Triebskorn, Rita [Animal Physiological Ecology, Institute for Evolution and Ecology, University of Tuebingen, Konrad-Adenauer-Str. 20, D-72072 Tuebingen (Germany); Steinbeis-Transfer Center for Ecotoxicology and Ecophysiology, Blumenstrasse 13, D-72108 Rottenburg (Germany); Rault, Magali [Universite d' Avignon et des Pays de Vaucluse, Laboratoire de Toxicologie Environnementale, UMR 406 UAPV/INRA, ' Abeilles et Environnement' , Domaine St Paul, Site Agroparc, 84914 Avignon Cedex 9 France (France)

    2011-01-15

    Apple orchards are highly manipulated crops in which large amounts of pesticides are used. Some of these pesticides lack target specificity and can cause adverse effects in non-target organisms. In order to evaluate the environmental risk of these products, the use of transplanted sentinel organisms avoids side-effects from past events and facilitate comparison of multiple sites in a short time. We released specimens of the terrestrial snail Xeropicta derbentina in each 5 of two kinds of apple orchards with either conventional or organic management strategies plus in a single abandoned orchard. After one month, individuals were retrieved in order to measure acetylcholinesterase (AChE) activity. Mean values of AChE activity were significantly reduced in all conventional apple orchards compared to the others. Results show that the measurement of biomarkers such as AChE inhibition in transplated X. derbentina could be useful in the environmental risk assessment of post-authorized pesticides. - Snails as sentinel species to evaluate insecticide impacts in apple orchards.

  15. Acetylcholinesterase activity in the terrestrial snail Xeropicta derbentina transplanted in apple orchards with different pesticide management strategies

    International Nuclear Information System (INIS)

    Mazzia, Christophe; Capowiez, Yvan; Sanchez-Hernandez, Juan C.; Koehler, Heinz-R.; Triebskorn, Rita; Rault, Magali

    2011-01-01

    Apple orchards are highly manipulated crops in which large amounts of pesticides are used. Some of these pesticides lack target specificity and can cause adverse effects in non-target organisms. In order to evaluate the environmental risk of these products, the use of transplanted sentinel organisms avoids side-effects from past events and facilitate comparison of multiple sites in a short time. We released specimens of the terrestrial snail Xeropicta derbentina in each 5 of two kinds of apple orchards with either conventional or organic management strategies plus in a single abandoned orchard. After one month, individuals were retrieved in order to measure acetylcholinesterase (AChE) activity. Mean values of AChE activity were significantly reduced in all conventional apple orchards compared to the others. Results show that the measurement of biomarkers such as AChE inhibition in transplated X. derbentina could be useful in the environmental risk assessment of post-authorized pesticides. - Snails as sentinel species to evaluate insecticide impacts in apple orchards.

  16. CADDIS Volume 2. Sources, Stressors and Responses: Insecticides - Detailed Conceptual Diagram

    Science.gov (United States)

    Introduction to the insecticides module, when to list insecticides as a candidate cause, ways to measure insecticides, simple and detailed conceptual diagrams for insecticides, insecticides module references and literature reviews.

  17. CADDIS Volume 2. Sources, Stressors and Responses: Insecticides - Simple Conceptual Diagram

    Science.gov (United States)

    Introduction to the insecticides module, when to list insecticides as a candidate cause, ways to measure insecticides, simple and detailed conceptual diagrams for insecticides, insecticides module references and literature reviews.

  18. Toxicological studies on the insecticides azinphosmethyl ( guthion ) and carbaryl in albion rats with special reference to the metabolism of 14 c- naphthyl

    International Nuclear Information System (INIS)

    Wafa, D.M.

    1992-01-01

    1-pesticides are among the group of foreign chemicals now polluting the environment, but also are essential to man's well being as they provide both protection of food crops from pests and humans from insect-borne disease. 2- in the present investigation, toxicological studies on the two insecticides: azinphosmethyl (organophosphorus) and carbaryl (carbamate) have been made. the comparative effects of the insecticides on acetylcholinesterase activity in brain, erthrocytes and plasma have been studied for different periods in albino rats. 3- there is considerable information available concerning the metabolism of azinphosmethyl (guthion), yet some aspects of carbaryl metabolism need further verifications. For this reason, the metabolism of labeled 14 c-naphthyl carbaryl has been studied in vivo in the present investigation to add further knowledge on the metabolism of carbaryl, and to find out possible relationship that may exist between carbaryl toxicity and its metabolism

  19. Malaria vector composition and insecticide susceptibility status in Guinea Conakry, West Africa.

    Science.gov (United States)

    Vezenegho, S B; Brooke, B D; Hunt, R H; Coetzee, M; Koekemoer, L L

    2009-12-01

    This study provides data on malaria vector species composition and insecticide susceptibility status from three localities in Guinea Conakry. A total of 497 mosquitoes were collected resting indoors and morphologically identified as belonging to the Anopheles gambiae complex. The majority of these were An. gambiae s.s. (99.6%), but a small percentage (0.4%) were identified as Anopheles arabiensis. Thirty-four Anopheles funestus s.s. were also collected. The molecular S form of An. gambiae s.s. was predominant over the M form in Siguiri (95%) and Boffa (97.4%), whereas at Mt Nimba the M form was more abundant (61.4%) than the S form (38.1%). One hybrid M/S specimen was recorded from Mt Nimba. Siguiri populations showed high levels of resistance to DDT, dieldrin and bendiocarb. Anopheles gambiae from Boffa were largely susceptible to the insecticides tested. At Mt Nimba, resistance to DDT and bendicocarb was detected. Biochemical enzyme analysis showed that an altered acetylcholinesterase is operating in the field at low levels. The frequency of the 1014F kdr allele in the An. gambiae S form was 0.24 at Siguiri and 0.14 at Mt Nimba. A single RR specimen was found in the M form. The heterogeneity in species composition and resistance profiles between sites requires vector control interventions to be tailored to each site based on the data collected from ongoing monitoring and surveillance.

  20. Mosquitocidal carbamates with low toxicity to agricultural pests: an advantageous property for insecticide resistance management.

    Science.gov (United States)

    Swale, Daniel R; Carlier, Paul R; Hartsel, Joshua A; Ma, Ming; Bloomquist, Jeffrey R

    2015-08-01

    Insecticide resistance in the malaria mosquito Anopheles gambiae is well documented, and widespread agricultural use of pyrethroids may exacerbate development of resistance when pyrethroids are used in vector control. We have developed carbamate anticholinesterases that possess a high degree of An. gambiae:human selectivity for enzyme inhibition. The purpose of this study was to assess the spectrum of activity of these carbamates against other mosquitoes and agricultural pests. Experimental carbamates were potent inhibitors of mosquito acetylcholinesterases, with IC50 values in the nanomolar range. Similar potencies were observed for Musca domestica and Drosophila melanogaster enzymes. Although meta-substituted carbamates were potent inhibitors, two ortho-substituted carbamates displayed poor enzyme inhibition (IC50 ≥ 10(-6)  M) in honey bee (Apis mellifera), Asian citrus psyllid (Diaphorina citri) and lepidopteran agricultural pests (Plutella xylostella and Ostrinia nubilalis). Enzyme inhibition results were confirmed by toxicity studies in caterpillars, where the new carbamates were 2-3-fold less toxic than propoxur and up to tenfold less active than bendiocarb, indicating little utility of these compounds for crop protection. The experimental carbamates were broadly active against mosquito species but not agricultural pests, which should mitigate selection for mosquito insecticide resistance by reducing agricultural uses of these compounds. © 2014 Society of Chemical Industry. © 2014 Society of Chemical Industry.

  1. Osmoregulatory function in ducks following ingestion of the organophosphorus insecticide fenthion

    Science.gov (United States)

    Rattner, B.A.; Fleming, W.J.; Murray, H.C.

    1983-01-01

    Salt gland function and osmoregulation in aquatic birds drinking hyperosmotic water has been suggested to be impaired by organophosphorus insecticides. To test this hypothesis, adult black ducks (Anas rubripes) were provided various regimens of fresh or salt (1.5% NaCl) water before, during, and after ingestion of mash containing 21 ppm fenthion. Ducks were bled by jugular venipuncture after I, 7. and 12 days of treatment, and were then killed. Brain and salt gland acetylcholinesterase activities were substantially inhibited (44-61% and 14-36%) by fenthion. However, salt gland weight and Na + -K + -ATPase activity, and plasma Na + , CI- , and osmolality, were uniformly elevated in all groups receiving salt water including those ingesting fenthion. In a second study, salt gland Na + -K + -ATPase activity in mallards (A. platyrhynchos) was not affected after in vitro incubation with either fenthion or fenthion oxon at concentrations ranging from 0.04 to 400 ?M, but was reduced in the presence of 40 and 400 ?M DDE (positive control). These findings suggest that environmentally realistic concentrations of organophosphorus insecticides do not markedly affect osmoregulatory function in adult black ducks.

  2. Impact of insecticide exposure on the predation activity of the European earwig Forficula auricularia.

    Science.gov (United States)

    Malagnoux, Laure; Capowiez, Yvan; Rault, Magali

    2015-09-01

    The European earwig Forficula auricularia is an effective predator in apple orchards. It is therefore crucial to study whether insecticides affect this natural pest control agent. Predation activity, i.e., the number of aphids eaten in 24 h, was determined under laboratory conditions after exposure of fourth-instar nymphs and adult earwigs to widely used insecticides (acetamiprid, chlorpyrifos-ethyl, deltamethrin, and spinosad), which were applied at the normal application rates. Inhibition of acetylcholinesterase and carboxylesterase activities were also measured as indicators of pesticide exposure. Predation activity decreased significantly in nymphs exposed to spinosad (62%) and chlorpyrifos-ethyl (98%) compared with controls. A similar response was found for both esterase activities. Spinosad had a stronger effect on AChE (-33%) whereas chlorpyrifos-ethyl affected CbE activity preferentially (-59%). Spinosad (20% of controls), acetamiprid (28%), and chlorpyrifos-ethyl (66%) also significantly decreased the predation behavior of adult male but not female (5 to 40%) earwigs. Adult AChE and CbE activities were also significantly reduced (28 to 67% of controls) in pesticide-exposed earwigs. Our results suggest that earwigs should be included in the environmental risk assessment framework for authorization of newly marketed plant protection products. Their predation behavior appears to be a sensitive and complementary biomarker.

  3. Insect-specific irreversible inhibitors of acetylcholinesterase in pests including the bed bug, the eastern yellowjacket, German and American cockroaches, and the confused flour beetle.

    Science.gov (United States)

    Polsinelli, Gregory A; Singh, Sanjay K; Mishra, Rajesh K; Suranyi, Robert; Ragsdale, David W; Pang, Yuan-Ping; Brimijoin, Stephen

    2010-09-06

    Insecticides directed against acetylcholinesterase (AChE) are facing increased resistance among target species as well as increasing concerns for human toxicity. The result has been a resurgence of disease vectors, insects destructive to agriculture, and residential pests. We previously reported a free cysteine (Cys) residue at the entrance to the AChE active site in some insects but not higher vertebrates. We also reported Cys-targeting methanethiosulfonate molecules (AMTSn), which, under conditions that spared human AChE, caused total irreversible inhibition of aphid AChE, 95% inhibition of AChE from the malaria vector mosquito (Anopheles gambia), and >80% inhibition of activity from the yellow fever mosquito (Aedes aegypti) and northern house mosquito (Culex pipiens). We now find the same compounds inhibit AChE from cockroaches (Blattella germanica and Periplaneta americana), the flour beetle (Tribolium confusum), the multi-colored Asian ladybird beetle (Harmonia axyridis), the bed bug (Cimex lectularius), and a wasp (Vespula maculifrons), with IC(50) values of approximately 1-11muM. Our results support further study of Cys-targeting inhibitors as conceptually novel insecticides that may be free of resistance in a range of insect pests and disease vectors and, compared with current compounds, should demonstrate much lower toxicity to mammals, birds, and fish. Copyright (c) 2010 Elsevier Ireland Ltd. All rights reserved.

  4. 2 Assessmen of the Efficiency of Insecticide

    African Journals Online (AJOL)

    Administrator

    malaria vectors and nuisance in West Africa – a-part. 2. Field evaluation. Malar J. 9: 341. Mosqueira B., Duchon S., Chandre F., Hougard, J. M., Carnevale P. and Mas-Coma S. (2010). Efficacy of an insecticide paint against insecticide- susceptible and resistant mosquitoes – b- Part 1: Laboratory evaluation. Malar J. 9: 340.

  5. Trifluoromethylphenyl amides as novel insecticides and fungicides

    Science.gov (United States)

    Because of increased resistance to insecticides in arthropods, it is necessary to identify new chemicals that may have novel modes of action. Following an extensive literature search for compounds with insecticidal and mosquito repellent activity, we have designed and synthesized a set of 20 trifluo...

  6. Insecticide Resistance Reducing Effectiveness of Malaria Control

    Centers for Disease Control (CDC) Podcasts

    2007-01-24

    Malaria prevention is increasingly insecticide based. Dr. John Gimnig, an entomologist with the Division of Parasitic Diseases, CDC, discusses evidence that mosquito resistance to insecticides, which is measured in the laboratory, could compromise malaria prevention in the field.  Created: 1/24/2007 by Emerging Infectious Diseases.   Date Released: 3/13/2007.

  7. Root Formation in Ethylene-Insensitive Plants1

    Science.gov (United States)

    Clark, David G.; Gubrium, Erika K.; Barrett, James E.; Nell, Terril A.; Klee, Harry J.

    1999-01-01

    Experiments with ethylene-insensitive tomato (Lycopersicon esculentum) and petunia (Petunia × hybrida) plants were conducted to determine if normal or adventitious root formation is affected by ethylene insensitivity. Ethylene-insensitive Never ripe (NR) tomato plants produced more belowground root mass but fewer aboveground adventitious roots than wild-type Pearson plants. Applied auxin (indole-3-butyric acid) increased adventitious root formation on vegetative stem cuttings of wild-type plants but had little or no effect on rooting of NR plants. Reduced adventitious root formation was also observed in ethylene-insensitive transgenic petunia plants. Applied 1-aminocyclopropane-1-carboxylic acid increased adventitious root formation on vegetative stem cuttings from NR and wild-type plants, but NR cuttings produced fewer adventitious roots than wild-type cuttings. These data suggest that the promotive effect of auxin on adventitious rooting is influenced by ethylene responsiveness. Seedling root growth of tomato in response to mechanical impedance was also influenced by ethylene sensitivity. Ninety-six percent of wild-type seedlings germinated and grown on sand for 7 d grew normal roots into the medium, whereas 47% of NR seedlings displayed elongated taproots, shortened hypocotyls, and did not penetrate the medium. These data indicate that ethylene has a critical role in various responses of roots to environmental stimuli. PMID:10482660

  8. Design of delay insensitive circuits using multi-ring structures

    DEFF Research Database (Denmark)

    Sparsø, Jens; Staunstrup, Jørgen; Dantzer-Sørensen, Michael

    1992-01-01

    The design and VLSI implementation of a delay insensitive circuit that computes the inner product of two vec·tors is described. The circuit is based on an iterative serial-parallel multiplication algorithm. The design is based on a data flow approach using pipelines and rings that are combined...

  9. Gender insensitivity and male bias in local advertising | Mate ...

    African Journals Online (AJOL)

    Gender insensitivity and male bias in local advertising. Rekopantswe Mate. Full Text: EMAIL FULL TEXT EMAIL FULL TEXT · DOWNLOAD FULL TEXT DOWNLOAD FULL TEXT · http://dx.doi.org/10.4314/safere.v3i1.23952 · AJOL African Journals Online. HOW TO USE AJOL... for Researchers · for Librarians · for Authors ...

  10. Acetylcholinesterase inhibitory effects of some plants from Rosaceae

    Directory of Open Access Journals (Sweden)

    S. Esmaeili

    2015-10-01

    Full Text Available Background and objectives: Alzheimer's disease (AD is an age dependent disorder. AD is associated with decrease of brain acetylcholine level. Nowadays, one of the methods for progression inhibition of AD is using acetylcholinesterase inhibitors. Rosaceae is a large plant family. Different biological effects of some species of this family have been reported. The aim of the present study was to assess the acetylcholinesterase inhibitory (AChEI activity of the selected plants belonging to Rosaceae family. Methods: AChEI activity of six species from Rosaceae including Cotoneaster nummularia, Cerasus microcarpa, Amygdalus scoparia, Agrimonia eupatoria, Rosa canina and Rosa damascena were evaluated based on Ellman’s method in concentration of 300 µg/mL using total extracts and methanol fractions which were obtained by maceration. Results: The results showed that the total extract and methanol fraction of the aerial parts of A. eupatoria demonstrated significant AChEI activity with 46.5% and 56.2% inhibition of the enzyme, respectively. Conclusion: According to the results of the AChEI activity of the methanol fraction of A. eupatoria, it seems that the polar components of the species such as flavonoids may be responsible for its effectiveness.

  11. Old and new acetylcholinesterase inhibitors for Alzheimer's disease.

    Science.gov (United States)

    Galimberti, Daniela; Scarpini, Elio

    2016-10-01

    To date, pharmacological treatment of Alzheimer's disease (AD) includes Acetylcholinesterase Inhibitors (AChEIs) for mild-to-moderate AD, and memantine for moderate-to-severe AD. AChEIs reversibly inhibit acetylcholinesterase (AChE), thus increasing the availability of acetylcholine in cholinergic synapses, enhancing cholinergic transmission. These drugs provide symptomatic short-term benefits, without clearly counteracting the progression of the disease. On the wake of successful clinical trials which lead to the marketing of AChEIs donepezil, rivastigmine and galantamine, many compounds with AChEI properties have been developed and tested mainly in Phase I-II clinical trials in the last twenty years. Here, we review clinical trials initiated and interrupted, and those ongoing so far. Despite many clinical trials with novel AChEIs have been carried out after the registration of those currently used to treat mild to moderate AD, none so far has been successful in a Phase III trial and marketed. Alzheimer's disease is a complex multifactorial disorder, therefore therapy should likely address not only the cholinergic system but also additional neurotransmitters. Moreover, such treatments should be started in very mild phases of the disease, and preventive strategies addressed in elderly people.

  12. Language impairment in Alzheimer's disease and benefits of acetylcholinesterase inhibitors

    Directory of Open Access Journals (Sweden)

    Ferris SH

    2013-08-01

    Full Text Available Steven H Ferris,1 Martin Farlow21Alzheimer's Disease Center, Comprehensive Center on Brain Aging, New York University Langone Medical Center, New York, NY, 2Department of Neurology, Indiana University School of Medicine, Indianapolis, IN, USAAbstract: Alzheimer's disease is characterized by progressively worsening deficits in several cognitive domains, including language. Language impairment in Alzheimer's disease primarily occurs because of decline in semantic and pragmatic levels of language processing. Given the centrality of language to cognitive function, a number of language-specific scales have been developed to assess language deficits throughout progression of the disease and to evaluate the effects of pharmacotherapy on language function. Trials of acetylcholinesterase inhibitors, used for the treatment of clinical symptoms of Alzheimer's disease, have generally focused on overall cognitive effects. However, in the current report, we review data indicating specific beneficial effects of acetylcholinesterase inhibitors on language abilities in patients with Alzheimer’s disease, with a particular focus on outcomes among patients in the moderate and severe disease stages, during which communication is at risk and preservation is particularly important.Keywords: Alzheimer's disease, donepezil, cognition, language, communication, clinical trials

  13. Acetylcholinesterase inhibition by somes promising Brazilian medicinal plants.

    Science.gov (United States)

    Feitosa, C M; Freitas, R M; Luz, N N N; Bezerra, M Z B; Trevisan, M T S

    2011-08-01

    A microplate assay and a thin-layer chromatography (TLC) "in situ" assay based on the Ellman assay was used to screen for acetylcholinesterase inhibitors from ethyl acetate and methanol extracts of Brazilian medicinal plants of families that, according to the literature, have traditional uses that might be connected with acetylcholinesterase inhibition. Eighteen species belonging to Convolvulaceae, Crassulaceae, Euphorbiaceae, Leguminosae, Malvaceae, Moraceae, Nyctaginaceae and Rutaceae families were tested. The most active plants were Ipomoea asarifolia (IC50 = 0.12 mg/mL), Jatropha curcas (IC50 = 0.25 mg/mL), Jatropha gossypiifolia (IC50 = 0.05 mg/mL), Kalanchoe brasiliensis (IC50 = 0.16 mg/mL) and Senna alata (IC50 = 0.08 mg/mL). The most promising extracts were the Jatropha gossypiifolia and Senna alata species assuming there were compounds with a similar activity to galanthamine, which should contain about 1% of an active compound, or if present at lower levels even more active compounds than galanthamine (IC50 = 0.37 x 10-3 mg/mL) should be present.

  14. Acetylcholinesterase inhibition by somes promising Brazilian medicinal plants

    Directory of Open Access Journals (Sweden)

    CM. Feitosa

    Full Text Available A microplate assay and a thin-layer chromatography (TLC "in situ" assay based on the Ellman assay was used to screen for acetylcholinesterase inhibitors from ethyl acetate and methanol extracts of Brazilian medicinal plants of families that, according to the literature, have traditional uses that might be connected with acetylcholinesterase inhibition. Eighteen species belonging to Convolvulaceae, Crassulaceae, Euphorbiaceae, Leguminosae, Malvaceae, Moraceae, Nyctaginaceae and Rutaceae families were tested. The most active plants were Ipomoea asarifolia (IC50 = 0.12 mg/mL, Jatropha curcas (IC50 = 0.25 mg/mL, Jatropha gossypiifolia (IC50 = 0.05 mg/mL, Kalanchoe brasiliensis (IC50 = 0.16 mg/mL and Senna alata (IC50 = 0.08 mg/mL. The most promising extracts were the Jatropha gossypiifolia and Senna alata species assuming there were compounds with a similar activity to galanthamine, which should contain about 1% of an active compound, or if present at lower levels even more active compounds than galanthamine (IC50 = 0.37 x 10-3 mg/mL should be present.

  15. Antioxidant Activity and Acetylcholinesterase Inhibition of Grape Skin Anthocyanin (GSA

    Directory of Open Access Journals (Sweden)

    Mehnaz Pervin

    2014-07-01

    Full Text Available We aimed to investigate the antioxidant and acetylcholinesterase inhibitory activities of the anthocyanin rich extract of grape skin. Grape skin anthocyanin (GSA neutralized free radicals in different test systems, such as 2,-2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS and 2,2-diphenyl-1-picrylhydrazyl (DPPH assays, to form complexes with Fe2+ preventing 2,2'-azobis(2-amidinopropane dihydrochloride (AAPH-induced erythrocyte hemolysis and oxidative DNA damage. Moreover, GSA decreased reactive oxygen species (ROS generation in isolated mitochondria thus inhibiting 2',-7'-dichlorofluorescin (DCFH oxidation. In an in vivo study, female BALB/c mice were administered GSA, at 12.5, 25, and 50 mg per kg per day orally for 30 consecutive days. Herein, we demonstrate that GSA administration significantly elevated the level of antioxidant enzymes in mice sera, livers, and brains. Furthermore, GSA inhibited acetylcholinesterase (AChE in the in vitro assay with an IC50 value of 363.61 µg/mL. Therefore, GSA could be an excellent source of antioxidants and its inhibition of cholinesterase is of interest with regard to neurodegenerative disorders such as Alzheimer’s disease.

  16. of Several Organophosphorus Insecticide Metabolites

    Directory of Open Access Journals (Sweden)

    Russell L. Carr

    2015-01-01

    Full Text Available Paraoxonase (PON1 is a calcium dependent enzyme that is capable of hydrolyzing organophosphate anticholinesterases. PON1 activity is present in most mammals and previous research established that PON1 activity differs depending on the species. These studies mainly used the organophosphate substrate paraoxon, the active metabolite of the insecticide parathion. Using serum PON1 from different mammalian species, we compared the hydrolysis of paraoxon with the hydrolysis of the active metabolites (oxons of two additional organophosphorus insecticides, methyl parathion and chlorpyrifos. Paraoxon hydrolysis was greater than that of methyl paraoxon, but the level of activity between species displayed a similar pattern. Regardless of the species tested, the hydrolysis of chlorpyrifos-oxon was significantly greater than that of paraoxon or methyl paraoxon. These data indicate that chlorpyrifos-oxon is a better substrate for PON1 regardless of the species. The pattern of species differences in PON1 activity varied with the change in substrate to chlorpyrifos-oxon from paraoxon or methyl paraoxon. For example, the sex difference observed here and reported elsewhere in the literature for rat PON1 hydrolysis of paraoxon was not present when chlorpyrifos-oxon was the substrate.

  17. Insecticide resistance and intracellular proteases.

    Science.gov (United States)

    Wilkins, Richard M

    2017-12-01

    Pesticide resistance is an example of evolution in action with mechanisms of resistance arising from mutations or increased expression of intrinsic genes. Intracellular proteases have a key role in maintaining healthy cells and in responding to stressors such as pesticides. Insecticide-resistant insects have constitutively elevated intracellular protease activity compared to corresponding susceptible strains. This increase was shown for some cases originally through biochemical enzyme studies and subsequently putatively by transcriptomics and proteomics methods. Upregulation and expression of proteases have been characterised in resistant strains of some insect species, including mosquitoes. This increase in proteolysis results in more degradation products (amino acids) of intracellular proteins. These may be utilised in the resistant strain to better protect the cell from stress. There are changes in insect intracellular proteases shortly after insecticide exposure, suggesting a role in stress response. The use of protease and proteasome inhibitors or peptide mimetics as synergists with improved application techniques and through protease gene knockdown using RNA interference (possibly expressed in crop plants) may be potential pest management strategies, in situations where elevated intracellular proteases are relevant. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

  18. Mechanisms of insecticide resistance in field populations of Aedes aegypti (L.) from Quintana Roo, Southern Mexico.

    Science.gov (United States)

    Flores, Adriana E; Grajales, Jaime Salomon; Salas, Ildefonso Fernandez; Garcia, Gustavo Ponce; Becerra, Ma Haydee Loaiza; Lozano, Saul; Brogdon, William G; Black, William C; Beaty, Barry

    2006-12-01

    Potential insecticide-resistance mechanisms were studied with the use of biochemical assays in Aedes aegypti (L.) collected from 5 municipalities representing the north part of Quintana Roo: Benito Juarez, Cozumel, Isla Mujeres, Lazaro Cardenas, and Solidaridad. The activities of alpha and beta esterases, mixed-function oxidases (MFO), glutathione-S-transferase (GST), acethylcholinesterase (AChE), and insensitive acethylcholinesterase (iAChE) were assayed in microplates. Three replicates were performed for each enzyme and 60 males and 60 females were analyzed in each population. The New Orleans (NO) susceptible strain of Ae. aegypti was used as a susceptible reference and the threshold criteria for each enzyme were the highest NO absorbance values. In none of the 6 tests were absorbance values correlated in males and females. alpha esterases were elevated in Benito Juarez, Cozumel females and in Lazaro Cardenas males and females. beta esterases were elevated in Benito Juarez, Cozumel females and in Cozumel and Lazaro Cardenas males. Elevated esterases suggest potential insecticide-resistance mechanisms against organophosphate, carbamate, and some pyrethroid insecticides. Slightly elevated levels of MFOs appeared in Lazaro Cardenas females and in Cozumel, Isla Mujeres, and Solidaridad males. Mechanisms involving iAChE or GST were not apparent.

  19. Susceptibility profile of Aedes aegypti from Santiago Island, Cabo Verde, to insecticides.

    Science.gov (United States)

    Rocha, Hélio Daniel Ribeiro; Paiva, Marcelo Henrique Santos; Silva, Norma Machado; de Araújo, Ana Paula; Camacho, Denise Dos Reis da Rosa de Azevedo; Moura, Aires Januário Fernandes da; Gómez, Lara Ferrero; Ayres, Constância Flávia Junqueira; Santos, Maria Alice Varjal de Melo

    2015-12-01

    In 2009, Cabo Verde diagnosed the first dengue cases, with 21,137 cases reported and Aedes aegypti was identified as the vector. Since the outbreak, chemical insecticides and source reduction were used to control the mosquito population. This study aimed to assess the susceptibility of A. aegypti populations from Santiago, Cabo Verde to insecticides and identify the mechanisms of resistance. Samples of A. aegypti eggs were obtained at two different time periods (2012 and 2014), using ovitraps in different locations in Santiago Island to establish the parental population. F1 larvae were exposed to different concentrations of insecticides (Bacillus thuringiensis var israelensis (Bti), diflubenzuron and temephos) to estimate the lethal concentrations (LC90) and calculate the respective rate of resistance (RR90). Semi-field tests using temephos-ABATE(®) were performed to evaluate the persistence of the product. Bottle tests using female mosquitoes were carried out to determine the susceptibility to the adulticides malathion, cypermethrin and deltamethrin. Biochemical and molecular tests were performed to investigate the presence of metabolic resistance mechanisms, associated with the enzymes glutathione S-transferases (GSTs), esterases and mixed-function oxidases (MFO) and to detect mutations or alterations in the sodium channel and acetylcholinesterase genes. A. aegypti mosquitoes from Santiago exhibited resistance to deltamethrin, cypermethrin (mortality<80%) and temephos (RR90=4.4) but susceptibility to malathion (mortality≥98%), Bti and diflubenzuron. The low level of resistance to temephos did not affect the effectiveness of Abate(®). The enzymatic analysis conducted in 2012 revealed slight changes in the activities of GST (25%), MFO (18%), α-esterase (19%) and β-esterase (17%), but no significant changes in 2014. Target site resistance mutations were not detected. Our results suggest that the A. aegypti population from Santiago is resistant to two major

  20. Insecticide control of vector-borne diseases: when is insecticide resistance a problem?

    Directory of Open Access Journals (Sweden)

    Ana Rivero

    Full Text Available Many of the most dangerous human diseases are transmitted by insect vectors. After decades of repeated insecticide use, all of these vector species have demonstrated the capacity to evolve resistance to insecticides. Insecticide resistance is generally considered to undermine control of vector-transmitted diseases because it increases the number of vectors that survive the insecticide treatment. Disease control failure, however, need not follow from vector control failure. Here, we review evidence that insecticide resistance may have an impact on the quality of vectors and, specifically, on three key determinants of parasite transmission: vector longevity, competence, and behaviour. We argue that, in some instances, insecticide resistance is likely to result in a decrease in vector longevity, a decrease in infectiousness, or in a change in behaviour, all of which will reduce the vectorial capacity of the insect. If this effect is sufficiently large, the impact of insecticide resistance on disease management may not be as detrimental as previously thought. In other instances, however, insecticide resistance may have the opposite effect, increasing the insect's vectorial capacity, which may lead to a dramatic increase in the transmission of the disease and even to a higher prevalence than in the absence of insecticides. Either way-and there may be no simple generality-the consequence of the evolution of insecticide resistance for disease ecology deserves additional attention.

  1. Weevil x Insecticide: Does 'Personality' Matter?

    Science.gov (United States)

    Morales, Juliana A; Cardoso, Danúbia G; Della Lucia, Terezinha Maria C; Guedes, Raul Narciso C

    2013-01-01

    An insect's behavior is the expression of its integrated physiology in response to external and internal stimuli, turning insect behavior into a potential determinant of insecticide exposure. Behavioral traits may therefore influence insecticide efficacy against insects, compromising the validity of standard bioassays of insecticide activity, which are fundamentally based on lethality alone. By extension, insect 'personality' (i.e., an individual's integrated set of behavioral tendencies that is inferred from multiple empirical measures) may also be an important determinant of insecticide exposure and activity. This has yet to be considered because the behavioral studies involving insects and insecticides focus on populations rather than on individuals. Even among studies of animal 'personality', the relative contributions of individual and population variation are usually neglected. Here, we assessed behavioral traits (within the categories: activity, boldness/shyness, and exploration/avoidance) of individuals from 15 populations of the maize weevil (Sitophilus zeamais), an important stored-grain pest with serious problems of insecticide resistance, and correlated the behavioral responses with the activity of the insecticide deltamethrin. This analysis was performed at both the population and individual levels. There was significant variation in weevil 'personality' among individuals and populations, but variation among individuals within populations accounted for most of the observed variation (92.57%). This result emphasizes the importance of individual variation in behavioral and 'personality' studies. When the behavioral traits assessed were correlated with median lethal time (LT50) at the population level and with the survival time under insecticide exposure, activity traits, particularly the distance walked, significantly increased survival time. Therefore, behavioral traits are important components of insecticide efficacy, and individual variation should be

  2. Research Advances and Detection Methodologies for Microbe-Derived Acetylcholinesterase Inhibitors: A Systemic Review

    Directory of Open Access Journals (Sweden)

    Jingqian Su

    2017-01-01

    Full Text Available Acetylcholinesterase inhibitors (AChEIs are an attractive research subject owing to their potential applications in the treatment of neurodegenerative diseases. Fungi and bacteria are major producers of AChEIs. Their active ingredients of fermentation products include alkaloids, terpenoids, phenylpropanoids, and steroids. A variety of in vitro acetylcholinesterase inhibitor assays have been developed and used to measure the activity of acetylcholinesterases, including modified Ellman’s method, thin layer chromatography bioautography, and the combined liquid chromatography-mass spectrometry/modified Ellman’s method. In this review, we provide an overview of the different detection methodologies, the microbe-derived AChEIs, and their producing strains.

  3. Fungal degradation of organophosphorous insecticides

    Energy Technology Data Exchange (ETDEWEB)

    Bumpus, J.A. [Notre Dame Univ., IN (United States); Kakar, S.N.; Coleman, R.D. [Argonne National Lab., IL (United States)

    1992-07-01

    Organophosphorous insecticides are used extensively to treat a variety of pests and insects. Although as a group they are easily degraded by bacteria in the environment, a number of them have half-lives of several months. Little is known about their biodegradation by fungi. We have shown that Phanerochaete chrysosporium can substantially degrade chlorpyrifos, fonofos, and terbufos (27.5%, 12.2%, and 26.6%, respectively) during 18-day incubation in nitrogen-limited stationary cultures. The results demonstrate that the clorinated pyridinyl ring of chlorpyrifos and the phenyl ring of fonofos undergo ring cleavage during biodegradation by the fungus. The usefulness of the fungus system for bioremediation is discussed. 16 refs., 7 figs., 2 tabs.

  4. Fungal degradation of organophosphorous insecticides

    Energy Technology Data Exchange (ETDEWEB)

    Bumpus, J.A. (Notre Dame Univ., IN (United States)); Kakar, S.N.; Coleman, R.D. (Argonne National Lab., IL (United States))

    1992-01-01

    Organophosphorous insecticides are used extensively to treat a variety of pests and insects. Although as a group they are easily degraded by bacteria in the environment, a number of them have half-lives of several months. Little is known about their biodegradation by fungi. We have shown that Phanerochaete chrysosporium can substantially degrade chlorpyrifos, fonofos, and terbufos (27.5%, 12.2%, and 26.6%, respectively) during 18-day incubation in nitrogen-limited stationary cultures. The results demonstrate that the clorinated pyridinyl ring of chlorpyrifos and the phenyl ring of fonofos undergo ring cleavage during biodegradation by the fungus. The usefulness of the fungus system for bioremediation is discussed. 16 refs., 7 figs., 2 tabs.

  5. Load Insensitive, Low Voltage Quadrature Oscillator Using Single Active Element

    Directory of Open Access Journals (Sweden)

    Jitendra Mohan

    2017-01-01

    Full Text Available In this paper, a load insensitive quadrature oscillator using single differential voltage dual-X second generation current conveyor operated at low voltage is proposed. The proposed circuit employs single active element, three grounded resistors and two grounded capacitors. The proposed oscillator offers two load insensitive quadrature current outputs and three quadrature voltage outputs simultaneously. Effects of non-idealities along with the effects of parasitic are further studied. The proposed circuit enjoys the feature of low active and passive sensitivities. Additionally, a resistorless realization of the proposed quadrature oscillator is also explored. Simulation results using PSPICE program on cadence tool using 90 nm Complementary Metal Oxide Semiconductor (CMOS process parameters confirm the validity and practical utility of the proposed circuit.

  6. High Efficiency Acetylcholinesterase Immobilization on DNA Aptamer Modified Surfaces

    Directory of Open Access Journals (Sweden)

    Orada Chumphukam

    2014-04-01

    Full Text Available We report here the in vitro selection of DNA aptamers for electric eel acetylcholinesterase (AChE. One selected aptamer sequence (R15/19 has a high affinity towards the enzyme (Kd = 157 ± 42 pM. Characterization of the aptamer showed its binding is not affected by low ionic strength (~20 mM, however significant reduction in affinity occurred at high ionic strength (~1.2 M. In addition, this aptamer does not inhibit the catalytic activity of AChE that we exploit through immobilization of the DNA on a streptavidin-coated surface. Subsequent immobilization of AChE by the aptamer results in a 4-fold higher catalytic activity when compared to adsorption directly on to plastic.

  7. Interleukin 6 modulates acetylcholinesterase activity of brain neurons

    International Nuclear Information System (INIS)

    Clarencon, D.; Multon, E.; Galonnier, M.; Estrade, M.; Fournier, C.; Mathieu, J.; Mestries, J.C.; Testylier, G.; Fatome, M.

    1995-01-01

    Classically, radiation injuries results in a peripheral inflammatory process, and we have previously observed an early systemic interleukin 6 (IL-6) release following whole-body irradiation. Besides, we have demonstrated an early decrease of rat or primate brain acetylcholinesterase (AChE) activity a gamma exposure. The object of the present study is to find possible IL-6 systemic effects on the brain AChE activity. We show that, though intravenous (i.v.) or intra-cerebro-ventricular (ICV) injection of IL-6 can induce a drop in rat brain AChE activity, this cytokine induces only a slight decrease of the AChE release in cultured brain cells. (author)

  8. Comedication and Treatment Length in Users of Acetylcholinesterase Inhibitors

    Directory of Open Access Journals (Sweden)

    Anne Sverdrup Efjestad

    2017-02-01

    Full Text Available Background/Aims: Reduced clinical effect on cognitive decline in dementia by acetylcholinesterase inhibitors (AChEIs may be due to concurrent use of drugs with anticholinergic properties. The aim was to analyze the incidence of AChEI use and comedication with drugs with anticholinergic properties and other potential unfavorable effects. Methods: A prospective study applying drug use data from the Norwegian Prescription Database. Anticholinergic Drug Scale (ADS scores were used as a measure of overall anticholinergic burden. Results: Patients with high ADS scores were more frequently discontinuing treatment early. Coprescribing of antipsychotics was strongly associated with early discontinuation of AChEI treatment. Conclusion: Coprescribing with potentially unfavorable medications was common. A high ADS score was associated with early discontinuation of treatment.

  9. Acetylcholinesterase and Nissl staining in the same histological section.

    Science.gov (United States)

    Shipley, M T; Ennis, M; Behbehani, M M

    1989-12-18

    Acetylcholinesterase (AChE) enzyme histochemistry and Nissl staining are commonly utilized in neural architectonic studies. However, the opaque reaction deposit produced by the most commonly used AChE histochemical methods is not compatible with satisfactory Nissl staining. As a result, precise correlation of AChE and Nissl staining necessitates time-consuming comparisons of adjacent sections which may have differential shrinkage. Here, we have modified the Koelle-Friedenwald histochemical reaction for AChE by omitting the final intensification steps. The modified reaction yields a non-opaque reaction product that is selectively visualized by darkfield illumination. This non-intensified darkfield AChE (NIDA) reaction allows clear visualization of Nissl staining in the same histological section. This combined AChE-Nissl method greatly facilitates detailed correlation of enzyme and cytoarchitectonic organization.

  10. Effect of fluorocarbons on acetylcholinesterase activity and some counter measures

    Science.gov (United States)

    Young, W.; Parker, J. A.

    1975-01-01

    An isolated vagal sympathetic heart system has been successfully used for the study of the effect of fluorocarbons (FCs) on cardiac performance and in situ enzyme activity. Dichlorodifluoromethane sensitizes this preparation to sympathetic stimulation and to exogenous epinephrine challenge. Partial and complete A-V block and even cardiac arrest have been induced by epinephrine challenge in the FC sensitized heart. Potassium chloride alone restores the rhythmicity but not the normal contractility of the heart in such a situation. Addition of glucose will, however, completely restore the normal function of the heart which is sensitized by dichlorodifluoromethane. The ED 50 values of acetylcholinesterase activity which are used as a measure of relative effectiveness of fluorocarbons are compared with the maximum permissible concentration. Kinetic studies indicate that all the fluorocarbons tested so far are noncompetitive.

  11. Evidence of auditory insensitivity to vocalization frequencies in two frogs

    DEFF Research Database (Denmark)

    Goutte, Sandra; Mason, Matthew J; Christensen-Dalsgaard, Jakob

    2017-01-01

    discrimination from background noise and heterospecific calls. However, we present here evidence that two anurans, Brachycephalus ephippium and B. pitanga, are insensitive to the sound of their own calls. Both species produce advertisement calls outside their hearing sensitivity range and their inner ears...... by their high toxicity might help to explain why calling has not yet disappeared, and that visual communication may have replaced auditory in these colourful, diurnal frogs....

  12. Preclinical and first-in-human evaluation of PRX-105, a PEGylated, plant-derived, recombinant human acetylcholinesterase-R

    International Nuclear Information System (INIS)

    Atsmon, Jacob; Brill-Almon, Einat; Nadri-Shay, Carmit; Chertkoff, Raul; Alon, Sari; Shaikevich, Dimitri; Volokhov, Inna; Haim, Kirsten Y.; Bartfeld, Daniel; Shulman, Avidor; Ruderfer, Ilya; Ben-Moshe, Tehila; Shilovitzky, Orit; Soreq, Hermona; Shaaltiel, Yoseph

    2015-01-01

    PRX-105 is a plant-derived recombinant version of the human ‘read-through’ acetylcholinesterase splice variant (AChE-R). Its active site structure is similar to that of the synaptic variant, and it displays the same affinity towards organophosphorus (OP) compounds. As such, PRX-105 may serve as a bio-scavenger for OP pesticides and chemical warfare agents. To assess its potential use in prophylaxis and treatment of OP poisoning we conducted several preliminary tests, reported in this paper. Intravenous (IV) PRX-105 was administered to mice either before or after exposure to an OP toxin. All mice who received an IV dose of 50 nmol/kg PRX-105, 2 min before being exposed to 1.33 × LD 50 and 1.5 × LD 50 of toxin and 10 min after exposure to 1.5 × LD 50 survived. The pharmacokinetic and toxicity profiles of PRX-105 were evaluated in mice and mini-pigs. Following single and multiple IV doses (50 to 200 mg/kg) no deaths occurred and no significant laboratory and histopathological changes were observed. The overall elimination half-life (t ½ ) in mice was 994 (± 173) min. Additionally, a first-in-human study, to assess the safety, tolerability and pharmacokinetics of the compound, was conducted in healthy volunteers. The t ½ in humans was substantially longer than in mice (average 26.7 h). Despite the small number of animals and human subjects who were assessed, the fact that PRX-105 exerts a protective and therapeutic effect following exposure to lethal doses of OP, its favorable safety profile and its relatively long half-life, renders it a promising candidate for treatment and prophylaxis against OP poisoning and warrants further investigation. - Highlights: • PRX-105 is a PEGylated plant-derived recombinant human acetylcholinesterase-R. • PRX-105 is a promising bio-scavenger for organophosphorous toxins at lethal doses. • PRX-105 was shown to protect animals both prophylactically and post-poisoning. • First-in-human study exhibited its safety

  13. Preclinical and first-in-human evaluation of PRX-105, a PEGylated, plant-derived, recombinant human acetylcholinesterase-R

    Energy Technology Data Exchange (ETDEWEB)

    Atsmon, Jacob [Clinical Research Center, Tel Aviv Sourasky Medical Center, Tel Aviv (Israel); Sackler Faculty of Medicine, Tel Aviv University (Israel); Brill-Almon, Einat; Nadri-Shay, Carmit; Chertkoff, Raul; Alon, Sari [Protalix Biotherapeutics, Science Park, Carmiel (Israel); Shaikevich, Dimitri; Volokhov, Inna; Haim, Kirsten Y. [Clinical Research Center, Tel Aviv Sourasky Medical Center, Tel Aviv (Israel); Sackler Faculty of Medicine, Tel Aviv University (Israel); Bartfeld, Daniel [Protalix Biotherapeutics, Science Park, Carmiel (Israel); Shulman, Avidor, E-mail: avidors@protalix.com [Protalix Biotherapeutics, Science Park, Carmiel (Israel); Ruderfer, Ilya; Ben-Moshe, Tehila; Shilovitzky, Orit [Protalix Biotherapeutics, Science Park, Carmiel (Israel); Soreq, Hermona [Department of Biological Chemistry, Institute of Life Sciences, The Hebrew University of Jerusalem (Israel); Shaaltiel, Yoseph [Protalix Biotherapeutics, Science Park, Carmiel (Israel)

    2015-09-15

    PRX-105 is a plant-derived recombinant version of the human ‘read-through’ acetylcholinesterase splice variant (AChE-R). Its active site structure is similar to that of the synaptic variant, and it displays the same affinity towards organophosphorus (OP) compounds. As such, PRX-105 may serve as a bio-scavenger for OP pesticides and chemical warfare agents. To assess its potential use in prophylaxis and treatment of OP poisoning we conducted several preliminary tests, reported in this paper. Intravenous (IV) PRX-105 was administered to mice either before or after exposure to an OP toxin. All mice who received an IV dose of 50 nmol/kg PRX-105, 2 min before being exposed to 1.33 × LD{sub 50} and 1.5 × LD{sub 50} of toxin and 10 min after exposure to 1.5 × LD{sub 50} survived. The pharmacokinetic and toxicity profiles of PRX-105 were evaluated in mice and mini-pigs. Following single and multiple IV doses (50 to 200 mg/kg) no deaths occurred and no significant laboratory and histopathological changes were observed. The overall elimination half-life (t{sub ½}) in mice was 994 (± 173) min. Additionally, a first-in-human study, to assess the safety, tolerability and pharmacokinetics of the compound, was conducted in healthy volunteers. The t{sub ½} in humans was substantially longer than in mice (average 26.7 h). Despite the small number of animals and human subjects who were assessed, the fact that PRX-105 exerts a protective and therapeutic effect following exposure to lethal doses of OP, its favorable safety profile and its relatively long half-life, renders it a promising candidate for treatment and prophylaxis against OP poisoning and warrants further investigation. - Highlights: • PRX-105 is a PEGylated plant-derived recombinant human acetylcholinesterase-R. • PRX-105 is a promising bio-scavenger for organophosphorous toxins at lethal doses. • PRX-105 was shown to protect animals both prophylactically and post-poisoning. • First-in-human study

  14. Transformation of the insecticide teflubenzuron by microorganisms

    NARCIS (Netherlands)

    Finkelstein, Z.I.; Baskunov, B.P.; Rietjens, I.M.C.M.; Boersma, M.G.; Vervoort, J.; Golovleva, L.A.

    2001-01-01

    Transformation of teflubenzuron, the active component in the insecticide commercialized as Nomolt, by soil microorganisms was studied. It was shown that microorganisms, belonging to Bacillus, Alcaligenes, Pseudomonas and Acinetobacter genera are capable to perform the hydrolytic cleavage of the

  15. Modeling Loop Reorganization Free Energies of Acetylcholinesterase: A Comparison of Explicit and Implicit Solvent Models

    National Research Council Canada - National Science Library

    Olson, Mark

    2004-01-01

    ... screening of charge-charge interactions. This paper compares different solvent models applied to the problem of estimating the free-energy difference between two loop conformations in acetylcholinesterase...

  16. EEG SPECTRA, BEHAVIORAL STATES AND MOTOR ACTIVITY IN RATS EXPOSED TO ACETYLCHOLINESTERASE INHIBITOR CHLORPYRIFOS.

    Science.gov (United States)

    Exposure to organophosphate pesticides (OP) has been associated with sleep disorders: insomnia and ?excessive dreaming'. However neuronal mechanisms of these effects have not been analyzed. OP inhibit acetylcholinesterase activity leading to a hyperativity of the brain cholin...

  17. N-[11C]methylpiperidine esters as acetylcholinesterase substrates: an in vivo structure-reactivity study

    International Nuclear Information System (INIS)

    Kilbourn, Michael R.; Nguyen, Thinh B.; Snyder, Scott E.; Sherman, Phillip

    1998-01-01

    A series of simple esters incorporating the N-[ 11 C]methylpiperidine structure were examined as in vivo substrates for acetylcholinesterase in mouse brain. 4-N-[ 11 C]Methylpiperidinyl esters, including the acetate, propionate and isobutyrate esters, are good in vivo substrates for mammalian cholinesterases. Introduction of a methyl group at the 4-position of the 4-piperidinol esters, to form the ester of a teritary alcohol, effectively blocks enzymatic action. Methylation of 4- N-[ 11 C]methylpiperidinyl propionate at the 3-position gives a derivative with increased in vivo reactivity toward acetylcholinesterase. Esters of piperidinecarboxylic acids (nipecotic, isonipecotic and pipecolinic acid ethyl esters) are not hydrolyzed by acetylcholinesterase in vivo, nor do they act as in vivo inhibitors of the enzyme. This study has identified simple methods to both increase and decrease the in vivo reactivity of piperidinyl esters toward acetylcholinesterase

  18. Acetylcholinesterase inhibitory activity of lycopodane-type alkaloids from the Icelandic Lycopodium annotinum ssp. alpestre

    DEFF Research Database (Denmark)

    Halldórsdóttir, Elsa Steinunn; Jaroszewski, Jerzy W; Olafsdottir, Elin Soffia

    2010-01-01

    The aim of this study was to investigate structures and acetylcholinesterase inhibitory activities of lycopodane-type alkaloids isolated from an Icelandic collection of Lycopodium annotinum ssp. alpestre. Ten alkaloids were isolated, including annotinine, annotine, lycodoline, lycoposerramine M...

  19. Triterpenoids from Azorella trifurcata (Gaertn.) Pers and their effect against the enzyme acetylcholinesterase

    Energy Technology Data Exchange (ETDEWEB)

    Areche, Carlos; Cejas, Patricia; Thomas, Pablo; San-Martin, Aurelio [University of Chile, Santiago (Chile). Faculty of Sciences. Dept. of Chemistry], e-mail: aurelio@uchile.cl; Astudillo, Luis; Gutierrez, Margarita [University of Talca, Talca (Chile). Inst. of Chemistry of Natural Resource; Loyola, Luis A. [University of Antofagasta (Chile). Faculty of Basic Sciences. Dept. of Chemistry

    2009-07-01

    The inhibition of the enzyme acetylcholinesterase is considered as a strategy for the treatment of Alzheimer's disease, senile dementia, ataxia, and myasthenia gravis. Three lanostane- and two cycloartane-type triterpenes, together with two mulinane-type diterpenes were isolated from petroleum ether extract of the whole shrub of Azorella trifurcata (Gaertn.) Pers. Their effect on the enzyme acetylcholinesterase was assessed as well. In addition, this is the first report of these triterpenes in the genus Azorella. (author)

  20. Triterpenoids from Azorella trifurcata (Gaertn.) Pers and their effect against the enzyme acetylcholinesterase

    International Nuclear Information System (INIS)

    Areche, Carlos; Cejas, Patricia; Thomas, Pablo; San-Martin, Aurelio; Astudillo, Luis; Gutierrez, Margarita; Loyola, Luis A.

    2009-01-01

    The inhibition of the enzyme acetylcholinesterase is considered as a strategy for the treatment of Alzheimer's disease, senile dementia, ataxia, and myasthenia gravis. Three lanostane- and two cycloartane-type triterpenes, together with two mulinane-type diterpenes were isolated from petroleum ether extract of the whole shrub of Azorella trifurcata (Gaertn.) Pers. Their effect on the enzyme acetylcholinesterase was assessed as well. In addition, this is the first report of these triterpenes in the genus Azorella. (author)

  1. NDIA 2018 IM and EM Technology Symposium: Innovative Insensitive Munition Solutions for Enhanced Warfighter Effectiveness

    Science.gov (United States)

    2018-04-26

    2018 IM & EM TECHNOLOGY SYMPOSIUM INNOVATIVE INSENSITIVE MUNITION SOLUTIONS FOR ENHANCED WARFIGHTER EFFECTIVENESS April 23 – 26, 2018 Doubletree by...IM & EM TECHNOLOGY SYMPOSIUM On behalf of the Insensitive Munitions and Energetic Materials Committee and our MSIAC partner, I would like to...welcome you to the 2018 Insensitive Munitions and Energetic Materials Technology Symposium. This international gathering of the top chemists, system

  2. The Effect of Parathion on Red Blood Cell Acetylcholinesterase in the Wistar Rat

    Directory of Open Access Journals (Sweden)

    Naofumi Bunya

    2016-01-01

    Full Text Available Organophosphorus (OP pesticide poisoning is a significant problem worldwide. Research into new antidotes for these acetylcholinesterase inhibitors, and even optimal doses for current therapies, is hindered by a lack of standardized animal models. In this study, we sought to characterize the effects of the OP pesticide parathion on acetylcholinesterase in a Wistar rat model that included comprehensive medical care. Methods. Male Wistar rats were intubated and mechanically ventilated and then poisoned with between 20 mg/kg and 60 mg/kg of intravenous parathion. Upon developing signs of poisoning, the rats were treated with standard critical care, including atropine, pralidoxime chloride, and midazolam, for up to 48 hours. Acetylcholinesterase activity was determined serially for up to 8 days after poisoning. Results. At all doses of parathion, maximal depression of acetylcholinesterase occurred at 3 hours after poisoning. Acetylcholinesterase recovered to nearly 50% of baseline activity by day 4 in the 20 mg/kg cohort and by day 5 in the 40 and 60 mg/kg cohorts. At day 8, most rats’ acetylcholinesterase had recovered to roughly 70% of baseline. These data should be useful in developing rodent models of acute OP pesticide poisoning.

  3. Modeling global distribution of agricultural insecticides in surface waters.

    Science.gov (United States)

    Ippolito, Alessio; Kattwinkel, Mira; Rasmussen, Jes J; Schäfer, Ralf B; Fornaroli, Riccardo; Liess, Matthias

    2015-03-01

    Agricultural insecticides constitute a major driver of animal biodiversity loss in freshwater ecosystems. However, the global extent of their effects and the spatial extent of exposure remain largely unknown. We applied a spatially explicit model to estimate the potential for agricultural insecticide runoff into streams. Water bodies within 40% of the global land surface were at risk of insecticide runoff. We separated the influence of natural factors and variables under human control determining insecticide runoff. In the northern hemisphere, insecticide runoff presented a latitudinal gradient mainly driven by insecticide application rate; in the southern hemisphere, a combination of daily rainfall intensity, terrain slope, agricultural intensity and insecticide application rate determined the process. The model predicted the upper limit of observed insecticide exposure measured in water bodies (n = 82) in five different countries reasonably well. The study provides a global map of hotspots for insecticide contamination guiding future freshwater management and conservation efforts. Copyright © 2014 Elsevier Ltd. All rights reserved.

  4. Acetylcholinesterase inhibition and gill lesions in Rasbora caverii, an indigenous fish inhabiting rice field associated waterbodies in Sri Lanka.

    Science.gov (United States)

    Wijeyaratne, W M D N; Pathiratne, Asoka

    2006-10-01

    The present study was aimed at applying condition factor (CF), brain acetylcholinesterase (AChE) and gill histology as biomarkers for detecting possible exposure/effect induced by pesticides in fish residing rice field associated waterbodies in Sri Lanka. Biomarkers of an indigenous fish, Rasbora caverii collected from five sampling sites including canals near rice fields, a river and a reservoir (the reference site) were evaluated at four sampling stages covering pesticide application periods during rice cultivation season in 2004. Results indicated that CF of the fish did not show significant alterations regardless of the sampling sites or sampling stages. Site specific differences in AChE activities of the fish were not evident either prior to application of pesticides or at 7 days after Paraquat application to the rice fields. Two days after the application of a mixture of Fenthion and Phenthoate to the rice fields, AChE activity of the fish collected from canals near rice fields was significantly depressed (65-75%) compared to the fish in the reference site. The activities remain depressed to 50-56% even at 65 days after the insecticides application. Laboratory studies showed that prior exposure of R. caverii to Paraquat (2 microg l(-1), 7 days) enhanced the extent of inhibition of brain AChE activity induced by Fenthion (3 microg l(-1)) or a mixture of Fenthion (3 microg l(-1)) and Phenthoate (5 microg l(-1)). Gills of fish collected from canals near rice fields exhibited abnormal multiple divisions at the tips of some secondary lamellae in addition to hyperplasia, hypertrophy and club shaped deformities. Results indicate that application of pesticides in rice culture could manifest a threat to native fish populations residing rice field associated waterbodies. The response of brain AChE and histological changes in the gills of R. caverii allowed differentiating sampling sites after insecticide applications to the rice fields. Hence, R. caverii may be

  5. The activity of detoxifying enzymes in the infective juveniles of Heterorhabditis bacteriophora strains: Purification and characterization of two acetylcholinesterases.

    Science.gov (United States)

    Mohamed, Magda A; Mahdy, El-Sayed M E; Ghazy, Abd-El-Hady M; Ibrahim, Nihal M; El-Mezayen, Hatem A; Ghanem, Manal M E

    2016-02-01

    The infectivity and detoxifying enzyme activities including glutathione-S-transferase (GST), acetylcholinesterase (AChE) and carboxylesterase (CaE) are investigated in the infective juveniles (IJs) of six different strains of Heterorhabditis bacteriophora as a biocontrol agent against insect pests. The specific activities ranged from 10.8-29.8 and 50-220units/mg protein for GST and AChE, respectively; and from 24.7-129 and 22.6-77.3units/mg protein for CaE as estimated by P-nitrophenyl and α-naphthyl acetates, respectively. H. bacteriophora EM2 strain has the highest infectivity and the highest enzymatic activities as well. AChE is the predominant detoxifying enzyme that might imply its major role in the detoxification of insecticide(s). The isoenzyme pattern demonstrated two major slow-moving isoforms in all EPN strains examined. Purification of two AChE isoforms, AChEAII and AChEBI, from H. bacteriophora EM2 strain is performed by ammonium sulfate precipitation, gel filtration on Sephacryl S-200 and chromatography on DEAE-Sepharose. AChEAII and AChEBII have specific activities of 1207 and 1560unit/mg protein, native molecular weights of 180 and 68kDa, and are found in dimeric and monomeric forms, respectively. Both isoforms showed optimum activity at pH8.5 and 35°C. AChEBI exhibited higher thermal stability and higher activation energy than AChEAII. The enzymatic activities of purified AChEs are completely inhibited by Hg(+2) and Ni(+2) and greatly enhanced by Mn(+2). The substrate specificity, the relative efficiency of substrates hydrolysis, substrate inhibition and inhibition by BW284C51, but not by iso-OMPA, clearly indicated that they are true AChEs; their properties are compared with those recorded for insects as target hosts for H. bacteriophora EM2. Copyright © 2015 Elsevier Inc. All rights reserved.

  6. Mapping insecticide resistance and characterization of resistance mechanisms in Anopheles arabiensis (Diptera: Culicidae) in Ethiopia.

    Science.gov (United States)

    Alemayehu, Eba; Asale, Abebe; Eba, Kasahun; Getahun, Kefelegn; Tushune, Kora; Bryon, Astrid; Morou, Evangelia; Vontas, John; Van Leeuwen, Thomas; Duchateau, Luc; Yewhalaw, Delenasaw

    2017-09-02

    The emergence and spread of insecticide resistance in the major African malaria vectors Anopheles gambiae (s.s.) and An. arabiensis may compromise the current vector control interventions and threatens the global malaria control and elimination efforts. Insecticide resistance was monitored in several study sites in Ethiopia from 2013 to 2015 using papers impregnated with discriminating concentrations of DDT, deltamethrin, bendiocarb, propoxur, malathion, fenitrothion and pirimiphos-methyl, following the WHO insecticide susceptibility test procedure. Mosquitoes sampled from different localities for WHO bioassay were morphologically identified as An. gambiae (s.l.) using standard taxonomic keys. Samples were identified to species using species-specific polymerase chain reaction (PCR) and screened for the presence of target site mutations L1014F, L1014S and N1575Y in the voltage gated sodium channel (VGSC) gene and G119S in the acethylcholinesterase (AChE) gene using allele-specific PCR. Biochemical assays were performed to assess elevated levels of acetylcholinesterases, carboxylcholinesterases, glutathione-S-transferases (GSTs) and cytochrome P450s monooxygenases in wild populations of An. arabiensis, compared to the fully susceptible Sekoru An. arabiensis laboratory strain. Populations of An. arabiensis were resistant to DDT and deltamethrin but were susceptible to fenitrothion in all the study sites. Reduced susceptibility to malathion, pirimiphos-methyl, propoxur and bendiocarb was observed in some of the study sites. Knockdown resistance (kdr L1014F) was detected in all mosquito populations with allele frequency ranging from 42 to 91%. Elevated levels of glutathione-S-transferases (GSTs) were detected in some of the mosquito populations. However, no elevated levels of monooxygenases and esterases were detected in any of the populations assessed. Anopheles arabiensis populations from all surveyed sites in Ethiopia exhibited resistance against DDT and pyrethroids

  7. Malaria Vector Control Still Matters despite Insecticide Resistance.

    Science.gov (United States)

    Alout, Haoues; Labbé, Pierrick; Chandre, Fabrice; Cohuet, Anna

    2017-08-01

    Mosquito vectors' resistance to insecticides is usually considered a major threat to the recent progresses in malaria control. However, studies measuring the impact of interventions and insecticide resistance reveal inconsistencies when using entomological versus epidemiological indices. First, evaluation tests that do not reflect the susceptibility of mosquitoes when they are infectious may underestimate insecticide efficacy. Moreover, interactions between insecticide resistance and vectorial capacity reveal nonintuitive outcomes of interventions. Therefore, considering ecological interactions between vector, parasite, and environment highlights that the impact of insecticide resistance on the malaria burden is not straightforward and we suggest that vector control still matters despite insecticide resistance. Copyright © 2017 Elsevier Ltd. All rights reserved.

  8. Temperature-insensitive laser frequency locking near absorption lines

    International Nuclear Information System (INIS)

    Kostinski, Natalie; Olsen, Ben A.; Marsland, Robert III; McGuyer, Bart H.; Happer, William

    2011-01-01

    Combined magnetically induced circular dichroism and Faraday rotation of an atomic vapor are used to develop a variant of the dichroic atomic vapor laser lock that eliminates lock sensitivity to temperature fluctuations of the cell. Operating conditions that eliminate first-order sensitivity to temperature fluctuations can be determined by low-frequency temperature modulation. This temperature-insensitive gyrotropic laser lock can be accurately understood with a simple model, that is in excellent agreement with observations in potassium vapor at laser frequencies in a 2 GHz range about the 770.1 nm absorption line. The methods can be readily adapted for other absorption lines.

  9. A rare case of congenital insensitivity to pain with anhydrosiss

    Directory of Open Access Journals (Sweden)

    Govardhani Yanamadala

    2015-01-01

    Full Text Available Congenital insensitivity to pain syndrome with anhydrosis (CIPA is a rare inherited disorder. It is characterized by loss of pain and temperature sensation, lack of sweating and mild mental retardation. This disorder belongs to hereditary sensory and autonomic neuropathy family (type IV. Because of these abnormalities, patients require special anesthetic care. They include titration of intraoperative opioids, an anesthetic to ensure co-operation and immobility and intra-operative temperature monitoring. Here we report a 7-year-old female child with CIPA posted for restoration and cementation for dental caries along with sural nerve and skin biopsy.

  10. A Comparative Analysis of Perinatal Development of Barrel Cortex in Rat, Mouse and Guinea Pig Using Acetylcholinesterase Histochemistry

    OpenAIRE

    ŞENDEMİR, Erdoğan

    2014-01-01

    The role of acetylcholinesterase (AChE) in the developing neocortex was reexamined by comparing its expression in rats, mice and guinea pigs, following the protocol for acetylcholinesterase histochemistry (described in Sendemir et al., 1996) in order to determine the suitability of the breeding colony at UludaÛ University for use as an animal model. A total of 103 pups as well as two adult animals of each species were used. In the rat pups, acetylcholinesterase-rich patches were d...

  11. Modeling global distribution of agricultural insecticides in surface waters

    International Nuclear Information System (INIS)

    Ippolito, Alessio; Kattwinkel, Mira; Rasmussen, Jes J.; Schäfer, Ralf B.; Fornaroli, Riccardo; Liess, Matthias

    2015-01-01

    Agricultural insecticides constitute a major driver of animal biodiversity loss in freshwater ecosystems. However, the global extent of their effects and the spatial extent of exposure remain largely unknown. We applied a spatially explicit model to estimate the potential for agricultural insecticide runoff into streams. Water bodies within 40% of the global land surface were at risk of insecticide runoff. We separated the influence of natural factors and variables under human control determining insecticide runoff. In the northern hemisphere, insecticide runoff presented a latitudinal gradient mainly driven by insecticide application rate; in the southern hemisphere, a combination of daily rainfall intensity, terrain slope, agricultural intensity and insecticide application rate determined the process. The model predicted the upper limit of observed insecticide exposure measured in water bodies (n = 82) in five different countries reasonably well. The study provides a global map of hotspots for insecticide contamination guiding future freshwater management and conservation efforts. - Highlights: • First global map on insecticide runoff through modelling. • Model predicts upper limit of insecticide exposure when compared to field data. • Water bodies in 40% of global land surface may be at risk of adverse effects. • Insecticide application rate, terrain slope and rainfall main drivers of exposure. - We provide the first global map on insecticide runoff to surface water predicting that water bodies in 40% of global land surface may be at risk of adverse effects

  12. Delay Insensitive Ternary CMOS Logic for Secure Hardware

    Directory of Open Access Journals (Sweden)

    Ravi S. P. Nair

    2015-09-01

    Full Text Available As digital circuit design continues to evolve due to progress of semiconductor processes well into the sub 100 nm range, clocked architectures face limitations in a number of cases where clockless asynchronous architectures generate less noise and produce less electro-magnetic interference (EMI. This paper develops the Delay-Insensitive Ternary Logic (DITL asynchronous design paradigm that combines design aspects of similar dual-rail asynchronous paradigms and Boolean logic to create a single wire per bit, three voltage signaling and logic scheme. DITL is compared with other delay insensitive paradigms, such as Pre-Charge Half-Buffers (PCHB and NULL Convention Logic (NCL on which it is based. An application of DITL is discussed in designing secure digital circuits resistant to side channel attacks based on measurement of timing, power, and EMI signatures. A Secure DITL Adder circuit is designed at the transistor level, and several variance parameters are measured to validate the efficiency of DITL in resisting side channel attacks. The DITL design methodology is then applied to design a secure 8051 ALU.

  13. Investigating the Antioxidant and Acetylcholinesterase Inhibition Activities of Gossypium herbaceam

    Directory of Open Access Journals (Sweden)

    Haji Akber Aisa

    2013-01-01

    Full Text Available Our previous research showed that standardized extract from the flowers of the Gossypium herbaceam labeled GHE had been used in clinical trials for its beneficial effects on brain functions, particularly in connection with age-related dementia and Alzheimer’s disease (AD. The aim of this work was to determine the components of this herb and the individual constituents of GHE. In order to better understand this herb for AD treatment, we investigated the acetylcholinesterase (AChE inhibition and antioxidant activity of GHE as well as the protective effects to PC12 cells against cytotoxicity induced by tertiary butyl hydroperoxide (tBHP using in vitro assays. The antioxidant activities were assessed by measuring their capabilities for scavenging 1,1-diphenyl-2-picylhydrazyl (DPPH and 2-2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS free radical as well as in inhibiting lipid peroxidation. Our data showed that GHE exhibited certain activities against AChE and also is an efficient free radical scavenger, which may be helpful in preventing or alleviating patients suffering from AD.

  14. Neurobehavioral toxicology of pyrethroid insecticides

    International Nuclear Information System (INIS)

    Crofton, K.M.

    1986-01-01

    Pyrethroid insecticides are classified as either Type I or Type II based upon in vivo toxic signs, and neurophysiological and biochemical data. Both axonal sodium channels and the γ-aminobutyric acid (GABA) receptor complex have been proposed as the major site of action of the Type II pyrethroids. This investigation characterized the behavior and biochemical effects of low dosages of pyrethroids in rats. Type I and II pyrethroids were tested for effects on figure-eight maze activity and the acoustic startle response (ASR). All compounds decreased figure-eight maze activity. Interactions of Type I and II pyrethroids with the three major binding sites on the GABA complex were determined in vivo. Radioligand binding experiments assessed in vitro interactions of pyrethroids with the three major GABA-complex binding sites. None of the pyrethroids competed for [ 3 H]-muscimol or [ 3 H]-flunitrazepam binding. Only Type II pyrethroids inhibited binding of [ 35 S]-t-butylbicyclophosphorothionate (TBPS) in cortical synaptosome preparations with K/sub i/ values of 5 to 10 μM. The [ 35 S]-TBPS data implicate the TBPS/picrotoxinin binding site in the mechanism of Type II pyrethroid toxicity. The results of these experiments support the classification of pyrethroids into two classes, and demonstrate the utility of the figure-eight maze and the ASR in studies to elucidate neurotoxic mechanisms. The interaction of the Type II pyrethroids is probably restricted to the TBPS/picrotoxinin binding domain on the GABA complex as shown by both the in vivo and in vitro studies

  15. Design of a macroalgae amperometric biosensor; application to the rapid monitoring of organophosphate insecticides in an agroecosystem.

    Science.gov (United States)

    Nunes, G S; Lins, J A P; Silva, F G S; Araujo, L C; Silva, F E P S; Mendonça, C D; Badea, M; Hayat, A; Marty, J-L

    2014-09-01

    The immobilization of enzymes onto transducer support is a mature technology and has been successfully implemented to improve biocatalytic processes for diverse applications. However, there exists still need to design more sophisticated and specialized strategies to enhance the functional properties of the biosensors. In this work, a biosensor platform based on innovative fabrication strategy was designed, and employed for the detection of organophosphate (OP) in natural waters. The biosensor was prepared by incorporating acetylcholinesterase enzyme (AChE) to the graphite paste modified with tetracyanoquinodimethane (TCNQ) mediator, along with the use of a macroalgae (Cladaphropsis membranous) as a functional immobilization support. The novel immobilization design resulted in a synergic effect, and led to enhanced stability and sensitivity of the biosensor. The designed biosensor was used to analyze methyl parathion OP insecticide in water samples collected from a demonstrably contaminated lake of São Luis Island, Maranhão, Northeast of Brazil. Water analysis revealed that the aquatic ecosystem was polluted by sub-ppm concentrations of the OP insecticide, and a good correlation was found between values obtained through biosensor and GC-MS techniques. Our results demonstrated that macroalgae-biosensor could be used as a low-cost and sensitive screening method to detect target analyte. Copyright © 2014 Elsevier Ltd. All rights reserved.

  16. Acute administration of fenproporex increased acetylcholinesterase activity in brain of young rats.

    Science.gov (United States)

    Teodorak, Brena P; Ferreira, Gabriela K; Scaini, Giselli; Wessler, Letícia B; Heylmann, Alexandra S; Deroza, Pedro; Valvassori, Samira S; Zugno, Alexandra I; Quevedo, João; Streck, Emilio L

    2015-08-01

    Fenproporex is the second most commonly amphetamine-based anorectic consumed worldwide; this drug is rapidly converted into amphetamine, in vivo, and acts by increasing dopamine levels in the synaptic cleft. Considering that fenproporex effects on the central nervous system are still poorly known and that acetylcholinesterase is a regulatory enzyme which is involved in cholinergic synapses and may indirectly modulate the release of dopamine, the present study investigated the effects of acute administration of fenproporex on acetylcholinesterase activity in brain of young rats. Young male Wistar rats received a single injection of fenproporex (6.25, 12.5 or 25mg/kg i.p.) or vehicle (2% Tween 80). Two hours after the injection, the rats were killed by decapitation and the brain was removed for evaluation of acetylcholinesterase activity. Results showed that fenproporex administration increased acetylcholinesterase activity in the hippocampus and posterior cortex, whereas in the prefrontal cortex, striatum and cerebellum the enzyme activity was not altered. In conclusion, in the present study we demonstrated that acute administration of fenproporex exerts an effect in the cholinergic system causing an increase in the activity of acetylcholinesterase in a dose-dependent manner in the hippocampus and posterior cortex. Thus, we suggest that the imbalance in cholinergic homeostasis could be considered as an important pathophysiological mechanism underlying the brain damage observed in patients who use amphetamines such as fenproporex.

  17. Acute administration of fenproporex increased acetylcholinesterase activity in brain of young rats

    Directory of Open Access Journals (Sweden)

    BRENA P. TEODORAK

    2015-08-01

    Full Text Available Fenproporex is the second most commonly amphetamine-based anorectic consumed worldwide; this drug is rapidly converted into amphetamine, in vivo, and acts by increasing dopamine levels in the synaptic cleft. Considering that fenproporex effects on the central nervous system are still poorly known and that acetylcholinesterase is a regulatory enzyme which is involved in cholinergic synapses and may indirectly modulate the release of dopamine, the present study investigated the effects of acute administration of fenproporex on acetylcholinesterase activity in brain of young rats. Young male Wistar rats received a single injection of fenproporex (6.25, 12.5 or 25mg/kg i.p. or vehicle (2% Tween 80. Two hours after the injection, the rats were killed by decapitation and the brain was removed for evaluation of acetylcholinesterase activity. Results showed that fenproporex administration increased acetylcholinesterase activity in the hippocampus and posterior cortex, whereas in the prefrontal cortex, striatum and cerebellum the enzyme activity was not altered. In conclusion, in the present study we demonstrated that acute administration of fenproporex exerts an effect in the cholinergic system causing an increase in the activity of acetylcholinesterase in a dose-dependent manner in the hippocampus and posterior cortex. Thus, we suggest that the imbalance in cholinergic homeostasis could be considered as an important pathophysiological mechanism underlying the brain damage observed in patients who use amphetamines such as fenproporex.

  18. Insecticide susceptibility status of human biting mosquitoes in ...

    African Journals Online (AJOL)

    Background: There has been a rapid emergence in insecticide resistance among mosquito population to commonly used public health insecticides. This situation presents a challenge to chemicals that are currently used to control mosquitoes in sub-Saharan African. Furthermore, there is limited information on insecticide ...

  19. Microbes as interesting source of novel insecticides: A review ...

    African Journals Online (AJOL)

    ... strains with good insecticidal properties can be identified, evaluated and utilized for pest control. This paper reviews the insecticidal properties of microbes and their potential utility in pest management. Keywords: Microbes, insecticides, metabolites, pest management. African Journal of Biotechnology, Vol 13(26) 2582- ...

  20. Metabolic control of the insecticides safety use

    Directory of Open Access Journals (Sweden)

    L.I. Solomenko

    2016-06-01

    Full Text Available The results of the conducted research affirm that the phosphororganic insecticides utilization can lead to the break in the nitrogen metabolism, breaking the protein formation, reducing the protein molecules renewal, causing the amino acid and amides accumulation in the active state. It has been revealed that the translocation and transformation of the insecticides under consideration are more closely connected with the changes of insoluble protein fraction. The stagnation point of the Phosphamide and Kaunter impact on the plant has been determined. And only the use of the preparation in optimal norms can influence stimulatingly the course of the process under consideration.

  1. Complete androgen insensitivity syndrome with paratesticular leiomyoma: A case report

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Ji Hoon; Oh, Hyung Woo; Lee, Mi Ja; Lim, Dong Hoon [Chosun University College of Medicine, Gwangju (Korea, Republic of)

    2017-03-15

    Complete androgen insensitivity syndrome (AIS) is a rare, X-linked recessive disorder. Patients with AIS may develop primary amenorrhea due to androgen receptor resistance, resulting in a normal female phenotype and male (XY) karyotype. We report a case of a 30-year-old woman who was diagnosed with complete AIS. Ultrasonography and magnetic resonance imaging revealed bilateral inguinal cryptorchidism and no ovaries and uterus. After gonadectomy, the inguinal mass was confirmed as testicular atrophy with hamartomatous proliferation of Leydig cells and paratesticular leiomyoma. Although these tumors have been reported in association with AIS, this is the first case of paratesticular leiomyoma with hamartomatous proliferation of Leydig cells in atrophic testes being reported in Korea.

  2. Complete androgen insensitivity syndrome with paratesticular leiomyoma: A case report

    International Nuclear Information System (INIS)

    Lee, Ji Hoon; Oh, Hyung Woo; Lee, Mi Ja; Lim, Dong Hoon

    2017-01-01

    Complete androgen insensitivity syndrome (AIS) is a rare, X-linked recessive disorder. Patients with AIS may develop primary amenorrhea due to androgen receptor resistance, resulting in a normal female phenotype and male (XY) karyotype. We report a case of a 30-year-old woman who was diagnosed with complete AIS. Ultrasonography and magnetic resonance imaging revealed bilateral inguinal cryptorchidism and no ovaries and uterus. After gonadectomy, the inguinal mass was confirmed as testicular atrophy with hamartomatous proliferation of Leydig cells and paratesticular leiomyoma. Although these tumors have been reported in association with AIS, this is the first case of paratesticular leiomyoma with hamartomatous proliferation of Leydig cells in atrophic testes being reported in Korea

  3. Humidity insensitive TOPAS polymer fiber Bragg grating sensor

    DEFF Research Database (Denmark)

    Yuan, Scott Wu; Khan, Lutul; Webb, David J.

    2011-01-01

    We report the first experimental demonstration of a humidity insensitive polymer optical fiber Bragg grating (FBG), as well as the first FBG recorded in a TOPAS polymer optical fiber in the important low loss 850nm spectral region. For the demonstration we have fabricated FBGs with resonance...... wavelength around 850 nm and 1550 nm in single-mode microstructured polymer optical fibers made of TOPAS and the conventional poly (methyl methacrylate) (PMMA). Characterization of the FBGs shows that the TOPAS FBG is more than 50 times less sensitive to humidity than the conventional PMMA FBG in both...... wavelength regimes. This makes the TOPAS FBG very appealing for sensing applications as it appears to solve the humidity sensitivity problem suffered by the PMMA FBG....

  4. Temperature-insensitive fiber Bragg grating dynamic pressure sensing system.

    Science.gov (United States)

    Guo, Tuan; Zhao, Qida; Zhang, Hao; Zhang, Chunshu; Huang, Guiling; Xue, Lifang; Dong, Xiaoyi

    2006-08-01

    Temperature-insensitive dynamic pressure measurement using a single fiber Bragg grating (FBG) based on reflection spectrum bandwidth modulation and optical power detection is proposed. A specifically designed double-hole cantilever beam is used to provide a pressure-induced axial strain gradient along the sensing FBG and is also used to modulate the reflection bandwidth of the grating. The bandwidth modulation is immune to spatially uniform temperature effects, and the pressure can be unambiguously determined by measuring the reflected optical power, avoiding the complex wavelength interrogation system. The system acquisition time is up to 85 Hz for dynamic pressure measurement, and the thermal fluctuation is kept less than 1.2% full-scale for a temperature range of -10 degrees C to 80 degrees C.

  5. Novel acetylcholinesterase target site for malaria mosquito control.

    Directory of Open Access Journals (Sweden)

    Yuan-Ping Pang

    2006-12-01

    Full Text Available Current anticholinesterase pesticides were developed during World War II and are toxic to mammals because they target a catalytic serine residue of acetylcholinesterases (AChEs in insects and in mammals. A sequence analysis of AChEs from 73 species and a three-dimensional model of a malaria-carrying mosquito (Anopheles gambiae AChE (AgAChE reported here show that C286 and R339 of AgAChE are conserved at the opening of the active site of AChEs in 17 invertebrate and four insect species, respectively. Both residues are absent in the active site of AChEs of human, monkey, dog, cat, cattle, rabbit, rat, and mouse. The 17 invertebrates include house mosquito, Japanese encephalitis mosquito, African malaria mosquito, German cockroach, Florida lancelet, rice leaf beetle, African bollworm, beet armyworm, codling moth, diamondback moth, domestic silkworm, honey bee, oat or wheat aphid, the greenbug, melon or cotton aphid, green peach aphid, and English grain aphid. The four insects are house mosquito, Japanese encephalitis mosquito, African malaria mosquito, and German cockroach. The discovery of the two invertebrate-specific residues enables the development of effective and safer pesticides that target the residues present only in mosquito AChEs rather than the ubiquitous serine residue, thus potentially offering an effective control of mosquito-borne malaria. Anti-AgAChE pesticides can be designed to interact with R339 and subsequently covalently bond to C286. Such pesticides would be toxic to mosquitoes but not to mammals.

  6. Comparative effect of pesticides on brain acetylcholinesterase in tropical fish.

    Science.gov (United States)

    Assis, Caio Rodrigo Dias; Linhares, Amanda Guedes; Oliveira, Vagne Melo; França, Renata Cristina Penha; Carvalho, Elba Veronica Matoso Maciel; Bezerra, Ranilson Souza; de Carvalho, Luiz Bezerra

    2012-12-15

    Monitoring of pesticides based on acetylcholinesterase (AChE; EC 3.1.1.7) inhibition in vitro avoids interference of detoxification defenses and bioactivation of some of those compounds in non-target tissues. Moreover, environmental temperature, age and stress are able to affect specific enzyme activities when performing in vivo studies. Few comparative studies have investigated the inter-specific differences in AChE activity in fish. Screening studies allow choosing the suitable species as source of AChE to detect pesticides in a given situation. Brain AChE from the tropical fish: pirarucu (Arapaima gigas), cobia (Rachycentron canadum) and Nile tilapia (Oreochromis niloticus) were characterized and their activities were assayed in the presence of pesticides (the organophosphates: dichlorvos, diazinon, chlorpyrifos, temephos, tetraethyl pyrophosphate- TEPP and the carbamates: carbaryl and carbofuran). Inhibition parameters (IC₅₀ and Ki) for each species were found and compared with commercial AChE from electric eel (Electrophorus electricus). Optimal pH and temperature were found to be 8.0 and 35-45 °C, respectively. A. gigas AChE retained 81% of the activity after incubation at 50 °C for 30 min. The electric eel enzyme was more sensitive to the compounds (mainly carbofuran, IC₅₀ of 5 nM), excepting the one from A. gigas (IC₅₀ of 9 nM) under TEPP inhibition. These results show comparable sensitivity between purified and non-purified enzymes suggesting them as biomarkers for organophosphorus and carbamate detection in routine environmental and food monitoring programs for pesticides. Copyright © 2012 Elsevier B.V. All rights reserved.

  7. Bivalent ligands derived from Huperzine A as acetylcholinesterase inhibitors.

    Science.gov (United States)

    Haviv, H; Wong, D M; Silman, I; Sussman, J L

    2007-01-01

    The naturally occurring alkaloid Huperzine A (HupA) is an acetylcholinesterase (AChE) inhibitor that has been used for centuries as a Chinese folk medicine in the context of its source plant Huperzia Serrata. The potency and relative safety of HupA rendered it a promising drug for the ameliorative treatment of Alzheimer's disease (AD) vis-à-vis the "cholinergic hypothesis" that attributes the cognitive decrements associated with AD to acetylcholine deficiency in the brain. However, recent evidence supports a neuroprotective role for HupA, suggesting that it could act as more than a mere palliative. Biochemical and crystallographic studies of AChE revealed two potential binding sites in the active-site gorge of AChE, one of which, the "peripheral anionic site" at the mouth of the gorge, was implicated in promoting aggregation of the beta amyloid (Abeta) peptide responsible for the neurodegenerative process in AD. This feature of AChE facilitated the development of dual-site binding HupA-based bivalent ligands, in hopes of concomitantly increasing AChE inhibition potency by utilizing the "chelate effect", and protecting neurons from Abeta toxicity. Crystal structures of AChE allowed detailed modeling and docking studies that were instrumental in enhancing the understanding of underlying principles of bivalent inhibitor-enzyme dynamics. This monograph reviews two categories of HupA-based bivalent ligands, in which HupA and HupA fragments serve as building blocks, with a focus on the recently solved crystallographic structures of Torpedo californica AChE in complex with such bifunctional agents. The advantages and drawbacks of such structured-based drug design, as well as species differences, are highlighted and discussed.

  8. The crop-residue of fiber hemp cv. Futura 75: from a waste product to a source of botanical insecticides.

    Science.gov (United States)

    Benelli, Giovanni; Pavela, Roman; Lupidi, Giulio; Nabissi, Massimo; Petrelli, Riccardo; Ngahang Kamte, Stephane L; Cappellacci, Loredana; Fiorini, Dennis; Sut, Stefania; Dall'Acqua, Stefano; Maggi, Filippo

    2018-04-01

    In the attempt to exploit the potential of the monoecious fiber hemp cv. Futura 75 in new fields besides textile, cosmetics and food industry, its crop-residue given by leaves and inflorescences was subjected to hydrodistillation to obtain the essential oils. These are niche products representing an ideal candidate for the development of natural insecticides for the control and management of mosquito vectors, houseflies and moth pests. After GC-MS analysis highlighting a safe and legal chemical profile (THC in the range 0.004-0.012% dw), the leaf and inflorescence essential oils were investigated for the insecticidal potential against three insect targets: the larvae of Culex quinquefasciatus and Spodoptera littoralis and the adults of Musca domestica. The essential oil from inflorescences, showing (E)-caryophyllene (21.4%), myrcene (11.3%), cannabidiol (CBD, 11.1%), α-pinene (7.8%), terpinolene (7.6%), and α-humulene (7.1%) as the main components, was more effective than leaf oil against these insects, with LD 50 values of 65.8 μg/larva on S. littoralis, 122.1 μg/adult on M. domestica, and LC 50 of 124.5 μl/l on C. quinquefasciatus larvae. The hemp essential oil moderately inhibited the acetylcholinesterase (AChE), which is a target enzyme in pesticide science. Overall, these results shed light on the future application of fiber hemp crop-residue for the development of effective, eco-friendly and sustainable insecticides.

  9. Insecticide resistance to permethrin and malathion and associated mechanisms in Aedes aegypti mosquitoes from St. Andrew Jamaica.

    Directory of Open Access Journals (Sweden)

    Sheena Francis

    Full Text Available The emergence of novel diseases spread by the Aedes aegypti mosquito in Jamaica and the Caribbean, has prompted studies on insecticide resistance towards effective management of the vector. Though Jamaica has been using the organophosphate insecticide malathion in its vector control program for more than 30 years, resistance to the pesticide has not been tested in over a decade. We analyzed resistance to malathion and the pyrethroid insecticide, permethrin on mosquitoes collected across St. Andrew, Jamaica, and analyzed the molecular basis of resistance. The Center for Disease Control (CDC bioassay revealed that Ae. aegypti mosquitoes from St. Andrew, Jamaica were resistant to permethrin (15 μg/bottle with mortalities at 0-8% at 30 minute exposure time, while contact with malathion (50 μg/bottle revealed ≤ 50% mortality at 15 minutes, which increased to 100% at 45 minutes. The standard susceptible New Orleans (NO strain exhibited 100% mortality within15 minutes. The activities of multifunction oxidases and p-nitro phenyl-acetate esterases were significantly greater in most Jamaican populations in comparison to the NO strain, while activities of glutathione-S-transferase, acetylcholinesterase, α-esterase and ß-esterase activity were relatively equal, or lower than that of the control strain. The frequency of knockdown resistance mutations in the voltage dependent sodium channel gene were measured. All collections were fixed for Cys1,534 while 56% of mosquitoes were Ile1,016/Val1,016 heterozygotes, and 33% were Ile1,016 homozygotes. Aedes aegypti from St. Andrew Jamaica are resistant to permethrin with variations in the mode of mechanism, and possibly developing resistance to malathion. Continued monitoring of resistance is critically important to manage the spread of the vector in the country.

  10. Immobilization of Acetylcholinesterase on Screen-Printed Electrodes. Application to the Determination of Arsenic(III

    Directory of Open Access Journals (Sweden)

    M. Julia Arcos-Martínez

    2010-03-01

    Full Text Available Enzymatic amperometric procedures for measuring arsenic, based on the inhibitive action of this metal on acetylcholinesterase enzyme activity, have been developed. Screen-printed carbon electrodes (SPCEs were used with acetylcholinesterase covalently bonded directly to its surface. The amperometric response of acetylcholinesterase was affected by the presence of arsenic ions, which caused a decrease in the current intensity. The experimental optimum working conditions of pH, substrate concentration and potential applied, were established. Under these conditions, repeatability and reproducibility of biosensors were determined, reaching values below 4% in terms of relative standard deviation. The detection limit obtained for arsenic was 1.1 × 10−8 M for Ach/SPCE biosensor. Analysis of the possible effect of the presence of foreign ions in the solution was performed. The method was applied to determine levels of arsenic in spiked tap water samples.

  11. A novel biosensor method for surfactant determination based on acetylcholinesterase inhibition

    International Nuclear Information System (INIS)

    Kucherenko, I S; Soldatkin, O O; Arkhypova, V M; Dzyadevych, S V; Soldatkin, A P

    2012-01-01

    A novel enzyme biosensor based on acetylcholinesterase inhibition for the determination of surfactants in aqueous solutions is described. Acetylcholinesterase-based bioselective element was deposited via glutaraldehyde on the surface of conductometric transducers. Different variants of inhibitory analysis of surfactants were tested, and finally surfactant's concentration was evaluated by measuring initial rate of acetylcholinesterase inhibition. Besides, we studied the effect of solution characteristics on working parameters of the biosensor for direct measurement of acetylcholine and for inhibitory determination of surfactants. The biosensor's sensitivity to anionic and cationic surfactants (0.35 mg l −1 ) was tested. The high operational stability of the biosensor during determination of acetylcholine (RSD 2%) and surfactants (RSD 11%) was shown. Finally, we discussed the selectivity of the biosensor toward surfactants and other AChE inhibitors. The proposed biosensor can be used as a component of the multibiosensor for ecological monitoring of toxicants. (paper)

  12. Evaluation of acetylcholinesterase inhibitory activity of Brazilian red macroalgae organic extracts

    Directory of Open Access Journals (Sweden)

    Levi P. Machado

    Full Text Available Abstract Alzheimer's disease affects nearly 36.5 million people worldwide, and acetylcholinesterase inhibition is currently considered the main therapeutic strategy against it. Seaweed biodiversity in Brazil represents one of the most important sources of biologically active compounds for applications in phytotherapy. Accordingly, this study aimed to carry out a quantitative and qualitative assessment of Hypnea musciformis (Wulfen J.V. Lamouroux, Ochtodes secundiramea (Montagne M.A. Howe, and Pterocladiella capillacea (S.G. Gmelin Santelices & Hommersand (Rhodophyta in order to determine the AChE effects from their extracts. As a matter of fact, the O. secundiramea extract showed 48% acetylcholinesterase inhibition at 400 μg/ml. The chemical composition of the bioactive fraction was determined by gas chromatography–mass spectrometry (GC–MS; this fraction is solely composed of halogenated monoterpenes, therefore allowing assignment of acetylcholinesterase inhibition activity to them.

  13. Biosensor-assisted selection of optimal parameters for designing molecularly imprinted polymers selective to phosmet insecticide.

    Science.gov (United States)

    Aftim, Nadin; Istamboulié, Georges; Piletska, Elena; Piletsky, Sergey; Calas-Blanchard, Carole; Noguer, Thierry

    2017-11-01

    Molecularly imprinted polymers (MIPs) for phosmet insecticide were synthesized by batch polymerization. The affinity of functional monomers to phosmet was tested using an original method involving an electrochemical biosensor based on acetylcholinesterase inhibition. It was demonstrated that association of phosmet with appropriate functional monomers resulted in a decrease of enzyme inhibition. Using this method, it was shown that N,N-methylenebis(acrylamide) displayed the highest interactions with phosmet using DMSO as solvent. These results were in good accordance with those obtained by conventional computational modeling. Molecularly imprinted polymers (MIPs) and non-imprinted polymers (NIPs) were synthesized and adsorption isotherms were studied to describe their interaction with phosmet. Freundlich isotherm was able to fit phosmet adsorption on MIPs with good agreement (R 2 = 0.9). The pre-exponential factor K F determined for MIPs was 1.439mg (1-N) g -1 L N , more that 10 times higher than for NIPs (0.125mg (1-N) g -1 . L N ), indicating an increase of binding sites number and average affinity. Copyright © 2017 Elsevier B.V. All rights reserved.

  14. Effect of selected insecticides on SF9 insect cell line

    International Nuclear Information System (INIS)

    Saleh, M.; Rahmo, A.; Hajjar, J.

    2013-01-01

    The toxic effect of three insecticides: dimethoate (organophosphate insecticide), acetamiprid (neonicotinoid insecticide) and deltamethrin (pyrethroid insecticide) were evaluated in vitro on cultured Sf9 cell line. Cell growth inhibition was measured by the 3- (4,5- dimethylthiazol - 2-yl) - 2,5 - diphenyl tetrazolium bromide (MTT) assay. Regression Analysis was used to estimate the 20% inhibition of cells growth (IC 20). The IC 20 values obtained for deltamethrin, acetamipridand dimethoate were: 46.8, 61.6 and 68.9 μM, respectively. The proportion of phagocytic cells was positively correlated with the applied concentrations of the insecticides. (author)

  15. Possibilities of Botanical Insecticides in Plant Protection

    Czech Academy of Sciences Publication Activity Database

    Pavela, R.; Sajfrtová, Marie; Sovová, Helena; Bárnet, M.

    2008-01-01

    Roč. 2, č. 1 (2008), s. 16-23 ISSN 1313-2563 Grant - others:MŠk(CZ) 2B08049 Institutional support: RVO:67985858 Keywords : botanical insecticides * plant extracts * supercritical fluid extraction Subject RIV: GF - Plant Pathology, Vermin, Weed, Plant Protection

  16. Possibilities of Botanical Insecticides in Plant Protection

    Czech Academy of Sciences Publication Activity Database

    Pavela, R.; Sajfrtová, Marie; Sovová, Helena; Bárnet, M.

    2008-01-01

    Roč. 2, č. 1 (2008), s. 16-23 ISSN 1313-2563 Grant - others:GA MŠMT(CZ) 2B08049 Institutional research plan: CEZ:AV0Z40720504 Keywords : botanical insecticides * plant exctracts * supercritical fluid extraction Subject RIV: GF - Plant Pathology, Vermin, Weed, Plant Protection

  17. Insecticidal and fungicidal compounds from Isatis tinctoria.

    Science.gov (United States)

    Seifert, K; Unger, W

    1994-01-01

    Tryptanthrin (1), indole-3-acetonitrile (2) and p-coumaric acid methylester (3) were isolated from the aerial parts of Isatis tinctoria L. The compounds show insecticidal and anti-feedant activity against termites (Reticulitermis santonensis), insect preventive and control activity against larvae of the house longhorn beetle (Hylotrupes bajulus) and fungicidal activity against the brown-rot fungus (Coniophora puteana).

  18. Novel coumarin derivatives bearing N-benzyl pyridinium moiety: potent and dual binding site acetylcholinesterase inhibitors.

    Science.gov (United States)

    Alipour, Masoumeh; Khoobi, Mehdi; Foroumadi, Alireza; Nadri, Hamid; Moradi, Alireza; Sakhteman, Amirhossein; Ghandi, Mehdi; Shafiee, Abbas

    2012-12-15

    A novel series of coumarin derivatives linked to benzyl pyridinium group were synthesized and biologically evaluated as inhibitors of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The enzyme inhibitory activity of synthesized compounds was measured using colorimetric Ellman's method. It was revealed that compounds 3e, 3h, 3l, 3r and 3s have shown higher activity compared with donepezil hydrochloride as standard drug. Most of the compounds in these series had nanomolar range IC(50) in which compound 3r (IC(50) = 0.11 nM) was the most active compound against acetylcholinesterase enzyme. Copyright © 2012 Elsevier Ltd. All rights reserved.

  19. Phenolic Lipids Affect the Activity and Conformation of Acetylcholinesterase from Electrophorus electricus (Electric eel)

    Science.gov (United States)

    Stasiuk, Maria; Janiszewska, Alicja; Kozubek, Arkadiusz

    2014-01-01

    Phenolic lipids were isolated from rye grains, cashew nutshell liquid (CNSL) from Anacardium occidentale, and fruit bodies of Merrulius tremellosus, and their effects on the electric eel acetylcholinesterase activity and conformation were studied. The observed effect distinctly depended on the chemical structure of the phenolic lipids that were available for interaction with the enzyme. All of the tested compounds reduced the activity of acetylcholinesterase. The degree of inhibition varied, showing a correlation with changes in the conformation of the enzyme tested by the intrinsic fluorescence of the Trp residues of the protein. PMID:24787269

  20. Is Apis mellifera more sensitive to insecticides than other insects?

    Science.gov (United States)

    Hardstone, Melissa C; Scott, Jeffrey G

    2010-11-01

    Honey bees (Apis mellifera L.) are among the most important pollinators in natural and agricultural settings. They commonly encounter insecticides, and the effects of insecticides on honey bees have been frequently noted. It has been suggested that honey bees may be (as a species) uniquely sensitive to insecticides, although no comparative toxicology study has been undertaken to examine this claim. An extensive literature review was conducted, using data in which adult insects were topically treated with insecticides. The goal of this review was to summarize insecticide toxicity data between A. mellifera and other insects to determine the relative sensitivity of honey bees to insecticides. It was found that, in general, honey bees were no more sensitive than other insect species across the 62 insecticides examined. In addition, honey bees were not more sensitive to any of the six classes of insecticides (carbamates, nicotinoids, organochlorines, organophosphates, pyrethroids and miscellaneous) examined. While honey bees can be sensitive to individual insecticides, they are not a highly sensitive species to insecticides overall, or even to specific classes of insecticides. However, all pesticides should be used in a way that minimizes honey bee exposure, so as to minimize possible declines in the number of bees and/or honey contamination. Copyright © 2010 Society of Chemical Industry.

  1. UJI BIOKIMIA UNTUK IDENTIFIKASI MEKANISME RESISTENSI GANDA VEKTOR MALARIA TERHADAP INSEKTISIDA DI JAWA TIMUR

    Directory of Open Access Journals (Sweden)

    Widiarti -

    2011-12-01

    Full Text Available Resistance is inherited and has proved to be the biggest single barrier to successful chemical control of insect vectors. The continuity of along time period insecticide usage can produce mosquitoes resistance. Resistance to insecticide as a results from three main mechanism : 1 insecticide penetration is reduce, 2 the insecticides is more efficiently metabolized by esterases, mixed function oxidases, or glutathione transferase enzyme and, 3 the target of the insecticide is modified (insensitive acetylcholinesterase. The objectives of this study was to determine the potency of malaria vector from East Java Province to be resistant to organophosphate, carbamate and pyrethroid insecticides. The research methods used were biochemical assays (microplate assays for elevated esterase and insensitive acetylcholinesterase. The esterase activity and insensitive acetylcholinesterase were measured at 450 nm and 405 nm with a Dytech Elisa plate reader. Biochemical assays indicated that susceptibility (resistant or tolerance, of the malaria vector collected from East Java Province natural population against insecticide were mostly decreased, although there were different level and mechanism occurs. Microplate enzymatic assay on individual Anopheles sundaicus collected from Banyuwangi, Pacitan, Jember, Malang Regency revealed that 31,25 %, 12,5 %, 45,2 % and 15,25 % population were resistant respectively due to elevated esterase activity mechanism. Base on the susceptibility test which was held using WHO method (as a cross-check An. sundaicus from Teleng village, Pacitan Regency was proven to have a double resistance agains Malathion 0,5 % (cause mortality 28 % and Bendiocarb 0,1 % (cause mortality 66 %. The percentage resistance of Anopheles aconitus population collected from Pacitan and Trenggalek Regency were 35,42 % and 29,17 % population respectively due to elevated esterase activity mechanism. There was no evidence of an altered acetylcholinesterase

  2. Spatial memory performance in androgen insensitive male rats.

    Science.gov (United States)

    Jones, Bryan A; Watson, Neil V

    2005-06-02

    Masculinization of the developing rodent brain critically depends on the process of aromatization of circulating testosterone (T) to its estrogenic metabolite 17beta-estradiol, which subsequently interacts with estrogen receptors to permanently masculinize the brain. However, it remains unclear what role other androgenic mechanisms may play in the process of masculinization. A novel way of examining this is through the study of male rats that express the tfm mutation of the androgen receptor (AR) gene; such males are fully androgen insensitive and manifest a female phenotype due to a failure of AR-mediated masculinization of peripheral structures. Because tfm-affected males develop secretory testes and have near-normal T titers during development, aromatization would be expected to proceed normally, and brain mechanisms may be developmentally masculinized despite the feminized periphery. We compared tfm-affected males (X(tfm)Y) with normal males and females in the Morris Water Maze, a task in which males typically perform better than females. Performance of tfm-affected males was intermediate between that of normal males and females. While an overall male superiority was found in the task, the X(tfm)Y group reached male-typical escape latencies faster than females. Furthermore, in the X(tfm)Y group, the granule cell layer of the dentate gyrus was significantly larger than in females. These results support the suggestion that that AR mediated mechanisms contribute to the masculinization of spatial behaviours and hippocampal morphology, and this may be independent of estrogenic processes.

  3. The clinical and molecular spectrum of androgen insensitivity syndromes

    Energy Technology Data Exchange (ETDEWEB)

    Hiort, O.; Sinnecker, G.H.G.; Holterhus, P.M.; Nitsche, E.M.; Kruse, K. [Medical Univ. of Luebeck (Germany)

    1996-05-03

    Androgen insensitivity syndromes (AIS) are due to end-organ resistance to androgenic steroids in males leading to defective virilization of the external genitalia. The phenotype encompasses a wide array of genital ambiguity and may range from completely female to undervirilized but unequivocally male with infertility. This disorder is caused by mutations of the androgen receptor and is an X-linked recessive trait. We have studied 47 patients with AIS and have characterized the underlying molecular abnormality in the androgen receptor gene. Twenty patients had complete AIS and twenty-seven had partial AIS. Of the latter, 11 were of predominantly female phenotypic appearance and gender was assigned accordingly, while 16 were raised as males. Within the group of complete AIS, two patients had gross deletions within the gene, one had a small deletion, and one had an insertion. In the other patients with complete AIS, as well as all individuals with partial AIS, single nucleotide substitutions within the coding region were detected, each leading to an amino acid alteration. Seven codons were involved in more than one mutation in different cases. In addition, in one patient with spinal and bulbar muscular atrophy, an elongation of a glutamine-repeat was characterized. We conclude that mutations in the androgen receptor gene may be present throughout the whole coding region. However, our study provides evidence that several mutational hot spots exist. 18 refs., 2 figs.

  4. Endonucleases induced TRAIL-insensitive apoptosis in ovarian carcinoma cells

    Energy Technology Data Exchange (ETDEWEB)

    Geel, Tessa M. [Department of Pathology and Medical Biology, Groningen University Institute for Drug Exploration (GUIDE), University Medical Center Groningen (UMCG), Hanzeplein 1, 9713 GZ, Groningen (Netherlands); Meiss, Gregor [Institute of Biochemistry, Justus-Liebig-University Giessen, D-35392 Giessen (Germany); Gun, Bernardina T. van der; Kroesen, Bart Jan; Leij, Lou F. de [Department of Pathology and Medical Biology, Groningen University Institute for Drug Exploration (GUIDE), University Medical Center Groningen (UMCG), Hanzeplein 1, 9713 GZ, Groningen (Netherlands); Zaremba, Mindaugas; Silanskas, Arunas [Institute of Biotechnology, Vilnius LT-02241 (Lithuania); Kokkinidis, Michael [IMBB/FORTH and University of Crete/Department of Biology, GR-71409 Heraklion/Crete (Greece); Pingoud, Alfred [Institute of Biochemistry, Justus-Liebig-University Giessen, D-35392 Giessen (Germany); Ruiters, Marcel H. [Department of Pathology and Medical Biology, Groningen University Institute for Drug Exploration (GUIDE), University Medical Center Groningen (UMCG), Hanzeplein 1, 9713 GZ, Groningen (Netherlands); Synvolux therapeutics, Groningen (Netherlands); McLaughlin, Pamela M. [Department of Pathology and Medical Biology, Groningen University Institute for Drug Exploration (GUIDE), University Medical Center Groningen (UMCG), Hanzeplein 1, 9713 GZ, Groningen (Netherlands); Rots, Marianne G., E-mail: m.g.rots@med.umcg.nl [Department of Pathology and Medical Biology, Groningen University Institute for Drug Exploration (GUIDE), University Medical Center Groningen (UMCG), Hanzeplein 1, 9713 GZ, Groningen (Netherlands)

    2009-09-10

    TRAIL induced apoptosis of tumor cells is currently entering phase II clinical settings, despite the fact that not all tumor types are sensitive to TRAIL. TRAIL resistance in ovarian carcinomas can be caused by a blockade upstream of the caspase 3 signaling cascade. We explored the ability of restriction endonucleases to directly digest DNA in vivo, thereby circumventing the caspase cascade. For this purpose, we delivered enzymatically active endonucleases via the cationic amphiphilic lipid SAINT-18{sup Registered-Sign }:DOPE to both TRAIL-sensitive and insensitive ovarian carcinoma cells (OVCAR and SKOV-3, respectively). Functional nuclear localization after delivery of various endonucleases (BfiI, PvuII and NucA) was indicated by confocal microscopy and genomic cleavage analysis. For PvuII, analysis of mitochondrial damage demonstrated extensive apoptosis both in SKOV-3 and OVCAR. This study clearly demonstrates that cellular delivery of restriction endonucleases holds promise to serve as a novel therapeutic tool for the treatment of resistant ovarian carcinomas.

  5. Chagas disease: modulation of the inflammatory response by acetylcholinesterase in hematological cells and brain tissue.

    Science.gov (United States)

    Silva, Aniélen D; Bottari, Nathieli B; do Carmo, Guilherme M; Baldissera, Matheus D; Souza, Carine F; Machado, Vanessa S; Morsch, Vera M; Schetinger, Maria Rosa C; Mendes, Ricardo E; Monteiro, Silvia G; Da Silva, Aleksandro S

    2018-01-01

    Chagas disease is an acute or chronic illness that causes severe inflammatory response, and consequently, it may activate the inflammatory cholinergic pathway, which is regulated by cholinesterases, including the acetylcholinesterase. This enzyme is responsible for the regulation of acetylcholine levels, an anti-inflammatory molecule linked to the inflammatory response during parasitic diseases. Thus, the aim of this study was to investigate whether Trypanosoma cruzi infection can alter the activity of acetylcholinesterase and acetylcholine levels in mice, and whether these alterations are linked to the inflammatory cholinergic signaling pathway. Twenty-four mice were divided into two groups: uninfected (control group, n = 12) and infected by T. cruzi, Y strain (n = 12). The animals developed acute disease with a peak of parasitemia on day 7 post-infection (PI). Blood, lymphocytes, and brain were analyzed on days 6 and 12 post-infection. In the brain, acetylcholine and nitric oxide levels, myeloperoxidase activity, and histopathology were analyzed. In total blood and brain, acetylcholinesterase activity decreased at both times. On the other hand, acetylcholinesterase activity in lymphocytes increased on day 6 PI compared with the control group. Infection by T. cruzi increased acetylcholine and nitric oxide levels and histopathological damage in the brain of mice associated to increased myeloperoxidase activity. Therefore, an intense inflammatory response in mice with acute Chagas disease in the central nervous system caused an anti-inflammatory response by the activation of the cholinergic inflammatory pathway.

  6. Screening of acetylcholinesterase inhibitors in snake venom by electrospray mass spectrometry

    NARCIS (Netherlands)

    Liesener, A.; Perchuc, Anna-Maria; Schöni, Reto; Schebb, Nils Helge; Wilmer, Marianne; Karst, U.

    2007-01-01

    An electrospray ionization/mass spectrometry (ESI/MS)-based assay for the determination of acetylcholinesterase (AChE)-inhibiting activity in snake venom was developed. It allows the direct monitoring of the natural AChE substrate acetylcholine (AC) and the respective product choline. The assay

  7. Evaluating the antioxidant and acetylcholinesterase inhibitory activity of three Centaurea species

    Directory of Open Access Journals (Sweden)

    H. Hajimehdipoor

    2014-01-01

    Full Text Available Factors such as oxidative stress and reduced acetylcholine level have been implicated in Alzheimer’s disease (AD pathology and recently there has been a trend towards natural product research to find potential sources of antioxidants and acetylcholinesterase inhibitors in the plants kingdom. Centaurea is a genus with about 500 species world wild, many of them have shown to possess biologic activity; Centaurea albonites, C. aucheri and C. pseudoscabiosa are three species which little investigation has been carried out about their biological properties. In the present study, the antioxidant and acetylcholinesterase inhibitory activity of the above mentioned species have been evaluated. The ability of the total extract and methanol fraction of the plants to scavenge free radicals has been assessed through DPPH radical scavenging assay, and the acetylcholinesterase inhibitory property has been evaluated by Ellman method. The total extract of all species exhibited moderate antioxidant activity whereas the extracts of C. pseudoscabiosa showed the strongest antioxidant property; its total extract also demonstrated the highest acetylcholinesterase inhibitory activity among the evaluated samples (19.2% inhibition. The results suggest the species as potential sources of natural antioxidants which could be focused in future studies of Alzheimer’s disease.

  8. Dual Binding Site and Selective Acetylcholinesterase Inhibitors Derived from Integrated Pharmacophore Models and Sequential Virtual Screening

    Directory of Open Access Journals (Sweden)

    Shikhar Gupta

    2014-01-01

    Full Text Available In this study, we have employed in silico methodology combining double pharmacophore based screening, molecular docking, and ADME/T filtering to identify dual binding site acetylcholinesterase inhibitors that can preferentially inhibit acetylcholinesterase and simultaneously inhibit the butyrylcholinesterase also but in the lesser extent than acetylcholinesterase. 3D-pharmacophore models of AChE and BuChE enzyme inhibitors have been developed from xanthostigmine derivatives through HypoGen and validated using test set, Fischer’s randomization technique. The best acetylcholinesterase and butyrylcholinesterase inhibitors pharmacophore hypotheses Hypo1_A and Hypo1_B, with high correlation coefficient of 0.96 and 0.94, respectively, were used as 3D query for screening the Zinc database. The screened hits were then subjected to the ADME/T and molecular docking study to prioritise the compounds. Finally, 18 compounds were identified as potential leads against AChE enzyme, showing good predicted activities and promising ADME/T properties.

  9. Inactivation of acetylcholinesterase by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine hydrochloride.

    Science.gov (United States)

    Zang, Lun-Yi; Misra, Hara P

    2003-12-01

    The neurotoxicant 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) has been shown to reversibly inhibit the activity of acetylcholinesterase. The inactivation of the enzyme was detected by monitoring the accumulation of yellow color produced from the reaction between thiocholine and dithiobisnitrobenzoate ion. The kinetic parameter, Km for the substrate (acetylthiocholine), was found to be 0.216 mM and Ki for MPTP inactivation of acetylcholinesterase was found to be 2.14 mM. The inactivation of enzyme by MPTP was found to be dose-dependent. It was found that MPTP is neither a substrate of AChE nor the time-dependent inactivator. The studies of reaction kinetics indicate the inactivation of AChE to be a linear mixed-type inhibition. The dilution assays indicate that MPTP is a reversible inhibitor for AChE. These data suggest that once MPTP enters the basal ganglia of the brain, it can inactivate the acetylcholinesterase enzyme and thereby increase the acetylcholine level in the basal ganglia of brain, leading to potential cell dysfunction. It appears that the nigrostriatal toxicity by MPTP leading to Parkinson's disease-like syndrome may, in part, be mediated via the acetylcholinesterase inactivation.

  10. Stabilizing Acetylcholinesterase on Carbon Electrodes Using Peptide Nanotubes to Produce Effective Biosensors

    Science.gov (United States)

    2012-03-22

    disposable, inhibition 1. Introduction Organophosphates (OPs) are acetyl cholinesterase (AChE) inhibitors with a broad range of potency and toxicity...5 Cholinesterase Biosensors...BIOSENSORS I. Introduction Background Organophosphates (OPs) are acetylcholinesterase (AChE) inhibitors with a broad range of potency and

  11. Antimicrobial activity and acetylcholinesterase inhibition by extracts from chromatin modulated fungi

    Directory of Open Access Journals (Sweden)

    Matheus Thomaz Nogueira Silva Lima

    Full Text Available ABSTRACT 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. Extracts from T. islandicus cultured or not with hydralazine inhibited Listeria monocytogenes growth in 57.66 ± 5.98% and 15.38 ± 1.99%, respectively. Increment in inhibition of acetylcholinesterase activity was observed for the extract from P. janthinellum grown with procainamide (100%, when compared to the control extract (39.62 ± 3.76%. Similarly, inhibition of acetylcholinesterase activity increased from 20.91 ± 3.90% (control to 92.20 ± 3.72% when the tested extract was obtained from T. pinophilus under a combination of suberohydroxamic acid and procainamide. Concluding, increases in antimicrobial activity and acetylcholinesterase inhibition were observed when fungal extracts in the presence of DNA methyltransferases and/or histone deacetylase modulators were tested.

  12. Two Bombyx mori acetylcholinesterase genes influence motor control and development in different ways

    Science.gov (United States)

    Among its other biological roles, acetylcholinesterase (AChE, EC 3.1.1.7), encoded by two ace genes in most insects, catalyses the breakdown of acetylcholine, thereby terminating synaptic transmission. ace1 encodes the synaptic enzyme and ace2 has other essential actions in many insect species, such...

  13. Bifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors

    Czech Academy of Sciences Publication Activity Database

    Šebestík, Jaroslav; Marques, S. M.; Falé, P. L.; Santos, S.; Arduíno, D. M.; Cardoso, S. M.; Oliveira, S. M.; Serralheiro, M. L. M.; Santos, A. M.

    Roč. 26, č. 4 (485), s. 497 ISSN 1475-6366 Institutional research plan: CEZ:AV0Z40550506 Keywords : acetylcholinesterase inhibitors * antioxidants * hybrid ligands * anti-neurodegeneratives * Alzheimer´s disease Subject RIV: CC - Organic Chemistry

  14. The interaction of quaternary reversible acetylcholinesterase inhibitors with the nicotinic receptor

    Czech Academy of Sciences Publication Activity Database

    Šepsová, V.; Krůšek, Jan; Zdarová Karasová, J.; Zemek, F.; Musílek, K.; Kuča, K.; Soukup, O.

    2014-01-01

    Roč. 63, č. 6 (2014), s. 771-777 ISSN 0862-8408 R&D Projects: GA ČR(CZ) GBP304/12/G069 Institutional support: RVO:67985823 Keywords : acetylcholinesterase inhibitor * nicotin receptor Subject RIV: ED - Physiology Impact factor: 1.293, year: 2014

  15. Fenugreek hydrogel–agarose composite entrapped gold nanoparticles for acetylcholinesterase based biosensor for carbamates detection

    Energy Technology Data Exchange (ETDEWEB)

    Kestwal, Rakesh Mohan; Bagal-Kestwal, Dipali; Chiang, Been-Huang, E-mail: bhchiang@ntu.edu.tw

    2015-07-30

    A biosensor was fabricated to detect pesticides in food samples. Acetylcholinesterase was immobilized in a novel fenugreek hydrogel–agarose matrix with gold nanoparticles. Transparent thin films with superior mechanical strength and stability were obtained with 2% fenugreek hydrogel and 2% agarose. Immobilization of acetylcholinesterase on the membrane resulted in high enzyme retention efficiency (92%) and a significantly prolonged shelf life of the enzyme (half-life, 55 days). Transmission electron microscopy revealed that, gold nanoparticles (10–20 nm in diameter) were uniformly dispersed in the fenugreek hydrogel–agarose–acetylcholinesterase membrane. This immobilized enzyme-gold nanoparticle dip-strip system detected various carbamates, including carbofuran, oxamyl, methomyl, and carbaryl, with limits of detection of 2, 21, 113, and 236 nM (S/N = 3), respectively. Furthermore, the fabricated biosensor exhibited good testing capabilities when used to detect carbamates added to various fruit and vegetable samples. - Highlights: • Acetylcholinesterase (AChE) dip-strip biosensor fabricated to detect carbamates. • AChE entrapped in fenugreek hydrogel–agarose matrix with gold nanoparticles (GNPs). • High enzyme retention efficiency (92%) and shelf life (half-life, 55 days). • Detection limits of carbofuran, oxamyl and methomyl: 2, 21 and 113 nM. • The biosensor had good testing capabilities to detect carbamates in food samples.

  16. Screening for acetylcholinesterase inhibitory activity in cyanobacteria of the genus Nostoc

    Czech Academy of Sciences Publication Activity Database

    Zelík, Petr; Lukešová, Alena; Voloshko, L. N.; Štys, D.; Kopecký, Jiří

    2009-01-01

    Roč. 24, č. 2 (2009), s. 531-536 ISSN 1475-6366 R&D Projects: GA MŠk ME 874 Institutional research plan: CEZ:AV0Z50200510; CEZ:AV0Z60660521 Keywords : acetylcholinesterase * bioactivity * inhibitors Subject RIV: EE - Microbiology, Virology Impact factor: 1.496, year: 2009

  17. Exploration of Novel Botanical Insecticide Leads: Synthesis and Insecticidal Activity of β-Dihydroagarofuran Derivatives.

    Science.gov (United States)

    Zhao, Ximei; Xi, Xin; Hu, Zhan; Wu, Wenjun; Zhang, Jiwen

    2016-02-24

    The discovery of novel leads and new mechanisms of action is of vital significance to the development of pesticides. To explore lead compounds for botanical insecticides, 77 β-dihydroagarofuran derivatives were designed and synthesized. Their structures were mainly confirmed by (1)H NMR, (13)C NMR, DEPT-135°, IR, MS, and HRMS. Their insecticidal activity was evaluated against the third-instar larvae of Mythimna separata Walker, and the results indicated that, of these derivatives, eight exhibited more promising insecticidal activity than the positive control, celangulin-V. Particularly, compounds 5.7, 6.6, and 6.7 showed LD50 values of 37.9, 85.1, and 21.1 μg/g, respectively, which were much lower than that of celangulin-V (327.6 μg/g). These results illustrated that β-dihydroagarofuran ketal derivatives can be promising lead compounds for developing novel mechanism-based and highly effective botanical insecticides. Moreover, some newly discovered structure-activity relationships are discussed, which may provide some important guidance for insecticide development.

  18. Ion channels: molecular targets of neuroactive insecticides.

    Science.gov (United States)

    Raymond-Delpech, Valérie; Matsuda, Kazuhiko; Sattelle, Benedict M; Rauh, James J; Sattelle, David B

    2005-11-01

    Many of the insecticides in current use act on molecular targets in the insect nervous system. Recently, our understanding of these targets has improved as a result of the complete sequencing of an insect genome, i.e., Drosophila melanogaster. Here we examine the recent work, drawing on genetics, genomics and physiology, which has provided evidence that specific receptors and ion channels are targeted by distinct chemical classes of insect control agents. The examples discussed include, sodium channels (pyrethroids, p,p'-dichlorodiphenyl-trichloroethane (DDT), dihydropyrazoles and oxadiazines); nicotinic acetylcholine receptors (cartap, spinosad, imidacloprid and related nitromethylenes/nitroguanidines); gamma-aminobutyric acid (GABA) receptors (cyclodienes, gamma-BHC and fipronil) and L-glutamate receptors (avermectins). Finally, we have examined the molecular basis of resistance to these molecules, which in some cases involves mutations in the molecular target, and we also consider the future impact of molecular genetic technologies in our understanding of the actions of neuroactive insecticides.

  19. An evaluation of the inhibition of human butyrylcholinesterase and acetylcholinesterase by the organophosphate chlorpyrifos oxon

    International Nuclear Information System (INIS)

    Shenouda, Josephine; Green, Paula; Sultatos, Lester

    2009-01-01

    Acetylcholinesterase (EC 3.1.1.7) and butyrylcholinesterase (EC 3.1.1.8) are enzymes that belong to the superfamily of α/β-hydrolase fold proteins. While they share many characteristics, they also possess many important differences. For example, whereas they have about 54% amino acid sequence identity, the active site gorge of acetylcholinesterase is considerably smaller than that of butyrylcholinesterase. Moreover, both have been shown to display simple and complex kinetic mechanisms, depending on the particular substrate examined, the substrate concentration, and incubation conditions. In the current study, incubation of butyrylthiocholine in a concentration range of 0.005-3.0 mM, with 317 pM human butyrylcholinesterase in vitro, resulted in rates of production of thiocholine that were accurately described by simple Michaelis-Menten kinetics, with a K m of 0.10 mM. Similarly, the inhibition of butyrylcholinesterase in vitro by the organophosphate chlorpyrifos oxon was described by simple Michaelis-Menten kinetics, with a k i of 3048 nM -1 h -1 , and a K D of 2.02 nM. In contrast to inhibition of butyrylcholinesterase, inhibition of human acetylcholinesterase by chlorpyrifos oxon in vitro followed concentration-dependent inhibition kinetics, with the k i increasing as the inhibitor concentration decreased. Chlorpyrifos oxon concentrations of 10 and 0.3 nM gave k i s of 1.2 and 19.3 nM -1 h -1 , respectively. Although the mechanism of concentration-dependent inhibition kinetics is not known, the much smaller, more restrictive active site gorge of acetylcholinesterase almost certainly plays a role. Similarly, the much larger active site gorge of butyrylcholinesterase likely contributes to its much greater reactivity towards chlorpyrifos oxon, compared to acetylcholinesterase.

  20. Brain acetylcholinesterase activity controls systemic cytokine levels through the cholinergic anti-inflammatory pathway

    Science.gov (United States)

    Pavlov, Valentin A.; Parrish, William R.; Rosas-Ballina, Mauricio; Ochani, Mahendar; Puerta, Margot; Ochani, Kanta; Chavan, Sangeeta; Al-Abed, Yousef; Tracey, Kevin J.

    2015-01-01

    The excessive release of cytokines by the immune system contributes importantly to the pathogenesis of inflammatory diseases. Recent advances in understanding the biology of cytokine toxicity led to the discovery of the “cholinergic anti-inflammatory pathway,” defined as neural signals transmitted via the vagus nerve that inhibit cytokine release through a mechanism that requires the alpha7 subunit-containing nicotinic acetylcholine receptor (α7nAChR). Vagus nerve regulation of peripheral functions is controlled by brain nuclei and neural networks, but despite considerable importance, little is known about the molecular basis for central regulation of the vagus nerve-based cholinergic anti-inflammatory pathway. Here we report that brain acetylcholinesterase activity controls systemic and organ specific TNF production during endotoxemia. Peripheral administration of the acetylcholinesterase inhibitor galantamine significantly reduced serum TNF levels through vagus nerve signaling, and protected against lethality during murine endotoxemia. Administration of a centrally-acting muscarinic receptor antagonist abolished the suppression of TNF by galantamine, indicating that suppressing acetylcholinesterase activity, coupled with central muscarinic receptors, controls peripheral cytokine responses. Administration of galantamine to α7nAChR knockout mice failed to suppress TNF levels, indicating that the α7nAChR-mediated cholinergic anti-inflammatory pathway is required for the anti-inflammatory effect of galantamine. These findings show that inhibition of brain acetylcholinesterase suppresses systemic inflammation through a central muscarinic receptor-mediated and vagal- and α7nAChR-dependent mechanism. Our data also indicate that a clinically used centrally-acting acetylcholinesterase inhibitor can be utilized to suppress abnormal inflammation to therapeutic advantage. PMID:18639629

  1. Comparison of Chlorpyrifos-Oxon and Paraoxon Acetylcholinesterase Inhibition Dynamics: Potential role of a peripheral binding site

    Energy Technology Data Exchange (ETDEWEB)

    Kousba, Ahmed A.; Sultatos, L G.; Poet, Torka S.; Timchalk, Chuck

    2004-08-02

    The primary mechanism of action for organophosphorus (OP) insecticides involves the inhibition of acetylcholinesterase (AChE) by oxygenated metabolites (oxons). This inhibition has been attributed to the phosphorylation of the serine hydroxyl group located in the active site of the AChE molecule. The rate of phosphorylation is described by the bimolecular inhibitory rate constant (ki), which has been utilized for quantification of OP inhibitory capacity. It has been previously proposed that a peripheral binding site exists on the AChE molecule, which when occupied, reduces the capacity of additional oxon molecules to phosphorylate the active site. The objective of the current study was to evaluate the interaction of chlorpyrifos oxon (CPO) and paraoxon (PO) with rat brain AChE using a modified Ellman assay in conjunction with a pharmacodynamic model to further assess the dynamics of AChE inhibition and the potential role of a peripheral binding site. The ki for AChE inhibition determined at oxon concentrations of 5 x 10{sup -4} 100 nM were 0.212 and 0.0216 nM-1h-1 for CPO and PO, respectively. The spontaneous reactivation rates of the inhibited AChE for CPO and PO were 0.087 and 0.078 h-1, respectively. In contrast, the ki estimated at a low oxon concentration (1 pM) were {approx} 1,000 and 10,000 -fold higher than those determined at high CPO and PO concentrations, respectively. At these low concentrations, the ki estimates were approximately similar for both CPO and PO (180 and 250 nM-1h-1, respectively). This implies that at low exposure concentrations, both oxons exhibited similar inhibitory potency in contrast to the marked difference exhibited at higher concentrations, which is consistent with the presence of a peripheral binding site on the AChE enzyme. These results support the potential importance of a secondary binding site associated with AChE kinetics, particularly at low environmentally relevant concentrations.

  2. Acetylcholinesterase activity of electric eel is increased or decreased by selected monoterpenoids and phenylpropanoids in a concentration-dependent manner.

    Science.gov (United States)

    López, María Dolores; Campoy, Francisco J; Pascual-Villalobos, María Jesús; Muñoz-Delgado, Encarnación; Vidal, Cecilio J

    2015-03-05

    The profitable insecticidal action of monoterpenoids prompted us to test their efficiency against stored-grain beetle species, via inhibition of acetylcholinesterase (AChE). For this, we first studied the ability of the monoterpenoids geraniol, linalool, camphor, fenchone, carvone and γ-terpinene, besides the phenylpropanoids trans-anethole and estragole to inhibit Electrophorus AChE. The results indicated that while AChE activity increased (15-35%) with 40 μM geraniol, camphor, γ-terpinene and linalool, the activity decreased (60-40%) with 5mM carvone, γ-terpinene, and fenchone. The Km for AChE was 0.52 ± 0.02 mM in control assays, which fell to 0.28 ± 0.01 mM or 0.32 ± 0.01 mM in assays with 20 μM linalool or γ-terpinene added. In the millimolar range, the terpenoids behaved as weak inhibitors. Unexpectedly, AChE inhibition by camphor, carvone, γ-terpinene, and fenchone gave Hill numbers ranging 2.04-1.57, supporting the idea that AChE was able to lodge more than one monoterpenoid molecule. The plots of 1/v vs. 1/S at varying monoterpenoid provided straight lines, fenchone and γ-terpinene acting as competitive inhibitors and carvone and camphor as non-competitive inhibitors. Moreover, the secondary plots of the slope KM(app)/Vmax(app) vs. [I] and of 1/Vmax(app) vs. [I] gave parabolic curves, which lent support to the proposed capacity of AChE to bind more than one monoterpenoid molecule. The fitting of the curves to a second-order polynomial equation allowed us to calculate the inhibition constants for the interaction of AChE with fenchone, γ-terpinene, carvone and camphor. The previously unnoticed increase in AChE activity with monoterpenoids should be considered as a reminder when advising the use of essential oils of plants or their constituents as anti-AChE agents to attenuate pathological signs of Alzheimer's disease. Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.

  3. Mixture for Controlling Insecticide-Resistant Malaria Vectors

    OpenAIRE

    Pennetier, Cédric; Costantini, Carlo; Corbel, Vincent; Licciardi, Séverine; Dabire, R. K.; Lapied, B.; Chandre, Fabrice; Hougard, Jean-Marc

    2008-01-01

    The spread of resistance to pyrethroids in the major Afrotropical malaria vectors Anopheles gambiae s.s. necessitates the development of new strategies to control resistant mosquito populations. To test the efficacy of nets treated with repellent and insecticide against susceptible and insecticide-resistant An. gambiae mosquito populations, we impregnated mosquito bed nets with an insect repellent mixed with a low dose of organophosphorous insecticide and tested them in a rice-growing area ne...

  4. CYP6 P450 enzymes and ACE-1 duplication produce extreme and multiple insecticide resistance in the malaria mosquito Anopheles gambiae.

    Science.gov (United States)

    Edi, Constant V; Djogbénou, Luc; Jenkins, Adam M; Regna, Kimberly; Muskavitch, Marc A T; Poupardin, Rodolphe; Jones, Christopher M; Essandoh, John; Kétoh, Guillaume K; Paine, Mark J I; Koudou, Benjamin G; Donnelly, Martin J; Ranson, Hilary; Weetman, David

    2014-03-01

    Malaria control relies heavily on pyrethroid insecticides, to which susceptibility is declining in Anopheles mosquitoes. To combat pyrethroid resistance, application of alternative insecticides is advocated for indoor residual spraying (IRS), and carbamates are increasingly important. Emergence of a very strong carbamate resistance phenotype in Anopheles gambiae from Tiassalé, Côte d'Ivoire, West Africa, is therefore a potentially major operational challenge, particularly because these malaria vectors now exhibit resistance to multiple insecticide classes. We investigated the genetic basis of resistance to the most commonly-applied carbamate, bendiocarb, in An. gambiae from Tiassalé. Geographically-replicated whole genome microarray experiments identified elevated P450 enzyme expression as associated with bendiocarb resistance, most notably genes from the CYP6 subfamily. P450s were further implicated in resistance phenotypes by induction of significantly elevated mortality to bendiocarb by the synergist piperonyl butoxide (PBO), which also enhanced the action of pyrethroids and an organophosphate. CYP6P3 and especially CYP6M2 produced bendiocarb resistance via transgenic expression in Drosophila in addition to pyrethroid resistance for both genes, and DDT resistance for CYP6M2 expression. CYP6M2 can thus cause resistance to three distinct classes of insecticide although the biochemical mechanism for carbamates is unclear because, in contrast to CYP6P3, recombinant CYP6M2 did not metabolise bendiocarb in vitro. Strongly bendiocarb resistant mosquitoes also displayed elevated expression of the acetylcholinesterase ACE-1 gene, arising at least in part from gene duplication, which confers a survival advantage to carriers of additional copies of resistant ACE-1 G119S alleles. Our results are alarming for vector-based malaria control. Extreme carbamate resistance in Tiassalé An. gambiae results from coupling of over-expressed target site allelic variants with

  5. Heating-insensitive scale increase caused by convective precipitation

    Science.gov (United States)

    Haerter, Jan; Moseley, Christopher; Berg, Peter

    2017-04-01

    The origin of intense convective extremes and their unusual temperature dependence has recently challenged traditional thermodynamic arguments, based on the Clausius-Clapeyron relation. In a sequence of studies (Lenderink and v. Mejgaard, Nat Geosc, 2008; Berg, Haerter, Moseley, Nat Geosc, 2013; and Moseley, Hohenegger, Berg, Haerter, Nat Geosc, 2016) the argument of convective-type precipitation overcoming the 7%/K increase in extremes by dynamical, rather than thermodynamic, processes has been promoted. How can the role of dynamical processes be approached for precipitating convective cloud? One-phase, non-precipitating Rayleigh-Bénard convection is a classical problem in complex systems science. When a fluid between two horizontal plates is sufficiently heated from below, convective rolls spontaneously form. In shallow, non-precipitating atmospheric convection, rolls are also known to form under specific conditions, with horizontal scales roughly proportional to the boundary layer height. Here we explore within idealized large-eddy simulations, how the scale of convection is modified, when precipitation sets in and intensifies in the course of diurnal solar heating. Before onset of precipitation, Bénard cells with relatively constant diameter form, roughly on the scale of the atmospheric boundary layer. We find that the onset of precipitation then signals an approximately linear (in time) increase in horizontal scale. This scale increase progresses at a speed which is rather insensitive to changes in surface temperature or changes in the rate at which boundary conditions change, hinting at spatial characteristics, rather than temperature, as a possible control on spatial scales of convection. When exploring the depth of spatial correlations, we find that precipitation onset causes a sudden disruption of order and a subsequent complete disintegration of organization —until precipitation eventually ceases. Returning to the initial question of convective

  6. Anti-acetylcholinesterase and Antioxidant Activity of Essential Oils from Hedychium gardnerianum Sheppard ex Ker-Gawl

    OpenAIRE

    Arruda, Miguel; Viana, Hugo; Rainha, Nuno; Neng, Nuno R.; Rosa, José Silvino; Nogueira, José M. F.; Barreto, Maria do Carmo

    2012-01-01

    Acetylcholinesterase inhibition, antioxidant and cytotoxic activities of Hedychium gardnerianum leaf essential oils from S. Miguel Island were determined. All the oils inhibited acetylcholinesterase, with IC50 values of approximately 1 mg/mL, showing no statistical differences between collection sites. Three oils presented mixed inhibition, whilst one was almost truly competitive. This activity can be attributed to the presence of sesquiterpenes, which constituted more than 60% of the composi...

  7. Insecticides suppress natural enemies and increase pest damage in cabbage.

    Science.gov (United States)

    Bommarco, Riccardo; Miranda, Freddy; Bylund, Helena; Björkman, Christer

    2011-06-01

    Intensive use of pesticides is common and increasing despite a growing and historically well documented awareness of the costs and hazards. The benefits from pesticides of increased yields from sufficient pest control may be outweighed by developed resistance in pests and killing of beneficial natural enemies. Other negative effects are human health problems and lower prices because of consumers' desire to buy organic products. Few studies have examined these trade-offs in the field. Here, we demonstrate that Nicaraguan cabbage (Brassica spp.) farmers may suffer economically by using insecticides as they get more damage by the main pest diamondback moth, Plutella xylostella (L.) (Lepidoptera: Plutellidae), at the same time as they spend economic resources on insecticides. Replicated similarly sized cabbage fields cultivated in a standardized manner were either treated with insecticides according common practice or not treated with insecticides over two seasons. Fields treated with insecticides suffered, compared with nontreated fields, equal or, at least in some periods of the seasons, higher diamondback moth pest attacks. These fields also had increased leaf damage on the harvested cabbage heads. Weight and size of the heads were not affected. The farmers received the same price on the local market irrespective of insecticide use. Rates of parasitized diamondback moth were consistently lower in the treated fields. Negative effects of using insecticides against diamondback moth were found for the density of parasitoids and generalist predatory wasps, and tended to affect spiders negatively. The observed increased leaf damages in insecticide-treated fields may be a combined consequence of insecticide resistance in the pest, and of lower predation and parasitization rates from naturally occurring predators that are suppressed by the insecticide applications. The results indicate biological control as a viable and economic alternative pest management strategy

  8. Diagnostic Doses of Insecticides for Adult Aedes aegypti to Assess Insecticide Resistance in Cuba.

    Science.gov (United States)

    Rodríguez, María Magdalena; Crespo, Ariel; Hurtado, Daymi; Fuentes, Ilario; Rey, Jorge; Bisset, Juan Andrés

    2017-06-01

    The objective of this study was to determine diagnostic doses (DDs) of 5 insecticides for the Rockefeller susceptible strain of Aedes aegypti , using the Centers for Disease Control and Prevention (CDC) bottle bioassay as a tool for monitoring insecticide resistance in the Cuban vector control program. The 30-min DD values determined in this study were 13.5 μg/ml, 6.5 μg/ml, 6 μg/ml, 90.0 μg/ml, and 15.0 μg/ml for cypermethrin, deltamethrin, lambda-cyhalothrin, chlorpyrifos, and propoxur, respectively. To compare the reliability of CDC bottle bioassay with the World Health Organization susceptible test, 3 insecticide-resistant strains were evaluated for deltamethrin and lambda-cyhalothrin. Results showed that the bottles can be used effectively from 21 to 25 days after treatment and reused up to 4 times, depending on the storage time. The CDC bottle bioassay is an effective tool to assess insecticide resistance in field populations of Ae. aegypti in Cuba and can be incorporated into vector management programs using the diagnostic doses determined in this study.

  9. Evaluating Diagnostic Value of Electrophysiological Testing (EMG-NCV Compared to the Activity Level of Acetylcholinesterase in Serum and Red Blood Cells of Patients with Moderate to Severe Organophosphate Poisoning

    Directory of Open Access Journals (Sweden)

    Fares Najari

    2017-05-01

    Full Text Available Background Organophosphate compounds cause poisoning and death more than any other insecticide. These toxins can cause peripheral neuropathy which is delayed for about 3 - 6 weeks and no method has been known for predicting the incidence. It has been claimed that electrophysiological tests (EMG - NCV can help in predicting the disorder. Objectives The main purpose of this research was to study EMG - NCV tests in patients with moderate to severe organophosphate poisoning. Methods This was a cross-sectional study conducted on patients with moderate to severe organophosphate poisoning from 2014 to 2016 in Imam Reza hospital of Mashhad. The minimum sample size was calculated as 68 patients and then all data was collected on the basis of inclusion and exclusion criteria using data collection form designed by the researcher, and finally data were analyzed using SPSS V.21 software, descriptive tests (including mean, median, mode and analytical tests (K square, ANOVA. Results Of all 78 patients with the mean age of 27.50 ± 10.0, 45 were female and the rest were male. Totally 29.5% of the patients had abnormal EMG - NCV. Although no significant differences were observed between electro diagnostic tests (EMG - NCV and age, gender, clinical symptoms and levels of acetylcholinesterase serum activity, the relationship between EMG - NCV and RBC levels of acetylcholinesterase activity was significant. Conclusions Electrophysiological tests are not associated with clinical symptoms (muscle weakness and they cannot be considered as a determining factor to discharge the patients; therefore, careful examination of the patients or evaluating the level of AChE activity in red blood cells is needed.

  10. Munitions having an insensitive detonator system for initiating large failure diameter explosives

    Science.gov (United States)

    Perry, III, William Leroy

    2015-08-04

    A munition according to a preferred embodiment can include a detonator system having a detonator that is selectively coupled to a microwave source that functions to selectively prime, activate, initiate, and/or sensitize an insensitive explosive material for detonation. The preferred detonator can include an explosive cavity having a barrier within which an insensitive explosive material is disposed and a waveguide coupled to the explosive cavity. The preferred system can further include a microwave source coupled to the waveguide such that microwaves enter the explosive cavity and impinge on the insensitive explosive material to sensitize the explosive material for detonation. In use the preferred embodiments permit the deployment and use of munitions that are maintained in an insensitive state until the actual time of use, thereby substantially preventing unauthorized or unintended detonation thereof.

  11. Searching for the variables that control human rule-governed "insensitivity".

    Science.gov (United States)

    Fox, Adam E; Kyonka, Elizabeth G E

    2017-09-01

    Verbal rules or instructions often exert obvious and meaningful control over human behavior. Sometimes instructions benefit the individual by enabling faster acquisition of a skill or by obviating an aversive consequence. However, research has also suggested a clear disadvantage: "insensitivity" to changing underlying contingencies. The two experiments described here investigated the variables that control initial rule-following behavior and rule-following insensitivity. When the initial rule was inaccurate, behavior was consistent with the rule for approximately half of participants and all participants' behavior was mostly insensitive to changing contingencies. When the initial rule was accurate, behavior of all participants was consistent with it and behavior for nearly all participants was insensitive to changes in underlying contingencies. These findings have implications for how best to establish and maintain rule-following behavior in applied settings when deviant behavior would be more reinforcing to the individual. © 2017 Society for the Experimental Analysis of Behavior.

  12. Emamectin benzoate: new insecticide against Helicoverpa armigera.

    Science.gov (United States)

    Fanigliulo, A; Sacchetti, M

    2008-01-01

    Emamectin benzoate is a new insecticide of Syngenta Crop Protection, with a new mechanism of action and a strong activity against Lepidoptera as well as with and a high selectivity on useful organisms. This molecule acts if swallowed and has some contact action. It penetrates leaf tissues (translaminar activity) and forms a reservoir within the leaf. The mechanism of action is unique in the panorama of insecticides. In facts, it inhibits muscle contraction, causing a continuous flow of chlorine ions in the GABA and H-Glutamate receptor sites. During 2006 and 2007, experimentation was performed by the Bioagritest test facility, according to EPPO guidelines and Principles of Good Experimental Practice (GEP), aiming at establishing the biological efficacy and the selectivity of Emamectin benzoate on industry tomato against Helicoverpa armigera (Lepidoptera: Noctuidoe). The study was performed in Tursi-Policoro (Matera), southern Italy. Experimental design consisted in random blocks, in 4 repetitions. A dosage of 1.5 Kg/ha of the formulate was compared with two commercial formulates: Spinosad 0.2 kg/ha (Laser, Dow Agrosciences Italia) and Indoxacarb 0.125 kg/ha (Steward EC insecticide, Dupont). Three foliage applications were applied every 8 days. The severity of damage induced by H. armigera was evaluated on fruits. Eventual phytotoxic effects were also evaluated. Climatic conditions were optimal for Lepidoptera development, so that the percentage of fruits attacked in 2007 at the first scouting was 68.28%. Emamectin benzoate has shown, in two years of testing, a high control of H. armigera if compared with the standards Indoxacarb and Spinosad. No effect of phytotoxicity was noticed on fruits.

  13. BACILLUS THURINGIENSIS ELASTASES WITH INSECTICIDE ACTIVITY

    Directory of Open Access Journals (Sweden)

    E. V. Matseliukh

    2015-10-01

    Full Text Available The purpose of the research was a screening of proteases with elastase activity among Bacillus thuringiensis strains, their isolation, partially purification, study of physicochemical properties and insecticide activity in relation to the larvae of the Colorado beetle. The objects of the investigation were 18 strains of B. thuringiensis, isolated from different sources: sea water, dry biological product "Bitoksibatsillin" and also from natural populations of Colorado beetles of the Crimea, Kherson, Odesa, Mykolaiv and Zaporizhiia regions of Ukraine. Purification of enzymes with elastase activity isolated from above mentioned strains was performed by gel-chromatography and insecticide activity was studied on the 3–4 larvae instar of Colorado beetle. The ability of a number of B. thuringiensis strains to synthesize the proteases with elastase activity has been established. The most active were enzymes obtained from strains IMV B-7465, IMV B-7324 isolated from sea water, and strains 9, 902, Bt-H and 0-239 isolated from Colorado beetles. The study of the physicochemical properties of the partially purified proteases of these strains showed that they belonged to enzymes of the serine type. Peptidases of a number of B. thuringiensis strains (IMV B-7324, IMV B-7465, 902, 0-239, 9 are metal-dependent enzymes. Optimal conditions of action of all tested enzymes are the neutral and alkaline рН values and the temperatures of 30–40 °С. The studies of influence of the complex enzyme preparations and partially purified ones of B. thuringiensis strains on the larvae instar of Colorado beetles indicated that enzymes with elastase activity could be responsible for insecticide action of the tested strains.

  14. Inhibition of Acetylcholinesterase and Fatty Acid Composition in Theobroma grandiflorum Seeds

    Directory of Open Access Journals (Sweden)

    Casandra Valentina Itriago

    2017-07-01

    Full Text Available Theobroma grandiflorum is an important fruit tree from Sterculiaceae family, native to the Brazilian Amazon, known in the region as cupuaçu. The seeds have a high fat content (24% with characteristics that resemble those of cocoa (Theobroma cacao butter with potential applications in the cosmetic, pharmaceutical and food industries. The main objective of this work was to explore the seed fats from T. grandiflorum that were analyzed for fatty acid composition by Gas Chromatography with Flame Ionization Detector (GC-FID and to analyze their activity for acetylcholinesterase inhibition. Chromatographic analysis provided detection of nine fatty acids. The major fatty acids found in the species were oleic (40.0%, stearic (32.7%, arachidic (10.4% and palmitic (8.0%. The acetylcholinesterase inhibition by fats from seeds was over 40.48%. DOI: http://dx.doi.org/10.17807/orbital.v0i0.894 

  15. Alpha-Bungarotoxin labeling and acetylcholinesterase localization at the Mauthner fiber giant synapse in the hatchetfish

    International Nuclear Information System (INIS)

    Day, J.W.; Hall, D.H.; Hall, L.M.; Bennett, M.V.

    1983-01-01

    Autoradiographic and histochemical techniques have been used to characterize further the pharmacology of transmission at the Mauthner fiber giant synapse of the South American hatchetfish. [ 125 I]alpha-Bungarotoxin was applied to hatchetfish medullae and a standard autoradiographic procedure was carried out on 3- to 4-microns sections of glutaraldehyde-fixed tissue. All Mauthner fiber giant synapses, as identified by light microscopic criteria, had closely associated silver grains. Labeling was blocked by d-tubocurarine. Glutaraldehyde-fixed slices of hatchetfish medulla were stained histochemically for acetylcholinesterase; all giant synapses that could be identified in the light microscope showed heavy deposits of reaction product. Staining was blocked by diisopropyl-fluorophosphate, which inhibits both pseudocholinesterase and acetylcholinesterase, but was not blocked by tetraisopropylpyrophosphoramide, a specific pseudocholinesterase inhibitor. This evidence strongly supports the suggestion that the Mauthner fiber giant synapse is nicotinic cholinergic

  16. alpha-Bungarotoxin labeling and acetylcholinesterase localization at the Mauthner fiber giant synapse in the hatchetfish

    International Nuclear Information System (INIS)

    Day, J.W.; Hall, D.H.; Hall, L.M.; Bennett, M.V.

    1983-01-01

    Autoradiographic and histochemical techniques have been used to characterize further the pharmacology of transmission at the Mauthner fiber giant synapse of the South American hatchetfish. [ 125 I]alpha-Bungarotoxin was applied to hatchetfish medullae and a standard autoradiographic procedure was carried out on 3- to 4-microns sections of glutaraldehyde-fixed tissue. All Mauthner fiber giant synapses, as identified by light microscopic criteria, had closely associated silver grains. Labeling was blocked by d-tubocurarine. Glutaraldehyde-fixed slices of hatchetfish medulla were stained histochemically for acetylcholinesterase; all giant synapses that could be identified in the light microscope showed heavy deposits of reaction product. Staining was blocked by diisopropyl-fluorophosphate, which inhibits both pseudocholinesterase and acetylcholinesterase, but was not blocked by tetraisopropylpyrophosphoramide, a specific pseudocholinesterase inhibitor. This evidence strongly supports the suggestion that the Mauthner fiber giant synapse is nicotinic cholinergic

  17. A New Acetylcholinesterase Inhibitor from Green Glycosylation of Trachyloban-19-oic Acid by Mucor plumbeus.

    Science.gov (United States)

    Santos, Gabriel F Dos; Takahashi, Jacqueline A

    2017-01-01

    The in vitro metabolism of a widespread natural product, trachyloban-19-oic acid (1), by the fungal species Mucor plumbeus was studied in a sucrose-yeast liquid medium. Two products were isolated, and their structures were determined by spectroscopic means as 7β-hydroxytrachyloban-19-oic acid (5) and trachyloban-19-O-β-D-glucopyranosyl ester (6). To the best of our knowledge, compound 6 is herein reported by the first time in the literature. These compounds were assayed for acetylcholinesterase inhibition along with some related compounds. Compound 6 showed the highest acetylcholinesterase inhibitory activity at 10000 µg/mL among the tested compounds, a result (92.89%) comparable to the activity of the positive control, galanthamine (94.21%). Therefore, biotransformation of the natural product 1 by M. plumbeus produced a novel compound with potential as a new lead to develop anti-Alzheimer medicines.

  18. A New Acetylcholinesterase Inhibitor from Green Glycosylation of Trachyloban-19-oic Acid by Mucor plumbeus

    Directory of Open Access Journals (Sweden)

    GABRIEL F. DOS SANTOS

    2017-10-01

    Full Text Available ABSTRACT The in vitro metabolism of a widespread natural product, trachyloban-19-oic acid (1, by the fungal species Mucor plumbeus was studied in a sucrose-yeast liquid medium. Two products were isolated, and their structures were determined by spectroscopic means as 7β-hydroxytrachyloban-19-oic acid (5 and trachyloban-19-O-β-D-glucopyranosyl ester (6. To the best of our knowledge, compound 6 is herein reported by the first time in the literature. These compounds were assayed for acetylcholinesterase inhibition along with some related compounds. Compound 6 showed the highest acetylcholinesterase inhibitory activity at 10000 µg/mL among the tested compounds, a result (92.89% comparable to the activity of the positive control, galanthamine (94.21%. Therefore, biotransformation of the natural product 1 by M. plumbeus produced a novel compound with potential as a new lead to develop anti-Alzheimer medicines.

  19. Alpha-Bungarotoxin labeling and acetylcholinesterase localization at the Mauthner fiber giant synapse in the hatchetfish

    Energy Technology Data Exchange (ETDEWEB)

    Day, J.W.; Hall, D.H.; Hall, L.M.; Bennett, M.V.

    1983-02-01

    Autoradiographic and histochemical techniques have been used to characterize further the pharmacology of transmission at the Mauthner fiber giant synapse of the South American hatchetfish. (/sup 125/I)alpha-Bungarotoxin was applied to hatchetfish medullae and a standard autoradiographic procedure was carried out on 3- to 4-microns sections of glutaraldehyde-fixed tissue. All Mauthner fiber giant synapses, as identified by light microscopic criteria, had closely associated silver grains. Labeling was blocked by d-tubocurarine. Glutaraldehyde-fixed slices of hatchetfish medulla were stained histochemically for acetylcholinesterase; all giant synapses that could be identified in the light microscope showed heavy deposits of reaction product. Staining was blocked by diisopropyl-fluorophosphate, which inhibits both pseudocholinesterase and acetylcholinesterase, but was not blocked by tetraisopropylpyrophosphoramide, a specific pseudocholinesterase inhibitor. This evidence strongly supports the suggestion that the Mauthner fiber giant synapse is nicotinic cholinergic.

  20. alpha-Bungarotoxin labeling and acetylcholinesterase localization at the Mauthner fiber giant synapse in the hatchetfish

    Energy Technology Data Exchange (ETDEWEB)

    Day, J.W.; Hall, D.H.; Hall, L.M.; Bennett, M.V.

    1983-02-01

    Autoradiographic and histochemical techniques have been used to characterize further the pharmacology of transmission at the Mauthner fiber giant synapse of the South American hatchetfish. (/sup 125/I)alpha-Bungarotoxin was applied to hatchetfish medullae and a standard autoradiographic procedure was carried out on 3- to 4-microns sections of glutaraldehyde-fixed tissue. All Mauthner fiber giant synapses, as identified by light microscopic criteria, had closely associated silver grains. Labeling was blocked by d-tubocurarine. Glutaraldehyde-fixed slices of hatchetfish medulla were stained histochemically for acetylcholinesterase; all giant synapses that could be identified in the light microscope showed heavy deposits of reaction product. Staining was blocked by diisopropyl-fluorophosphate, which inhibits both pseudocholinesterase and acetylcholinesterase, but was not blocked by tetraisopropylpyrophosphoramide, a specific pseudocholinesterase inhibitor. This evidence strongly supports the suggestion that the Mauthner fiber giant synapse is nicotinic cholinergic.

  1. Chlorpyrifos-induced hormesis in insecticide-resistant and -susceptible Plutella xylostella under normal and high temperatures.

    Science.gov (United States)

    Deng, Z Z; Zhang, F; Wu, Z L; Yu, Z Y; Wu, G

    2016-06-01

    Hormesis induced by insecticides at the dosage lower than what ostensibly directly causes death on insects was studied. This paper reports the effects of the in vivo application of varied concentrations of chlorpyrifos (CPF) on Plutella xylostella (DBM). The insecticide concentrations applied included 0.000025-2.5 mg l-1, which are far lower than LC1 (7.2 mg l-1), for the CPF-susceptable (Si) DBM, and 250 mg l-1 which is far below LC1 (1286 mg l-1), for the CPF-resistant (Rc) DBM, as well as LC10- and LC50-doses for both strains. Significant hormesis was found with the 'hermetic-CPFs', i.e., 0.0025 mg l-1 for Si DBM and 2.5 mg l-1 for Rc DBM, at the normal or high temperature either in a 24 h or under a long-term treatment. These doses of CPF significantly stimulated the development and increased the fecundity of Si and Rc DBM at 25°C with approximately 23.5-29.8% activity increase on acetylcholinesterase (AChE) and 30.5-91.3% increase on glutathione S-transferases (GSTs) at 25 or 38°C in 4-24 h. The enzymatic activities were significantly reduced by LC50-CPF at 25°C in vivo, but the inhibition was relieved significantly, if the insects were first subjected to a hormetic-CPF pretreatment. It was remarkable that the average rates of enzymatic activity increase were 67.5-76.6% for AChE and 366-546% for GSTs. Consequently, it was concluded that the hormesis on Si and Rc DBM could be induced by CPF doses far below LC1 at normal or high temperature in short- or long-term treatment. These findings might help to improve the current insect control practices in the field.

  2. Gene transcription in Daphnia magna: effects of acute exposure to a carbamate insecticide and an acetanilide herbicide.

    Science.gov (United States)

    Pereira, Joana Luísa; Hill, Christopher J; Sibly, Richard M; Bolshakov, Viacheslav N; Gonçalves, Fernando; Heckmann, Lars-Henrik; Callaghan, Amanda

    2010-05-05

    Daphnia magna is a key invertebrate in the freshwater environment and is used widely as a model in ecotoxicological measurements and risk assessment. Understanding the genomic responses of D. magna to chemical challenges will be of value to regulatory authorities worldwide. Here we exposed D. magna to the insecticide methomyl and the herbicide propanil to compare phenotypic effects with changes in mRNA expression levels. Both pesticides are found in drainage ditches and surface water bodies standing adjacent to crops. Methomyl, a carbamate insecticide widely used in agriculture, inhibits acetylcholinesterase, a key enzyme in nerve transmission. Propanil, an acetanilide herbicide, is used to control grass and broad-leaf weeds. The phenotypic effects of single doses of each chemical were evaluated using a standard immobilisation assay. Immobilisation was linked to global mRNA expression levels using the previously estimated 48h-EC(1)s, followed by hybridization to a cDNA microarray with more than 13,000 redundant cDNA clones representing >5000 unique genes. Following exposure to methomyl and propanil, differential expression was found for 624 and 551 cDNAs, respectively (one-way ANOVA with Bonferroni correction, P

  3. Polarization Insensitive Wavelength Conversion Based on Four-Wave Mixing in a Silicon Nanowire

    DEFF Research Database (Denmark)

    Pu, Minhao; Hu, Hao; Peucheret, Christophe

    2012-01-01

    We experimentally demonstrate, for the first time, polarization-insensitive wavelength conversion of a 10 Gb/s NRZ-OOK data signal based on four-wave mixing in a silicon nanowire with bit-error rate measurements.......We experimentally demonstrate, for the first time, polarization-insensitive wavelength conversion of a 10 Gb/s NRZ-OOK data signal based on four-wave mixing in a silicon nanowire with bit-error rate measurements....

  4. 40 Gbit/s NRZ Packet-Length Insensitive Header Extraction for Optical Label Switching Networks

    DEFF Research Database (Denmark)

    Seoane, Jorge; Kehayas, E; Avramopoulos, H.

    2006-01-01

    A simple method for 40 Gbit/s NRZ header extraction based on envelope detection for optical label switching networks is presented. The scheme is insensitive to packet length and spacing and can be single-chip integrated cost-effectively......A simple method for 40 Gbit/s NRZ header extraction based on envelope detection for optical label switching networks is presented. The scheme is insensitive to packet length and spacing and can be single-chip integrated cost-effectively...

  5. Polarization Insensitive One-to-Six WDM Multicasting in a Silicon Nanowire

    DEFF Research Database (Denmark)

    Pu, Minhao; Hu, Hao; Peucheret, Christophe

    2012-01-01

    We present polarization insensitive one-to-six WDM multicasting based on nondegenerate four-wave mixing in a silicon nanowire with angled-pump scheme. Bit-error rate measurements are performed and error-free operation is achieved.......We present polarization insensitive one-to-six WDM multicasting based on nondegenerate four-wave mixing in a silicon nanowire with angled-pump scheme. Bit-error rate measurements are performed and error-free operation is achieved....

  6. Effectiveness and profitability of insecticide formulations used for ...

    African Journals Online (AJOL)

    To identify optimal pest control with lower economic risks to farmers, we investigated the effectiveness and profitability of different insecticides and insecticide formulations against bean fly (Ophiomyia spp.) and bean flower thrips (Megalurothrips sjostedtii). Two separate experiments were conducted during 2009 to 2012.

  7. Effects of insecticide spray application on insect pest infestation and ...

    African Journals Online (AJOL)

    USER

    2010-03-15

    Mar 15, 2010 ... This study provides information on the incidence of major insect pests of cowpea as well as the minimum insecticide control intervention necessary for effectively reducing cowpea yield losses on the field. Two insecticide spray regimes (once at flowering and podding) significantly reduced insect population ...

  8. Effects of insecticide spray application on insect pest infestation and ...

    African Journals Online (AJOL)

    Field studies were conducted during the 2008 - 2009 cropping season to determine the minimal insecticide application which can reduce cowpea yield losses on the field due to insect pest infestations in the Transkei region of South Africa. Treatments consisted of five cowpea varieties and four regimes of insecticide spray ...

  9. Design, Synthesis and Insecticidal Activities of Novel Phenyl Substituted Isoxazolecarboxamides

    Institute of Scientific and Technical Information of China (English)

    LIU Peng-fei; ZHANG Ji-feng; YAN Tao; XIONG Li-xia; LI Zheng-ming

    2012-01-01

    Thirteen novel phenyl substituted isoxazolecarboxamides were synthesized,and their structures were characterized by 1H NMR,elementary analysis and high-resolution mass spectrometry(HRMS) techniques.Their evaluated insecticidal activities against oriental armyworm(Mythimna separata) indicate that the phcnyl substituted isoxazolecarboxamides exhibited moderate insecticidal activities,among which compounds 9c and 9k showed comparatively higher activities.

  10. Mechanistic modeling of insecticide risks to breeding birds in ...

    Science.gov (United States)

    Insecticide usage in the United States is ubiquitous in urban, suburban, and rural environments. In evaluating data for an insecticide registration application and for registration review, scientists at the United States Environmental Protection Agency (USEPA) assess the fate of the insecticide and the risk the insecticide poses to the environment and non-target wildlife. At the present time, current USEPA risk assessments do not include population-level endpoints. In this paper, we present a new mechanistic model, which allows risk assessors to estimate the effects of insecticide exposure on the survival and seasonal productivity of birds known to use agricultural fields during their breeding season. The new model was created from two existing USEPA avian risk assessment models, the Terrestrial Investigation Model (TIM v.3.0) and the Markov Chain Nest Productivity model (MCnest). The integrated TIM/MCnest model has been applied to assess the relative risk of 12 insecticides used to control corn pests on a suite of 31 avian species known to use cornfields in midwestern agroecosystems. The 12 insecticides that were assessed in this study are all used to treat major pests of corn (corn root worm borer, cutworm, and armyworm). After running the integrated TIM/MCnest model, we found extensive differences in risk to birds among insecticides, with chlorpyrifos and malathion (organophosphates) generally posing the greatest risk, and bifenthrin and ë-cyhalothrin (

  11. Expression of melanin and insecticidal protein from Rhodotorula ...

    African Journals Online (AJOL)

    Both the salmon/red melanin and the insecticidal producing genes of Rhodotorula glutinis was successfully expressed in Escherichia coli using plasmid pZErO-1. This work suggests that in Rhodotorula species melanin and insecticidal toxin are co-expressed and therefore possibly co-evolved. Keywords: Rhodotorula ...

  12. Guide to testing insecticides on coniferous forest defoliators

    Science.gov (United States)

    Carroll B Jr. Williams; David A. Sharpnack; Liz Maxwell; Patrick J. Shea; Mark D. McGregor

    1985-01-01

    This report provides a guide to techniques for designing field tests of candidate insecticides, and for carrying out pilot tests and control projects. It describes experimental designs for testing hypotheses, and for sampling trees to estimate insect population densities and percent reduction after treatments. Directions for applying insecticides by aircraft and for...

  13. Biological efficacy of the ecotoxically favourable insecticides and ...

    African Journals Online (AJOL)

    Administrator

    2011-05-30

    May 30, 2011 ... different, studies done in natural conditions should be favored. Key words: Insecticides ... insecticide was applied on synthetic or natural food of the target insect ..... Pozsgay M, Fast P, Kaplan H, Carey PR (1987). The effect of ...

  14. Ecdysone Agonist: New Insecticides with Novel Mode of Action

    Directory of Open Access Journals (Sweden)

    Y. Andi Trisyono

    2002-12-01

    Full Text Available Development of insect resistance to insecticide has been the major driving force for the development of new insecticides. Awareness and demand from public for more environmentally friendly insecticides have contributed in shifting the trend from using broad spectrum to selective insecticides. As a result, scientists have looked for new target sites beyond the nervous system. Insect growth regulators (IGRs are more selective insecticides than conventional insecticides, and ecdysone agonists are the newest IGRs being commercialized, e.g. tebufenozide, methoxyfenozide, and halofenozide. Ecdysone agonists bind to the ecdysteroid receptors, and they act similarly to the molting hormone 20-hydroxyecdysone. The binding provides larvae or nymphs with a signal to enter a premature and lethal molting cycle. In addition, the ecdysone agonists cause a reduction in the number of eggs laid by female insects. The ecdysone agonists are being developed as selective biorational insecticides. Tebufenozide and methoxyfenozide are used to control lepidopteran insect pests, whereas halofenozide is being used to control coleopteran insect pests. Their selectivity is due to differences in the binding affinity between these compounds to the receptors in insects from different orders. The selectivity of these compounds makes them candidates to be used in combinations with other control strategies to develop integrated pest management programs in agricultural ecosystems. Key words: new insecticides, selectivity, ecdysone agonists

  15. Identification and cloning of two insecticidal protein genes from ...

    African Journals Online (AJOL)

    Bacillus thuringiensis (Bt) is the most widely applied type of microbial pesticide due to its high specificity and environmental safety. The activity of Bt is largely attributed to the insecticidal crystal protein encoded by the cry genes. Different insecticidal crystal proteins of Bt have different bioactivity against distinct agricultural ...

  16. Interactions of transgenic Bacillus thuringiensis insecticidal crops with spiders (Araneae)

    Science.gov (United States)

    Genetically modified crops expressing insecticidal proteins from Bacillus thuringiensis (Bt) have dramatically increased in acreage since their introduction in the mid-1990’s. Although the insecticidal mechanisms of Bt target specific pests, concerns persist regarding direct and indirect effects on...

  17. Conifer flavonoid compounds inhibit detoxification enzymes and synergize insecticides.

    Science.gov (United States)

    Wang, Zhiling; Zhao, Zhong; Cheng, Xiaofei; Liu, Suqi; Wei, Qin; Scott, Ian M

    2016-02-01

    Detoxification by glutathione S-transferases (GSTs) and esterases are important mechanisms associated with insecticide resistance. Discovery of novel GST and esterase inhibitors from phytochemicals could provide potential new insecticide synergists. Conifer tree species contain flavonoids, such as taxifolin, that inhibit in vitro GST activity. The objectives were to test the relative effectiveness of taxifolin as an enzyme inhibitor and as an insecticide synergist in combination with the organophosphorous insecticide, Guthion (50% azinphos-methyl), and the botanical insecticide, pyrethrum, using an insecticide-resistant Colorado potato beetle (CPB) Leptinotarsa decemlineata (Say) strain. Both taxifolin and its isomer, quercetin, increased the mortality of 1(st) instar CPB larvae after 48h when combined with Guthion, but not pyrethrum. Taxifolin had greater in vitro esterase inhibition compared with the commonly used esterase inhibitor, S, S, S-tributyl phosphorotrithioate (DEF). An in vivo esterase and GST inhibition effect after ingestion of taxifolin was measured, however DEF caused a greater suppression of esterase activity. This study demonstrated that flavonoid compounds have both in vitro and in vivo esterase inhibition, which is likely responsible for the insecticide synergism observed in insecticide-resistant CPB. Crown Copyright © 2015. Published by Elsevier Inc. All rights reserved.

  18. Chemical composition and acetylcholinesterase inhibitory activity of Artemisia maderaspatana essential oil.

    Science.gov (United States)

    Jyotshna; Srivastava, Nidhi; Singh, Bhuwanendra; Chanda, Debabrata; Shanker, Karuna

    2015-01-01

    To date, there are no reports to validate the Indian traditional and folklore claims of Artemisia maderaspatana L. (syn. Grangea maderaspatana L.) (Asteraceae) for the treatment of Alzheimer's disease. The present study characterizes the volatile components (non-polar compounds) of A. maderaspatana and evaluates its acetylcholinesterase inhibition potential. The essential oils (yield 0.06% v/w) were obtained from fresh aerial part of A. maderaspatana. The characterization of volatile components (non-polar compounds) was performed by GC-MS data and with those of reference compounds compiled in the spectral library of in-house database. The in vitro acetylcholinesterase (AChE) inhibition of the volatile organic constituents (VOC's) of A. maderaspatana aerial part was evaluated in varying concentration ranges (0.70-44.75 µg/mL) with Ellman's method. The major components were α-humulene (46.3%), β-caryophyllene (9.3%), α-copaene (8.2%), β-myrcene (4.3%), Z(E)-α-farnesene (3.7%), and calarene (3.5%). Chemical variability among other Artemisia spp. from different climatic regions of India and countries namely Iran and France was observed. The experimental results showed that diverse volatile organic constituents of A. maderaspatana have significant acetylcholinesterase inhibitory activity (an IC50 value of 31.33 ± 1.03 µg/mL). This is the first report on the inhibition of acetylcholinesterase properties of essential oil of A. maderaspatana obtained from fresh aerial part. The present results indicate that essential oil of A. maderaspatana isolated from the northern region of India could inhibit AChE moderately. Therefore, the possibility of novel AChE inhibitors might exist in VOCs of this plant.

  19. Acute administration of fenproporex increased acetylcholinesterase activity in brain of young rats

    OpenAIRE

    TEODORAK, BRENA P.; FERREIRA, GABRIELA K.; SCAINI, GISELLI; WESSLER, LETÍCIA B.; HEYLMANN, ALEXANDRA S.; DEROZA, PEDRO; VALVASSORI, SAMIRA S.; ZUGNO, ALEXANDRA I.; QUEVEDO, JOÃO; STRECK, EMILIO L.

    2015-01-01

    Fenproporex is the second most commonly amphetamine-based anorectic consumed worldwide; this drug is rapidly converted into amphetamine, in vivo, and acts by increasing dopamine levels in the synaptic cleft. Considering that fenproporex effects on the central nervous system are still poorly known and that acetylcholinesterase is a regulatory enzyme which is involved in cholinergic synapses and may indirectly modulate the release of dopamine, the present study investigated the effects of acute...

  20. Methyl jasmonate enhances memory performance through inhibition of oxidative stress and acetylcholinesterase activity in mice.

    Science.gov (United States)

    Eduviere, Anthony T; Umukoro, S; Aderibigbe, Adegbuyi O; Ajayi, Abayomi M; Adewole, Folashade A

    2015-07-01

    Current research effort focuses on the development of safer natural compounds with multipronged mechanisms of action that could be used to ameliorate memory deficits in patients with Alzheimer's disease, as cure for the disease still remains elusive. In this study, we evaluated the effect of methyl jasmonate (MJ), a naturally occurring bioactive compound on memory, acetylcholinesterase activity and biomarkers of oxidative stress in mice. Male Swiss mice were treated with intraperitoneal injection of MJ (10-40 mg/kg) alone or in combination with scopolamine (3mg/kg) once daily for 7 days. Thirty minutes after the last treatment, memory functions were assessed using Y-maze and object recognition tests. Thereafter, acetylcholinesterase activity and levels of biomarkers of oxidative stress were assessed in mice brains using standard biochemical procedures. MJ significantly enhanced memory performance and reversed scopolamine-induced cognitive impairment in mice. MJ demonstrated significant inhibition of acetylcholinesterase activity suggesting increased cholinergic neurotransmission. It further decreased malondialdehyde concentrations in mouse brain indicating antioxidant activity. Moreover, MJ significantly increased glutathione levels and activity of antioxidant enzymes (catalase and superoxide dismutase) in mice brains. The increased oxidative stress; evidenced by elevated levels of malondialdehyde and decreased antioxidant defense systems in scopolamine-treated mice was attenuated by MJ. The results of this study suggest that MJ may be useful in conditions associated with memory dysfunctions or age-related cognitive decline. The positive effect of MJ on memory may be related to inhibition of oxidative stress and enhancement of cholinergic neurotransmission through inhibition of acetylcholinesterase activity. Copyright © 2015 Elsevier Inc. All rights reserved.

  1. Phytochemical Characterization, Antibacterial, Acetylcholinesterase Inhibitory and Cytotoxic Properties of Cryptostephanus vansonii, an Endemic Amaryllid

    Czech Academy of Sciences Publication Activity Database

    Moyo, M.; Aremu, A.O.; Chukwujekwu, J. C.; Grúz, Jiří; Skořepa, Jiří; Doležal, Karel; Katsvanga, C. A. T.; Van Staden, J.

    2017-01-01

    Roč. 31, č. 5 (2017), s. 713-720 ISSN 0951-418X R&D Projects: GA MŠk(CZ) LO1204; GA MŠk LK21306 Institutional support: RVO:61389030 Keywords : in-vitro * alzheimers-disease * alkaloids * extracts * antioxidant * coumarins * apoptosis * phylogeny * medicine * bacteria * acetylcholinesterase inhibition * Amaryllidaceae * antibacterial * cytotoxicity * flavonoids * phenolic acids Subject RIV: EB - Genetics ; Molecular Biology OBOR OECD: Plant sciences, botany Impact factor: 3.092, year: 2016

  2. O2-insensitive photosynthesis in C3 plants: its occurrence and a possible explanation

    International Nuclear Information System (INIS)

    Sharkey, T.D.

    1985-01-01

    Leaves of C 3 plants which exhibit a normal O 2 inhibition of CO 2 fixation at less than saturating light intensity were found to exhibit O 2 -insensitive photosynthesis at high light. This behavior was observed in Phaseolus vulgaris L., Xanthium strumarium L., and Scrophularia desertorum (Shaw.) Munz. O 2 -insensitive photosynthesis has been reported in nine other C 3 species and usually occurred when the intercellular CO 2 pressure was about double the normal pressure. A lack of O 2 inhibition of photosynthesis was always accompanied by a failure of increased CO 2 pressure to stimulate photosynthesis to the expected degree. O 2 -insensitive photosynthesis also occurred after plants had been water stressed. Under such conditions, however, photosynthesis became O 2 and CO 2 insensitive at physiological CO 2 pressures. Postillumination CO 2 exchange kinetics showed that O 2 and CO 2 insensitivity was not the result of elimination of photorespiration. It is proposed that O 2 and CO 2 insensitivity occurs when the concentration of phosphate in the chloroplast stroma cannot be both high enough to allow photophosphorylation and low enough to allow starch and sucrose synthesis at the rates required by the rest of the photosynthetic component processes. Under these conditions, the energy diverted to photorespiration does not adversely affect the potential for CO 2 assimilation

  3. Botanical insecticides inspired by plant-herbivore chemical interactions.

    Science.gov (United States)

    Miresmailli, Saber; Isman, Murray B

    2014-01-01

    Plants have evolved a plethora of secondary chemicals to protect themselves against herbivores and pathogens, some of which have been used historically for pest management. The extraction methods used by industry render many phytochemicals ineffective as insecticides despite their bioactivity in the natural context. In this review, we examine how plants use their secondary chemicals in nature and compare this with how they are used as insecticides to understand why the efficacy of botanical insecticides can be so variable. If the commercial production of botanical insecticides is to become a viable pest management option, factors such as production cost, resource availability, and extraction and formulation techniques need be considered alongside innovative application technologies to ensure consistent efficacy of botanical insecticides. Copyright © 2013 Elsevier Ltd. All rights reserved.

  4. Ecotoxicological study of insecticide effects on arthropods in common bean.

    Science.gov (United States)

    de Barros, Emerson Cristi; Ventura, Hudson Vaner; Gontijo, Pablo Costa; Pereira, Renata Ramos; Picanço, Marcelo Coutinho

    2015-01-01

    Arthropods are an important group of macroorganisms that work to maintain ecosystem health. Despite the agricultural benefits of chemical control against arthropod pests, insecticides can cause environmental damage. We examined the effects of one and two applications of the insecticides chlorfenapyr (0.18 liters a.i. ha-1) and methamidophos (0.45 liters a.i. ha-1), both independently and in combination, on arthropods in plots of common bean. The experiment was repeated for two growing seasons. Principal response curve, richness estimator, and Shannon-Wiener diversity index analyses were performed. The insecticides generally affected the frequency, richness, diversity, and relative abundance of the arthropods. In addition, the arthropods did not experience recovery after the insecticide applications. The results suggest that the insecticide impacts were sufficiently drastic to eliminate many taxa from the studied common bean plots. © The Author 2015. Published by Oxford University Press on behalf of the Entomological Society of America.

  5. An Operational Framework for Insecticide Resistance Management Planning.

    Science.gov (United States)

    Chanda, Emmanuel; Thomsen, Edward K; Musapa, Mulenga; Kamuliwo, Mulakwa; Brogdon, William G; Norris, Douglas E; Masaninga, Freddie; Wirtz, Robert; Sikaala, Chadwick H; Muleba, Mbanga; Craig, Allen; Govere, John M; Ranson, Hilary; Hemingway, Janet; Seyoum, Aklilu; Macdonald, Michael B; Coleman, Michael

    2016-05-01

    Arthropod vectors transmit organisms that cause many emerging and reemerging diseases, and their control is reliant mainly on the use of chemical insecticides. Only a few classes of insecticides are available for public health use, and the increased spread of insecticide resistance is a major threat to sustainable disease control. The primary strategy for mitigating the detrimental effects of insecticide resistance is the development of an insecticide resistance management plan. However, few examples exist to show how to implement such plans programmatically. We describe the formulation and implementation of a resistance management plan for mosquito vectors of human disease in Zambia. We also discuss challenges, steps taken to address the challenges, and directions for the future.

  6. Antioxidant activity, acetylcholinesterase and tyrosinase inhibitory potential of Pulmonaria officinalis and Centarium umbellatum extracts

    Directory of Open Access Journals (Sweden)

    Elena Neagu

    2018-03-01

    Full Text Available In this study several investigations and tests were performed to determine the antioxidant activity and the acetylcholinesterase and tyrosinase inhibitory potential of Pulmonaria officinalis and Centarium umbellatum aqueous extracts (10% mass and ethanolic extracts (10% mass and 70% ethanol, respectively. Moreover, for each type of the prepared extracts of P. officinalis and of C. umbellatum the content in the biologically active compounds – polyphenols, flavones and proanthocyanidins was determined. The antioxidant activity was assessed using two methods, namely the 2,2-diphenyl-1-picrylhydrazyl (DPPH assay and reducing power assay. The analyzed plant extracts showed a high acetylcholinesterase and tyrosinase inhibitory activity in the range of 72.24–94.24% (at the highest used dose – 3 mg/mL, 66.96% and 94.03% (at 3 mg/mL, respectively correlated with a high DPPH radical inhibition – 70.29–84.9% (at 3 mg/mL. These medicinal plants could provide a potential natural source of bioactive compounds and could be beneficial to the human health, especially in the neurodegenerative disorders and as sources of natural antioxidants in food industry. Keywords: Acetylcholinesterase inhibitory activity, Tyrosinase inhibitory activity, Antioxidant activity, Pulmonaria officinalis and Centarium umbellatum

  7. Acetylcholinesterase inhibitors rapidly activate Trk neurotrophin receptors in the mouse hippocampus

    Science.gov (United States)

    Autio, Henri; Mätlik, Kert; Rantamäki, Tomi; Lindemann, Lothar; Hoener, Marius C; Chao, Moses; Arumäe, Urmas; Castrén, Eero

    2014-01-01

    Acetylcholinesterase inhibitors are first-line therapies for Alzheimer's disease. These drugs increase cholinergic tone in the target areas of the cholinergic neurons of the basal forebrain. Basal forebrain cholinergic neurons are dependent upon trophic support by nerve growth factor (NGF) through its neurotrophin receptor, TrkA. In the present study, we investigated whether the acetylcholinesterase inhibitors donepezil and galantamine could influence neurotrophin receptor signaling in the brain. Acute administration of donepezil (3 mg/kg, i.p.) led to the rapid autophosphorylation of TrkA and TrkB neurotrophin receptors in the adult mouse hippocampus. Similarly, galantamine dose-dependently (3, 9 mg/kg, i.p.) increased TrkA and TrkB phosphorylation in the mouse hippocampus. Both treatments also increased the phosphorylation of transcription factor CREB and tended to increase the phosphorylation of AKT kinase but did not alter the activity of MAPK42/44. Chronic treatment with galantamine (3 mg/kg, i.p., 14 days), did not induce changes in hippocampal NGF and BDNF synthesis or protein levels. Our findings show that acetylcholinesterase inhibitors are capable of rapidly activating hippocampal neurotrophin signaling and thus suggest that therapies targeting Trk signaling may already be in clinical use in the treatment of AD. PMID:21820453

  8. Upregulation of α7 Nicotinic Receptors by Acetylcholinesterase C-Terminal Peptides

    Science.gov (United States)

    Bond, Cherie E.; Zimmermann, Martina; Greenfield, Susan A.

    2009-01-01

    Background The alpha-7 nicotinic acetylcholine receptor (α7-nAChR) is well known as a potent calcium ionophore that, in the brain, has been implicated in excitotoxicity and hence in the underlying mechanisms of neurodegenerative disorders such as Alzheimer's disease. Previous research implied that the activity of this receptor may be modified by exposure to a peptide fragment derived from the C-terminal region of the enzyme acetylcholinesterase. This investigation was undertaken to determine if the functional changes observed could be attributed to peptide binding interaction with the α7-nAChR, or peptide modulation of receptor expression. Methodology/Principal Findings This study provides evidence that two peptides derived from the C-terminus of acetylcholinesterase, not only selectively displace specific bungarotoxin binding at the α7-nAChR, but also alter receptor binding properties for its familiar ligands, including the alternative endogenous agonist choline. Of more long-term significance, these peptides also induce upregulation of α7-nAChR mRNA and protein expression, as well as enhancing receptor trafficking to the plasma membrane. Conclusions/Significance The results reported here demonstrate a hitherto unknown relationship between the α7-nAChR and the non-enzymatic functions of acetylcholinesterase, mediated independently by its C-terminal domain. Such an interaction may prove valuable as a pharmacological tool, prompting new approaches for understanding, and combating, the process of neurodegeneration. PMID:19287501

  9. Optimization of sol-gel medium for entrapment of acetylcholinesterase enzyme in biosensor for pesticide detection

    Science.gov (United States)

    Wijayanti, S. D.; Rahayu, F. S.; Widyaningsih, T. D.

    2018-03-01

    Pesticides are chemical substances used to kill and control pests or diseases that can damage crops. The use of pesticides should be done precisely because the accumulation of chemicals contained in pesticides can cause various health effects. Therefore, detection of pesticide residues on plants is important to reduce the risk of poisoning due to pesticide residues. Some of the conventional methods that have been done to detect pesticide residues have weaknesses among expensive tools, takes a long time, and are generally performed by trained laboratory technicians. Biosensors are analytical devices that can measure the quantitative or semi-quantitative targets of analyte by utilizing a bioreceptor such as enzyme. Several studies have shown that enzyme-based acetylcholinesterase-based biosensors can be used to detect pesticide residues in vegetable samples. The objective of this research was to get a proper silica based sol-gel formulation with molar ratio of H2O:TEOS and NaOH concentration as immobilization medium of acetylcholinesterase enzyme for biosensor application. Response Surface Methodology (RSM) was used in order to determine the interaction between the parameters studied and resulting responses which were amount and activity of acetylcholinesterase enzyme. Based on the research, the best result for immobilized enzyme activity was shown by molar ratio (H2O: TEOS) 1: 8 and 4 mM NaOH treatment.

  10. Computational study of substrate isotope effect probes of transition state structure for acetylcholinesterase catalysis

    International Nuclear Information System (INIS)

    Sikorski, R.S.; Malany, S.; Seravalli, J.; Quinn, D.M.

    2002-01-01

    Secondary isotope effects for carbonyl addition reactions of methyl thioacetate, acetone and acetaldehyde have been calculated by ab initio quantum mechanical methods in an effect to interpret measured β-deuterium isotope effects on acetylcholinesterase-catalysed hydrolysis of acetylthiocholine. The calculated β-deuterium isotope effect for equilibrium addition of methanol to methyl thioacetate is D3 K eq = 0.965, and the corresponding effect for addition of methoxide ion to methyl thioacetate wherein three waters are hydrogen bonded to the carbonyl oxyanion is D3 K eq = 1.086. Neither of these calculated isotope effects is an inverse as the experimental β-deuterium isotope effect for acetylcholinesterase-catalysed hydrolysis of acetylthiocholine, D3 K eq = 0.90±0.03. Structural comparisons show that the water-solvated methoxide adduct of methyl thioacetate is more expanded than is the natural methanol addition adduct, and suggest that the degree of which the isotope effect is inverse (i.e. less than) is inversely correlated to the degree of expansion of the adduct. A similar correlation of α-deuterium and β-deuterium secondary isotope effects with the degree of expansion of the adducts is found for equilibrium additions of methanol and methoxide ion to acetylaldehyde. These computational results suggest that the markedly inverse β-deuterium isotope effect for the acetylcholinesterase reaction arises from enzymatic compression of the transition state. (author)

  11. Influence of acetylcholinesterase immobilization on the photoluminescence properties of mesoporous silicon surface

    Energy Technology Data Exchange (ETDEWEB)

    Saleem, Muhammad [Department of Chemistry, Kongju National University, Gongju, Chungnam 314-701 (Korea, Republic of); Rafiq, Muhammad; Seo, Sung-Yum [Department of Biology, Kongju National University, Gongju, Chungnam 314-701 (Korea, Republic of); Lee, Ki Hwan, E-mail: khlee@kongju.ac.kr [Department of Chemistry, Kongju National University, Gongju, Chungnam 314-701 (Korea, Republic of)

    2014-07-01

    Acetylcholinesterase immobilized p-type porous silicon surface was prepared by covalent attachment. The immobilization procedure was based on support surface chemical oxidation, silanization, surface activation with cyanuric chloride and finally covalent attachment of free enzyme on the cyanuric chloride activated porous silicon surface. Different pore diameter of porous silicon samples were prepared by electrochemical etching in HF based electrolyte solution and appropriate sample was selected suitable for enzyme immobilization with maximum trapping ability. The surface modification was studied through field emission scanning electron microscope, EDS, FT-IR analysis, and photoluminescence measurement by utilizing the fluctuation in the photoluminescence of virgin and enzyme immobilized porous silicon surface. Porous silicon showed strong photoluminescence with maximum emission at 643 nm and immobilization of acetylcholinesterase on porous silicon surface cause considerable increment on the photoluminescence of porous silicon material while acetylcholinesterase free counterpart did not exhibit any fluorescence in the range of 635–670 nm. The activities of the free and immobilized enzymes were evaluated by spectrophotometric method by using neostigmine methylsulfate as standard enzyme inhibitor. The immobilized enzyme exhibited considerable response toward neostigmine methylsulfate in a dose dependent manner comparable with that of its free counterpart alongside enhanced stability, easy separation from the reaction media and significant saving of enzyme. It was believed that immobilized enzyme can be exploited in organic and biomolecule synthesis possessing technical and economical prestige over free enzyme and prominence of easy separation from the reaction mixture.

  12. Maytenus distichophylla and Salacia crassifolia: source of products with potential acetylcholinesterase inhibition

    Directory of Open Access Journals (Sweden)

    Fernanda L. Ferreira

    Full Text Available ABSTRACT The phytochemical study of the extract leaves from Maytenus distichophylla Mart. and Salacia crassifolia (Mart. ex Schult. G. Don, Celastraceae, resulted in the isolation of 3-oxofriedelane, 3β-hydroxyfriedelane, 3β,24-dihydroxyfriedelane, 3-oxo-28,29-dihydroxyfriedelane, two mixtures of pentacyclic triterpenes (α-amyrin with β-amyrin and 3β-stearyloxy-urs-12-ene with 3β-stearyloxy-olean-12-ene, 3β-palmityloxy-urs-12-ene, the steroid β-sitosterol and its glycosylated derivative β-glucosyl-β-sitosterol, tritriacontanoic acid and the natural polymer gutta percha. The chemical structures of these constituents were established by IR, 1H and 13C NMR spectral data. Crude extracts, the mixtures of triterpenes and the isolated constituents were subjected to in vitro acetylcholinesterase inhibitory evaluation. Acetylcholinesterase inhibitory effect was observed for crude chloroform extract leaves from M. distichophylla (100% and S. crassifolia (97.93 ± 5.63% and for the triterpenes 3β,24-dihydroxyfriedelane (99.05 ± 1.12%, 3-oxo-28,29-dihydroxyfriedelane (90.59 ± 3.76% and 3β-palmityloxy-urs-12-ene (97.93 ± 1.47%. The percent inhibitions induced by these natural products were very similar to those produced by physostigmine (93.94 ± 2.10% a standard acetylcholinesterase inhibitor. Therefore, these results open perspectives for the use of these species as source of compounds with similar physostigmine pharmacological effect.

  13. Hairy-root organ cultures for the production of human acetylcholinesterase

    Directory of Open Access Journals (Sweden)

    Mor Tsafrir S

    2008-12-01

    Full Text Available Abstract Background Human cholinesterases can be used as a bioscavenger of organophosphate toxins used as pesticides and chemical warfare nerve agents. The practicality of this approach depends on the availability of the human enzymes, but because of inherent supply and regulatory constraints, a suitable production system is yet to be identified. Results As a promising alternative, we report the creation of "hairy root" organ cultures derived via Agrobacterium rhizogenes-mediated transformation from human acetylcholinesterase-expressing transgenic Nicotiana benthamiana plants. Acetylcholinesterase-expressing hairy root cultures had a slower growth rate, reached to the stationary phase faster and grew to lower maximal densities as compared to wild type control cultures. Acetylcholinesterase accumulated to levels of up to 3.3% of total soluble protein, ~3 fold higher than the expression level observed in the parental plant. The enzyme was purified to electrophoretic homogeneity. Enzymatic properties were nearly identical to those of the transgenic plant-derived enzyme as well as to those of mammalian cell culture derived enzyme. Pharmacokinetic properties of the hairy-root culture derived enzyme demonstrated a biphasic clearing profile. We demonstrate that master banking of plant material is possible by storage at 4°C for up to 5 months. Conclusion Our results support the feasibility of using plant organ cultures as a successful alternative to traditional transgenic plant and mammalian cell culture technologies.

  14. Influence of acetylcholinesterase immobilization on the photoluminescence properties of mesoporous silicon surface

    International Nuclear Information System (INIS)

    Saleem, Muhammad; Rafiq, Muhammad; Seo, Sung-Yum; Lee, Ki Hwan

    2014-01-01

    Acetylcholinesterase immobilized p-type porous silicon surface was prepared by covalent attachment. The immobilization procedure was based on support surface chemical oxidation, silanization, surface activation with cyanuric chloride and finally covalent attachment of free enzyme on the cyanuric chloride activated porous silicon surface. Different pore diameter of porous silicon samples were prepared by electrochemical etching in HF based electrolyte solution and appropriate sample was selected suitable for enzyme immobilization with maximum trapping ability. The surface modification was studied through field emission scanning electron microscope, EDS, FT-IR analysis, and photoluminescence measurement by utilizing the fluctuation in the photoluminescence of virgin and enzyme immobilized porous silicon surface. Porous silicon showed strong photoluminescence with maximum emission at 643 nm and immobilization of acetylcholinesterase on porous silicon surface cause considerable increment on the photoluminescence of porous silicon material while acetylcholinesterase free counterpart did not exhibit any fluorescence in the range of 635–670 nm. The activities of the free and immobilized enzymes were evaluated by spectrophotometric method by using neostigmine methylsulfate as standard enzyme inhibitor. The immobilized enzyme exhibited considerable response toward neostigmine methylsulfate in a dose dependent manner comparable with that of its free counterpart alongside enhanced stability, easy separation from the reaction media and significant saving of enzyme. It was believed that immobilized enzyme can be exploited in organic and biomolecule synthesis possessing technical and economical prestige over free enzyme and prominence of easy separation from the reaction mixture.

  15. Foetal and adult human CYP3A isoforms in the bioactivation of organophosphorothionate insecticides.

    Science.gov (United States)

    Buratti, Franca M; Leoni, Claudia; Testai, Emanuela

    2006-12-15

    In humans organophosphorothionate pesticides (OPT) prenatal exposure has been demonstrated. Since OPT-induced neurodevelopmental effects may be due to in situ bioactivation by foetal enzymes, the catalytic activity of the foetal CYP3A7 toward chlorpyrifos (CPF), parathion (PAR), malathion (MAL) and fenthion (FEN) has been assessed by using recombinant enzymes. A comparison with the adult isoforms CYP3A4 and CYP3A5 has been also carried out. CYP3A7 was able to produce significant levels of oxon or sulfoxide from the four OPTs in the range of tested concentrations (0.05-200 microM). When the efficiencies of CYP3A isoforms were compared, the ranking, expressed as CLi values, were: CPF=3A4>3A5>3A7; PAR=3A4>3A7>3A5; MAL=3A4>3A7>3A5; FEN (sulfoxide formation)=3A4>3A5>3A7. The CYP3A5 efficiency appeared to be more dependent on the single insecticide than its related isozyme CYP3A4. Our results indicate that the levels of toxic metabolite formed in situ by CYP3A7 from CPF, MAL and PAR but not from FEN have the chance to inhibit acetylcholinesterase, following prenatal exposure to OPTs. However, due to the smaller weight of foetal liver, the contribution to total OPT biotransformation is relatively low. On the other hand, our results clearly indicate that at low CPF concentrations, the formation of the non-toxic metabolites is highly favoured in the foetus.

  16. Nanoparticle-Based Electrochemical Immunosensor for the Detection of Phosphorylated Acetylcholinesterase: An Exposure Biomarker of Organophosphate Pesticides and Nerve AgentsOrganophosphate Pesticides and Nerve Agents

    Energy Technology Data Exchange (ETDEWEB)

    Liu, Guodong; Wang, Jun; Barry, Richard C.; Petersen, Catherine E.; Timchalk, Charles; Gassman, Paul L.; Lin, Yuehe

    2008-11-01

    A nanoparticle-based electrochemical immunosensor has been developed for the detection of phosphorylated acetylcholinesterase (AChE) adducts, which is a potential exposure biomarker for organophosphate pesticides (OP) and chemical warfare nerve agent exposures. Zirconia nanoparticles (ZrO2 NPs) were used as selective sorbents to capture the phosphorylated AChE adduct, and quantum dots (ZnS@CdS, QDs) were used as tags to label monoclonal anti-AChE antibody to track the immunorecognition events. The sandwich-like immunoreactions were performed among the ZrO2 NPs, which were pre-coated on a screen printed electrode (SPE) by electrodeposition, phosphorylated AChE and QD-anti-AChE. The captured QD tags were determined on the SPE by electrochemical stripping analysis of its metallic component (cadmium) after an acid-dissolution step. Paraoxon was used as a model OP insecticide to prepare the phosphorylated AChE adduct to demonstrate the proof of principle for this sensor technology. The paraoxon-AChE adduct was characterized by Fourier Transform Infrared Spectrum, and the binding affinity of anti-AChE to the paraoxon-AChE was validated with an enzyme-linked immunosorbent assay. The parameters (e.g., amount of ZrO2 NP, QD-anti-AChE concentration,) that govern the electrochemical response of immunosensors were optimized. The voltammetric response of the immunosensor is highly linear over the range of 10 pM to 4 nM paraoxon-AChE, and the limit of detection is estimated to be 8 pM. This new nanoparticle-based electrochemical immunosensor thus provides a sensitive and quantitative tool for biomonitoring exposure to OP pesticides and nerve agents.

  17. Insecticide resistance status of three malaria vectors, Anopheles gambiae (s.l.), An. funestus and An. mascarensis, from the south, central and east coasts of Madagascar.

    Science.gov (United States)

    Rakotoson, Jean-Desire; Fornadel, Christen M; Belemvire, Allison; Norris, Laura C; George, Kristen; Caranci, Angela; Lucas, Bradford; Dengela, Dereje

    2017-08-23

    Insecticide-based vector control, which comprises use of insecticide-treated bed nets (ITNs) and indoor residual spraying (IRS), is the key method to malaria control in Madagascar. However, its effectiveness is threatened as vectors become resistant to insecticides. This study investigated the resistance status of malaria vectors in Madagascar to various insecticides recommended for use in ITNs and/or IRS. WHO tube and CDC bottle bioassays were performed on populations of Anopheles gambiae (s.l.), An. funestus and An. mascarensis. Adult female An. gambiae (s.l.) mosquitoes reared from field-collected larvae and pupae were tested for their resistance to DDT, permethrin, deltamethrin, alpha-cypermethrin, lambda-cyhalothrin, bendiocarb and pirimiphos-methyl. Resting An. funestus and An. mascarensis female mosquitoes collected from unsprayed surfaces were tested against permethrin, deltamethrin and pirimiphos-methyl. The effect on insecticide resistance of pre-exposure to the synergists piperonyl-butoxide (PBO) and S,S,S-tributyl phosphorotrithioate (DEF) also was assessed. Molecular analyses were done to identify species and determine the presence of knock-down resistance (kdr) and acetylcholinesterase resistance (ace-1 R ) gene mutations. Anopheles funestus and An. mascarensis were fully susceptible to permethrin, deltamethrin and pirimiphos-methyl. Anopheles gambiae (s.l.) was fully susceptible to bendiocarb and pirimiphos-methyl. Among the 17 An. gambiae (s.l.) populations tested for deltamethrin, no confirmed resistance was recorded, but suspected resistance was observed in two sites. Anopheles gambiae (s.l.) was resistant to permethrin in four out of 18 sites (mortality 68-89%) and to alpha-cypermethrin (89% mortality) and lambda-cyhalothrin (80% and 85%) in one of 17 sites, using one or both assay methods. Pre-exposure to PBO restored full susceptibility to all pyrethroids tested except in one site where only partial restoration to permethrin was observed. DEF

  18. Rice Production without Insecticide in Smallholder Farmer's Field

    Directory of Open Access Journals (Sweden)

    M. P. Ali

    2017-05-01

    Full Text Available Highlights:Use of perching, sweeping, and need based insecticide (IPM technique useage produce at par yields compared to prophylactic insecticide useage in rice fields.There exists a technique that can reduce 75% of insecticide useage in rice field.The results were obtained in cooperation between smallholder rice farmers and researchers of Bangladesh.Currently rice protection from insect pests solely depends on chemical pesticides which have tremendous impact on biodiversity, environment, animal, and human health. To reduce their impact from our society we need to cut pesticide use from agricultural practices. To address this issue, we did an experiment to identify realistic solutions that could help farmers build sustainable crop protection systems and minimize useage of insecticides and thus reduce the impact of pesticides in the environment. Innovations developed jointly by farmers and researchers and evaluated for their potential to be adopted by more farmers. In this paper we tested four management practices jointly with smallholder farmer fields in order to select the best one. Four management practices were used namely, T1 = Prophylactic use of insecticide where insecticide was applied in rice field at every 15 days interval without judging the infestation level; T2 = Perching (that is, placing roosting (perching sites for insectivorous birds within the rice field and concurrent sweep net samples along with need-based insecticide application; T3 = Perching only; and T4 = Farmer's own practices. The results revealed that routine application of insecticides for crop protection is not mandatory which is commonly found at use in rice farmers. In our experiment, where prophylactic method or farmers used 3–4 times insecticides without judging the insect pests infestation level, the similar pest population was found when compared to the field where insecticide was not applied. Our management system reduced by 75% the use of insecticides even

  19. Differential physiological effects of neonicotinoid insecticides on honey bees: A comparison between Apis mellifera and Apis cerana.

    Science.gov (United States)

    Li, Zhiguo; Li, Meng; He, Jingfang; Zhao, Xiaomeng; Chaimanee, Veeranan; Huang, Wei-Fone; Nie, Hongyi; Zhao, Yazhou; Su, Songkun

    2017-08-01

    Acute toxicities (LD50s) of imidacloprid and clothianidin to Apis mellifera and A. cerana were investigated. Changing patterns of immune-related gene expressions and the activities of four enzymes between the two bee species were compared and analyzed after exposure to sublethal doses of insecticides. Results indicated that A. cerana was more sensitive to imidacloprid and clothianidin than A. mellifera. The acute oral LD50 values of imidacloprid and clothianidin for A. mellifera were 8.6 and 2.0ng/bee, respectively, whereas the corresponding values for A. cerana were 2.7 and 0.5ng/bee. The two bee species possessed distinct abilities to mount innate immune response against neonicotinoids. After 48h of imidacloprid treatment, carboxylesterase (CCE), prophenol oxidase (PPO), and acetylcholinesterase (AChE) activities were significantly downregulated in A. mellifera but were upregulated in A. cerana. Glutathione-S-transferase (GST) activity was significantly elevated in A. mellifera at 48h after exposure to imidacloprid, but no significant change was observed in A. cerana. AChE was downregulated in both bee species at three different time points during clothianidin exposure, and GST activities were upregulated in both species exposed to clothianidin. Different patterns of immune-related gene expression and enzymatic activities implied distinct detoxification and immune responses of A. cerana and A. mellifera to imidacloprid and clothianidin. Copyright © 2017 Elsevier Inc. All rights reserved.

  20. Insecticide-induced hormesis and arthropod pest management.

    Science.gov (United States)

    Guedes, Raul Narciso C; Cutler, G Christopher

    2014-05-01

    Ecological backlashes such as insecticide resistance, resurgence and secondary pest outbreaks are frequent problems associated with insecticide use against arthropod pest species. The last two have been particularly important in sparking interest in the phenomenon of insecticide-induced hormesis within entomology and acarology. Hormesis describes a biphasic dose-response relationship that is characterized by a reversal of response between low and high doses of a stressor (e.g. insecticides). Although the concept of insecticide-induced hormesis often does not receive sufficient attention, or has been subject to semantic confusion, it has been reported in many arthropod pest species and natural enemies, and has been linked to pest outbreaks and potential problems with insecticide resistance. The study of hormesis remains largely neglected in entomology and acarology. Here, we examined the concept of insecticide-induced hormesis in arthropods, its functional basis and potential fitness consequences, and its importance in arthropod pest management and other areas. © 2013 Society of Chemical Industry.

  1. Induced tolerance from a sublethal insecticide leads to cross-tolerance to other insecticides.

    Science.gov (United States)

    Hua, Jessica; Jones, Devin K; Relyea, Rick A

    2014-04-01

    As global pesticide use increases, the ability to rapidly respond to pesticides by increasing tolerance has important implications for the persistence of nontarget organisms. A recent study of larval amphibians discovered that increased tolerance can be induced by an early exposure to low concentrations of a pesticide. Since natural systems are often exposed to a variety of pesticides that vary in mode of action, we need to know whether the induction of increased tolerance to one pesticide confers increased tolerance to other pesticides. Using larval wood frogs (Lithobates sylvaticus), we investigated whether induction of increased tolerance to the insecticide carbaryl (AChE-inhibitor) can induce increased tolerance to other insecticides that have the same mode of action (chlorpyrifos, malathion) or a different mode of action (Na(+)channel-interfering insecticides; permethrin, cypermethrin). We found that embryonic exposure to sublethal concentrations of carbaryl induced higher tolerance to carbaryl and increased cross-tolerance to malathion and cypermethrin but not to chlorpyrifos or permethrin. In one case, the embryonic exposure to carbaryl induced tolerance in a nonlinear pattern (hormesis). These results demonstrate that that the newly discovered phenomenon of induced tolerance also provides induced cross-tolerance that is not restricted to pesticides with the same mode of action.

  2. Quantitative structure-activity relationship (QSAR) for insecticides: development of predictive in vivo insecticide activity models.

    Science.gov (United States)

    Naik, P K; Singh, T; Singh, H

    2009-07-01

    Quantitative structure-activity relationship (QSAR) analyses were performed independently on data sets belonging to two groups of insecticides, namely the organophosphates and carbamates. Several types of descriptors including topological, spatial, thermodynamic, information content, lead likeness and E-state indices were used to derive quantitative relationships between insecticide activities and structural properties of chemicals. A systematic search approach based on missing value, zero value, simple correlation and multi-collinearity tests as well as the use of a genetic algorithm allowed the optimal selection of the descriptors used to generate the models. The QSAR models developed for both organophosphate and carbamate groups revealed good predictability with r(2) values of 0.949 and 0.838 as well as [image omitted] values of 0.890 and 0.765, respectively. In addition, a linear correlation was observed between the predicted and experimental LD(50) values for the test set data with r(2) of 0.871 and 0.788 for both the organophosphate and carbamate groups, indicating that the prediction accuracy of the QSAR models was acceptable. The models were also tested successfully from external validation criteria. QSAR models developed in this study should help further design of novel potent insecticides.

  3. Insecticidal defenses of Piperaceae from the neotropics.

    Science.gov (United States)

    Bernard, C B; Krishanmurty, H G; Chauret, D; Durst, T; Philogène, B J; Sánchez-Vindas, P; Hasbun, C; Poveda, L; San Román, L; Arnason, J T

    1995-06-01

    Insecticidal and growth-reducing properties of extracts of 14 species of American neotropical Piperaceae were investigated by inclusion in diets of a polyphagous lepidopteran, the European corn borer,Ostrinia nubilalis. Nutritional indices suggested most extracts acted by postdigestive toxicity.Piper aduncum, P. tuberculatum, andP. decurrens were among the most active species and were subjected to bioassay-guided isolation of the active components. Dillapiol was isolated from the active fraction ofP. aduncum, piperlonguminine was isolated fromP. tuberculatum, and a novel neolignan fromP. decurrens. The results support other studies on Asian and AfricanPiper species, which suggest that lignans and isobutyl amides are the active defence compounds in this family.

  4. Insecticidal Constituents from Buddlej aalbiflora Hemsl.

    Science.gov (United States)

    Zhang, Xiu-Yun; Shen, Jing; Zhou, Yu; Wei, Zhi-Ping; Gao, Jin-Ming

    2017-06-01

    Eleven known compounds, deoxymikanolide (1), 1,3-dihydroxyxanthone (2), kumatakenin (3), apigenin (4), chrysin (5), kaempferol (6), Iso-kaempferol (7), luteolin (8), luteolin-3',4'-dimethylether-7-O-β-glucoside (9), luteolin-7-O-β-glucoside (10) and quercetin (11) were identified in MeOH extract of Buddleja albiflora Hemsl (Oleaceae). These compounds (each, 1, 0.5 and 0.25 mg mL -1 ) were tested for insecticidal activity against 3rd and 4th-instar larvae of Plutella xylostella, 3rd-instar larvae of Mythimna separata and 3rd-instar larvae of Macrosiphoniella sanborni. The lowest 50% anti-feedant concentration (AFC 50 ) against P. xylostella and 50% lethal concentration (LC 50 ) against P. xylostella and M. sanborni were observed as 0.0058, 0.0046 and 3.4048 mg L -1 , respectively.

  5. Insecticidal Activity of Cyanohydrin and Monoterpenoid Compounds

    Directory of Open Access Journals (Sweden)

    Joel R. Coats

    2000-04-01

    Full Text Available The insecticidal activities of several cyanohydrins, cyanohydrin esters and monoterpenoid esters (including three monoterpenoid esters of a cyanohydrin were evaluated. Topical toxicity to Musca domestica L. adults was examined, and testing of many compounds at 100 mg/fly resulted in 100% mortality. Topical LD50 values of four compounds for M. domestica were calculated. Testing of many of the reported compounds to brine shrimp (Artemia franciscana Kellog resulted in 100% mortality at 10 ppm, and two compounds caused 100% mortality at 1 ppm. Aquatic LC50 values were calculated for five compounds for larvae of the yellow fever mosquito (Aedes aegypti (L.. Monoterpenoid esters were among the most toxic compounds tested in topical and aquatic bioassays.

  6. Inhibition of acetylcholinesterase activity in brain and behavioral analysis in adult rats after chronic administration of fenproporex.

    Science.gov (United States)

    Rezin, Gislaine T; Scaini, Giselli; Ferreira, Gabriela K; Cardoso, Mariane R; Gonçalves, Cinara L; Constantino, Larissa S; Deroza, Pedro F; Ghedim, Fernando V; Valvassori, Samira S; Resende, Wilson R; Quevedo, João; Zugno, Alexandra I; Streck, Emilio L

    2012-12-01

    Fenproporex is an amphetamine-based anorectic and it is rapidly converted in vivo into amphetamine. It elevates the levels of extracellular dopamine in the brain. Acetylcholinesterase is a regulatory enzyme which is involved in cholinergic synapses and may indirectly modulate the release of dopamine. Thus, we investigated whether the effects of chronic administration of fenproporex in adult rats alters acquisition and retention of avoidance memory and acetylcholinesterase activity. Adult male Wistar rats received repeated (14 days) intraperitoneal injection of vehicle or fenproporex (6.25, 12.5 or 25 mg/kg i.p.). For behavioral assessment, animals were submitted to inhibitory avoidance (IA) tasks and continuous multiple trials step-down inhibitory avoidance (CMIA). Acetylcholinesterase activity was measured in the prefrontal cortex, hippocampus, hypothalamus and striatum. The administration of fenproporex (6.25, 12.5 and 25 mg/kg) did not induce impairment in short and long-term IA or CMIA retention memory in rats. In addition, longer periods of exposure to fenproporex administration decreased acetylcholinesterase activity in prefrontal cortex and striatum of rats, but no alteration was verified in the hippocampus and hypothalamus. In conclusion, the present study showed that chronic fenproporex administration decreased acetylcholinesterase activity in the rat brain. However, longer periods of exposure to fenproporex did not produce impairment in short and long-term IA or CMIA retention memory in rats.

  7. Interleukin 6 modulates acetylcholinesterase activity of brain neurons; Effet de l`interleukine 6 sur l`activite de l`acetylcholinesterase des neurones centraux

    Energy Technology Data Exchange (ETDEWEB)

    Clarencon, D.; Multon, E.; Galonnier, M.; Estrade, M.; Fournier, C.; Mathieu, J.; Mestries, J.C.; Testylier, G.; Fatome, M.

    1995-12-31

    Classically, radiation injuries results in a peripheral inflammatory process, and we have previously observed an early systemic interleukin 6 (IL-6) release following whole-body irradiation. Besides, we have demonstrated an early decrease of rat or primate brain acetylcholinesterase (AChE) activity a gamma exposure. The object of the present study is to find possible IL-6 systemic effects on the brain AChE activity. We show that, though intravenous (i.v.) or intra-cerebro-ventricular (ICV) injection of IL-6 can induce a drop in rat brain AChE activity, this cytokine induces only a slight decrease of the AChE release in cultured brain cells. (author). 3 refs.

  8. Role of Imaging in the Diagnosis and Management of Complete Androgen Insensitivity Syndrome in Adults

    Directory of Open Access Journals (Sweden)

    Marco Nezzo

    2013-01-01

    Full Text Available Complete androgen insensitivity syndrome is an X-linked recessive androgen receptor disorder characterized by a female phenotype with an XY karyotype. Individuals affected by this syndrome have normal female external genitalia but agenesis of the Müllerian duct derivatives, that is, absence of the Fallopian tubes, uterus, cervix, and the proximal part of the vagina, with presence of endoabdominal, labial, or inguinal testes. The estimated prevalence is between 1 and 5 in 100,000 genetic males. Complete androgen insensitivity syndrome can be diagnosed as a result of mismatch between the prenatal sex prediction and the phenotype at birth, can be detected by chance, or remain undetected until investigations for primary amenorrhea. Imaging can be important both to diagnose the pathology and to localize gonads prior to surgical treatment. In this paper, we present three cases of complete androgen insensitivity syndrome in adult women of 34, 22, and 38 years old.

  9. Impact of a program to diminish gender insensitivity and sexual harassment at a medical school.

    Science.gov (United States)

    Jacobs, C D; Bergen, M R; Korn, D

    2000-05-01

    To measure the effect of an intervention to reduce gender insensitivity and sexual harassment at one medical school. Stanford University School of Medicine undertook a multifaceted program to educate faculty and students regarding gender issues and to diminish sexual harassment. The authors developed a survey instrument to assess the faculty's perceptions regarding environment (five scales) and incidences of sexual harassment. Faculty were surveyed twice during the interventions (1994 and 1995). Between the two years, the authors measured significant improvements in mean ratings for positive climate (p = .004) and cohesion (p = .006) and decreases in the faculty's perceptions of sexual harassment (p = 0006), gender insensitivity (p = .001), and gender discrimination (p = .004). The faculty also reported fewer observations of harassing behavior during the study period. An intervention program to diminish gender insensitivity and sexual harassment can measurably improve a medical school's environment.

  10. Teenage organophosphate insecticide poisoning: An ugly trend in ...

    African Journals Online (AJOL)

    UNIBEN

    is worsened by uncontrolled sale of organophosphorus insecticides on the streets and in open markets. We report ..... Nicotinic activity results in autonomic nervous system .... optimize outcome.23 Oximes are cholinesterase re-activators used ...

  11. Gas Chromaotography-Mass Spectrometry Analysis of Insecticidal ...

    African Journals Online (AJOL)

    Insecticidal Essential Oil Derived from Chinese Ainsliaea fragrans Champ ex Benth ... Methods: The essential oil of A. fragrans aerial parts was obtained by hydrodistillation and analyzed by ..... toxicity than the crude oil. Caryophyllene showed.

  12. Scepticism towards insecticide treated mosquito nets for malaria ...

    African Journals Online (AJOL)

    Scepticism towards insecticide treated mosquito nets for malaria control in rural ... especially among under-five year children and pregnant women in poor rural ... through social marketing strategy for malaria control prior to the introduction of ...

  13. Design, Synthesis and Insecticidal Activity of Novel Phenylurea Derivatives

    Directory of Open Access Journals (Sweden)

    Jialong Sun

    2015-03-01

    Full Text Available A series of novel phenylurea derivatives were designed and synthesized according to the method of active groups linkage and the principle of aromatic groups bioisosterism in this study. The structures of the novel phenylurea derivatives were confirmed based on ESI-MS, IR and 1H-NMR spectral data. All of the compounds were evaluated for the insecticidal activity against the third instars larvae of Spodoptera exigua Hiibner, Plutella xyllostella Linnaeus, Helicoverpa armigera Hubner and Pieris rapae Linne respectively, at the concentration of 10 mg/L. The results showed that all of the derivatives displayed strong insecticidal activity. Most of the compounds presented higher insecticidal activity against S. exigua than the reference compounds tebufenozide, chlorbenzuron and metaflumizone. Among the synthesized compounds, 3b, 3d, 3f, 4b and 4g displayed broad spectrum insecticidal activity.

  14. Neurotoxicological effects and the mode of action of pyrethroid insecticides

    NARCIS (Netherlands)

    Vijverberg, H.P.M.; Bercken, Joep van den

    1990-01-01

    Neuroexcitatory symptoms of acute poisoning of vertebrates by pyrethroids are related to the ability of these insecticides to modify electrical activity in various parts of the nervous system. Repetitive nerve activity, particularly in the sensory nervous system, membrane depolarization, and

  15. Effect of natural and chemical insecticides on Hyalopterus pruni and ...

    African Journals Online (AJOL)

    STORAGESEVER

    2008-06-17

    Jun 17, 2008 ... Anthmis pseudocotula and their mixtures with chemical insecticide (Malathion) on growth of ... ed the use of natural extracts of Fagonia arabica, Salix ..... Studies on the efficacy of neem products against the aphid Aphis.

  16. Process optimization and insecticidal activity of alkaloids from the ...

    African Journals Online (AJOL)

    Process optimization and insecticidal activity of alkaloids from the root bark of Catalpa ovata G. Don by response surface methodology. ... Tropical Journal of Pharmaceutical Research. Journal Home · ABOUT THIS JOURNAL · Advanced ...

  17. Insect P450 inhibitors and insecticides: challenges and opportunities.

    Science.gov (United States)

    Feyereisen, René

    2015-06-01

    P450 enzymes are encoded by a large number of genes in insects, often over a hundred. They play important roles in insecticide metabolism and resistance, and growing numbers of P450 enzymes are now known to catalyse important physiological reactions, such as hormone metabolism or cuticular hydrocarbon synthesis. Ways to inhibit P450 enzymes specifically or less specifically are well understood, as P450 inhibitors are found as drugs, as fungicides, as plant growth regulators and as insecticide synergists. Yet there are no P450 inhibitors as insecticides on the market. As new modes of action are constantly needed to support insecticide resistance management, P450 inhibitors should be considered because of their high potential for insect selectivity, their well-known mechanisms of action and the increasing ease of rational design and testing. © 2014 Society of Chemical Industry.

  18. Gas Chromatography-Mass Spectrometric Analysis and Insecticidal ...

    African Journals Online (AJOL)

    HP

    Original Research Article. Gas Chromatography-Mass Spectrometric Analysis and ... into a natural fumigant/insecticide for the control of stored product insects. Keywords: Mallotus ..... stability as well as reduce cost. ACKNOWLEDGEMENT.

  19. Gas Chromatography-Mass Spectrometric Analysis and Insecticidal ...

    African Journals Online (AJOL)

    Tropical Journal of Pharmaceutical Research ... apelta aerial parts was analyzed by gas chromatography/mass spectrometric (GC/MS) to determine its composition. ... into a natural fumigant/insecticide for the control of stored product insects.

  20. Federal Insecticide, Fungicide, and Rodenticide Act Section 18 Database

    Data.gov (United States)

    U.S. Environmental Protection Agency — Section 18 of Federal Insecticide, Fungicide, and Rodenticide Act (FIFRA) authorizes EPA to allow an unregistered use of a pesticide for a limited time if EPA...

  1. PRN 73-4: Residual Insecticides in Food Handling Establishments

    Science.gov (United States)

    This notice provides a copy of a Federal Register notice published July 6, 1973, regarding certain insecticides used in food-handling establishments. It establishes certain definitions and requirements related to approval for crack and crevice treatment.

  2. Antioxidant and anti-acetylcholinesterase activities of extracts from Rapistrum rugosum in Tunisia

    Directory of Open Access Journals (Sweden)

    Omri Hichri Amel

    2017-07-01

    Full Text Available Objective: To investigate the antioxidant potential and anti-acetylcholinesterase activity of Rapistrum rugosum extracts. Methods: The crude, ethyl acetate, butanol and water extracts prepared from flowers, roots, stems and leaves of Rapistrum rugosum were tested at 1 mg/mL to determine their total polyphenol content, total flavonoid content and total condensed tannin content. Their antioxidant activity was assessed at different concentrations (0.0312, 0.0625, 0.1250, 0.25, 0.50 and 1.00 mg/ mL by using DPPH, ABTS, reducing power and β-carotene bleAChIng inhibition activity. Antiacetylcholinesterase activity was also determined. Results: The extract of leaves and stems had the highest total phenolic content [(110.45依0.03 mg gallic acid equivalent/g dry weight]. The ethyl acetate extract of flowers had the highest total flavonoid content [(24.62依0.13 mg quercetin equivalent/g dry weight]. The butanolic fraction of flowers had the highest total condensed tannin content [(317.85依0.01 mg catechin equivalent/g dry weight]. The crude extracts of flowers exhibited an interesting antioxidant activity for DPPH assay (93.00依0.01% at 1 mg/mL. The greatest acetylcholinesterase inhibitory activity (IC50=1.60 mg/mL was exhibited by the crude extracts from the flowers. Conclusions: The results demonstrated that Rapistrum rugosum contains active constituents which possess antioxidant and anti-acetylcholinesterase activities.

  3. Polarization insensitive wavelength conversion in a dispersion-engineered silicon waveguide

    DEFF Research Database (Denmark)

    Pu, Minhao; Hu, Hao; Peucheret, Christophe

    2012-01-01

    We experimentally demonstrate polarization-insensitive all optical wavelength conversion of a 10-Gb/s DPSK data signal based on four-wave mixing in a silicon waveguide with an angled-pump scheme. Dispersion engineering is applied to the silicon waveguide to obtain similar four-wave mixing convers...... conversion performances for both the TE and TM modes. Bit-error rate measurements are performed and error-free operation is achieved. We also demonstrate polarization-insensitive wavelength conversion with a large separation between the idler and signal using a dual-pump configuration....

  4. Flexible manipulation of terahertz wave reflection using polarization insensitive coding metasurfaces.

    Science.gov (United States)

    Jiu-Sheng, Li; Ze-Jiang, Zhao; Jian-Quan, Yao

    2017-11-27

    In order to extend to 3-bit encoding, we propose notched-wheel structures as polarization insensitive coding metasurfaces to control terahertz wave reflection and suppress backward scattering. By using a coding sequence of "00110011…" along x-axis direction and 16 × 16 random coding sequence, we investigate the polarization insensitive properties of the coding metasurfaces. By designing the coding sequences of the basic coding elements, the terahertz wave reflection can be flexibly manipulated. Additionally, radar cross section (RCS) reduction in the backward direction is less than -10dB in a wide band. The present approach can offer application for novel terahertz manipulation devices.

  5. Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase

    Directory of Open Access Journals (Sweden)

    Xiaofei Jiang

    2017-01-01

    Full Text Available Jatrorrhizine was considered as one of the active constituents of Coptis chinensis Franch. Herein, jatrorrhizine derivatives with substituted amino groups linked at the 3-position were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Jatrorrhizine derivatives inhibited the activity of acetylcholinesterase (AChE to a greater extent than the lead compound jatrorrhizine. All these jatrorrhizine derivatives were proved to be potent inhibitors of acetylcholinesterase (AChE with submicromolar IC50 values, but less sensitive to butyrylcholinesterase (BuChE, which suggests that these jatrorrhizine derivatives are selective for AChE/BuChE. Compound 3g gave the most potent inhibitor activity for AChE (IC50 = 0.301 μM, which is greater than the lead compound jatrorrhizine. All these results demonstrated that these jatrorrhizine derivatives are potential inhibitors for AChE.

  6. Acetylcholinesterase Inhibition and in Vitro and in Vivo Antioxidant Activities of Ganoderma lucidum Grown on Germinated Brown Rice

    Directory of Open Access Journals (Sweden)

    Beong Ou Lim

    2013-06-01

    Full Text Available In this study, the acetylcholinesterase inhibition and in vitro and in vivo antioxidant activities of Ganoderma lucidum grown on germinated brown rice (GLBR were evaluated. In antioxidant assays in vitro, GLBR was found to have strong metal chelating activity, DPPH, ABTS, hydroxyl and superoxide radical scavenging activity. Cell-based antioxidant methods were used, including lipid peroxidation on brain homogenate and AAPH-induced erythrocyte haemolysis. In antioxidant assays in vivo, mice were administered with GLBR and this significantly enhanced the activities of antioxidant enzymes in the mice sera, livers and brains. The amount of total phenolic and flavonoid compounds were 43.14 mg GAE/g and 13.36 mg CE/g dry mass, respectively. GLBR also exhibited acetylcholinesterase inhibitory activity. In addition, HPLC analyses of GLBR extract revealed the presence of different phenolic compounds. These findings demonstrate the remarkable potential of GLBR extract as valuable source of antioxidants which exhibit interesting acetylcholinesterase inhibitory activity.

  7. Theoretical NMR and conformational analysis of solvated oximes for organophosphates-inhibited acetylcholinesterase reactivation

    Science.gov (United States)

    da Silva, Jorge Alberto Valle; Modesto-Costa, Lucas; de Koning, Martijn C.; Borges, Itamar; França, Tanos Celmar Costa

    2018-01-01

    In this work, quaternary and non-quaternary oximes designed to bind at the peripheral site of acetylcholinesterase previously inhibited by organophosphates were investigated theoretically. Some of those oximes have a large number of degrees of freedom, thus requiring an accurate method to obtain molecular geometries. For this reason, the density functional theory (DFT) was employed to refine their molecular geometries after conformational analysis and to compare their 1H and 13C nuclear magnetic resonance (NMR) theoretical signals in gas-phase and in solvent. A good agreement with experimental data was achieved and the same theoretical approach was employed to obtain the geometries in water environment for further studies.

  8. Pharmacological evaluation of [11c]donepezil as tracer for visualization of acetylcholinesterase by PET

    International Nuclear Information System (INIS)

    Vos, F. de; Santens, P.; Vermeirsch, H.; Dewolf, I.; Dumont, F.; Slegers, G.; Dierckx, R.A.; Reuck, J. de

    2000-01-01

    Donepezil is a highly potent and selective reversible acetylcholinesterase inhibitor. [ 11 C]Donepezil is prepared by methylation with [ 11 C]CH 3 I of the corresponding 6'-O-desmethylprecursor. Tissue distribution in mice revealed a high uptake in brain and rapid clearance from the blood. Metabolization studies in mice indicated the formation of one 11 C-labeled polar metabolite that didn't penetrate the blood-brain barrier. Regional brain distribution in rabbits didn't reflect the measured achetylcholinesterase distribution in rabbit brain

  9. [Memantine as add-on medication to acetylcholinesterase inhibitor therapy for Alzheimer dementia].

    Science.gov (United States)

    Haussmann, R; Donix, M

    2017-01-01

    Currently available data indicate superior therapeutic effects of combination treatment for Alzheimer dementia with memantine and acetylcholine esterase inhibitors in certain clinical contexts. Out of five randomized, placebo-controlled, double-blind trials two showed superior therapeutic effects in comparison to monotherapy with acetylcholinesterase inhibitors regarding various domains. Recently published meta-analyses and cost-benefit analyses also showed positive results. Recently published German guidelines for dementia treatment also take these new data into account and recommend combination treatment in patients with severe dementia on stable donepezil medication. This article gives an overview of current evidence for combination therapy.

  10. Nanomaterials-Based Optical Techniques for the Detection of Acetylcholinesterase and Pesticides

    Directory of Open Access Journals (Sweden)

    Ning Xia

    2014-12-01

    Full Text Available The large amount of pesticide residues in the environment is a threat to global health by inhibition of acetylcholinesterase (AChE. Biosensors for inhibition of AChE have been thus developed for the detection of pesticides. In line with the rapid development of nanotechnology, nanomaterials have attracted great attention and have been intensively studied in biological analysis due to their unique chemical, physical and size properties. The aim of this review is to provide insight into nanomaterial-based optical techniques for the determination of AChE and pesticides, including colorimetric and fluorescent assays and surface plasmon resonance.

  11. Dihydroagarofuranoid Sesquiterpenes as Acetylcholinesterase Inhibitors from Celastraceae Plants: Maytenus disticha and Euonymus japonicus.

    Science.gov (United States)

    Alarcón, Julio; Cespedes, Carlos L; Muñoz, Evelyn; Balbontin, Cristian; Valdes, Francisco; Gutierrez, Margarita; Astudillo, Luis; Seigler, David S

    2015-12-02

    Natural cholinesterase inhibitors have been found in many biological sources. Nine compounds with agarofuran (epoxyeudesmane) skeletons were isolated from seeds and aerial parts of Maytenus disticha and Euonymus japonicus. The identification and structural elucidation of compounds were based on spectroscopic data analyses. All compounds had inhibitory acetylcholinesterase (AChE) activity. These natural compounds, which possessed mixed or uncompetitive mechanisms of inhibitory activity against AChE, may be considered as models for the design and development of new naturally occurring drugs for management strategies for neurodegenerative diseases. This is the first report of these chemical structures for seeds of M. disticha.

  12. Log bioassay of residual effectiveness of insecticides against bark beetles

    Science.gov (United States)

    Richard H. Smith

    1982-01-01

    Residual effectiveness of nine insecticides applied to bark was tested against western, mountain, and Jeffrey pine beetles. Ponderosa and Jeffrey pine trees were treated and logs cut from them 2 to 13 months later, and bioassayed with the three beetles. The insecticides were sprayed at the rate of 1 gal (3.8 l) per 40- or 80-ft² (3.6 or 7.2 m²) bark surface at varying...

  13. The use of insecticides to control insect pests

    OpenAIRE

    M Wojciechowska; P Stepnowski; M Gołębiowski

    2016-01-01

    Pesticides are used as plants protection products. Among those, insecticides serve as agents to control insects. When incorrectly applied, however these substances may negatively affect people's health and natural environment. Administration routes of insecticides depend on many factors and vary from spraying to fertilizers. These different methods influence how insects prey and how pests develop. Additionally, too frequent use of the same chemicals can lead to development of resi...

  14. Insecticidal activity of Trichilia claussenii (Meliaceae) fruits against Spodoptera frugiperda

    International Nuclear Information System (INIS)

    Nebo, Liliane; Matos, Andrea Pereira; Vieira, Paulo Cezar; Fernandes, Joao Batista; Silva, Maria Fatima das Gracas Fernandes da; Rodrigues, Ricardo Ribeiro

    2010-01-01

    An evaluation of the insecticidal activity of the fruits extracts of Trichilia claussenii was carried out and the methanol extract revealed to have strong insecticidal activity. The fractionation of methanol extract of T. claussenii seeds bioassay-guided against Spodoptera frugiperda has led to the identification of the ω-phenylalkyl and alkenyl fatty acids as active compounds in this extract. The structures of the compounds were proposed by spectroscopic analysis and comparison with literature data. (author)

  15. Organochlorine insecticide poisoning in Golden Langurs Trachypithecus geei

    Directory of Open Access Journals (Sweden)

    D.C. Pathak

    2011-07-01

    Full Text Available Organochlorine insecticide poisoning was recorded in three Golden Langurs (Trachypithecus geei in Chakrashila Wildlife Sanctuary (CWS in Kokrajhar district of Assam during the month of December, 2008. The poisoning was due to prolonged ingestion of rubber plant leaves sprayed with the insecticide in a rubber plantation adjacent to the sanctuary. Though no specific gross lesions were observed, histopathologically, centilobular hepatic necrosis, mild renal degeneration, necrotic enteritis, pulmonary congestion and neuronal degeneration were recorded in all three animals.

  16. Plant compounds insecticide activity against Coleoptera pests of stored products

    OpenAIRE

    MOREIRA, M.D.; PICANÇO, M.C.; BARBOSA, L.C. de A.; GUEDES, R.N.C.; CAMPOS, M.R. de; SILVA, G.A.; MARTINS, J.C.

    2008-01-01

    The objective of this work was to screen plants with insecticide activity, in order to isolate, identify and assess the bioactivity of insecticide compounds present in these plants, against Coleoptera pests of stored products: Oryzaephilus surinamensis L. (Silvanidae), Rhyzopertha dominica F. (Bostrichidae) and Sitophilus zeamais Mots. (Curculionidae). The plant species used were: basil (Ocimum selloi Benth.), rue (Ruta graveolens L.), lion's ear (Leonotis nepetifolia (L.) R.Br.), jimson weed...

  17. Identification of a trypsin-like site associated with acetylcholinesterase by affinity labelling with (/sup 3/H)diisopropyl fluorophosphate

    Energy Technology Data Exchange (ETDEWEB)

    Small, D.H.; Chubb, I.W.

    1988-07-01

    In addition to its ability to hydrolyze acetylcholine, purified eel acetylcholinesterase possesses a trypsin-like endopeptidase activity. The tryptic activity is associated with a serine residue at a site that is distinct from the esteratic site. To label both the esteratic and tryptic sites, the enzyme was incubated with the serine hydrolase inhibitor (/sup 3/H)diisopropyl fluorophosphate. This compound labelled the protein in a biphasic manner, with both slow and rapid labelling kinetics. The time course of the rapid phase was similar to the time course of inactivation of the esteratic activity. The time course of the slow phase was similar to the time course of inactivation of the tryptic activity. Labelling of the nonesteratic site was inhibited by the trypsin inhibitor N alpha-p-tosyl-L-lysine chloromethyl ketone. The total number of sites labelled by (/sup 3/H)diisopropyl fluorophosphate on eel acetylcholinesterase was 2.6 mol/280,000 g protein, whereas the number of tryptic sites was less (0.52 mol/280,000 g). The results suggest that a subpopulation of acetylcholinesterase molecules may possess tryptic activity. Extensive chromatography of the purified enzyme by ion-exchange and gel filtration failed to separate the labelled tryptic component from acetylcholinesterase. On sodium dodecyl sulfate-polyacrylamide gels, the labelled tryptic component comigrated with a polypeptide of 50,000 molecular weight, which is a major proteolytic digestion product derived from the intact acetylcholinesterase monomer. Because of its localization in many noncholinergic peptide-containing cells, acetylcholinesterase could act as a neuropeptide processing enzyme in these cells.

  18. Impact of some selected insecticides application on soil microbial respiration.

    Science.gov (United States)

    Latif, M A; Razzaque, M A; Rahman, M M

    2008-08-15

    The aim of present study was to investigate the impact of selected insecticides used for controlling brinjal shoot and fruit borer on soil microorganisms and to find out the insecticides or nontoxic to soil microorganism the impact of nine selected insecticides on soil microbial respiration was studied in the laboratory. After injection of different insecticides solutions, the soil was incubated in the laboratory at room temperature for 32 days. The amount of CO2 evolved due to soil microbial respiration was determined at 2, 4, 8, 16, 24 and 32 days of incubation. Flubendiamide, nimbicidine, lambda-cyhalothrin, abamectin and thiodicarb had stimulatory effect on microbial respiration during the initial period of incubation. Chlorpyriphos, cartap and carbosulfan had inhibitory effect on microbial respiration and cypermethrin had no remarkable effect during the early stage of incubation. The negative effect of chlorpyriphos, cartap and carbosulfan was temporary, which was disappeared after 4 days of insecticides application. No effect of the selected insecticides on soil microorganisms was observed after 24 or 32 days of incubation.

  19. Insecticide mixtures could enhance the toxicity of insecticides in a resistant dairy population of Musca domestica L [corrected].

    Directory of Open Access Journals (Sweden)

    Hafiz Azhar Ali Khan

    Full Text Available House flies, Musca domestica L., are important pests of dairy operations worldwide, with the ability to adapt wide range of environmental conditions. There are a number of insecticides used for their management, but development of resistance is a serious problem. Insecticide mixtures could enhance the toxicity of insecticides in resistant insect pests, thus resulting as a potential resistance management tool. The toxicity of bifenthrin, cypermethrin, deltamethrin, chlorpyrifos, profenofos, emamectin benzoate and fipronil were assessed separately, and in mixtures against house flies. A field-collected population was significantly resistant to all the insecticides under investigation when compared with a laboratory susceptible strain. Most of the insecticide mixtures like one pyrethroid with other compounds evaluated under two conditions (1∶1-"A" and LC50: LC50-"B" significantly increased the toxicity of pyrethroids in the field population. Under both conditions, the combination indices of pyrethroids with other compounds, in most of the cases, were significantly below 1, suggesting synergism. The enzyme inhibitors, PBO and DEF, when used in combination with insecticides against the resistant population, toxicities of bifenthrin, cypermethrin, deltamethrin and emamectin were significantly increased, suggesting esterase and monooxygenase based resistance mechanism. The toxicities of bifenthrin, cypermethrin and deltamethrin in the resistant population of house flies could be enhanced by the combination with chlorpyrifos, profenofos, emamectin and fipronil. The findings of the present study might have practical significance for resistance management in house flies.

  20. Insecticide Mixtures Could Enhance the Toxicity of Insecticides in a Resistant Dairy Population of Musca domestica L

    Science.gov (United States)

    Khan, Hafiz Azhar Ali; Akram, Waseem; Shad, Sarfraz Ali; Lee, Jong-Jin

    2013-01-01

    House flies, Musca domestica L., are important pests of dairy operations worldwide, with the ability to adapt wide range of environmental conditions. There are a number of insecticides used for their management, but development of resistance is a serious problem. Insecticide mixtures could enhance the toxicity of insecticides in resistant insect pests, thus resulting as a potential resistance management tool. The toxicity of bifenthrin, cypermethrin, deltamethrin, chlorpyrifos, profenofos, emamectin benzoate and fipronil were assessed separately, and in mixtures against house flies. A field-collected population was significantly resistant to all the insecticides under investigation when compared with a laboratory susceptible strain. Most of the insecticide mixtures like one pyrethroid with other compounds evaluated under two conditions (1∶1-“A” and LC50: LC50-“B”) significantly increased the toxicity of pyrethroids in the field population. Under both conditions, the combination indices of pyrethroids with other compounds, in most of the cases, were significantly below 1, suggesting synergism. The enzyme inhibitors, PBO and DEF, when used in combination with insecticides against the resistant population, toxicities of bifenthrin, cypermethrin, deltamethrin and emamectin were significantly increased, suggesting esterase and monooxygenase based resistance mechanism. The toxicities of bifenthrin, cypermethrin and deltamethrin in the resistant population of house flies could be enhanced by the combination with chlorpyrifos, profenofos, emamectin and fipronil. The findings of the present study might have practical significance for resistance management in house flies. PMID:23613758

  1. The gut microbiota of insecticide-resistant insects houses insecticide-degrading bacteria: A potential source for biotechnological exploitation

    Science.gov (United States)

    de Almeida, Luis Gustavo; de Moraes, Luiz Alberto Beraldo; Trigo, José Roberto; Omoto, Celso

    2017-01-01

    The exploration of new niches for microorganisms capable of degrading recalcitrant molecules is still required. We hypothesized the gut microbiota associated with insect-resistant lines carry pesticide degrading bacteria, and predicted they carry bacteria selected to degrade pesticides they were resistant to. We isolated and accessed the pesticide-degrading capacity of gut bacteria from the gut of fifth instars of Spodoptera frugiperda strains resistant to lambda-cyhalothrin, deltamethrin, chlorpyrifos ethyl, spinosad and lufenuron, using insecticide-selective media. Sixteen isolates belonging to 10 phylotypes were obtained, from which four were also associated with the susceptible strain. However, growth of gut bacteria associated with larvae from the susceptible strain was not obtained in any of the insecticide-based selective media tested. Growth of isolates was affected by the concentration of insecticides in the media, and all grew well up to 40 μg/ml. The insecticide-degrading capacity of selected isolates was assessed by GC or LC-MS/MS analyses. In conclusion, resistant strains of S. frugiperda are an excellent reservoir of insecticide-degrading bacteria with bioremediation potential. Moreover, gut-associated bacteria are subjected to the selection pressure imposed by insecticides on their hosts and may influence the metabolization of pesticides in insects. PMID:28358907

  2. The gut microbiota of insecticide-resistant insects houses insecticide-degrading bacteria: A potential source for biotechnological exploitation.

    Directory of Open Access Journals (Sweden)

    Luis Gustavo de Almeida

    Full Text Available The exploration of new niches for microorganisms capable of degrading recalcitrant molecules is still required. We hypothesized the gut microbiota associated with insect-resistant lines carry pesticide degrading bacteria, and predicted they carry bacteria selected to degrade pesticides they were resistant to. We isolated and accessed the pesticide-degrading capacity of gut bacteria from the gut of fifth instars of Spodoptera frugiperda strains resistant to lambda-cyhalothrin, deltamethrin, chlorpyrifos ethyl, spinosad and lufenuron, using insecticide-selective media. Sixteen isolates belonging to 10 phylotypes were obtained, from which four were also associated with the susceptible strain. However, growth of gut bacteria associated with larvae from the susceptible strain was not obtained in any of the insecticide-based selective media tested. Growth of isolates was affected by the concentration of insecticides in the media, and all grew well up to 40 μg/ml. The insecticide-degrading capacity of selected isolates was assessed by GC or LC-MS/MS analyses. In conclusion, resistant strains of S. frugiperda are an excellent reservoir of insecticide-degrading bacteria with bioremediation potential. Moreover, gut-associated bacteria are subjected to the selection pressure imposed by insecticides on their hosts and may influence the metabolization of pesticides in insects.

  3. Switching an O2 sensitive glucose oxidase bioelectrode into an almost insensitive one by cofactor redesign.

    Science.gov (United States)

    Tremey, Emilie; Suraniti, Emmanuel; Courjean, Olivier; Gounel, Sébastien; Stines-Chaumeil, Claire; Louerat, Frédéric; Mano, Nicolas

    2014-06-04

    In the 5-8 mM glucose concentration range, of particular interest for diabetes management, glucose oxidase bioelectrodes are O2 dependent, which decrease their efficiencies. By replacing the natural cofactor of glucose oxidase, we succeeded in turning an O2 sensitive bioelectrode into an almost insensitive one.

  4. Can Parents' Involvement in Children's Education Offset the Effects of Early Insensitivity on Academic Functioning?

    Science.gov (United States)

    Monti, Jennifer D.; Pomerantz, Eva M.; Roisman, Glenn I.

    2014-01-01

    Data from the National Institute of Child Health and Human Development Study of Early Child Care and Youth Development (N = 1,312) were analyzed to examine whether the adverse effects of early insensitive parenting on children's academic functioning can be offset by parents' later involvement in children's education. Observations of mothers' early…

  5. A Chroma-based Tempo-insensitive Distance Measure for Cover Song Identification

    DEFF Research Database (Denmark)

    Jensen, Jesper Højvang; Ellis, Dan P. W.; Christensen, Mads Græsbøll

    In the context of music, a cover version is a remake of a song, often with significant stylistic variation. In this paper we describe a distance measure between sampled audio files that is designed to be insensitive to instrumentation, time shift, temporal scaling and transpositions. The algorithm...

  6. DEFECTS IN INSULIN-SECRETION IN NIDDM - B-CELL GLUCOSE INSENSITIVITY OR GLUCOSE TOXICITY

    NARCIS (Netherlands)

    VANHAEFTEN, TW

    In NIDDM, first-phase insulin release to glucose is (almost) absent. However, in contrast to older studies which suggested that in NIDDM the B-cell is ''blind'' for glucose, recent evidence indicates that the B-cell is not insensitive for glucose as far as second phase release is concerned. This

  7. Using metrics for proof rules for recursively defined delay-insensitive specifications

    NARCIS (Netherlands)

    Mallon, WC; Udding, JT

    1997-01-01

    An advantage of algebraic specifications of delay insensitive asynchronous processes over most other formalisms is that it allows the recursive definition of processes, and correctness proofs of an implementation through fixpoint induction. On the other hand, proofs by fixpoint induction are

  8. Progressing Insensitive Munitions: Benefits and Techniques for Proactively Addressing Environmental Regulations

    Science.gov (United States)

    2012-05-01

    X Worm Tubifex tubifex X X X Black worm Lumbriculus X Asiatic clam Corbicula fluminea X Estuarine/marine water column Mysid shrimp Americamysis...Objective: Characterize traditional and insensitive munitions (IMs) impacts on amphibian larvae to manage a candidate for T&E status that inhabit

  9. 320 Gb/s Nyquist OTDM received by polarization-insensitive time-domain OFT

    DEFF Research Database (Denmark)

    Hu, Hao; Kong, Deming; Palushani, Evarist

    2014-01-01

    We have demonstrated the generation of a 320 Gb/s Nyquist-OTDM signal by rectangular filtering on an RZ-OTDM signal with the filter bandwidth (320 GHz) equal to the baud rate (320 Gbaud) and the reception of such a Nyquist-OTDM signal using polarization-insensitive time-domain optical Fourier tra...

  10. In vitro toxicity, antiplatelet and acetylcholinesterase inhibition of Buddleja thyrsoides Lam. leaves.

    Science.gov (United States)

    Mahlke, Janaína Dorneles; Boligon, Aline Augusti; Machado, Michel Mansur; Athayde, Margareth Linde

    2012-01-01

    Alzheimer's disease (AD) is a neurodegenerative disorder resulting in impaired memory and behaviour of remarkable socio-economic impact. A decrease in cholinergic activity is a key event in the biochemical of AD. Buddleja thyrsoides is a plant widely distributed in Southern parts of South America. In Brazilian traditional medicine, the infusion of its leaves and flowers is used for the treatment of bronchitis and cough. Crude ethanolic (70%) extract and fractions (dichloromethane, ethyl acetate and n-butanolic) were investigated regarding their toxicities in vitro and antiplatelet action. The enzyme acetylcholinesterase inhibition was evaluated to study the crude extract. The crude extract and fractions were evaluated by means of Brine Shrimp Lethality test and they showed low activities with LC(50) values 1698, 2818, 2187 and 3672 µg mL(-1) for dichloromethane, ethyl acetate, n-butanolic fractions and crude extract, respectively. Buddleja thyrsoides presented great antiplatelet action. The IC(50) values obtained for crude extract and dichloromethane, ethyl acetate and n-butanolic fractions were 361.29, 354.23, 368.75 and 344.30, respectively, while the IC(50) for the standard AAS was 257.01 µg mL(-1). The crude extract showed an inhibition of 22.8% of the acetylcholinesterase enzyme in 24 h.

  11. Screening of acetylcholinesterase inhibitors in marine organisms from the Caribbean Sea.

    Science.gov (United States)

    Castellanos, Fabio; Amaya-García, Fabián; Tello, Edisson; Ramos, Freddy Alejandro; Umaña, Adriana; Puyana, Mónica; Resende, Jackson A L C; Castellanos, Leonardo

    2018-06-04

    The acetylcholinesterase inhibitory activity of 89 organic extracts from marine organisms was evaluated through a TLC bioautography methodology. Extracts from soft corals (Eunicea and Plexaura) were the most active compared with extracts from sponges. The bioguided chemical study of the most active extract, obtained from Pseudoplexaura porosa, led to the isolation of a diterpene with spectroscopic properties consistent to those published to the cembrane Steylolide. However, further analysis by X-ray diffraction indicated that the compound was the 14-acetoxycrassine (1), correcting the structure reported to the Styelolide. Additionally, the acetylcholinesterase inhibitory activity of fourteen cembranoids (2-15) isolated from soft corals Eunicea knighti and Pseudoplexaura flagellosa was evaluated. Cembranoids 2, 3 and 4 were the most active compounds in the TLC bioassay. Then, the most promising cembranoids, 14-acetoxycrassine (1) and asperdiol (2), were tested quantitatively and they exhibited IC 50 values of 1.40 ± 0.113 and 0.358 ± 0.130 μM, respectively.

  12. Acetylcholinesterase-Inhibiting Activity of Salicylanilide N-Alkylcarbamates and Their Molecular Docking

    Directory of Open Access Journals (Sweden)

    Josef Jampilek

    2012-08-01

    Full Text Available A series of twenty-five novel salicylanilide N-alkylcarbamates were investigated as potential acetylcholinesterase inhibitors. The compounds were tested for their ability to inhibit acetylcholinesterase (AChE from electric eel (Electrophorus electricus L.. Experimental lipophilicity was determined, and the structure-activity relationships are discussed. The mode of binding in the active site of AChE was investigated by molecular docking. All the discussed compounds expressed significantly higher AChE inhibitory activity than rivastigmine and slightly lower than galanthamine. Disubstitution by chlorine in C'(3,4 of the aniline ring and the optimal length of hexyl-undecyl alkyl chains in the carbamate moiety provided the most active AChE inhibitors. Monochlorination in C'(4 exhibited slightly more effective AChE inhibitors than in C'(3. Generally it can be stated that compounds with higher lipophilicity showed higher inhibition, and the activity of the compounds is strongly dependent on the length of the N-alkyl chain.

  13. Global loss of acetylcholinesterase activity with mitochondrial complexes inhibition and inflammation in brain of hypercholesterolemic mice.

    Science.gov (United States)

    Paul, Rajib; Borah, Anupom

    2017-12-20

    There exists an intricate relationship between hypercholesterolemia (elevated plasma cholesterol) and brain functions. The present study aims to understand the impact of hypercholesterolemia on pathological consequences in mouse brain. A chronic mouse model of hypercholesterolemia was induced by giving high-cholesterol diet for 12 weeks. The hypercholesterolemic mice developed cognitive impairment as evident from object recognition memory test. Cholesterol accumulation was observed in four discrete brain regions, such as cortex, striatum, hippocampus and substantia nigra along with significantly damaged blood-brain barrier by hypercholesterolemia. The crucial finding is the loss of acetylcholinesterase activity with mitochondrial dysfunction globally in the brain of hypercholesterolemic mice, which is related to the levels of cholesterol. Moreover, the levels of hydroxyl radical were elevated in the regions of brain where the activity of mitochondrial complexes was found to be reduced. Intriguingly, elevations of inflammatory stress markers in the cholesterol-rich brain regions were observed. As cognitive impairment, diminished brain acetylcholinesterase activity, mitochondrial dysfunctions, and inflammation are the prima facie pathologies of neurodegenerative diseases, the findings impose hypercholesterolemia as potential risk factor towards brain dysfunction.

  14. A reversed-phase compatible thin-layer chromatography autography for the detection of acetylcholinesterase inhibitors.

    Science.gov (United States)

    Ramallo, I Ayelen; García, Paula; Furlan, Ricardo L E

    2015-11-01

    A dual readout autographic assay to detect acetylcholinesterase inhibitors present in complex matrices adsorbed on reversed-phase or normal-phase thin-layer chromatography plates is described. Enzyme gel entrapment with an amphiphilic copolymer was used for assay development. The effects of substrate and enzyme concentrations, pH, incubation time, and incubation temperature on the sensitivity and the detection limit of the assay were evaluated. Experimental design and response surface methodology were used to optimize conditions with a minimum number of experiments. The assay allowed the detection of 0.01% w/w of physostigmine in both a spiked Sonchus oleraceus L. extract chromatographed on normal phase and a spiked Pimenta racemosa (Mill.) J.W. Moore leaf essential oil chromatographed on reversed phase. Finally, the reversed-phase thin-layer chromatography assay was applied to reveal the presence of an inhibitor in the Cymbopogon citratus (DC.) Stapf essential oil. The developed assay is able to detect acetylcholinesterase inhibitors present in complex matrixes that were chromatographed in normal phase or reversed-phase thin-layer chromatography. The detection limit for physostigmine on both normal and reversed phase was of 1×10(-4) μg. The results can be read by a change in color and/or a change in fluorescence. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  15. An acetylcholinesterase biosensor based on graphene-gold nanocomposite and calcined layered double hydroxide.

    Science.gov (United States)

    Zhai, Chen; Guo, Yemin; Sun, Xia; Zheng, Yuhe; Wang, Xiangyou

    2014-05-10

    In this study, a novel acetylcholinesterase-based biosensor was fabricated. Acetylcholinesterase (AChE) was immobilized onto a glassy carbon electrode (GCE) with the aid of Cu-Mg-Al calcined layered double hydroxide (CLDH). CLDH can provide a bigger effective surface area for AChE loading, which could improve the precision and stability of AChE biosensor. However, the poor electroconductibility of CLDHs could lead to the low sensitivity of AChE biosensor. In order to effectively compensate the disadvantages of CLDHs, graphene-gold nanocomposites were used for improving the electron transfer rate. Thus, the graphene-gold nanocomposite (GN-AuNPs) was firstly modified onto the GCE, and then the prepared CLDH-AChE composite was immobilized onto the modified GCE to construct a sensitive AChE biosensor for pesticides detection. Relevant parameters were studied in detail and optimized, including the pH of the acetylthiocholine chloride (ATCl) solution, the amount of AChE immobilized on the biosensor and the inhibition time governing the analytical performance of the biosensor. The biosensor detected chlorpyrifos at concentrations ranging from 0.05 to 150μg/L. The detection limit for chlorpyrifos was 0.05μg/L. Copyright © 2014 Elsevier Inc. All rights reserved.

  16. Virtual Screening of Acetylcholinesterase Inhibitors Using the Lipinski’s Rule of Five and ZINC Databank

    Directory of Open Access Journals (Sweden)

    Pablo Andrei Nogara

    2015-01-01

    Full Text Available Alzheimer’s disease (AD is a progressive and neurodegenerative pathology that can affect people over 65 years of age. It causes several complications, such as behavioral changes, language deficits, depression, and memory impairments. One of the methods used to treat AD is the increase of acetylcholine (ACh in the brain by using acetylcholinesterase inhibitors (AChEIs. In this study, we used the ZINC databank and the Lipinski’s rule of five to perform a virtual screening and a molecular docking (using Auto Dock Vina 1.1.1 aiming to select possible compounds that have quaternary ammonium atom able to inhibit acetylcholinesterase (AChE activity. The molecules were obtained by screening and further in vitro assays were performed to analyze the most potent inhibitors through the IC50 value and also to describe the interaction models between inhibitors and enzyme by molecular docking. The results showed that compound D inhibited AChE activity from different vertebrate sources and butyrylcholinesterase (BChE from Equus ferus (EfBChE, with IC50 ranging from 1.69 ± 0.46 to 5.64 ± 2.47 µM. Compound D interacted with the peripheral anionic subsite in both enzymes, blocking substrate entrance to the active site. In contrast, compound C had higher specificity as inhibitor of EfBChE. In conclusion, the screening was effective in finding inhibitors of AChE and BuChE from different organisms.

  17. Selective radiolabeling and isolation of the hydrophobic membrane-binding domain of human erythrocyte acetylcholinesterase

    International Nuclear Information System (INIS)

    Roberts, W.L.; Rosenberry, T.L.

    1986-01-01

    The hydrophobic, membrane-binding domain of purified human erythrocyte acetylcholinesterase was labeled with the photoactivated reagent 3-(trifluoromethyl)-3-(m-[ 125 I]iodophenyl)diazirine. The radiolabel was incorporated when the enzyme was prepared in detergent-free aggregates, in detergent micelles, or in phospholipid liposomes, but the highest percentage of labeling occurred in the detergent-free aggregates. Papain digestion of the enzyme released the hydrophobic domain, and polyacrylamide gel electrophoresis in sodium dodecyl sulfate or gel exclusion chromatography demonstrated that the label was localized exclusively in the cleaved hydrophobic domain fragment. This fragment was purified in a three-step procedure. Digestion was conducted with papain attached to Sepharose CL-4B, and the supernatant was adsorbed to acridinium affinity resin to remove the hydrophilic enzyme fragment. The nonretained fragment associated with Triton X-100 micelles was then chromatographed on Sepharose CL-6B, and finally detergent was removed by chromatography on Sephadex LH-60 in an ethanol-formic acid solvent. The fragment exhibited an apparent molecular weight of 3100 on the Sephadex LH-60 column when compared with peptide standards. However, amino acid analysis of the purified fragment revealed only 1 mol each of histidine and glycine per mole of fragment in contrast to the 25-30 mole of amino acids expected on the basis of the molecular weight estimate. This result suggests a novel non-amino acid structure for the hydrophobic domain of human erythrocyte acetylcholinesterase

  18. Identification, cloning and characterization of sis7 and sis10 sugar-insensitive mutants of Arabidopsis

    Directory of Open Access Journals (Sweden)

    Biddle Kelly D

    2008-10-01

    Full Text Available Abstract Background The levels of soluble sugars, such as glucose and sucrose, help regulate many plant metabolic, physiological and developmental processes. Genetic screens are helping identify some of the loci involved in plant sugar response and reveal extensive cross-talk between sugar and phytohormone response pathways. Results A forward genetic screen was performed to identify mutants with increased resistance to the inhibitory effects of high levels of exogenous sugars on early Arabidopsis seedling development. The positional cloning and characterization of two of these sugar insensitive (sis mutants, both of which are also involved in abscisic acid (ABA biosynthesis or response, are reported. Plants carrying mutations in SIS7/NCED3/STO1 or SIS10/ABI3 are resistant to the inhibitory effects of high levels of exogenous Glc and Suc. Quantitative RT-PCR analyses indicate transcriptional upregulation of ABA biosynthesis genes by high concentrations of Glc in wild-type germinating seeds. Gene expression profiling revealed that a significant number of genes that are expressed at lower levels in germinating sis7-1/nced3-4/sto1-4 seeds than in wild-type seeds are implicated in auxin biosynthesis or transport, suggesting cross-talk between ABA and auxin response pathways. The degree of sugar insensitivity of different sis10/abi3 mutant seedlings shows a strong positive correlation with their level of ABA insensitivity during seed germination. Conclusion Mutations in the SIS7/NCED3/STO1 gene, which is primarily required for ABA biosynthesis under drought conditions, confer a sugar-insensitive phenotype, indicating that a constitutive role in ABA biosynthesis is not necessary to confer sugar insensitivity. Findings presented here clearly demonstrate that mutations in ABI3 can confer a sugar-insensitive phenotype and help explain previous, mixed reports on this topic by showing that ABA and sugar insensitivity exhibit a strong positive correlation in

  19. Dynamics of multiple insecticide resistance in the malaria vector Anopheles gambiae in a rice growing area in South-Western Burkina Faso

    Directory of Open Access Journals (Sweden)

    Ouédraogo Jean-Bosco

    2008-09-01

    Full Text Available Abstract Background Insecticide resistance of the main malaria vector, Anopheles gambiae, has been reported in south-western Burkina Faso, West Africa. Cross-resistance to DDT and pyrethroids was conferred by alterations at site of action in the sodium channel, the Leu-Phe kdr mutation; resistance to organophosphates and carbamates resulted from a single point mutation in the oxyanion hole of the acetylcholinesterase enzyme designed as ace-1R. Methods An entomological survey was carried out during the rainy season of 2005 at Vallée du Kou, a rice growing area in south-western Burkina Faso. At the Vallée du Kou, both insecticide resistance mechanisms have been previously described in the M and S molecular forms of An. gambiae. This survey aimed i to update the temporal dynamics and the circumsporozoite infection rate of the two molecular forms M and S of An. gambiae ii to update the frequency of the Leu-Phe kdr mutation within these forms and finally iii to investigate the occurrence of the ace-1R mutation. Mosquitoes collected by indoor residual collection and by human landing catches were counted and morphologically identified. Species and molecular forms of An. gambiae, ace-1R and Leu-Phe kdr mutations were determined using PCR techniques. The presence of the circumsporozoite protein of Plasmodium falciparum was determined using ELISA. Results Anopheles gambiae populations were dominated by the M form. However the S form occurred in relative important proportion towards the end of the rainy season with a maximum peak in October at 51%. Sporozoite rates were similar in both forms. The frequency of the Leu-Phe kdr mutation in the S form reached a fixation level while it is still spreading in the M form. Furthermore, the ace-1R mutation prevailed predominately in the S form and has just started spreading in the M form. The two mutations occurred concomitantly both in M and S populations. Conclusion These results showed that the Vallée du Kou

  20. Tea saponin reduces the damage of Ectropis obliqua to tea crops, and exerts reduced effects on the spiders Ebrechtella tricuspidata and Evarcha albaria compared to chemical insecticides

    Directory of Open Access Journals (Sweden)

    Chi Zeng

    2018-03-01

    Full Text Available Background Tea is one of the most economically important crops in China. However, the tea geometrid (Ectropis obliqua, a serious leaf-feeding pest, causes significant damage to tea crops and reduces tea yield and quality. Spiders are the most dominant predatory enemies in the tea plantation ecosystem, which makes them potentially useful biological control agents of E. obliqua. These highlight the need for alternative pest control measures. Our previous studies have shown that tea saponin (TS exerts insecticidal activity against lepidopteran pests. Here, we investigate whether TS represents a potentially new alternative insecticide with no harm to spiders. Methods We investigated laboratory bioactivities and the field control properties of TS solution against E. obliqua. (i A leaf-dip bioassay was used to evaluate the toxicity of TS to 3rd-instar E. obliqua larvae and effects of TS on the activities of enzymes glutathione-S-transferase (GST, acetylcholinesterase (AChE, carboxylesterase (CES and peroxidase (POD of 3rd-instar E. obliqua larvae in the laboratory. (ii Topical application was used to measure the toxicity of 30% TS (w/v and two chemical insecticides (10% bifenthrin EC and 50% diafenthiuron SC to two species of spider, Ebrechtella tricuspidata and Evarcha albaria. (iii Field trials were used to investigate the controlling efficacy of 30% TS against E. obliqua larvae and to classify the effect of TS to spiders in the tea plantation. Results The toxicity of TS to 3rd-instar E. obliqua larvae occurred in a dose-dependent manner and the LC50 was 164.32 mg/mL. Activities of the detoxifying-related enzymes, GST and POD, increased in 3rd-instar E. obliqua larvae, whereas AChE and CES were inhibited with time by treatment with TS. Mortalities of E. tricuspidata and E. albaria after 48 h with 30% TS treatment (16.67% and 20%, respectively were significantly lower than those with 10% bifenthrin EC (80% and 73.33%, respectively and 50

  1. Enzymes and Inhibitors in Neonicotinoid Insecticide Metabolism

    Science.gov (United States)

    Shi, Xueyan; Dick, Ryan A.; Ford, Kevin A.; Casida, John E.

    2009-01-01

    Neonicotinoid insecticide metabolism involves considerable substrate specificity and regioselectivity of the relevant CYP450, aldehyde oxidase, and phase II enzymes. Human CYP450 recombinant enzymes carry out the following conversions: CYP3A4, 2C19 and 2B6 for thiamethoxam (TMX) to clothianidin (CLO); 3A4, 2C19 and 2A6 for CLO to desmethyl-CLO; 2C19 for TMX to desmethyl-TMX. Human liver aldehyde oxidase reduces the nitro substituent of CLO to nitroso much more rapidly than that of TMX. Imidacloprid (IMI), CLO and several of their metabolites do not give detectable N-glucuronides but 5-hydroxy-IMI, 4,5-diol-IMI and 4-hydroxy-thiacloprid are converted to O-glucuronides in vitro with mouse liver microsomes and UDP-glucuronic acid or in vivo in mice. Mouse liver cytosol with S-adenosylmethionine converts desmethyl-CLO to CLO but not desmethyl-TMX to TMX. Two organophosphorus CYP450 inhibitors partially block IMI, thiacloprid and CLO metabolism in vivo in mice, elevating the brain and liver levels of the parent compounds while reducing amounts of the hydroxylated metabolites. PMID:19391582

  2. Azobenzene Modified Imidacloprid Derivatives as Photoswitchable Insecticides: Steering Molecular Activity in a Controllable Manner

    Science.gov (United States)

    Xu, Zhiping; Shi, Lina; Jiang, Danping; Cheng, Jiagao; Shao, Xusheng; Li, Zhong

    2015-10-01

    Incorporating the photoisomerizable azobenzene into imidacloprid produced a photoswitchable insecticidal molecule as the first neonicotinoid example of remote control insecticide performance with spatiotemporal resolution. The designed photoswitchable insecticides showed distinguishable activity against Musca both in vivo and in vitro upon irradiation. Molecular docking study further suggested the binding difference of the two photoisomers. The generation of these photomediated insecticides provides novel insight into the insecticidal activity facilitating further investigation on the functions of insect nicotinic acetylcholine receptors and opens a novel way to control and study insect behavior on insecticide poisoning using light.

  3. Loss of peroxisomes causes oxygen insensitivity of the histochemical assay of glucose-6-phosphate dehydrogenase activity to detect cancer cells

    NARCIS (Netherlands)

    Frederiks, Wilma M.; Vreeling-Sindelárová, Heleen; van Noorden, Cornelis J. F.

    2007-01-01

    Oxygen insensitivity of carcinoma cells and oxygen sensitivity of non-cancer cells in the histochemical assay of glucose-6-phosphate dehydrogenase (G6PD) enables detection of carcinoma cells in unfixed cell smears or cryostat sections of biopsies. The metabolic background of oxygen insensitivity is

  4. Peripheral site ligand conjugation to a non-quaternary oxime enhances reactivation of nerve agent-inhibited human acetylcholinesterase

    NARCIS (Netherlands)

    Koning, M.C. de; Grol, M. van; Noort, D.

    2011-01-01

    Commonly employed pyridinium-oxime (charged) reactivators of nerve agent inhibited acetylcholinesterase (AChE) do not readily pass the blood brain barrier (BBB) because of the presence of charge(s). Conversely, non-ionic oxime reactivators often suffer from a lack of reactivating potency due to a

  5. High-performance liquid chromatography-mass spectrometry-based acetylcholinesterase assay for the screening of inhibitors in natural extracts

    NARCIS (Netherlands)

    de Jong, C.F.; Derks, R.J.E.; Bruyneel, B.; Niessen, W.M.A.; Irth, H.

    2006-01-01

    The present paper describes a High-performance liquid chromatography-mass spectrometry (LC-MS) methodology for the screening of acetylcholinesterase (AChE) inhibitors in natural extracts. AChE activity of sample components is monitored by a post-column biochemical assay that is based on the

  6. Docking and molecular dynamics studies of peripheral site ligand–oximes as reactivators of sarin-inhibited human acetylcholinesterase

    NARCIS (Netherlands)

    Almeida, J.S.F.D. de; Cuya Guizado, T.R.; Guimarães, A.P.; Ramalho, T.C.; Gonçalves, A.S.; Koning, M.C. de; França, T.C.C.

    2016-01-01

    In the present work, we performed docking and molecular dynamics simulations studies on two groups of long-tailored oximes designed as peripheral site binders of acetylcholinesterase (AChE) and potential penetrators on the blood brain barrier. Our studies permitted to determine how the tails anchor

  7. Design and synthesis of dual inhibitors of acetylcholinesterase and serotonin transporter targeting potential agents for Alzheimer's disease.

    Science.gov (United States)

    Kogen, Hiroshi; Toda, Narihiro; Tago, Keiko; Marumoto, Shinji; Takami, Kazuko; Ori, Mayuko; Yamada, Naho; Koyama, Kazuo; Naruto, Shunji; Abe, Kazumi; Yamazaki, Reina; Hara, Takao; Aoyagi, Atsushi; Abe, Yasuyuki; Kaneko, Tsugio

    2002-10-03

    Highly efficient acetylcholinesterase (AChE) and serotonin transporter (SERT) dual inhibitors, (S)-4 and (R)-13 were designed and synthesized on the basis of the hypothetical model of AChE active site. Both compounds showed potent inhibitory activities against AChE and SERT. [structure: see text

  8. Use of cytectrene marked by the technetium 99 to study the activity of Acetylcholinesterase in the rat brain

    International Nuclear Information System (INIS)

    Mejri, Najoua

    2007-01-01

    Alzheimer's disease is a degenerative neurological disorder that causes progressive and irreversible loss of mental functions. It is the most common form of dementia and is characterized by a decrease in serotonergic neurons that carry the 5HT1A receptors. Derivatives piperidine with a tertiary amine and ester are similar to acetylcholine [natural substrate of acetylcholinesterase)], we used the cytectrene [molecule based piperidine marked the technetium 99m] as a substrate to investigate the activity of Acetylcholinesterase in the brain. The use of cytectrene for the quantitative measurement of the activity of the Acetylcholinesterase in the brain depends on the rate of hydrolysis and the enzymatic specificity. The results showed that the cytectrene can be used as a substrate for a precise and quantitative determination of the activity of this enzyme. The use of cytectrene as a substrate of Acetylcholinesterase and determination of its activity can use this molecule as an agent for early diagnosis of Alzheimer's disease. The results will, therefore, not only their importance on a fundamental level but also on a plan applied in the medical field. (Author)

  9. Inhibitory and enzyme-kinetic investigation of chelerythrine and lupeol isolated from Zanthoxylum rhoifolium against krait snake venom acetylcholinesterase

    Energy Technology Data Exchange (ETDEWEB)

    Ahmad, Mustaq, E-mail: mushtaq213@yahoo.com [University of Science and Technology, Bannu, (Pakistan). Department of Biotechnology; Weber, Andrea D.; Zanon, Graciane; Tavares, Luciana de C.; Ilha, Vinicius; Dalcol, Ionara I.; Morel, Ademir F., E-mail: ademirfariasm@gmail.com [Universidade Federal de Santa Maria, RS (Brazil). Dept. de Quimica

    2014-01-15

    The in vitro activity of chelerythrine and lupeol, two metabolites isolated from Zanthoxylum rhoifolium were studied against the venom of the snake Bungarus sindanus (Elapidae). The venom, which is highly toxic to humans, consists mainly by the enzyme acetylcholinesterase (AChE). Both compounds showed activity against the venom, and the alkaloid chelerythrine presented higher activity than did triterpene lupeol. (author)

  10. Development of a bifunctional sensor using haptenized acetylcholinesterase and application for the detection of cocaine and organophosphates

    NARCIS (Netherlands)

    Teller, Carsten; Halamek, J.; Žeravík, Jiri; Stöcklein, Walter F.M.; Scheller, Frieder W.

    2008-01-01

    We developed a dual piezoelectric/amperometric sensor for the detection of two unrelated analytes in one experiment that uses propidium to anchor acetylcholinesterases (AChE) at the surface. This mass-sensitive sensor does not only allow the examination of the interaction between AChE and the

  11. Insecticides resistance in the Culex quinquefasciatus populations from northern Thailand and possible resistance mechanisms.

    Science.gov (United States)

    Yanola, Jintana; Chamnanya, Saowanee; Lumjuan, Nongkran; Somboon, Pradya

    2015-09-01

    The mosquito vector Culex quinquefasciatus is known to be resistant to insecticides worldwide, including Thailand. This study was the first investigation of the insecticide resistance mechanisms, involving metabolic detoxification and target site insensitivity in C. quinquefasciatus from Thailand. Adult females reared from field-caught larvae from six provinces of northern Thailand were determined for resistant status by exposing to 0.05% deltamethrin, 0.75% permethrin and 5% malathion papers using the standard WHO susceptibility test. The overall mortality rates were 45.8%, 11.4% and 80.2%, respectively. A fragment of voltage-gated sodium channel gene was amplified and sequenced to identify the knock down resistance (kdr) mutation. The ace-1 gene mutation was determined by using PCR-RFLP. The L1014F kdr mutation was observed in all populations, but the homozygous mutant F/F1014 genotype was found only in two of the six provinces where the kdr mutation was significantly correlated with deltamethrin resistance. However, none of mosquitoes had the G119S mutation in the ace-1 gene. A laboratory deltamethrin resistant strain, Cq_CM_R, has been established showing a highly resistant level after selection for a few generations. The mutant F1014 allele frequency was significantly increased after one generation of selection. A synergist assay was performed to assess the metabolic detoxifying enzymes. Addition of bis(4-nitrophenyl)-phosphate (BNPP) and diethyl maleate (DEM), inhibitors of esterases and glutathione S-transferases (GST), respectively, into the larval bioassay of the Cq_CM strain with deltamethrin showed no significant reduction. By contrast, addition of piperonyl butoxide (PBO), an inhibitor of cytochrome P450 monooxygenases, showed a 9-fold reduction of resistance. Resistance to pyrethroids in C. quinquefasciatus is widely distributed in northern Thailand. This study reports for the first time for the detection of the L1014F kdr mutation in wild populations

  12. Plant compounds insecticide activity against Coleoptera pests of stored products

    Energy Technology Data Exchange (ETDEWEB)

    Moreira, Marcio Dionizio; Picanco, Marcelo Coutinho; Guedes, Raul Narciso Carvalho; Campos, Mateus Ribeiro de; Silva, Gerson Adriano; Martins, Julio Claudio [Universidade Federal de Vicosa (UFV), MG (Brazil). Dept. de Biologia Animal]. E-mail: marcio.dionizio@gmail.com; picanco@ufv.br; guedes@ufv.br; mateusc3@yahoo.com.br; agronomiasilva@yahoo.com.br

    2007-07-15

    The objective of this work was to screen plants with insecticide activity, in order to isolate, identify and assess the bioactivity of insecticide compounds present in these plants, against Coleoptera pests of stored products: Oryzaephilus surinamensis L. (Silvanidae), Rhyzopertha dominica F. (Bostrichidae) and Sitophilus zeamais Mots. (Curculionidae). The plant species used were: basil (Ocimum selloi Benth.), rue (Ruta graveolens L.), lion's ear (Leonotis nepetifolia (L.) R.Br.), jimson weed (Datura stramonium L.), baleeira herb (Cordia verbenacea L.), mint (Mentha piperita L.), wild balsam apple (Mormodica charantia L.), and billy goat weed or mentrasto (Ageratum conyzoides L.). The insecticide activity of hexane and ethanol extracts from those plants on R. dominica was evaluated. Among them, only hexane extract of A. conyzoides showed insecticide activity; the hexane extract of this species was successively fractionated by silica gel column chromatography, for isolation and purification of the active compounds. Compounds 5,6,7,8,3',4',5'-heptamethoxyflavone; 5,6,7,8,3'-pentamethoxy-4',5'-methilenedioxyflavone and coumarin were identified. However, only coumarin showed insecticide activity against three insect pests (LD{sub 50} from 2.72 to 39.71 mg g{sup -1} a.i.). The increasing order of insects susceptibility to coumarin was R. dominica, S. zeamais and O. surinamensis. (author)

  13. Insecticide mixtures for mosquito net impregnation against malaria vectors

    Directory of Open Access Journals (Sweden)

    Corbel V.

    2002-09-01

    Full Text Available Insecticides belonging to the pyrethroid family are the only compounds currently available for the treatment of mosquito nets. Unfortunately, some malaria vector species have developed resistance to pyrethroids and the lack of alternative chemical categories is a great concern. One strategy for resistance management would be to treat mosquito nets with a mixture associating two insecticides having different modes of action. This study presents the results obtained with insecticide mixtures containing several proportions of bifenthrin (a pyrethroid insecticide and carbosulfan (a carbamate insecticide. The mixtures were sprayed on mosquito net samples and their efficacy were tested against a susceptible strain of Anopheles gambiae, the major malaria vector in Africa. A significant synergism was observed with a mixture containing 25 mg/m2 of bifenthrin (half the recommended dosage for treated nets and 6.25 mg/m2 of carbosulfan (about 2 % of the recommended dosage. The observed mortality was significantly more than expected in the absence of any interaction (80 % vs 41 % and the knock-down effect was maintained, providing an effective barrier against susceptible mosquitoes.

  14. Mass spectrometric analyses of organophosphate insecticide oxon protein adducts.

    Science.gov (United States)

    Thompson, Charles M; Prins, John M; George, Kathleen M

    2010-01-01

    Organophosphate (OP) insecticides continue to be used to control insect pests. Acute and chronic exposures to OP insecticides have been documented to cause adverse health effects, but few OP-adducted proteins have been correlated with these illnesses at the molecular level. Our aim was to review the literature covering the current state of the art in mass spectrometry (MS) used to identify OP protein biomarkers. We identified general and specific research reports related to OP insecticides, OP toxicity, OP structure, and protein MS by searching PubMed and Chemical Abstracts for articles published before December 2008. A number of OP-based insecticides share common structural elements that result in predictable OP-protein adducts. The resultant OP-protein adducts show an increase in molecular mass that can be identified by MS and correlated with the OP agent. Customized OP-containing probes have also been used to tag and identify protein targets that can be identified by MS. MS is a useful and emerging tool for the identification of proteins that are modified by activated organophosphate insecticides. MS can characterize the structure of the OP adduct and also the specific amino acid residue that forms the key bond with the OP. Each protein that is modified in a unique way by an OP represents a unique molecular biomarker that with further research can lead to new correlations with exposure.

  15. Insecticides promote viral outbreaks by altering herbivore competition.

    Science.gov (United States)

    Pan, Huipeng; Preisser, Evan L; Chu, Dong; Wang, Shaoli; Wu, Qingjun; Carriére, Yves; Zhou, Xuguo; Zhang, Youjun

    2015-09-01

    While the management of biological invasions is often characterized by a series of single-specieg decisions, invasive species exist within larger food webs. These biotic interactions can alter the impact of control/eradication programs and may cause suppression efforts to inadvertently facilitate invasion spread and impact. We document the rapid replacement of the invasive Bemisia Middle East-Asia Minor I (MEAM1) cryptic biotype by the cryptic Mediterranean (MED) biotype throughout China and demonstrate that MED is more tolerant of insecticides and a better vector of tomato yellow leaf curl virus (TYLCV) than MEAMJ. While MEAM1 usually excludes MED under natural conditions, insecticide application reverses the MEAM1-MED competitive hierarchy and allows MED to exclude MEAMI. The insecticide-mediated success of MED has led to TYLCV outbreaks throughout China. Our work strongly supports the hypothesis that insecticide use in China reverses the MEAMl-MED competitive hierarchy and allows MED to displace MEAM1 in managed landscapes. By promoting the dominance of a Bemisia species that is a competent viral vector, insecticides thus increase the spread and impact of TYLCV in heterogeneous agroecosystems.

  16. The global status of insect resistance to neonicotinoid insecticides.

    Science.gov (United States)

    Bass, Chris; Denholm, Ian; Williamson, Martin S; Nauen, Ralf

    2015-06-01

    The first neonicotinoid insecticide, imidacloprid, was launched in 1991. Today this class of insecticides comprises at least seven major compounds with a market share of more than 25% of total global insecticide sales. Neonicotinoid insecticides are highly selective agonists of insect nicotinic acetylcholine receptors and provide farmers with invaluable, highly effective tools against some of the world's most destructive crop pests. These include sucking pests such as aphids, whiteflies, and planthoppers, and also some coleopteran, dipteran and lepidopteran species. Although many insect species are still successfully controlled by neonicotinoids, their popularity has imposed a mounting selection pressure for resistance, and in several species resistance has now reached levels that compromise the efficacy of these insecticides. Research to understand the molecular basis of neonicotinoid resistance has revealed both target-site and metabolic mechanisms conferring resistance. For target-site resistance, field-evolved mutations have only been characterized in two aphid species. Metabolic resistance appears much more common, with the enhanced expression of one or more cytochrome P450s frequently reported in resistant strains. Despite the current scale of resistance, neonicotinoids remain a major component of many pest control programmes, and resistance management strategies, based on mode of action rotation, are of crucial importance in preventing resistance becoming more widespread. In this review we summarize the current status of neonicotinoid resistance, the biochemical and molecular mechanisms involved, and the implications for resistance management. Copyright © 2015 Elsevier Inc. All rights reserved.

  17. Plant compounds insecticide activity against Coleoptera pests of stored products

    Energy Technology Data Exchange (ETDEWEB)

    Moreira, Marcio Dionizio; Picanco, Marcelo Coutinho; Guedes, Raul Narciso Carvalho; Campos, Mateus Ribeiro de; Silva, Gerson Adriano; Martins, Julio Claudio [Universidade Federal de Vicosa (UFV), MG (Brazil). Dept. de Biologia Animal; br, picanco@ufv; br, guedes@ufv; br, mateusc3@yahoo com; br, agronomiasilva@yahoo com

    2007-07-15

    The objective of this work was to screen plants with insecticide activity, in order to isolate, identify and assess the bioactivity of insecticide compounds present in these plants, against Coleoptera pests of stored products: Oryzaephilus surinamensis L. (Silvanidae), Rhyzopertha dominica F. (Bostrichidae) and Sitophilus zeamais Mots. (Curculionidae). The plant species used were: basil (Ocimum selloi Benth.), rue (Ruta graveolens L.), lion's ear (Leonotis nepetifolia (L.) R.Br.), jimson weed (Datura stramonium L.), baleeira herb (Cordia verbenacea L.), mint (Mentha piperita L.), wild balsam apple (Mormodica charantia L.), and billy goat weed or mentrasto (Ageratum conyzoides L.). The insecticide activity of hexane and ethanol extracts from those plants on R. dominica was evaluated. Among them, only hexane extract of A. conyzoides showed insecticide activity; the hexane extract of this species was successively fractionated by silica gel column chromatography, for isolation and purification of the active compounds. Compounds 5,6,7,8,3',4',5'-heptamethoxyflavone; 5,6,7,8,3'-pentamethoxy-4',5'-methilenedioxyflavone and coumarin were identified. However, only coumarin showed insecticide activity against three insect pests (LD{sub 50} from 2.72 to 39.71 mg g{sup -1} a.i.). The increasing order of insects susceptibility to coumarin was R. dominica, S. zeamais and O. surinamensis. (author)

  18. Plant compounds insecticide activity against Coleoptera pests of stored products

    International Nuclear Information System (INIS)

    Moreira, Marcio Dionizio; Picanco, Marcelo Coutinho; Guedes, Raul Narciso Carvalho; Campos, Mateus Ribeiro de; Silva, Gerson Adriano; Martins, Julio Claudio; julioufv@yahoo.com.br

    2007-01-01

    The objective of this work was to screen plants with insecticide activity, in order to isolate, identify and assess the bioactivity of insecticide compounds present in these plants, against Coleoptera pests of stored products: Oryzaephilus surinamensis L. (Silvanidae), Rhyzopertha dominica F. (Bostrichidae) and Sitophilus zeamais Mots. (Curculionidae). The plant species used were: basil (Ocimum selloi Benth.), rue (Ruta graveolens L.), lion's ear (Leonotis nepetifolia (L.) R.Br.), jimson weed (Datura stramonium L.), baleeira herb (Cordia verbenacea L.), mint (Mentha piperita L.), wild balsam apple (Mormodica charantia L.), and billy goat weed or mentrasto (Ageratum conyzoides L.). The insecticide activity of hexane and ethanol extracts from those plants on R. dominica was evaluated. Among them, only hexane extract of A. conyzoides showed insecticide activity; the hexane extract of this species was successively fractionated by silica gel column chromatography, for isolation and purification of the active compounds. Compounds 5,6,7,8,3',4',5'-heptamethoxyflavone; 5,6,7,8,3'-pentamethoxy-4',5'-methilenedioxyflavone and coumarin were identified. However, only coumarin showed insecticide activity against three insect pests (LD 50 from 2.72 to 39.71 mg g -1 a.i.). The increasing order of insects susceptibility to coumarin was R. dominica, S. zeamais and O. surinamensis. (author)

  19. An insecticidal toxin from Nephila clavata spider venom.

    Science.gov (United States)

    Jin, Lin; Fang, Mingqian; Chen, Mengrou; Zhou, Chunling; Ombati, Rose; Hakim, Md Abdul; Mo, Guoxiang; Lai, Ren; Yan, Xiuwen; Wang, Yumin; Yang, Shilong

    2017-07-01

    Spiders are the most successful insect predators given that they use their venom containing insecticidal peptides as biochemical weapons for preying. Due to the high specificity and potency of peptidic toxins, discoveries of insecticidal toxins from spider venom have provided an opportunity to obtain natural compounds for agricultural applications without affecting human health. In this study, a novel insecticidal toxin (μ-NPTX-Nc1a) was identified and characterized from the venom of Nephila clavata. Its primary sequence is GCNPDCTGIQCGWPRCPGGQNPVMDKCVSCCPFCPPKSAQG which was determined by automated Edman degradation, cDNA cloning, and MS/MS analysis. BLAST search indicated that Nc1a shows no similarity with known peptides or proteins, indicating that Nc1a belongs to a novel family of insecticidal peptide. Nc1a displayed inhibitory effects on Na V and K V channels in cockroach dorsal unpaired median neurons. The median lethal dose (LD50) of Nc1a on cockroach was 573 ng/g. Herein, a study that identifies a novel insecticidal toxin, which can be a potential candidate and/or template for the development of bioinsecticides, is presented.

  20. Antidotal effects of varthemia persica DC extract in organophosphate poisoning or warfare agents by measuring whole blood acetylcholinesterase

    International Nuclear Information System (INIS)

    Kalantari, H.; Siahapoosh, A.; Farsani, K. M.

    2009-01-01

    The organophosphates (ORPs) or war fare agents toxicity results from inhibition of acetylcholinesterase (AchE). phosphylation of the active serin of AchE leads to accumulation of acetylcholine in synaptic clefts leading to generalized cholinergic over-stimulation. Standard treatment of ORP poisoning includes a muscarinic antagonist such as Atropine, and acetylcholinesterase reactivator (oxime). Presently, oximes like abidoxime and pralidoxime are approved as antidotes against ORP poisoning but are considered to be rather ineffective against certain ORP. Like Soman. In this study, the protective effect of Varthemia persica DC extract on acetylcholinesterase was examined in rats. Animals in weight range of 200-225 g were divided in 8 groups. The negative control group received only 0.4 ml normal saline, reference group, received ethylparaoxone in dose of 50 percent of LD50, positive control group, received ethylparaoxone (50% LD50) and one minute later 50 mol of pralidoxime. Test group 1: received ethylparaoxone and one minute later single dose of methanolic extract of Varthemia persica (250 mg/kg), Test Group 2: daily received methanolic extract of V.persica (250 mg/kg) in six days and one minute after last dose of extract, ethylparaoxone (50% LD50) were injected, Test Group 3: received ethylparaoxone (50% LD50) and then six doses of methanolic extract of V.persica (250 mg/kg) in six continuous days. Test Group 4: received ethylparaoxone and then single dose of dichloromethane extract of V.persica (250 mg/kg). Test Group 5: received ethylparaoxone and one minute later single high dose of methanolic extract of V.persica (1000 mg/kg). Then blood withdrawn and acetylcholinesterase activity was measured according to modified Ellman's method. Only in groups which received extract of V. persica before and after injection of ethylparaoxone, the mean of acetylcholinesterase activity was significantly different with reference group (p 0.05) but no significant difference with

  1. Influence on sensitivity to insecticides: a case study of a settled area ...

    African Journals Online (AJOL)

    monitoring for successful alternative insecticides. There are currently two ... behaviour or modification avoid landing on insecticide .... aquarium fish food18. When they .... National Statistical Office (NSO) Malawi Government 1998 Census. 16.

  2. Mechanistic modeling of insecticide risks to breeding birds in North American agroecosystems

    Science.gov (United States)

    Insecticide usage in the United States is ubiquitous in urban, suburban, and rural environments. In evaluating data for an insecticide registration application and for registration review, scientists at the United States Environmental Protection Agency (USEPA) assess the fate of ...

  3. Influence of Pyrethroid Insecticides on Sodium and Calcium Influx in Neocortical Neurons

    Science.gov (United States)

    Pyrethroid insecticides bind to voltage-gated sodium channels and modify their gating kinetics, thereby disrupting neuronal function. Using murine neocortical neurons in primary culture, we have compared the ability of 11 structurally diverse pyrethroid insecticides to evoke Na+ ...

  4. Elicitation of dopaminergic features of Parkinson's disease in C. elegans by monocrotophos, an organophosphorous insecticide.

    Science.gov (United States)

    Ali, Shaheen Jafri; Rajini, Padmanabhan Sharda

    2012-12-01

    Positive correlations have been suggested between usage of pesticides and the incidence of Parkinson's disease (PD) through epidemiological as well as few experimental evidences. Organophosphorus insecticides (OPI), which are extensively used in agricultural and household insect control, have been the subject of increasing concern in the past decades due to their neurotoxic potential. However, very few studies have demonstrated the potentials of OPI to induce features of PD in model organisms. In the present study, Caenorhabditis elegans was selected as the model organism to evaluate the potential of monocrotophos (MCP), an OPI, to elicit dopaminergic features of Parkinson's disease in terms of dopamine content, basic movement and integrity of dopaminergic neurons along with its effect on acetylcholinesterase (AChE) activity and life span. All the responses elicited by MCP were compared with that elicited by 1-methyl-4-phenyl- 1, 2, 3, 6-tetrahydropyridine (MPTP) in both N2 and BZ555 worms. N2 worms were exposed to varying concentrations of MCP (50, 100 and 200 μM) or MPTP (200, 300 and 400 μM) for 48 hours and locomotory rate, as measured by the number of body bends made in 20 seconds, was enumerated. Worms subjected to the same dose paradigms were also analyzed for the dopamine content by HPLC. The results indicated a significant reduction in the dopamine levels in the worms that were treated with MCP/MPTP and this correlated with the changes in locomotion compared to untreated worms. Worms treated with MCP also exhibited significant reduction in AChE activity. Both MPTP and MCP caused a marked reduction in life span in the worms. Transgenic worms (BZ555, which has GFP tagged to its 8 dopaminergic neurons) exposed to MCP and MPTP at the above concentrations showed a dose-dependent reduction in the number of green pixels in CEP and ADE neurons which also correlated with the neurodegeneration as visualized by decreased fluorescence in photomicrographs. Taken

  5. Efficacy of an insecticide paint against insecticide-susceptible and resistant mosquitoes - Part 1: Laboratory evaluation

    Directory of Open Access Journals (Sweden)

    Carnevale Pierre

    2010-11-01

    Full Text Available Abstract Background The main malaria vector Anopheles gambiae and the urban pest nuisance Culex quinquefasciatus are increasingly resistant to pyrethroids in many African countries. There is a need for new products and strategies. Insecticide paint Inesfly 5A IGR™, containing two organophosphates (OPs, chlorpyrifos and diazinon, and insect growth regulator (IGR, pyriproxyfen, was tested under laboratory conditions for 12 months following WHOPES Phase I procedures. Methods Mosquitoes used were laboratory strains of Cx. quinquefasciatus susceptible and resistant to OPs. The paint was applied at two different doses (1 kg/6 m2 and 1 kg/12 m2 on different commonly used surfaces: porous (cement and stucco and non-porous (softwood and hard plastic. Insecticide efficacy was studied in terms of delayed mortality using 30-minute WHO bioassay cones. IGR efficacy on fecundity, fertility and larval development was studied on OP-resistant females exposed for 30 minutes to cement treated and control surfaces. Results After treatment, delayed mortality was high (87-100% even against OP-resistant females on all surfaces except cement treated at 1 kg/12 m2. Remarkably, one year after treatment delayed mortality was 93-100% against OP-resistant females on non-porous surfaces at both doses. On cement, death rates were low 12 months after treatment regardless of the dose and the resistance status. Fecundity, fertility and adult emergence were reduced after treatment even at the lower dose (p -3. A reduction in fecundity was still observed nine months after treatment at both doses (p -3 and adult emergence was reduced at the higher dose (p -3. Conclusions High mortality rates were observed against laboratory strains of the pest mosquito Cx. quinquefasciatus susceptible and resistant to insecticides. Long-term killing remained equally important on non-porous surfaces regardless the resistance status for over 12 months. The paint's effect on fecundity, fertility and

  6. Contemporary evolution of resistance at the major insecticide target site gene Ace-1 by mutation and copy number variation in the malaria mosquito Anopheles gambiae

    Science.gov (United States)

    Weetman, David; Mitchell, Sara N; Wilding, Craig S; Birks, Daniel P; Yawson, Alexander E; Essandoh, John; Mawejje, Henry D; Djogbenou, Luc S; Steen, Keith; Rippon, Emily J; Clarkson, Christopher S; Field, Stuart G; Rigden, Daniel J; Donnelly, Martin J

    2015-01-01

    Functionally constrained genes are ideal insecticide targets because disruption is often fatal, and resistance mutations are typically costly. Synaptic acetylcholinesterase (AChE) is an essential neurotransmission enzyme targeted by insecticides used increasingly in malaria control. In Anopheles and Culex mosquitoes, a glycine–serine substitution at codon 119 of the Ace-1 gene confers both resistance and fitness costs, especially for 119S/S homozygotes. G119S in Anopheles gambiae from Accra (Ghana) is strongly associated with resistance, and, despite expectations of cost, resistant 119S alleles are increasing significantly in frequency. Sequencing of Accra females detected only a single Ace-1 119S haplotype, whereas 119G diversity was high overall but very low at non-synonymous sites, evidence of strong purifying selection driven by functional constraint. Flanking microsatellites showed reduced diversity, elevated linkage disequilibrium and high differentiation of 119S, relative to 119G homozygotes across up to two megabases of the genome. Yet these signals of selection were inconsistent and sometimes weak tens of kilobases from Ace-1. This unexpected finding is attributable to apparently ubiquitous amplification of 119S alleles as part of a large copy number variant (CNV) far exceeding the size of the Ace-1 gene, whereas 119G alleles were unduplicated. Ace-1 CNV was detectable in archived samples collected when the 119S allele was rare in Ghana. Multicopy amplification of resistant alleles has not been observed previously and is likely to underpin the recent increase in 119S frequency. The large CNV compromised localization of the strong selective sweep around Ace-1, emphasizing the need to integrate CNV analysis into genome scans for selection. PMID:25865270

  7. Contemporary evolution of resistance at the major insecticide target site gene Ace-1 by mutation and copy number variation in the malaria mosquito Anopheles gambiae.

    Science.gov (United States)

    Weetman, David; Mitchell, Sara N; Wilding, Craig S; Birks, Daniel P; Yawson, Alexander E; Essandoh, John; Mawejje, Henry D; Djogbenou, Luc S; Steen, Keith; Rippon, Emily J; Clarkson, Christopher S; Field, Stuart G; Rigden, Daniel J; Donnelly, Martin J

    2015-06-01

    Functionally constrained genes are ideal insecticide targets because disruption is often fatal, and resistance mutations are typically costly. Synaptic acetylcholinesterase (AChE) is an essential neurotransmission enzyme targeted by insecticides used increasingly in malaria control. In Anopheles and Culex mosquitoes, a glycine-serine substitution at codon 119 of the Ace-1 gene confers both resistance and fitness costs, especially for 119S/S homozygotes. G119S in Anopheles gambiae from Accra (Ghana) is strongly associated with resistance, and, despite expectations of cost, resistant 119S alleles are increasing significantly in frequency. Sequencing of Accra females detected only a single Ace-1 119S haplotype, whereas 119G diversity was high overall but very low at non-synonymous sites, evidence of strong purifying selection driven by functional constraint. Flanking microsatellites showed reduced diversity, elevated linkage disequilibrium and high differentiation of 119S, relative to 119G homozygotes across up to two megabases of the genome. Yet these signals of selection were inconsistent and sometimes weak tens of kilobases from Ace-1. This unexpected finding is attributable to apparently ubiquitous amplification of 119S alleles as part of a large copy number variant (CNV) far exceeding the size of the Ace-1 gene, whereas 119G alleles were unduplicated. Ace-1 CNV was detectable in archived samples collected when the 119S allele was rare in Ghana. Multicopy amplification of resistant alleles has not been observed previously and is likely to underpin the recent increase in 119S frequency. The large CNV compromised localization of the strong selective sweep around Ace-1, emphasizing the need to integrate CNV analysis into genome scans for selection. © 2015 The Authors. Molecular Ecology published by John Wiley & Sons Ltd.

  8. Insecticide Usage and Chemical Contamination Assessment in Asiatic Pennywort

    Science.gov (United States)

    Bumroongsook, S.

    2017-07-01

    The insecticide usage in commercially grown asiatic pennywort plantations in Nakhonpatum and Nonthaburi province, Thailand was surveyed during January-June, 2016. The results showed that asiatic pennywort cuttworms was leaf destructive and caused the most damge to the production. The growers used organophosphate insecticides to control the caterpillars the most, followed by pyrethoid, abamectin, carbamate and organochlorine, respectively. The chemical contaminants of pennywort from 9 fresh markets in Bangkok was monitored, the result indicated that lead was not detected in the samples. The amount of arsenic was less than 0.075 mg / kg. The insecticide residue measurement of dicofol, chlorpyrifos and methidathion was 0.98, 2.84 and 0.46 mg / kg, respectively.

  9. POTENTIATION OF COPAÍBA OIL-RESIN WITH SYNTHETIC INSECTICIDES TO CONTROL OF FALL ARMYWORM

    OpenAIRE

    ALMEIDA, WALDIANE ARAÚJO DE; SILVA, IGOR HONORATO LEDUÍNO DA; SANTOS, ANA CLÁUDIA VIEIRA DOS; BARROS JÚNIOR, AURÉLIO PAES; SOUSA, ADALBERTO HIPÓLITO DE

    2017-01-01

    ABSTRACT The control of Spodoptera frugiperda (J. E. SMITH) (Lepidoptera: Noctuidae) has been carried out mainly with pyrethroids and organophosphates insecticides. The continuous and indiscriminate use of synthetic insecticides, for decades, has led to the selection of resistant populations and has caused concerns for human health and the environment. An alternative is the use of botanical insecticides, including through the mixtures with synthetic insecticides. This study aimed to investiga...

  10. Tolerance of photoperiod insensitive mutant of Sesbania rostrata to salinity and pH

    International Nuclear Information System (INIS)

    Ramani, Saradha; Joshua, D.C.; Shaikh, M.S.; Athalye, V.V.

    1998-01-01

    The photoperiod insensitive mutant, TSR-1 of Sesbania rostrata was compared with the parent variety for its response to soil salinity and different levels of pH in hydroponics. The plant growth and stem nodulation were not significantly affected by salinity. However, salinity in soil without farmyard manure stimulated plant growth. Radiotracer studies showed that the translocation of Na to stem and leaves was much less compared to uptake in both parent and mutant. The growth of TSR-1 was comparable to or marginally better than that of the parent variety in the pH range of 3.5-8.0. Root nodulation was less with low pH. The nitrogen content was not adversely affected by pH, but it was reduced with 200 mM NaCl. This mutant in addition to being short-day insensitive, is tolerant to low to moderate salinity levels and pH like its parent. (author)

  11. Optimal Design of an Achromatic Angle-Insensitive Phase Retarder Used in MWIR Imaging Polarimetry

    International Nuclear Information System (INIS)

    Guo-Guo, Kang; Qiao-Feng, Tan; Guo-Fan, Jin

    2009-01-01

    Dielectric gratings with period in the range from λ/10 to λ/4 with λ being the illumination wavelength not only exclude higher order diffractions but also exhibit strong dispersion of effective indices which are proportional to the wavelength. Moreover, they are insensitive to the incident angle of the illumination wave. With these features, we can design a true zero-order achromatic and angle-insensitive phase retarder which can be used as the polarization state analyzer in middle wave infrared (MWIR) imaging polarimetry. A design method using effective medium theory is described, and the performance of the designed phase retarder is evaluated by rigorous coupled wave analysis theory. The calculation results demonstrate that the retardance deviates from 45° by < ±1.6° within a field of view ±10° over the MWIR bandwidth (3–5 μm). (fundamental areas of phenomenology (including applications))

  12. Broadband temperature-insensitivity of dispersion-engineered waveguides and resonators

    Science.gov (United States)

    Xu, Lijuan; He, Liuqing; Guo, Yuhao; Li, Guifang; Zhang, Lin

    2018-02-01

    Photonic circuits suffer from thermal drift of device performance, which is a key obstacle to the development of commercial optoelectronic products. Temperature-insensitive integrated waveguides and resonators have been demonstrated by using materials with a negative TOC at a single wavelength, which are not suitable for WDM devices and wideband nonlinear devices. Here, we propose a waveguide structure with temperature-insensitivity over a bandwidth of 780 nm (1280 to 2060 nm) with an ultra-small effective TOC within +/-1×10-6/K. Uniquely, the waveguide has small anomalous dispersion (from 66 to 329 ps/nm/km) over the same band and is suitable for frequency comb generation without being affected by intra-cavity thermal dynamics.

  13. A natural frameshift mutation in Campanula EIL2 correlates with ethylene insensitivity in flowers

    DEFF Research Database (Denmark)

    Jensen, Line; Hegelund, Josefine Nymark; Olsen, Andreas

    2016-01-01

    BACKGROUND: The phytohormone ethylene plays a central role in development and senescence of climacteric flowers. In ornamental plant production, ethylene sensitive plants are usually protected against negative effects of ethylene by application of chemical inhibitors. In Campanula, flowers...... are sensitive to even minute concentrations of ethylene. RESULTS: Monitoring flower longevity in three Campanula species revealed C. portenschlagiana (Cp) as ethylene sensitive, C. formanekiana (Cf) with intermediate sensitivity and C. medium (Cm) as ethylene insensitive. We identified key elements in ethylene...... signal transduction, specifically in Ethylene Response Sensor 2 (ERS2), Constitutive Triple Response 1 (CTR1) and Ethylene Insensitive 3- Like 1 and 2 (EIL1 and EIL2) homologous. Transcripts of ERS2, CTR1 and EIL1 were constitutively expressed in all species both throughout flower development...

  14. Polarization-insensitive quantum-dot coupled quantum-well semiconductor optical amplifier

    International Nuclear Information System (INIS)

    Huang Lirong; Yu Yi; Tian Peng; Huang Dexiu

    2009-01-01

    The optical gain of a quantum-dot semiconductor optical amplifier is usually seriously dependent on polarization; we propose a quantum-dot coupled tensile-strained quantum-well structure to obtain polarization insensitivity. The tensile-strained quantum well not only serves as a carrier injection layer of quantum dots but also offers gain to the transverse-magnetic mode. Based on the polarization-dependent coupled carrier rate-equation model, we study carrier competition among quantum well and quantum dots, and study the polarization dependence of the quantum-dot coupled quantum-well semiconductor optical amplifier. We also analyze polarization-dependent photon-mediated carrier distribution among quantum well and quantum dots. It is shown that polarization-insensitive gain can be realized by optimal design

  15. The molecular basis of acid insensitivity in the African naked mole-rat.

    Science.gov (United States)

    Smith, Ewan St John; Omerbašić, Damir; Lechner, Stefan G; Anirudhan, Gireesh; Lapatsina, Liudmila; Lewin, Gary R

    2011-12-16

    Acid evokes pain by exciting nociceptors; the acid sensors are proton-gated ion channels that depolarize neurons. The naked mole-rat (Heterocephalus glaber) is exceptional in its acid insensitivity, but acid sensors (acid-sensing ion channels and the transient receptor potential vanilloid-1 ion channel) in naked mole-rat nociceptors are similar to those in other vertebrates. Acid inhibition of voltage-gated sodium currents is more profound in naked mole-rat nociceptors than in mouse nociceptors, however, which effectively prevents acid-induced action potential initiation. We describe a species-specific variant of the nociceptor sodium channel Na(V)1.7, which is potently blocked by protons and can account for acid insensitivity in this species. Thus, evolutionary pressure has selected for an Na(V)1.7 gene variant that tips the balance from proton-induced excitation to inhibition of action potential initiation to abolish acid nociception.

  16. Wafer defect detection by a polarization-insensitive external differential interference contrast module.

    Science.gov (United States)

    Nativ, Amit; Feldman, Haim; Shaked, Natan T

    2018-05-01

    We present a system that is based on a new external, polarization-insensitive differential interference contrast (DIC) module specifically adapted for detecting defects in semiconductor wafers. We obtained defect signal enhancement relative to the surrounding wafer pattern when compared with bright-field imaging. The new DIC module proposed is based on a shearing interferometer that connects externally at the output port of an optical microscope and enables imaging thin samples, such as wafer defects. This module does not require polarization optics (such as Wollaston or Nomarski prisms) and is insensitive to polarization, unlike traditional DIC techniques. In addition, it provides full control of the DIC shear and orientation, which allows obtaining a differential phase image directly on the camera (with no further digital processing) while enhancing defect detection capabilities, even if the size of the defect is smaller than the resolution limit. Our technique has the potential of future integration into semiconductor production lines.

  17. Polarization insensitive metamaterial absorber based on E-shaped all-dielectric structure

    Directory of Open Access Journals (Sweden)

    Liyang Li

    2015-03-01

    Full Text Available In this paper, we designed a metamaterial absorber performed in microwave frequency band. This absorber is composed of E-shaped dielectrics which are arranged along different directions. The E-shaped all-dielectric structure is made of microwave ceramics with high permittivity and low loss. Within about 1 GHz frequency band, more than 86% absorption efficiency was observed for this metamaterial absorber. This absorber is polarization insensitive and is stable for incident angles. It is figured out that the polarization insensitive absorption is caused by the nearly located varied resonant modes which are excited by the E-shaped all-dielectric resonators with the same size but in the different direction. The E-shaped dielectric absorber contains intensive resonant points. Our research work paves a way for designing all-dielectric absorber.

  18. Dye and pigment-free structural colors and angle-insensitive spectrum filters

    Energy Technology Data Exchange (ETDEWEB)

    Guo, Lingjie Jay; Hollowell, Andrew E.; Wu, Yi-Kuei

    2017-01-17

    Optical spectrum filtering devices displaying minimal angle dependence or angle insensitivity are provided. The filter comprises a localized plasmonic nanoresonator assembly having a metal material layer defining at least one nanogroove and a dielectric material disposed adjacent to the metal material layer. The dielectric material is disposed within the nanogroove(s). The localized plasmonic nanoresonator assembly is configured to funnel and absorb a portion of an electromagnetic spectrum in the at least one nanogroove via localized plasmonic resonance to generate a filtered output having a predetermined range of wavelengths that displays angle insensitivity. Thus, flexible, high efficiency angle independent color filters having very small diffraction limits are provided that are particularly suitable for use as pixels for various display devices or for use in anti-counterfeiting and cryptography applications. The structures can also be used for colored print applications and the elements can be rendered as pigment-like particles.

  19. Polarization Insensitivity in Double-Split Ring and Triple-Split Ring Terahertz Resonators

    International Nuclear Information System (INIS)

    Wu Qian-Nan; Lan Feng; Tang Xiao-Pin; Yang Zi-Qiang

    2015-01-01

    A modified double-split ring resonator and a modified triple-split ring resonator, which offer polarization-insensitive performance, are investigated, designed and fabricated. By displacing the two gaps of the conventional double-split ring resonator away from the center, the second resonant frequency for the 0° polarized wave and the resonant frequency for the 90° polarized wave become increasingly close to each other until they are finally identical. Theoretical and experimental results show that the modified double-split ring resonator and the modified triple-split ring resonator are insensitive to different polarized waves and show strong resonant frequency dips near 433 and 444 GHz, respectively. The results of this work suggest new opportunities for the investigation and design of polarization-dependent terahertz devices based on split ring resonators. (paper)

  20. Observing Local Realism Violations with a Combination of Sensitive and Insensitive Detectors

    International Nuclear Information System (INIS)

    Yurke, B.; Stoler, D.

    1997-01-01

    Several systems are exhibited in which the establishment of local realism violation is achieved even when some of the detectors employed are insensitive. The insensitive detectors are homodyne detectors whose task is to determine if the amplitude of a coherent state is α or -α . This determination can be achieved with low quantum efficiency detectors when |α| is large. The other detectors employed determine whether there is an even number or an odd number of photons in a state. These detectors are sensitive since they are required to resolve the difference of one photon. For the examples given, the local realism violation is not diminished as |α| is increased. copyright 1997 The American Physical Society

  1. Optimal Cotton Insecticide Application Termination Timing: A Meta-Analysis.

    Science.gov (United States)

    Griffin, T W; Zapata, S D

    2016-08-01

    The concept of insecticide termination timing is generally accepted among cotton (Gossypium hirsutum) researchers; however, exact timings are often disputed. Specifically, there is uncertainty regarding the last economic insecticide application to control fruit-feeding pests including tarnished plant bug (Lygus lineolaris (Palisot de Beauvois)), boll weevil (Anthonomus grandis), bollworm (Helicoverpa zea), tobacco budworm (Heliothis virescens), and cotton fleahopper (Pseudatomoscelis seriatus). A systematic review of prior studies was conducted within a meta-analytic framework. Nine publicly available articles were amalgamated to develop an optimal timing principle. These prior studies reported 53 independent multiple means comparison field experiments for a total of 247 trial observations. Stochastic plateau theory integrated with econometric meta-analysis methodology was applied to the meta-database to determine the shape of the functional form of both the agronomic optimal insecticide termination timing and corresponding yield potential. Results indicated that current university insecticide termination timing recommendations are later than overall estimated timing suggested. The estimated 159 heat units (HU) after the fifth position above white flower (NAWF5) was found to be statistically different than the 194 HU termination used as the status quo recommended termination timing. Insecticides applied after 159 HU may have been applied in excess, resulting in unnecessary economic and environmental costs. Empirical results also suggested that extending the insecticide termination time by one unit resulted in a cotton lint yield increase of 0.27 kilograms per hectare up to the timing where the plateau began. Based on economic analyses, profit-maximizing producers may cease application as soon as 124 HU after NAWF5. These results provided insights useful to improve production systems by applying inputs only when benefits were expected to be in excess of the

  2. Insecticide resistance in vector Chagas disease: evolution, mechanisms and management.

    Science.gov (United States)

    Mougabure-Cueto, Gastón; Picollo, María Inés

    2015-09-01

    Chagas disease is a chronic parasitic infection restricted to America. The disease is caused by the protozoa Trypanosoma cruzi, which is transmitted to human through the feces of infected triatomine insects. Because no treatment is available for the chronic forms of the disease, vector chemical control represents the best way to reduce the incidence of the disease. Chemical control has been based principally on spraying dwellings with insecticide formulations and led to the reduction of triatomine distribution and consequent interruption of disease transmission in several areas from endemic region. However, in the last decade it has been repeatedly reported the presence triatomnes, mainly Triatoma infestans, after spraying with pyrethroid insecticides, which was associated to evolution to insecticide resistance. In this paper the evolution of insecticide resistance in triatomines is reviewed. The insecticide resistance was detected in 1970s in Rhodnius prolixus and 1990s in R. prolixus and T. infestans, but not until the 2000s resistance to pyrthroids in T. infestans associated to control failures was described in Argentina and Bolivia. The main resistance mechanisms (i.e. enhanced metabolism, altered site of action and reduced penetration) were described in the T. infestans resistant to pyrethrods. Different resistant profiles were demonstrated suggesting independent origin of the different resistant foci of Argentina and Bolivia. The deltamethrin resistance in T. infestans was showed to be controlled by semi-dominant, autosomally inherited factors. Reproductive and developmental costs were also demonstrated for the resistant T. infestans. A discussion about resistance and tolerance concepts and the persistence of T. infestans in Gran Chaco region are presented. In addition, theoretical concepts related to toxicological, evolutionary and ecological aspects of insecticide resistance are discussed in order to understand the particular scenario of pyrethroid

  3. Improving the knowledge on Piper betle: targeted metabolite analysis and effect on acetylcholinesterase.

    Science.gov (United States)

    Valentão, Patrícia; Gonçalves, Rui F; Belo, Cristóvão; de Pinho, Paula Guedes; Andrade, Paula B; Ferreres, Federico

    2010-10-01

    Piper betle is a species growing in South East Asia, where its leaves are economically and medicinally important. To screen the highest possible number of volatile and semivolatile components, the leaves were subjected to headspace solid-phase microextraction, hydrodistillation and Soxhlet extraction, prior to analysis by GC/MS. Fifty compounds (identified by comparison with standard compounds or tentatively by National Institute of Standards and Technology database) were determined, 23 being described for the first time in this matrix. An aqueous extract was also analysed, in which only seven compounds were characterized. The organic acids' composition of this extract was determined by HPLC/UV and eight compounds are reported for the first time in P. betle. This extract also displayed acetylcholinesterase inhibitory capacity.

  4. Synthesis, Biological Evaluation and Molecular Modelling of 2′-Hydroxychalcones as Acetylcholinesterase Inhibitors

    Directory of Open Access Journals (Sweden)

    Sri Devi Sukumaran

    2016-07-01

    Full Text Available A series of 2′-hydroxy- and 2′-hydroxy-4′,6′-dimethoxychalcones was synthesised and evaluated as inhibitors of human acetylcholinesterase (AChE. The majority of the compounds were found to show some activity, with the most active compounds having IC50 values of 40–85 µM. Higher activities were generally observed for compounds with methoxy substituents in the A ring and halogen substituents in the B ring. Kinetic studies on the most active compounds showed that they act as mixed-type inhibitors, in agreement with the results of molecular modelling studies, which suggested that they interact with residues in the peripheral anionic site and the gorge region of AChE.

  5. Effect of viologen-phosphorus dendrimers on acetylcholinesterase and butyrylcholinesterase activities.

    Science.gov (United States)

    Ciepluch, Karol; Weber, Monika; Katir, Nadia; Caminade, Anne-Marie; El Kadib, Abdelkrim; Klajnert, Barbara; Majoral, Jean Pierre; Bryszewska, Maria

    2013-03-01

    The inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) is the first step in checking whether new compounds can be considered as drugs for treating neurodegenerative diseases. The effect of viologen-phosphorus dendrimers on AChE and BChE activities was studied. The results show that the effects on the cholinesterase activities depend on dendrimer type and size. Viologen dendrimers can interact with the enzymes in two ways: they can bind either to a peripheral site of the enzyme or to amino acids located near the active site, inhibiting catalysis by both cholinesterases. All tested non-toxic viologen-phosphorus dendrimers inhibited the activities of both cholinesterases, showing their potential as new drugs for treating neurodegenerative diseases. Copyright © 2012 Elsevier B.V. All rights reserved.

  6. Molecular interaction of acetylcholinesterase with carnosic acid derivatives: a neuroinformatics study.

    Science.gov (United States)

    Merad, M; Soufi, W; Ghalem, S; Boukli, F; Baig, M H; Ahmad, K; Kamal, Mohammad A

    2014-04-01

    Alzheimer's disease is a progressive degenerative disease of the brain marked by gradual and irreversible declines in cognitive functions. Acetylcholinesterase (AChE) plays a biological role in the termination of nerve impulse transmissions at cholinergic synapses by rapid hydrolysis of its substrate, "acetylcholine". The deficit level of acetylcholine leads to deprived nerve impulse transmission. Thus the cholinesterase inhibitors would reverse the deficit in acetylcholine level and consequently may reverse the memory impairments, which is characteristic of the Alzheimer's disease. The molecular interactions between AChE and Carnosic acid, a well known antioxidant substance found in the leaves of the rosemary plant has always been an area of interest. Here in this study we have performed in silico approach to identify carnosic acid derivatives having the potential of being a possible drug candidate against AChE. The best candidates were selected on the basis of the results of different scoring functions.

  7. Dementia post-radiotherapy: improvement with acetylcholinesterase inhibitor A case report

    Directory of Open Access Journals (Sweden)

    Antonio Eduardo Damin

    Full Text Available Abstract Cognitive decline associated with radiotherapy is a progressive complication that affects many patients submitted to this form of treatment. The lack of an effective treatment drives research for new treatment options to improve the quality of life of patients with this disorder. We report the case of a 64 year-old man who developed a severe dementia of the frontal subcortical type, which was associated with subcortical frontal lesions and appeared as a late complication of radiotherapy used to treat a pituitary tumor. After many pharmacological attempts to improve his cognitive and behavioral problems, the patient showed a significant improvement in the cognitive, functional and behavioral impairments after treatment with an acetylcholinesterase inhibitor. This report discusses hypotheses for the positive effect of this treatment.

  8. A radiotracer for In vivo studies of acetylcholinesterase: p-[{sup 18}F]fluorodonepezil

    Energy Technology Data Exchange (ETDEWEB)

    Lee, S. Y.; Choi, Y. S.; Choi, Y.; Kim, S. E.; Lee, K. H.; Kim, B. T. [Samsung Medical Center, Seoul (Korea, Republic of); Lee, J. W. [Seoul National Univ., Seoul (Korea, Republic of)

    1999-05-01

    Alzheimer's disease (AD) is one of senile dementia caused by lack of acetylcholine in central nervous system, and in vivo studies of acetylcholinesterase (AChE) have been carried out using many radiolabeled AChE inhibitors (donepezil, tacrine, physostigmine, CP-126,998, etc). Donepezil, a FDA approved drug for AD is now in clinical use. Therefore, we synthesized and evaluated p-[{sup 18}F]fluorodonepezil in mice. Biodistribution studies demonstrated that p-[{sup 18}F]fluorodonepezil binds non-specifically in vivo and does not suffer from metabolism in mouse brain. This study suggests that radioligands with higher binding affinity may be required to visualize AChE in vivo and further studies are needed to develop better radiotracers.

  9. Effects of endosulfan on brain acetylcholinesterase activity in juvenile bluegill sunfish

    International Nuclear Information System (INIS)

    Dutta, Hiran M.; Arends, Dane A.

    2003-01-01

    The effects of endosulfan upon brain acetylcholinesterase (AChE) activity were measured in juvenile blue gill sunfish (Lepomis macrochirus). Based on exposure durations of 0, 24, 48, 72, and 96 h and 1 week at 1.0 μg/L (just below the LC50 of 1.2 μg/L for this species), step-wise decreases in AChE activity were noted, corresponding to 0%, 3.57%, 12.65%, 14.23%, 16.31%, and 3.11% inhibition, respectively. Total brain protein concentrations were measured to test the accuracy of the Ache data with no significant anomalies. The duration of exposure was related to the reduction in the AChE activities which reflected the biotoxicity of endosulfan. The changes in the AChE activities will certainly affect the normal behavior of the juvenile blue gill which is detrimental to their very existence in the natural habitat

  10. Detection of Carbofuran with Immobilized Acetylcholinesterase Based on Carbon Nano tubes-Chitosan Modified Electrode

    International Nuclear Information System (INIS)

    Zhang, Sh.; Li, Sh.; Ma, J.; Xiong, F.; Qu, S.; Zhang, Sh.; Li, Sh.

    2013-01-01

    A sensitive and stable enzyme biosensor based on efficient immobilization of acetylcholinesterase (AChE) to MWNTs-modified glassy carbon electrode (GCE) with chitosan (CS) by layer-by-layer (LBL) technique for rapid determination of carbofuran has been devised. According to the inhibitory effect of carbamate pesticide on the enzymatic activity of AChE, we use carbofuran as a model pesticide. The inhibitory effect of carbofuran on the biosensor was proportional to concentration of carbofuran in the range from 10 -10  g/L to 10 -3  g/L with a detection limit of 10 -12  g/L. This biosensor is a promising new method for pesticide analysis

  11. Catalytic recruitment in the inactivation of acetylcholinesterase by soman: temperature dependence of the solvent isotope effect

    International Nuclear Information System (INIS)

    Kovach, I.M.; Huber, J.H.A.; Schowen, R.L.

    1988-01-01

    3,3-Dimethyl-2-butyl methylphosphonofluoridate (soman) recruits at least 60-70% of the catalytic power of acetylcholinesterase during phosphonylation of the active-site serine, as compared with the acetylation by acetylcholine. The solvent isotope effect is 1.34 +/- 0.11 and is temperature independent within experimental error between 5 and 45 0 C. This observation is quite similar to what has been found for the reactions of aryl acetates and anilides. Average activation parameters for the same temperature range are ΔH* = 7.3 +/- 0.6 kcal/mol and ΔS* = -4 +/- 2 eu (H 2 O) and ΔH* = 7.1 +/- 0.4 kcal/mol and ΔS* = -6 +/- 1 eu (D 2 O). A rate-limiting process with 50% contribution of an induced-fit conformational change is supported by the data

  12. Synthesis and study of thiocarbonate derivatives of choline as potential inhibitors of acetylcholinesterase.

    Science.gov (United States)

    Boyle, N A; Talesa, V; Giovannini, E; Rosi, G; Norton, S J

    1997-09-12

    Fourteen alkyl and aryl thiocarbonate derivatives of choline were synthesized and studied as potential inhibitors of acetylcholinesterase (AChE). Twelve of the compounds inhibited AChEs derived from calf forebrain, human red blood cells, and octopus brain ranging from low to moderately high inhibition potency. The concentration of each inhibitory compound giving 50% inhibition of enzyme activity (IC50 values, which ranged from 1 x 10(-2) to 8 x 10(-7) M) was determined and is reported; inhibitor constants (Ki values) for the most inhibitory compounds, (1-pentylthiocarbonyl)choline chloride and (1-heptylthiocarbonyl)choline chloride, were calculated from kinetic data and are also reported. The inhibitors are competitive with substrate, and they are not hydrolyzed by the AChE activities. Certain of these new compounds may provide direction for the development of new drugs that have anticholinesterase activity and may be used for the treatment of Alzheimer's disease.

  13. Acetylcholinesterase inhibition-based biosensor for aluminum(III) chronoamperometric determination in aqueous media.

    Science.gov (United States)

    Barquero-Quirós, Miriam; Domínguez-Renedo, Olga; Alonso-Lomillo, Maria Asunción; Arcos-Martínez, María Julia

    2014-05-07

    A novel amperometric biosensor for the determination of Al(III) based on the inhibition of the enzyme acetylcholinesterase has been developed. The immobilization of the enzyme was performed on screen-printed carbon electrodes modified with gold nanoparticles. The oxidation signal of acetylthiocholine iodide enzyme substrate was affected by the presence of Al(III) ions leading to a decrease in the amperometric current. The developed system has a detection limit of 2.1 ± 0.1 μM for Al(III). The reproducibility of the method is 8.1% (n = 4). Main interferences include Mo(VI), W(VI) and Hg(II) ions. The developed method was successfully applied to the determination of Al(III) in spiked tap water . The analysis of a certified standard reference material was also carried out. Both results agree with the certified values considering the respective associated uncertainties.

  14. Humidity insensitive step-index polymer optical fibre Bragg grating sensors

    DEFF Research Database (Denmark)

    Woyessa, Getinet; Fasano, Andrea; Stefani, Alessio

    2015-01-01

    We have fabricated and characterised a humidity insensitive step index(SI) polymer optical fibre(POF) Bragg grating sensors. The fibre was made based on the injection molding technique, which is an efficient method for fast, flexible and cost effective preparation of the fibre preform. The fabric...... poly-methyl-methacrylate (PMMA) based SIPOFs. The fibre has a minimum loss of similar to 6dB/m at 770nm....

  15. Long-term sensitization of mechanosensitive and -insensitive afferents in mice with persistent colorectal hypersensitivity

    OpenAIRE

    Feng, Bin; La, Jun-ho; Schwartz, Erica S.; Tanaka, Takahiro; McMurray, Timothy P.; Gebhart, G. F.

    2012-01-01

    Afferent input contributes significantly to the pain and colorectal hypersensitivity that characterize irritable bowel syndrome. In the present study, we investigated the contributions of mechanically sensitive and mechanically insensitive afferents (MIAs; or silent afferents) to colorectal hypersensitivity. The visceromotor response to colorectal distension (CRD; 15–60 mmHg) was recorded in mice before and for weeks after intracolonic treatment with zymosan or saline. After CRD tests, the di...

  16. The arcuate artery in renal transplants: An insensitive indicator of rejection

    International Nuclear Information System (INIS)

    McIntire, J.N.; Angtuaco, T.L.; Boyd, C.; Flanigan, W.J.

    1987-01-01

    The authors performed 65 duplex US examinations in 28 patients within 2 years of transplantation. During this time 15 episodes of rejection were diagnosed by US and confirmed clinically. Of the remaining 50 examinations, 14 showed negligible or absent diastolic flow (suggesting rejection) in the arcuate arteries with normal diastolic flow in the main renal, segmental, and interlobar branches. No other criteria for rejection were present in these patients. It is concluded that the arcuate artery is an insensitive indicator of transplant rejection

  17. Eksplozivne materije za neosetljiva ubojna sredstva / Explosive substances for insensitive munitions

    Directory of Open Access Journals (Sweden)

    Radun Jeremić

    2005-03-01

    Full Text Available U skladu sa sve strožim zahtevima za očuvanje životne sredine i većom bezbednošću, tendencije u razvoju suvremenih ubojnih sredstava (UbS, pored povećanja pouzdanosti i efikasnosti, usmerene su i na povećanje sigurnosti pri njihovoj proizvodnji, skladištenju, manipulaciji i upotrebi. Na taj način dobijena je nova kategorija UbS, tzv. neosetljiva UbS, kod kojih je verovatnoća neželjenog aktiviranja pod dejstvom spoljnih impulsa svedena na minimum. Suština rešavanja ovog problema je primena eksplozivnih materija koje su mnogo manje osetljive na spoljne uticaje u odnosu na standardne. Osnovni zahtev koji se pri tome postavlja je da taktičko-tehničke karakteristike ostanu na nivou ili budu bolje u odnosu na postojeća UbS. U radu je ukratko objašnjen koncept razvoja neosetljivih UbS i dat pregled najznačajnijih rezultata istraživanja u oblasti eksplozivnih materija koje zadovoljavaju zahteve za primenu u neosetljivim UbS. / According to severe environment protection and safety requirements, tendencies in development of modern munitions, besides of increasing reliability and efficiency, are directed to decreasing of danger during their processing, storing, handling and operating. In that manner the new category of munitions has been obtained, named insensitive munitions, with a minimum probability of unplanned activating. The best method for solving this problem is using of explosive substances that are more insensitive according to standard ones. The main requirement is the tactical and technical characteristics stay at the level or to be better according to the existing munitions. In this paper the developing concept of insensitive munitions is shortly explained and presented a review of most important research results of explosive materials that fulfill requirements for applying in insensitive munitions.

  18. Compact temperature-insensitive modulator based on a silicon microring assistant Mach—Zehnder interferometer

    International Nuclear Information System (INIS)

    Zhang Xue-Jian; Feng Xue; Zhang Deng-Ke; Huang Yi-Dong

    2012-01-01

    On the silicon-on-insulator platform, an ultra compact temperature-insensitive modulator based on a cascaded microring assistant Mach—Zehnder interferometer is proposed and demonstrated with numerical simulation. According to the calculated results, the tolerated variation of ambient temperature can be as high as 134 °C while the footprint of such a silicon modulator is only 340 μm 2 . (electromagnetism, optics, acoustics, heat transfer, classical mechanics, and fluid dynamics)

  19. Laser ignitibility of insensitive secondary explosive 1,1-diamino-2,2-dinitroethene (FOX-7)

    International Nuclear Information System (INIS)

    Fang, Xiao; McLuckie, Warren G

    2015-01-01

    Highlights: • Carbon black (CB) is an efficient optical sensitizer compatible with 1,1-diamino-2,2-dinitroethene (FOX-7). • A CB doped insensitive explosive FOX-7 can be ignited by a low-power diode laser. • Laser ignitibility of the optically sensitized FOX-7 is mainly affected by laser power among the other parameters. • Inhomogeneities in the explosive affect laser ignition reliability. - Abstract: An experimental investigation into laser ignitibility of insensitive secondary explosives, 1,1-diamino-2,2-dinitroethene (FOX-7) has been carried out, using a diode laser of continuous wave at the laser wavelength of 974 nm. The direct optical ignition of an insensitive explosive will add more safety features to insensitive munitions (IM) or explosive devices. In this study, effects of laser parameters on the ignitibility were analysed in terms of laser ignition threshold, the times to initiate the ignition and full combustion, and burning sustainability. The results have shown that carbon black (CB) as an optical sensitizer is compatible with FOX-7, and significantly enhances laser ignitibility of the explosive when a small amount of CB is uniformly doped in FOX-7. The delay times for ignition and subsequent development of sustainable burning of the material are mainly determined by ignition laser power, although the other laser parameters have effects. The minimum laser power required to ignite the optically sensitized FOX-7 was found below 10 W and a fast ignition was initiated in as short as 70 μs by a laser power of 40 W. Also the effect of the mixture uniformity of FOX-7/CB on laser ignition performance was evaluated in this study

  20. Field and Laboratory Evaluations of Insecticides for Southern Pine Beetle Control

    Science.gov (United States)

    Felton L. Hastings; Jack E. Coster; [Editors

    1981-01-01

    Reports results of laboratory screenings and field studies of insecticides for use against the southern pine beetle. Preventive as webas remedial efficacywere observed, along with phytotoxicity to pine and understory hardwood species, effects of insecticides on soil microbial and mesofaunal populations, and degradation of insecticides by selected soil microbes.

  1. Pollution Of Insecticide Residues In PPTN Pasar Jumat Area

    International Nuclear Information System (INIS)

    Syahrir, Ulfa T.; Chairul, Sofnie M.

    2000-01-01

    Measurement of insecticide residue pollution from some organochlorin and organo-phosphat in soil and water samples were carried out 1999-2000 periode. The aim of the measurement was to get information about impact of laboratorium activity on insecticide contents in PPTN PASAR JUMAT. Gas chromatograph with electron capture and flame ionization detector were used to measure the pesticide content. Result of the measurement in PPTN area showed that organo-chlorin were alpha BHC, endosulfan band DDT and organo-phosphat were klorphyriphos and malation and were lower than tolerance level

  2. Characterizing the insecticide resistance of Anopheles gambiae in Mali.

    Science.gov (United States)

    Cisse, Moussa B M; Keita, Chitan; Dicko, Abdourhamane; Dengela, Dereje; Coleman, Jane; Lucas, Bradford; Mihigo, Jules; Sadou, Aboubacar; Belemvire, Allison; George, Kristen; Fornadel, Christen; Beach, Raymond

    2015-08-22

    The impact of indoor residual spraying (IRS) and long-lasting insecticide nets (LLINs), key components of the national malaria control strategy of Mali, is threatened by vector insecticide resistance. The objective of this study was to assess the level of insecticide resistance in Anopheles gambiae sensu lato populations from Mali against four classes of insecticide recommended for IRS: organochlorines (OCs), pyrethroids (PYs), carbamates (CAs) and organophosphates (OPs). Characterization of resistance was done in 13 sites across southern Mali and assessed presence and distribution of physiological mechanisms that included target-site modifications: knockdown resistance (kdr) and altered acetycholinesterase (AChE), and/or metabolic mechanisms: elevated esterases, glutathione S-transferases (GSTs), and monooxygenases. The World Health Organization (WHO) tube test was used to determine phenotypic resistance of An. gambiae s.l. to: dichlorodiphenyltrichloroethane (DDT) (OC), deltamethrin (PY), lambda-cyhalothrin (PY), bendiocarb (CA), and fenitrothion (OP). Identification of sibling species and presence of the ace-1 (R) and Leu-Phe kdr, resistance-associated mutations, were determined using polymerase chain reaction (PCR) technology. Biochemical assays were conducted to detect increased activity of GSTs, oxidases and esterases. Populations tested showed high levels of resistance to DDT in all 13 sites, as well as increased resistance to deltamethrin and lambda-cyhalothrin in 12 out of 13 sites. Resistance to fenitrothion and bendiocarb was detected in 1 and 4 out of 13 sites, respectively. Anopheles coluzzii, An. gambiae sensu stricto and Anopheles arabiensis were identified with high allelic frequencies of kdr in all sites where each of the species were found (13, 12 and 10 sites, respectively). Relatively low allelic frequencies of ace-1 (R) were detected in four sites where this assessment was conducted. Evidence of elevated insecticide metabolism, based on oxidase

  3. Surface modification of chitosan/PEO nanofibers by air dielectric barrier discharge plasma for acetylcholinesterase immobilization

    Energy Technology Data Exchange (ETDEWEB)

    Dorraki, Naghme, E-mail: n.dorraki@web.sbu.ac.ir [Laser and Plasma Research Institute, Shahid Beheshti University, Evin 1983963113, Tehran (Iran, Islamic Republic of); Safa, Nasrin Navab [Laser and Plasma Research Institute, Shahid Beheshti University, Evin 1983963113, Tehran (Iran, Islamic Republic of); Jahanfar, Mehdi [Protein Research Center, Shahid Beheshti University, Evin 1983963113, Tehran (Iran, Islamic Republic of); Ghomi, Hamid [Laser and Plasma Research Institute, Shahid Beheshti University, Evin 1983963113, Tehran (Iran, Islamic Republic of); Ranaei-Siadat, Seyed-Omid [Protein Research Center, Shahid Beheshti University, Evin 1983963113, Tehran (Iran, Islamic Republic of)

    2015-09-15

    Highlights: • We used an economical and effective method for surface modification. • Chitosan/PEO nanofibrous membranes were modified by air-DBD plasma. • The most NH{sub 3}{sup +} group was generated on the 6 min plasma modified membrane. • We immobilized acetylcholinesterase on the plasma modified and unmodified membranes. • More enzyme activity was detected on the modified membrane by plasma. - Abstract: There are different methods to modify polymer surfaces for biological applications. In this work we have introduced air-dielectric barrier discharge (DBD) plasma at atmospheric pressure as an economical and safe method for modifying the surface of electrospun chitosan/PEO (90/10) nanofibers for acetylcholinesterase (AChE) immobilization. According to the contact angle measurement results, the nanofibers become highly hydrophilic when they are exposed to the DBD plasma for 6 min in compared to unmodified membrane. Attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) results reveal hydroxyl, C=O and NH{sub 3}{sup +} polar groups increment after 6 min plasma treatment. Contact angle measurements and ATR-FTIR results are confirmed by X-ray photoelectron spectroscopy (XPS). AChE at pH 7.4 carries a negative charge and after immobilization on the surface of plasma-treated nanofibrous membrane attracts the NH{sub 3}{sup +} group and more enzyme activity is detected on the plasma-modified nanofibers for 6 min in compared to unmodified nanofibers. Atomic force microscopy (AFM) and scanning electron microscopy (SEM) are used for the surface topography and morphology characterization. The results have proved that air-DBD plasma is a suitable method for chitosan/PEO nanofibrous membrane modification as a biodegradable and functionalized substrate for enzyme immobilization.

  4. Phytochemical Quantification and the In Vitro Acetylcholinesterase Inhibitory Activity of Phellodendron chinense and Its Components.

    Science.gov (United States)

    Kim, Yu Jin; Lim, Hye-Sun; Kim, Yoonju; Lee, Jun; Kim, Bu-Yeo; Jeong, Soo-Jin

    2017-06-02

    The dried bark of Phellodendron chinense has been used as a traditional herbal medicine to remove damp heat, relieve consumptive fever, and cure dysentery and diarrhea. In the present study, we performed quantitative analyses of the two components of P. chinense , phellodendrine and berberine, using high-performance liquid chromatography. A 70% ethanol extract of P. chinense was prepared and the two components were separated on a C-18 analytical column using a gradient solvent system of acetonitrile and 0.1% ( v / v ) aqueous trifluoroacetic acid. The ultraviolet wavelength used for detection was 200 nm for phellodendrine and 226 nm for berberine. The analytical method established here showed high linearity (correlation coefficient, ≥0.9991). The amount of phellodendrine and berberine used was 22.255 ± 0.123 mg/g and 269.651 ± 1.257 mg/g, respectively. Moreover, we performed an in vitro acetylcholinesterase (AChE) activity assay and an amyloid-β aggregation test to examine the biological properties of phellodendrine and berberine as therapeutic drugs for Alzheimer's disease. Phellodendrine and berberine inhibited AChE activity in a dose-dependent manner (IC 50 = 36.51 and 0.44 μM, respectively). In contrast, neither phellodendrine nor berberine had an effect on amyloid-β aggregation. The P. chinense extract and phellodendrine, but not berberine, exhibited antioxidant activity by increasing radical scavenging activity. Moreover, P. chinense demonstrated a neuroprotective effect in hydrogen peroxide-treated HT22 hippocampal cells. Overall, our findings suggest that P. chinense has potential as an anti-Alzheimer's agent via the suppression of the enzymatic activity of acetylcholinesterase and the stimulation of antioxidant activity.

  5. Isoflurane-induced spatial memory impairment in mice is prevented by the acetylcholinesterase inhibitor donepezil.

    Directory of Open Access Journals (Sweden)

    Diansan Su

    Full Text Available Although many studies have shown that isoflurane exposure impairs spatial memory in aged animals, there are no clinical treatments available to prevent this memory deficit. The anticholinergic properties of volatile anesthetics are a biologically plausible cause of cognitive dysfunction in elderly subjects. We hypothesized that pretreatment with the acetylcholinesterase inhibitor donepezil, which has been approved by the Food and Drug Administration (FDA for the treatment of Alzheimer's disease, prevents isoflurane-induced spatial memory impairment in aged mice. In present study, eighteen-month-old mice were administered donepezil (5 mg/kg or an equal volume of saline by oral gavage with a feeding needle for four weeks. Then the mice were exposed to isoflurane (1.2% for six hours. Two weeks later, mice were subjected to the Morris water maze to examine the impairment of spatial memory after exposure to isoflurane. After the behavioral test, the mice were sacrificed, and the protein expression level of acetylcholinesterase (AChE, choline acetylase (ChAT and α7 nicotinic receptor (α7-nAChR were measured in the brain. Each group consisted of 12 mice. We found that isoflurane exposure for six hours impaired the spatial memory of the mice. Compared with the control group, isoflurane exposure dramatically decreased the protein level of ChAT, but not AChE or α7-nAChR. Donepezil prevented isoflurane-induced spatial memory impairments and increased ChAT levels, which were downregulated by isoflurane. In conclusions, pretreatment with the AChE inhibitor donepezil prevented isoflurane-induced spatial memory impairment in aged mice. The mechanism was associated with the upregulation of ChAT, which was decreased by isoflurane.

  6. Insecticide applications to soil contribute to the development of Burkholderia mediating insecticide resistance in stinkbugs.

    Science.gov (United States)

    Tago, Kanako; Kikuchi, Yoshitomo; Nakaoka, Sinji; Katsuyama, Chie; Hayatsu, Masahito

    2015-07-01

    Some soil Burkholderia strains are capable of degrading the organophosphorus insecticide, fenitrothion, and establish symbiosis with stinkbugs, making the host insects fenitrothion-resistant. However, the ecology of the symbiotic degrading Burkholderia adapting to fenitrothion in the free-living environment is unknown. We hypothesized that fenitrothion applications affect the dynamics of fenitrothion-degrading Burkholderia, thereby controlling the transmission of symbiotic degrading Burkholderia from the soil to stinkbugs. We investigated changes in the density and diversity of culturable Burkholderia (i.e. symbiotic and nonsymbiotic fenitrothion degraders and nondegraders) in fenitrothion-treated soil using microcosms. During the incubation with five applications of pesticide, the density of the degraders increased from less than the detection limit to around 10(6)/g of soil. The number of dominant species among the degraders declined with the increasing density of degraders; eventually, one species predominated. This process can be explained according to the competitive exclusion principle using V(max) and K(m) values for fenitrothion metabolism by the degraders. We performed a phylogenetic analysis of representative strains isolated from the microcosms and evaluated their ability to establish symbiosis with the stinkbug Riptortus pedestris. The strains that established symbiosis with R. pedestris were assigned to a cluster including symbionts commonly isolated from stinkbugs. The strains outside the cluster could not necessarily associate with the host. The degraders in the cluster predominated during the initial phase of degrader dynamics in the soil. Therefore, only a few applications of fenitrothion could allow symbiotic degraders to associate with their hosts and may cause the emergence of symbiont-mediated insecticide resistance. © 2015 John Wiley & Sons Ltd.

  7. Congenital insensitivity to pain and anhidrosis: A case report from South India

    Directory of Open Access Journals (Sweden)

    Carounanidy Udayashankar

    2012-01-01

    Full Text Available Congenital insensitivity to pain with anhidrosis, also known as hereditary sensory and autonomic neuropathy type IV, is an autosomal recessive disorder characterized by the congenital lack of pain sensation, inability to sweat, episodes of recurrent hyperpyrexia, mental retardation, and self-mutilating behavior. It is an extremely rare disorder with only a handful of reports from India. A five- year- old boy, born to second-degree consanguineous parents after uneventful antenatal period, presented to us with history of recurrent unexplained fever, recurrent ulcers in the lower limbs, insensitivity to painful stimuli (like injections, vaccination and self-mutilating behavior from early childhood. Cutaneous examination showed multiple ulcers, loss of teeth, loss of tip of the tongue (due to biting, scarring of finger tips, xerosis and lichenification. Sensory examination showed complete loss of pain and temperature sensations, but fine touch and vibration were preserved. Deep tendon reflexes were normal. Evaluation for Hansen′s disease was non-contributory. An intradermal injection of histamine did not show any flare response. Based on clinical as well as compatible histological features a diagnosis of congenital insensitivity to pain with anhidrosis was made. The ulcers were treated with appropriate antibiotics and daily dressings. The parents were counseled about appropriate care of the child.

  8. Formulation development and characterization of cellulose acetate nitrate based propellants for improved insensitive munitions properties

    Directory of Open Access Journals (Sweden)

    Thelma Manning

    2014-06-01

    Full Text Available Cellulose acetate nitrate (CAN was used as an insensitive energetic binder to improve the insensitive munitions (IM properties of gun propellants to replace the M1 propellant used in 105 mm artillery charges. CAN contains the energetic nitro groups found in nitrocellulose (NC, but also acetyl functionalities, which lowered the polymer's sensitivity to heat and shock, and therefore improved its IM properties relative to NC. The formulation, development and small-scale characterization testing of several CAN-based propellants were done. The formulations, using insensitive energetic solid fillers and high-nitrogen modifiers in place of nitramine were completed. The small scale characterization testing, such as closed bomb testing, small scale sensitivity, thermal stability, and chemical compatibility were done. The mechanical response of the propellants under high-rate uni-axial compression at, hot, cold, and ambient temperatures were also completed. Critical diameter testing, hot fragment conductive ignition (HFCI tests were done to evaluate the propellants' responses to thermal and shock stimuli. Utilizing the propellant chemical composition, theoretical predictions of erosivity were completed. All the small scale test results were utilized to down-select the promising CAN based formulations for large scale demonstration testing such as the ballistic performance and fragment impact testing in the 105 mm M67 artillery charge configurations. The test results completed in the small and large scale testing are discussed.

  9. Ethylene signaling renders the jasmonate response of Arabidopsis insensitive to future suppression by salicylic Acid.

    Science.gov (United States)

    Leon-Reyes, Antonio; Du, Yujuan; Koornneef, Annemart; Proietti, Silvia; Körbes, Ana P; Memelink, Johan; Pieterse, Corné M J; Ritsema, Tita

    2010-02-01

    Cross-talk between jasmonate (JA), ethylene (ET), and Salicylic acid (SA) signaling is thought to operate as a mechanism to fine-tune induced defenses that are activated in response to multiple attackers. Here, 43 Arabidopsis genotypes impaired in hormone signaling or defense-related processes were screened for their ability to express SA-mediated suppression of JA-responsive gene expression. Mutant cev1, which displays constitutive expression of JA and ET responses, appeared to be insensitive to SA-mediated suppression of the JA-responsive marker genes PDF1.2 and VSP2. Accordingly, strong activation of JA and ET responses by the necrotrophic pathogens Botrytis cinerea and Alternaria brassicicola prior to SA treatment counteracted the ability of SA to suppress the JA response. Pharmacological assays, mutant analysis, and studies with the ET-signaling inhibitor 1-methylcyclopropene revealed that ET signaling renders the JA response insensitive to subsequent suppression by SA. The APETALA2/ETHYLENE RESPONSE FACTOR transcription factor ORA59, which regulates JA/ET-responsive genes such as PDF1.2, emerged as a potential mediator in this process. Collectively, our results point to a model in which simultaneous induction of the JA and ET pathway renders the plant insensitive to future SA-mediated suppression of JA-dependent defenses, which may prioritize the JA/ET pathway over the SA pathway during multi-attacker interactions.

  10. Calcitonin gene-related peptide alters the firing rates of hypothalamic temperature sensitive and insensitive neurons

    Directory of Open Access Journals (Sweden)

    Grimm Eleanor R

    2008-07-01

    Full Text Available Abstract Background Transient hyperthermic shifts in body temperature have been linked to the endogenous hormone calcitonin gene-related peptide (CGRP, which can increase sympathetic activation and metabolic heat production. Recent studies have demonstrated that these centrally mediated responses may result from CGRP dependent changes in the activity of thermoregulatory neurons in the preoptic and anterior regions of the hypothalamus (POAH. Results Using a tissue slice preparation, we recorded the single-unit activity of POAH neurons from the adult male rat, in response to temperature and CGRP (10 μM. Based on the slope of firing rate as a function of temperature, neurons were classified as either warm sensitive or temperature insensitive. All warm sensitive neurons responded to CGRP with a significant decrease in firing rate. While CGRP did not alter the firing rates of some temperature insensitive neurons, responsive neurons showed an increase in firing rate. Conclusion With respect to current models of thermoregulatory control, these CGRP dependent changes in firing rate would result in hyperthermia. This suggests that both warm sensitive and temperature insensitive neurons in the POAH may play a role in producing this hyperthermic shift in temperature.

  11. Incorporating mesh-insensitive structural stress into the fatigue assessment procedure of common structural rules for bulk carriers

    Directory of Open Access Journals (Sweden)

    Seong-Min Kim

    2015-01-01

    Full Text Available This study introduces a fatigue assessment procedure using mesh-insensitive structural stress method based on the Common Structural Rules for Bulk Carriers by considering important factors, such as mean stress and thickness effects. The fatigue assessment result of mesh-insensitive structural stress method have been compared with CSR procedure based on equivalent notch stress at major hot spot points in the area near the ballast hold for a 180 K bulk carrier. The possibility of implementing mesh-insensitive structural stress method in the fatigue assessment procedure for ship structures is discussed.

  12. Molecular interaction studies of acetylcholinesterase with potential acetylcholinesterase inhibitors from the root of Rhodiola crenulata using molecular docking and isothermal titration calorimetry methods.

    Science.gov (United States)

    Li, Fa-Jie; Liu, Yuan; Yuan, Yuan; Yang, Bin; Liu, Zhen-Ming; Huang, Lu-Qi

    2017-11-01

    (-)-Epicatechin gallate ((-)-ECG), 1,2,3,4,6-O-pentagalloylglucose (PGG), rhodionin, herbacetin and rhodiosin isolated from the root of Rhodiola crenulata exhibited potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC 50 ranged from 57.50±5.83 to 2.43±0.34μg/mL. With the aim of explaining the differences in activity of these active ingredients and clarifying how they inhibit AChE, the AChE-inhibitor interactions were further explored using molecular docking and isothermal titration calorimetry (ITC) methods in the present study. Molecular docking studies revealed that all compounds except PGG showed binding energy values ranging from -10.30 to -8.00kcal/mol while the binding energy of galantamine, a known AChE inhibitor, was -9.53kcal/mol; they inhibited the AChE by binding into the ligand pocket with the similar binding pattern to that of galantamine by interacting with Glu199 of AChE. Inhibition constant of these active ingredients had a positive correlation with binding energy. The interaction between AChE and PGG was further evaluated with the ITC method and the results indicated that the PGG-AChE interaction was relevant to AChE concentration. The results revealed a possible mechanism for the AChE inhibition activity of these bioactive ingredients, which may provide some help in lead compounds optimization in the future. Copyright © 2017 Elsevier B.V. All rights reserved.

  13. Role of cytochrome P450s in insecticide resistance: impact on the control of mosquito-borne diseases and use of insecticides on Earth.

    Science.gov (United States)

    David, Jean-Philippe; Ismail, Hanafy Mahmoud; Chandor-Proust, Alexia; Paine, Mark John Ingraham

    2013-02-19

    The fight against diseases spread by mosquitoes and other insects has enormous environmental, economic and social consequences. Chemical insecticides remain the first line of defence but the control of diseases, especially malaria and dengue fever, is being increasingly undermined by insecticide resistance. Mosquitoes have a large repertoire of P450s (over 100 genes). By pinpointing the key enzymes associated with insecticide resistance we can begin to develop new tools to aid the implementation of control interventions and reduce their environmental impact on Earth. Recent technological advances are helping us to build a functional profile of the P450 determinants of insecticide metabolic resistance in mosquitoes. Alongside, the cross-responses of mosquito P450s to insecticides and pollutants are also being investigated. Such research will provide the means to produce diagnostic tools for early detection of P450s linked to resistance. It will also enable the design of new insecticides with optimized efficacy in different environments.

  14. Screening of plants used in the European traditional medicine to treat memory disorders for acetylcholinesterase inhibitory activity and anti amyloidogenic activity

    DEFF Research Database (Denmark)

    Lobbens, Eva S B; Vissing, Karina J.; Jorgensen, Lene

    2017-01-01

    and the ability to inhibit the enzymatic activity of acetylcholinesterase was evaluated monitoring the hydrolysis of acetylthiocholine Results Under the experimental conditions investigated, extracts of two plants, Carum carvi and Olea sylvestris, inhibited amyloid beta fibrillation considerably, eight plant...

  15. Insecticidal and acetylcholine esterase inhibition activity of Asteraceae plant essential oils and their constituents against adults of the German cockroach (Blattella germanica).

    Science.gov (United States)

    Yeom, Hwa-Jeong; Jung, Chan-Sik; Kang, Jaesoon; Kim, Junheon; Lee, Jae-Hyeon; Kim, Dong-Soo; Kim, Hyun-Seok; Park, Pil-Sun; Kang, Kyu-Suk; Park, Il-Kwon

    2015-03-04

    The fumigant and contact toxicities of 16 Asteraceae plant essential oils and their constituents against adult male and female Blattella germanica were examined. In a fumigant toxicity test, tarragon oil exhibited 100% and 90% fumigant toxicity against adult male German cockroaches at 5 and 2.5 mg/filter paper, respectively. Fumigant toxicities of Artemisia arborescens and santolina oils against adult male German cockroaches were 100% at 20 mg/filter paper, but were reduced to 60% and 22.5% at 10 mg/filter paper, respectively. In contact toxicity tests, tarragon and santolina oils showed potent insecticidal activity against adult male German cockroaches. Components of active oils were analyzed using gas chromatography, gas chromatography-mass spectrometry, or nuclear magnetic resonance spectrometer. Among the identified compounds from active essential oils, estragole demonstrated potent fumigant and contact toxicity against adult German cockroaches. β-Phellandrene exhibited inhibition of male and female German cockroach acetylcholinesterase activity with IC50 values of 0.30 and 0.28 mg/mL, respectively.

  16. Acetylcholinesterase of the Sand Fly, Phlebotomus papatasi (Scopoli): Construction, Expression and Biochemical Properties of the G119S Orthologous Mutant

    Science.gov (United States)

    2014-12-10

    C, Pasteur N, Philips A, Fort P, Raymond M: Insecticide resistance in mosquito vectors. Nature 2003, 423:136–137. 27. Weill W, Lutfalla G, Mogensen K...Chandre F, Berthomieu A, Berticat C, Pasteur N, Philips A, Fort P, Raymond M: Corrigendum:Insecticide resistance in mosquito vectors. Nature 2003...1 biochemical properties. Comp Biochem Physiol B 2008, 150:271–277. 46. Alout H, Labbé P, Berthomieu A, Pasteur N, Weill M: Multiple duplications of

  17. Acetylcholinesterase of the Sand Fly, Phlebotomus papatasi (Scopoli): cDNA Sequence, Baculovirus Expression, and Biochemical Properties

    Science.gov (United States)

    2013-01-01

    Iraq: 6. Evaluation of insecticides for the control of sand flies. J Med Entomol 2011, 48:584–599. 16. Hemingway J, Ranson H: Insecticide resistance...leishmaniasis in Morocco. Parasit Vectors 2012, 5:51. 18. Surendran SN, Karunaratne SHPP, Adams Z, Hemingway J, Hawkes NJ: Molecular and biochemical...2002, 37:213–218. 45. Vontas JG, Hejazi MJ, Hawkes NJ, Cosmidis N, Loukas M, Hemingway J: Resistance-associated point mutations of organophosphate

  18. Role of cytochrome P450s in insecticide resistance: impact on the control of mosquito-borne diseases and use of insecticides on Earth

    OpenAIRE

    David, Jean-Philippe; Ismail, Hanafy Mahmoud; Chandor-Proust, Alexia; Paine, Mark John Ingraham

    2013-01-01

    The fight against diseases spread by mosquitoes and other insects has enormous environmental, economic and social consequences. Chemical insecticides remain the first line of defence but the control of diseases, especially malaria and dengue fever, is being increasingly undermined by insecticide resistance. Mosquitoes have a large repertoire of P450s (over 100 genes). By pinpointing the key enzymes associated with insecticide resistance we can begin to develop new tools to aid the implementat...

  19. Insecticidal Potential of an Orally Administered Metabolic Extract of ...

    African Journals Online (AJOL)

    The insecticidal activity of Aspergillus niger IHCS-4 metabolic extract against Chrysomya chloropyga larvae was examined in vitro. The toxicity test revealed that 0.04 mg/g and 0.08 mg/g extract concentration significantly (P>0.05) affected the insect larvae, inducing 20% and 65% mortality respectively, within 24 hours.

  20. Effectiveness of plant based insecticides as a sustainable means of ...

    African Journals Online (AJOL)

    Cucumber (Cucumis sativus) is an important crop in Pakistan. It is affected by many biotic and abiotic factors. Among these, Cucumber mosaic virus is the important disease with economic losses. The purpose of this study was to evaluate the effectiveness of plant based insecticides as a sustainable means to control the ...

  1. Studies .on the efficacy of some biorational insecticides against the ...

    African Journals Online (AJOL)

    W. Tin znara*, C. Na11kinga, l Kashaija & W. Tu.vhemereirwe ... Biorat!onal insecticides obtained from tobacco, ash, urine, pepper and a concoction (mixture) were ... Cultural control ... single components were made by adding I 00 ml of tap.

  2. Risk of transmission of viral haemorrhagic fevers and the insecticide ...

    African Journals Online (AJOL)

    ... of transmission of viral haemorrhagic fevers and the insecticide susceptibility status of Ae. aegypti in some sites in Accra, Ghana. Design: Larval surveys were carried to inspect containers within households and estimate larval indices and adult Aedes mosquitoes were collected using human landing collection technique.

  3. The comparative insecticidal and residual efficacy of sniper and ...

    African Journals Online (AJOL)

    Otoigiakih

    Chemical control is still the main approach for urban pest control (Castle et al., 1999; Rozendaal, 1997; Marrs,. 1993; Lee and Yap, 2003; Tidwell et al., 1994). The use of insecticides is seen as the most effective tool in cockroach control program (WHO, 1996; Chavasse and. Yap, 1997; Lee and Yap, 2003; Tidwell et al., ...

  4. Susceptibility of Adult Mosquitoes to Insecticides in Aqueous Sucrose Baits

    Science.gov (United States)

    2011-06-01

    Lee, and A.H. Azahari. 2005. Adult and larval insecticide susceptibility status of Culex quinquefasciatus (Say) mosquitoes in Kuala Lumpur Malaysia ...Trop. Biomed. 22: 63-68. Nayar, J.K. and D.M. Sauerman, Jr. 1971. The effects of diet on life-span, fecundity and flight potential of Aedes

  5. Efficacy of some synthetic insecticides for control of cotton bollworms ...

    African Journals Online (AJOL)

    ... and Betsulfan at 3.2 l ha-1 recorded the highest and lowest yields, respectively. For effective control of cotton bollworms for maximum yield in the ecology, Thionex applied at 2.8 l ha-1 is recommended. Keywords: Control, cotton bollworms, efficacy, Ghana, synthetic insecticides. African Crop Science Journal, Vol. 20, No.

  6. Insecticide use and practices among cotton farmers in northern ...

    African Journals Online (AJOL)

    Cotton (Gossypium hirsutum L.) is an important cash crop in Uganda. Insecticide application practices among cotton growers in northern Uganda were examined to determine the pests targeted and the compliance of control measures with the standards recommended by the Uganda's Cotton Development Organization ...

  7. Pyrethroid insecticides in urban salmon streams of the Pacific Northwest

    Energy Technology Data Exchange (ETDEWEB)

    Weston, D.P., E-mail: dweston@berkeley.edu [Department of Integrative Biology, University of California, 3060 Valley Life Sciences Bldg., Berkeley, CA 94720-3140 (United States); Asbell, A.M., E-mail: aasbell@berkeley.edu [Department of Integrative Biology, University of California, 3060 Valley Life Sciences Bldg., Berkeley, CA 94720-3140 (United States); Hecht, S.A., E-mail: scott.hecht@noaa.gov [NOAA Fisheries, Office of Protected Resources, 510 Desmond Drive S.E., Lacey, WA 98503 (United States); Scholz, N.L., E-mail: nathaniel.scholz@noaa.gov [NOAA Fisheries, Northwest Fisheries Science Center, 2725 Montlake Blvd. E., Seattle, WA 98112 (United States); Lydy, M.J., E-mail: mlydy@siu.edu [Fisheries and Illinois Aquaculture Center and Department of Zoology, Southern Illinois University, 171 Life Sciences II, Carbondale, IL 62901 (United States)

    2011-10-15

    Urban streams of the Pacific Northwest provide spawning and rearing habitat for a variety of salmon species, and food availability for developing salmon could be adversely affected by pesticide residues in these waterbodies. Sediments from Oregon and Washington streams were sampled to determine if current-use pyrethroid insecticides from residential neighborhoods were reaching aquatic habitats, and if they were at concentrations acutely toxic to sensitive invertebrates. Approximately one-third of the 35 sediment samples contained measurable pyrethroids. Bifenthrin was the pyrethroid of greatest concern with regards to aquatic life toxicity, consistent with prior studies elsewhere. Toxicity to Hyalella azteca and/or Chironomus dilutus was found in two sediment samples at standard testing temperature (23 deg. C), and in one additional sample at a more environmentally realistic temperature (13 deg. C). Given the temperature dependency of pyrethroid toxicity, low temperatures typical of northwest streams can increase the potential for toxicity above that indicated by standard testing protocols. - Highlights: > Salmon-bearing creeks can be adversely impacted by insecticides from urban runoff. > Pyrethroid insecticides were found in one-third of the creeks in Washington and Oregon. > Two creeks contained concentrations acutely lethal to sensitive invertebrates. > Bifenthrin was of greatest concern, though less than in prior studies. > Standard toxicity testing underestimates the ecological risk of pyrethroids. - Pyrethroid insecticides are present in sediments of urban creeks of Oregon and Washington, though less commonly than in studies elsewhere in the U.S.

  8. Pyrethroid insecticides in urban salmon streams of the Pacific Northwest

    International Nuclear Information System (INIS)

    Weston, D.P.; Asbell, A.M.; Hecht, S.A.; Scholz, N.L.; Lydy, M.J.

    2011-01-01

    Urban streams of the Pacific Northwest provide spawning and rearing habitat for a variety of salmon species, and food availability for developing salmon could be adversely affected by pesticide residues in these waterbodies. Sediments from Oregon and Washington streams were sampled to determine if current-use pyrethroid insecticides from residential neighborhoods were reaching aquatic habitats, and if they were at concentrations acutely toxic to sensitive invertebrates. Approximately one-third of the 35 sediment samples contained measurable pyrethroids. Bifenthrin was the pyrethroid of greatest concern with regards to aquatic life toxicity, consistent with prior studies elsewhere. Toxicity to Hyalella azteca and/or Chironomus dilutus was found in two sediment samples at standard testing temperature (23 deg. C), and in one additional sample at a more environmentally realistic temperature (13 deg. C). Given the temperature dependency of pyrethroid toxicity, low temperatures typical of northwest streams can increase the potential for toxicity above that indicated by standard testing protocols. - Highlights: → Salmon-bearing creeks can be adversely impacted by insecticides from urban runoff. → Pyrethroid insecticides were found in one-third of the creeks in Washington and Oregon. → Two creeks contained concentrations acutely lethal to sensitive invertebrates. → Bifenthrin was of greatest concern, though less than in prior studies. → Standard toxicity testing underestimates the ecological risk of pyrethroids. - Pyrethroid insecticides are present in sediments of urban creeks of Oregon and Washington, though less commonly than in studies elsewhere in the U.S.

  9. Metaflumizone is a novel sodium channel blocker insecticide.

    Science.gov (United States)

    Salgado, V L; Hayashi, J H

    2007-12-15

    Metaflumizone is a novel semicarbazone insecticide, derived chemically from the pyrazoline sodium channel blocker insecticides (SCBIs) discovered at Philips-Duphar in the early 1970s, but with greatly improved mammalian safety. This paper describes studies confirming that the insecticidal action of metaflumizone is due to the state-dependent blockage of sodium channels. Larvae of the moth Spodoptera eridania injected with metaflumizone became paralyzed, concomitant with blockage of all nerve activity. Furthermore, tonic firing of abdominal stretch receptor organs from Spodoptera frugiperda was blocked by metaflumizone applied in the bath, consistent with the block of voltage-dependent sodium channels. Studies on native sodium channels, in primary-cultured neurons isolated from the CNS of the larvae of the moth Manduca sexta and on Para/TipE sodium channels heterologously expressed in Xenopus (African clawed frog) oocytes, confirmed that metaflumizone blocks sodium channels by binding selectively to the slow-inactivated state, which is characteristic of the SCBIs. The results confirm that metaflumizone is a novel sodium channel blocker insecticide.

  10. Insecticide resistance testing in malaria vectors in Tanzania ...

    African Journals Online (AJOL)

    mosquito survived much better and the scientists had a total of 467 mosquitoes to run the insecticide susceptibility tests. Innovative ways are necessary under field conditions for mosquito breeding in susceptibility studies. Key words: Malaria, Anopheles gambiae complex, larvae, fabric, resistance, susceptibility, Tanzania.

  11. Effective utilization period of long-lasting insecticide treated nets ...

    African Journals Online (AJOL)

    The study was conducted to evaluate the bioefficacy of long-lasting insecticide treated nets (LLITNs) (PermaNet®2.0) over time and the species composition of Anopheles mosquitoes around Bahir Dar. The space spray collection method was used to determine the species composition of indoor resting Anopheles ...

  12. Insecticide resistance and glutathione S-transferases in mosquitoes ...

    African Journals Online (AJOL)

    Mosquito glutathione S-transferases (GSTs) have received considerable attention in the last 20 years because of their role in insecticide metabolism producing resistance. Many different compounds, including toxic xenobiotics and reactive products of intracellular processes such as lipid peroxidation, act as GST substrates.

  13. Larvicidal, pupicidal and insecticidal activities of Cosmos bipinnatus ...

    African Journals Online (AJOL)

    Purpose: To evaluate the larvicidal, pupicidal and insecticidal activities of Cosmos bipinnatus, Foenuculum vulgare and Tagetes minuta leaf extracts against Culex quinquefasciatus mosquitoes. Methods: The leaves of the plants were extracted with distilled water, ethanol (95 %), and hexane and the extracts screened for ...

  14. Effect of natural and chemical insecticides on Hyalopterus pruni and ...

    African Journals Online (AJOL)

    Experiments were carried out to evaluate the effect of water extracts of Fagonia arabica, Salix alba and Anthmis pseudocotula and their mixtures with chemical insecticide (Malathion) on growth of. Hyalopterus pruni and characters of Armeniaca vulgaris plants and their soils. The data revealed that F.arabica extract at 20% ...

  15. Biological efficacy of the ecotoxically favourable insecticides and ...

    African Journals Online (AJOL)

    The high biologic efficacy, mechanism of action, resistance to water rinsing, high selectivity, and small quantities of application, anticipated a bright future for them. Since results of researches of biological efficacy of insecticides in laboratory and field conditions are statistically different, studies done in natural conditions ...

  16. Insecticide assays against the brown stink bug feeding on pecan

    Science.gov (United States)

    The brown stink bug, Euschistus servus (Say) (Hemiptera: Pentatomidae), is an economic pest of pecan, Carya illinoinensis (Wangenh) K. Koch (Juglandaceae), and other agronomic crops across the southeastern U.S. Management of this pest is mainly via insecticides. Many commercial products indicate o...

  17. Environmental insecticide residues from tsetse fly control measures in Uganda

    International Nuclear Information System (INIS)

    Sserunjoji-Sebalija, J.

    1976-01-01

    Up to June 1974 areas in Uganda totalling 8600km 2 have been successfully reclaimed from tsetse fly infestation by ground spray of 3% dieldrin water emulsions. A search for equally effective but less persistent and toxic compounds against tsetse flies has been unsuccessful. Fourteen insecticide formulations have been tested for their persistence on tree bark surfaces and, therefore, their availability and toxicity to the target tsetse flies. Only those compounds with a high immediate insecticidal activity (some higher than dieldrin) like endosulfan, Chlorfenvinphos and propoxur could merit further consideration in tsetse control. While some were toxic to tsetse as fresh deposits, they lacked sufficient persistence. A study of the environmental implication from the continued use of the highly persistent and toxic dieldrin has provided useful data on residues likely to be found both in terrestrial and aquatic fauna and flora. These are generally low. Moreover, there is evidence of degradation in some fish species (Protopterus aethiopicus and Clarias). Also, dilution factors and adsorption involving the muddy nature of water run-off, etc., and controlled burning of grasses after tsetse eradication would tend to inactivate the residual insecticide and protect aquatic systems. The general findings have indicated less risk than anticipated of the environmental contamination from tsetse control by application of persistent and toxic insecticides. (author)

  18. Ethnobotany of plants used as insecticides, repellents and ...

    African Journals Online (AJOL)

    An ethnobotanical study on plants used for the prevention and treatment of malaria was conducted to document the indigenous knowledge particularly associated with the use and conservation of anti-malarial, insecticide and insect repellent medicinal plants. In this study, five sampling sites were selected based on the ...

  19. Chemical Composition and Insecticidal Activity of the Essential Oil of ...

    African Journals Online (AJOL)

    Purpose: To investigate the chemical composition and insecticidal activity of the essential oil of the aerial parts of Ostericum grosseserratum against the maize weevil, Sitophilus zeamaisD. Methods: Steam distillation of the aerial parts of O. grosseserratum during the flowering stage was carried out using a Clavenger ...

  20. Chemical composition and insecticidal properties of essential oil ...

    African Journals Online (AJOL)

    Purpose: To determine the insecticidal properties of essential oil from Mosla soochowensis aerial parts against two insect pests, Sitophilus zeamais and Tribolium castaneum. Methods: Hydro-distillation of M. soochowensis was used to extract the essential oil. Gas chromatography/mass spectrometry (GC/MS) analysis was ...

  1. Bio-insecticides and mating disruption in cranberries

    Science.gov (United States)

    Surveys of native entomopathogenic nematodes in Wisconsin have produced a new bio-insecticide involving two particular nematode species (Oscheius onirici and Heterorhabditis georgiana). In field studies, these nematodes have shown high virulence against flea beetles; in the laboratory, these nematod...

  2. Insecticide Use Practices in Cocoa Production in Four Regions in ...

    African Journals Online (AJOL)

    Most of the insecticides used are classified as class II under WHO Hazard category, and the farmers used very minimal protective clothing during pesticides application. The results of this study show that there is the need to intensify education on safe handling and use of pesticides to reduce pesticide abuse, especially by ...

  3. Cytotoxic effects of delfin insecticide (Bacillus thuringiensis) on cell ...

    African Journals Online (AJOL)

    STORAGESEVER

    2008-08-04

    Aug 4, 2008 ... In acute exposure cells showed deformities such as swelling of cells, oval shaped deformity, and ... Commercial grade of delfin insecticide used in this study was manufactured by .... exposure to cigarette extracts. Antibiotics caused .... administration of a neem pesticide on rat metabolic enzymes. J. Environ.

  4. Material gain: bednets treated with insecticides improve the lives of ...

    International Development Research Centre (IDRC) Digital Library (Canada)

    2011-07-15

    ... 700 mosquito nets each day, marketed under brand names such as "Health Net" and ... Material gain: bednets treated with insecticides improve the lives of Tanzanians. July 15, 2011. Image ... The kit is one of the key elements of PSI's Social Marketing of ... The national strategy will work to change this by involving the full ...

  5. Flupyradifurone: a brief profile of a new butenolide insecticide

    Science.gov (United States)

    Nauen, Ralf; Jeschke, Peter; Velten, Robert; Beck, Michael E; Ebbinghaus-Kintscher, Ulrich; Thielert, Wolfgang; Wölfel, Katharina; Haas, Matthias; Kunz, Klaus; Raupach, Georg

    2015-01-01

    BACKGROUND The development and commercialisation of new chemical classes of insecticides for efficient crop protection measures against destructive invertebrate pests is of utmost importance to overcome resistance issues and to secure sustainable crop yields. Flupyradifurone introduced here is the first representative of the novel butenolide class of insecticides active against various sucking pests and showing an excellent safety profile. RESULTS The discovery of flupyradifurone was inspired by the butenolide scaffold in naturally occurring stemofoline. Flupyradifurone acts reversibly as an agonist on insect nicotinic acetylcholine receptors but is structurally different from known agonists, as shown by chemical similarity analysis. It shows a fast action on a broad range of sucking pests, as demonstrated in laboratory bioassays, and exhibits excellent field efficacy on a number of crops with different application methods, including foliar, soil, seed treatment and drip irrigation. It is readily taken up by plants and translocated in the xylem, as demonstrated by phosphor imaging analysis. Flupyradifurone is active on resistant pests, including cotton whiteflies, and is not metabolised by recombinantly expressed CYP6CM1, a cytochrome P450 conferring metabolic resistance to neonicotinoids and pymetrozine. CONCLUSION The novel butenolide insecticide flupyradifurone shows unique properties and will become a new tool for integrated pest management around the globe, as demonstrated by its insecticidal, ecotoxicological and safety profile. © 2014 The Authors. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry. PMID:25351824

  6. Seed coating with a neonicotinoid insecticide negatively affects wild bees.

    Science.gov (United States)

    Rundlöf, Maj; Andersson, Georg K S; Bommarco, Riccardo; Fries, Ingemar; Hederström, Veronica; Herbertsson, Lina; Jonsson, Ove; Klatt, Björn K; Pedersen, Thorsten R; Yourstone, Johanna; Smith, Henrik G

    2015-05-07

    Understanding the effects of neonicotinoid insecticides on bees is vital because of reported declines in bee diversity and distribution and the crucial role bees have as pollinators in ecosystems and agriculture. Neonicotinoids are suspected to pose an unacceptable risk to bees, partly because of their systemic uptake in plants, and the European Union has therefore introduced a moratorium on three neonicotinoids as seed coatings in flowering crops that attract bees. The moratorium has been criticized for being based on weak evidence, particularly because effects have mostly been measured on bees that have been artificially fed neonicotinoids. Thus, the key question is how neonicotinoids influence bees, and wild bees in particular, in real-world agricultural landscapes. Here we show that a commonly used insecticide seed coating in a flowering crop can have serious consequences for wild bees. In a study with replicated and matched landscapes, we found that seed coating with Elado, an insecticide containing a combination of the neonicotinoid clothianidin and the non-systemic pyrethroid β-cyfluthrin, applied to oilseed rape seeds, reduced wild bee density, solitary bee nesting, and bumblebee colony growth and reproduction under field conditions. Hence, such insecticidal use can pose a substantial risk to wild bees in agricultural landscapes, and the contribution of pesticides to the global decline of wild bees may have been underestimated. The lack of a significant response in honeybee colonies suggests that reported pesticide effects on honeybees cannot always be extrapolated to wild bees.

  7. Biological alterations and self-reported symptoms among insecticides-exposed workers in Burkina Faso.

    Science.gov (United States)

    Toe, Adama M; Ilboudo, Sylvain; Ouedraogo, Moustapha; Guissou, Pierre I

    2012-03-01

    Occupationally exposed workers, farm workers and plant protection agents in the Sahel region of Burkina Faso were interviewed to assess adverse health effects of insecticides. The subjects were also examined for changes in both hematological and biochemical parameters. The prevalence of liver and kidney dysfunction was found to be quite high among insecticide applicators, especially among plant protection agents. The prevalence of biochemical alterations seems to be correlated to the frequency of insecticide use. However, no significant differences were found between the hematological parameters among farm workers and plant protection agents. The hematological parameters of all the insecticide applicators were normal. The great majority of insecticide applicators (85%) reported symptoms related to insecticide exposure. The use of insecticides in the agriculture of Burkina Faso is threatening to human health.

  8. Toxicity of some insecticides to the haemocytes of giant honeybee, Apis dorsata F. under laboratory conditions

    Directory of Open Access Journals (Sweden)

    Nighat Perveen

    2017-07-01

    Full Text Available Quantitative studies concerning total and differential haemocyte counts and abnormalities were performed under laboratory conditions for larvae, pupae and adults collected from a wild Apis dorsata colony. Haemolymph samples were observed immediately, thirty and sixty minutes after field recommended concentration exposure of five different insecticides. Total haemocyte counts were significantly higher for larvae and pupae but less for adult bees, however, differential haemocyte counts insignificantly different. Exposure of insecticides showed variable response for tested insecticides with immediate increased change with ethofenprox, diafenthiuron and imidacloprid but decreased for all tested insecticides after sixty minutes. For differential haemocyte counts, plasmatocytes and granulocytes increased with exposure of insecticides. Immune response of haemocytes against insecticides showed different degrees of abnormalities like agglutination, denucleation and cell shape distortion. Such studies may help in possible identification of insect defense mechanisms against their exposure to external hazards for instance insecticide exposure.

  9. Inhibitors of the mitochondrial cytochrome b-c1 complex inhibit the cyanide-insensitive respiration of Trypanosoma brucei.

    Science.gov (United States)

    Turrens, J F; Bickar, D; Lehninger, A L

    1986-06-01

    The cyanide-insensitive respiration of bloodstream trypomastigote forms of Trypanosoma brucei (75 +/- 8 nmol O2 min-1(mg protein)-1) is completely inhibited by the mitochondrial ubiquinone-like inhibitors 2-hydroxy-3-undecyl-1,4-naphthoquinone (UHNQ) and 5-n-undecyl-6-hydroxy-4,7-dioxobenzothiazole (UHDBT). The Ki values for UHDBT (30 nM) and UHNQ (2 microM) are much lower than the reported Ki for salicylhydroxamic acid (SHAM) (5 microM), a widely used inhibitor of the cyanide-insensitive oxidase. UHNQ also stimulated the glycerol-3-phosphate-dependent reduction of phenazine methosulfate, demonstrating that the site of UHNQ inhibition is on the terminal oxidase of the cyanide-insensitive respiration of T. brucei. These results suggest that a ubiquinone-like compound may act as an electron carrier between the two enzymatic components of the cyanide-insensitive glycerol-3-phosphate oxidase.

  10. Radiation fixation of vinyl chloride in an insecticide aerosol container

    International Nuclear Information System (INIS)

    Kagiya, V.T.; Takemoto, K.

    1975-01-01

    Recently, a large quantity of vinyl chloride has been used as spraying additive for insecticide aerosols. Since January 1974 when the Food and Drug Administration of the United States of America announced that vinyl chloride causes liver cancer, it has been forbidden in Japan and the United States of America to market insecticide aerosol containers containing vinyl chloride. In Japan, following a government order, about 20 million insecticide aerosol containers have been collected and put into storage. A report is given on the radiation fixation of vinyl chloride as polyvinylchloride powder by gamma-ray-induced polymerization in the aerosol container. Insecticide aerosol containers containing vinyl chloride were irradiated by gamma rays from 60 Co at room temperature. Vinyl chloride polymerized to form powdered polymer in the container. Polymerization conversion increased with the irradiation dose, and after 10 Mrad irradiation, vinyl chloride was not found in the sprayed gas. This establishes that vinyl chloride can be fixed by gamma-ray irradiation in the aerosol container. To accelerate the reaction rate, the effect of various additives on the reaction was investigated. It was found that halogenated hydrocarbons, such as chloroform and carbon tetrachloride, accelerated the initiation of the polymerization, and that a vinyl monomer such as vinyl acetate accelerated the reaction rate due to the promotion of the initiation and the high reactivity of the polyvinylacetate radical to vinyl chloride. Consequently, the required irradiation dose for the fixation of vinyl chloride was decreased to less than 5 Mrad by the addition of various kinds of additives. Following the request of the Ministry of Public Welfare, various technical problems for large-scale treatment are being studied with the co-operation of the Federation of Insecticide Aerosols. (author)

  11. Agricultural insecticides threaten surface waters at the global scale.

    Science.gov (United States)

    Stehle, Sebastian; Schulz, Ralf

    2015-05-05

    Compared with nutrient levels and habitat degradation, the importance of agricultural pesticides in surface water may have been underestimated due to a lack of comprehensive quantitative analysis. Increasing pesticide contamination results in decreasing regional aquatic biodiversity, i.e., macroinvertebrate family richness is reduced by ∼30% at pesticide concentrations equaling the legally accepted regulatory threshold levels (RTLs). This study provides a comprehensive metaanalysis of 838 peer-reviewed studies (>2,500 sites in 73 countries) that evaluates, for the first time to our knowledge on a global scale, the exposure of surface waters to particularly toxic agricultural insecticides. We tested whether measured insecticide concentrations (MICs; i.e., quantified insecticide concentrations) exceed their RTLs and how risks depend on insecticide development over time and stringency of environmental regulation. Our analysis reveals that MICs occur rarely (i.e., an estimated 97.4% of analyses conducted found no MICs) and there is a complete lack of scientific monitoring data for ∼90% of global cropland. Most importantly, of the 11,300 MICs, 52.4% (5,915 cases; 68.5% of the sites) exceeded the RTL for either surface water (RTLSW) or sediments. Thus, the biological integrity of global water resources is at a substantial risk. RTLSW exceedances depend on the catchment size, sampling regime, and sampling date; are significantly higher for newer-generation insecticides (i.e., pyrethroids); and are high even in countries with stringent environmental regulations. These results suggest the need for worldwide improvements to current pesticide regulations and agricultural pesticide application practices and for intensified research efforts on the presence and effects of pesticides under real-world conditions.

  12. Insecticide resistance status of Aedes aegypti (L.) from Colombia.

    Science.gov (United States)

    Fonseca-González, Idalyd; Quiñones, Martha L; Lenhart, Audrey; Brogdon, William G

    2011-04-01

    To evaluate the insecticide susceptibility status of Aedes aegypti (L.) in Colombia, and as part of the National Network of Insecticide Resistance Surveillance, 12 mosquito populations were assessed for resistance to pyrethroids, organophosphates and DDT. Bioassays were performed using WHO and CDC methodologies. The underlying resistance mechanisms were investigated through biochemical assays and RT-PCR. All mosquito populations were susceptible to malathion, deltamethrin and cyfluthrin, and highly resistant to DDT and etofenprox. Resistance to lambda-cyhalothrin, permethrin and fenitrothion ranged from moderate to high in some populations from Chocó and Putumayo states. In Antioquia state, the Santa Fe population was resistant to fenitrothion. Biochemical assays showed high levels of both cytochrome P450 monooxygenases (CYP) and non-specific esterases (NSE) in some of the fenitrothion- and pyrethroid-resistant populations. All populations showed high levels of glutathione-S-transferase (GST) activity. GSTe2 gene was found overexpressed in DDT-resistant populations compared with Rockefeller susceptible strain. Differences in insecticide resistance status were observed between insecticides and localities. Although the biochemical assay results suggest that CYP and NSE could play an important role in the pyrethroid and fenitrothion resistance detected, other mechanisms remain to be investigated, including knockdown resistance. Resistance to DDT was high in all populations, and GST activity is probably the main enzymatic mechanism associated with this resistance. The results of this study provide baseline data on insecticide resistance in Colombian A. aegypti populations, and will allow comparison of changes in susceptibility status in this vector over time. Copyright © 2011 Society of Chemical Industry.

  13. Underpinning sustainable vector control through informed insecticide resistance management.

    Directory of Open Access Journals (Sweden)

    Edward K Thomsen

    Full Text Available There has been rapid scale-up of malaria vector control in the last ten years. Both of the primary control strategies, long-lasting pyrethroid treated nets and indoor residual spraying, rely on the use of a limited number of insecticides. Insecticide resistance, as measured by bioassay, has rapidly increased in prevalence and has come to the forefront as an issue that needs to be addressed to maintain the sustainability of malaria control and the drive to elimination. Zambia's programme reported high levels of resistance to the insecticides it used in 2010, and, as a result, increased its investment in resistance monitoring to support informed resistance management decisions.A country-wide survey on insecticide resistance in Zambian malaria vectors was performed using WHO bioassays to detect resistant phenotypes. Molecular techniques were used to detect target-site mutations and microarray to detect metabolic resistance mechanisms. Anopheles gambiae s.s. was resistant to pyrethroids, DDT and carbamates, with potential organophosphate resistance in one population. The resistant phenotypes were conferred by both target-site and metabolic mechanisms. Anopheles funestus s.s. was largely resistant to pyrethroids and carbamates, with potential resistance to DDT in two locations. The resistant phenotypes were conferred by elevated levels of cytochrome p450s.Currently, the Zambia National Malaria Control Centre is using these results to inform their vector control strategy. The methods employed here can serve as a template to all malaria-endemic countries striving to create a sustainable insecticide resistance management plan.

  14. Insecticidal Activity of Melaleuca alternifolia Essential Oil and RNA-Seq Analysis of Sitophilus zeamais Transcriptome in Response to Oil Fumigation.

    Directory of Open Access Journals (Sweden)

    Min Liao

    Full Text Available The cereal weevil, Sitophilus zeamais is one of the most destructive pests of stored cereals worldwide. Frequent use of fumigants for managing stored-product insects has led to the development of resistance in insects. Essential oils from aromatic plants including the tea oil plant, Melaleuca alternifolia may provide environmentally friendly alternatives to currently used pest control agents. However, little is known about molecular events involved in stored-product insects in response to plant essential oil fumigation.M. alternifolia essential oil was shown to possess the fumigant toxicity against S. zeamais. The constituent, terpinen-4-ol was the most effective compound for fumigant toxicity. M. alternifolia essential oil significantly inhibited the activity of three enzymes in S. zeamais, including two detoxifying enzymes, glutathione S-transferase (GST, and carboxylesterase (CarE, as well as a nerve conduction enzyme, acetylcholinesterase (AChE. Comparative transcriptome analysis of S. zeamais through RNA-Seq identified a total of 3,562 differentially expressed genes (DEGs, of which 2,836 and 726 were up-regulated and down-regulated in response to M. alternifolia essential oil fumigation, respectively. Based on gene ontology (GO analysis, the majority of DEGs were involved in insecticide detoxification and mitochondrial function. Furthermore, an abundance of DEGs mapped into the metabolism pathway in the Kyoto Encyclopedia of Genes and Genomes (KEGG pathway database were associated with respiration and metabolism of xenobiotics, including cytochrome P450s, CarEs, GSTs, and ATP-binding cassette transporters (ABC transporters. Some DEGs mapped into the proteasome and phagosome pathway were found to be significantly enriched. These results led us to propose a model of insecticide action that M. alternifolia essential oil likely directly affects the hydrogen carrier to block the electron flow and interfere energy synthesis in mitochondrial

  15. Insecticidal Activity of Melaleuca alternifolia Essential Oil and RNA-Seq Analysis of Sitophilus zeamais Transcriptome in Response to Oil Fumigation.

    Science.gov (United States)

    Liao, Min; Xiao, Jin-Jing; Zhou, Li-Jun; Liu, Yang; Wu, Xiang-Wei; Hua, Ri-Mao; Wang, Gui-Rong; Cao, Hai-Qun

    2016-01-01

    The cereal weevil, Sitophilus zeamais is one of the most destructive pests of stored cereals worldwide. Frequent use of fumigants for managing stored-product insects has led to the development of resistance in insects. Essential oils from aromatic plants including the tea oil plant, Melaleuca alternifolia may provide environmentally friendly alternatives to currently used pest control agents. However, little is known about molecular events involved in stored-product insects in response to plant essential oil fumigation. M. alternifolia essential oil was shown to possess the fumigant toxicity against S. zeamais. The constituent, terpinen-4-ol was the most effective compound for fumigant toxicity. M. alternifolia essential oil significantly inhibited the activity of three enzymes in S. zeamais, including two detoxifying enzymes, glutathione S-transferase (GST), and carboxylesterase (CarE), as well as a nerve conduction enzyme, acetylcholinesterase (AChE). Comparative transcriptome analysis of S. zeamais through RNA-Seq identified a total of 3,562 differentially expressed genes (DEGs), of which 2,836 and 726 were up-regulated and down-regulated in response to M. alternifolia essential oil fumigation, respectively. Based on gene ontology (GO) analysis, the majority of DEGs were involved in insecticide detoxification and mitochondrial function. Furthermore, an abundance of DEGs mapped into the metabolism pathway in the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway database were associated with respiration and metabolism of xenobiotics, including cytochrome P450s, CarEs, GSTs, and ATP-binding cassette transporters (ABC transporters). Some DEGs mapped into the proteasome and phagosome pathway were found to be significantly enriched. These results led us to propose a model of insecticide action that M. alternifolia essential oil likely directly affects the hydrogen carrier to block the electron flow and interfere energy synthesis in mitochondrial respiratory chain

  16. Acetylcholinesterase inhibition starting from extracts of Bauhinia variegata L., Bauhinia var. candida (Aiton) Buch.-Ham., and Bauhinia ungulata L.

    Science.gov (United States)

    Santos, Kamilla Monteiro dos; Gonçalves, Priscila Sant'Ana; Paiva, Maria José Nunes de; Lacerda, Guilherme Araújo

    2011-01-01

    A treatment to the Alzheimer's disease consists inhibition of the acetylcholinesterase, which is responsible for the acetylcholine control in the synapses. We have investigated the potential of inhibition of the acetylcholinesterase produced by hexane extracts of leaves, branches, and flowers from three Bauhinia specimens, which is based on the technique of thin layer chromatography and on identifying the organ of the plant that possesses larger concentration of inhibitors. Retention factor analysis shows values of 0.31aA, 0.31aA, and 0.46aB for flowers B. variegata, B. var. candida, and B. ungulata, respectively. The flower extract of B. ungulata is the most suitable for further studies on this inhibition.

  17. Broadband Polarization-Insensitive Wavelength Conversion Based on Non-Degenerate Four-Wave Mixing in a Silicon Nanowire

    DEFF Research Database (Denmark)

    Pu, Minhao; Hu, Hao; Ji, Hua

    2012-01-01

    We experimentally demonstrate broadband polarization-insensitive one-to-two wavelength conversion of a 10-Gb/s DPSK data signal based on non-degenerate four-wave mixing in a silicon nanowire with bit-error rate measurements.......We experimentally demonstrate broadband polarization-insensitive one-to-two wavelength conversion of a 10-Gb/s DPSK data signal based on non-degenerate four-wave mixing in a silicon nanowire with bit-error rate measurements....

  18. In Vitro Ability of Currently Available Oximes to Reactivate Organophosphate Pesticide-Inhibited Human Acetylcholinesterase and Butyrylcholinesterase

    OpenAIRE

    Kamil Musilek; Kamil Kuca; Daniel Jun; Lucie Musilova

    2011-01-01

    We have in vitro tested the ability of common, commercially available, cholinesterase reactivators (pralidoxime, obidoxime, methoxime, trimedoxime and HI-6) to reactivate human acetylcholinesterase (AChE), inhibited by five structurally different organophosphate pesticides and inhibitors (paraoxon, dichlorvos, DFP, leptophos-oxon and methamidophos). We also tested reactivation of human butyrylcholinesterase (BChE) with the aim of finding a potent oxime, suitable to serve as a “pseudocatalytic...

  19. In Search of an Effective in vivo Reactivator for Organophosphorus Nerve Agent-Inhibited Acetylcholinesterase in the Central Nervous System

    Science.gov (United States)

    2012-01-01

    nerve agents, such as sarin (GB), cyclosarin (GF), and VX, are potent inhibitors of the enzyme cholinesterase (ChE). Their toxic effects are due to...three nerve agents. Keywords: acetylcholinesterase; brain; cholinesterase inhibition; cholinesterase reactivation; cyclosarin; diacetylmonoxime...attributed, at least in part, to nuclophilic impedance [Ekstrom et al., 2006a; b; Hoskovcova et al., 2007]. Other AChE- inhibitors , such as soman, become

  20. Assessing the concept of structure sensitivity or insensitivity for sub-nanometer catalyst materials

    Science.gov (United States)

    Crampton, Andrew S.; Rötzer, Marian D.; Ridge, Claron J.; Yoon, Bokwon; Schweinberger, Florian F.; Landman, Uzi; Heiz, Ueli

    2016-10-01

    The nature of the nano-catalyzed hydrogenation of ethylene, yielding benchmark information pertaining to the concept of structure sensitivity/insensitivity and its applicability at the bottom of the catalyst particle size-range, is explored with experiments on size-selected Ptn (n = 7-40) clusters soft-landed on MgO, in conjunction with first-principles simulations. As in the case of larger particles both the direct ethylene hydrogenation channel and the parallel hydrogenation-dehydrogenation ethylidyne-producing route must be considered, with the fundamental uncovering that at the reaction exhibits characteristics consistent with structure sensitivity, in contrast to the structure insensitivity found for larger particles. In this size-regime, the chemical properties can be modulated and tuned by a single atom, reflected by the onset of low temperature hydrogenation at T > 150 K catalyzed by Ptn (n ≥ 10) clusters, with maximum room temperature reactivity observed for Pt13 using a pulsed molecular beam technique. Structure insensitive behavior, inherent for specific cluster sizes at ambient temperatures, can be induced in the more active sizes, e.g. Pt13, by a temperature increase, up to 400 K, which opens dehydrogenation channels leading to ethylidyne formation. This reaction channel was, however found to be attenuated on Pt20, as catalyst activity remained elevated after the 400 K step. Pt30 displayed behavior which can be understood from extrapolating bulk properties to this size range; in particular the calculated d-band center. In the non-scalable sub-nanometer size regime, however, precise control of particle size may be used for atom-by-atom tuning and manipulation of catalyzed hydrogenation activity and selectivity.

  1. Flavonoids, Antioxidant Potential, and Acetylcholinesterase Inhibition Activity of the Extracts from the Gametophyte and Archegoniophore of Marchantia polymorpha L.

    Directory of Open Access Journals (Sweden)

    Xin Wang

    2016-03-01

    Full Text Available Marchantia polymorpha L. is a representative bryophyte used as a traditional Chinese medicinal herb for scald and pneumonia. The phytochemicals in M. polymorpha L. are terpenoids and flavonoids, among which especially the flavonoids show significant human health benefits. Many researches on the gametophyte of M. polymorpha L. have been reported. However, as the reproductive organ of M. polymorpha L., the bioactivity and flavonoids profile of the archegoniophore have not been reported, so in this work the flavonoid profiles, antioxidant and acetylcholinesterase inhibition activities of the extracts from the archegoniophore and gametophyte of M. polymorpha L. were compared by radical scavenging assay methods (DPPH, ABTS, O2−, reducing power assay, acetylcholinesterase inhibition assay and LC-MS analysis. The results showed that the total flavonoids content in the archegoniophore was about 10-time higher than that of the gametophyte. Differences between the archegoniophore and gametophyte of M. polymorpha L. were observed by LC-MS analysis. The archegoniophore extracts showed stronger bio-activities than those of the gametophyte. The archegoniophore extract showed a significant acetylcholinesterase inhibition, while the gametophyte extract hardly inhibited it.

  2. Distribution of intravenously administered acetylcholinesterase inhibitor and acetylcholinesterase activity in the adrenal gland: 11C-donepezil PET study in the normal rat.

    Science.gov (United States)

    Watabe, Tadashi; Naka, Sadahiro; Ikeda, Hayato; Horitsugi, Genki; Kanai, Yasukazu; Isohashi, Kayako; Ishibashi, Mana; Kato, Hiroki; Shimosegawa, Eku; Watabe, Hiroshi; Hatazawa, Jun

    2014-01-01

    Acetylcholinesterase (AChE) inhibitors have been used for patients with Alzheimer's disease. However, its pharmacokinetics in non-target organs other than the brain has not been clarified yet. The purpose of this study was to evaluate the relationship between the whole-body distribution of intravenously administered (11)C-Donepezil (DNP) and the AChE activity in the normal rat, with special focus on the adrenal glands. The distribution of (11)C-DNP was investigated by PET/CT in 6 normal male Wistar rats (8 weeks old, body weight  = 220 ± 8.9 g). A 30-min dynamic scan was started simultaneously with an intravenous bolus injection of (11)C-DNP (45.0 ± 10.7 MBq). The whole-body distribution of the (11)C-DNP PET was evaluated based on the Vt (total distribution volume) by Logan-plot analysis. A fluorometric assay was performed to quantify the AChE activity in homogenized tissue solutions of the major organs. The PET analysis using Vt showed that the adrenal glands had the 2nd highest level of (11)C-DNP in the body (following the liver) (13.33 ± 1.08 and 19.43 ± 1.29 ml/cm(3), respectively), indicating that the distribution of (11)C-DNP was the highest in the adrenal glands, except for that in the excretory organs. The AChE activity was the third highest in the adrenal glands (following the small intestine and the stomach) (24.9 ± 1.6, 83.1 ± 3.0, and 38.5 ± 8.1 mU/mg, respectively), indicating high activity of AChE in the adrenal glands. We demonstrated the whole-body distribution of (11)C-DNP by PET and the AChE activity in the major organs by fluorometric assay in the normal rat. High accumulation of (11)C-DNP was observed in the adrenal glands, which suggested the risk of enhanced cholinergic synaptic transmission by the use of AChE inhibitors.

  3. Distribution of intravenously administered acetylcholinesterase inhibitor and acetylcholinesterase activity in the adrenal gland: 11C-donepezil PET study in the normal rat.

    Directory of Open Access Journals (Sweden)

    Tadashi Watabe

    Full Text Available PURPOSE: Acetylcholinesterase (AChE inhibitors have been used for patients with Alzheimer's disease. However, its pharmacokinetics in non-target organs other than the brain has not been clarified yet. The purpose of this study was to evaluate the relationship between the whole-body distribution of intravenously administered (11C-Donepezil (DNP and the AChE activity in the normal rat, with special focus on the adrenal glands. METHODS: The distribution of (11C-DNP was investigated by PET/CT in 6 normal male Wistar rats (8 weeks old, body weight  = 220 ± 8.9 g. A 30-min dynamic scan was started simultaneously with an intravenous bolus injection of (11C-DNP (45.0 ± 10.7 MBq. The whole-body distribution of the (11C-DNP PET was evaluated based on the Vt (total distribution volume by Logan-plot analysis. A fluorometric assay was performed to quantify the AChE activity in homogenized tissue solutions of the major organs. RESULTS: The PET analysis using Vt showed that the adrenal glands had the 2nd highest level of (11C-DNP in the body (following the liver (13.33 ± 1.08 and 19.43 ± 1.29 ml/cm(3, respectively, indicating that the distribution of (11C-DNP was the highest in the adrenal glands, except for that in the excretory organs. The AChE activity was the third highest in the adrenal glands (following the small intestine and the stomach (24.9 ± 1.6, 83.1 ± 3.0, and 38.5 ± 8.1 mU/mg, respectively, indicating high activity of AChE in the adrenal glands. CONCLUSIONS: We demonstrated the whole-body distribution of (11C-DNP by PET and the AChE activity in the major organs by fluorometric assay in the normal rat. High accumulation of (11C-DNP was observed in the adrenal glands, which suggested the risk of enhanced cholinergic synaptic transmission by the use of AChE inhibitors.

  4. Genetics of flowering time in bread wheat Triticum aestivum: complementary interaction between vernalization-insensitive and photoperiod-insensitive mutations imparts very early flowering habit to spring wheat.

    Science.gov (United States)

    Kumar, Sushil; Sharma, Vishakha; Chaudhary, Swati; Tyagi, Anshika; Mishra, Poonam; Priyadarshini, Anupama; Singh, Anupam

    2012-01-01

    Time to flowering in the winter growth habit bread wheat is dependent on vernalization (exposure to cold conditions) and exposure to long days (photoperiod). Dominant Vrn-1 (Vrn-A1, Vrn-B1 and Vrn-D1) alleles are associated with vernalization independent spring growth habit. The semidominant Ppd-D1a mutation confers photoperiod-insensitivity or rapid flowering in wheat under short day and long day conditions. The objective of this study was to reveal the nature of interaction between Vrn-1 and Ppd-D1a mutations (active alleles of the respective genes vrn-1 and Ppd-D1b). Twelve Indian spring wheat cultivars and the spring wheat landrace Chinese Spring were characterized for their flowering times by seeding them every month for five years under natural field conditions in New Delhi. Near isogenic Vrn-1 Ppd-D1 and Vrn-1 Ppd-D1a lines constructed in two genetic backgrounds were also phenotyped for flowering time by seeding in two different seasons. The wheat lines of Vrn-A1a Vrn-B1 Vrn-D1 Ppd-D1a, Vrn-A1a Vrn-B1 Ppd-D1a and Vrn-A1a Vrn-D1 Ppd-D1a (or Vrn-1 Ppd-D1a) genotypes flowered several weeks earlier than that of Vrn-A1a Vrn-B1 Vrn-D1 Ppd-D1b, Vrn-A1b Ppd-D1b and Vrn-D1 Ppd-D1b (or Vrn-1 Ppd-D1b) genotypes. The flowering time phenotypes of the isogenic vernalization-insensitive lines confirmed that Ppd-D1a hastened flowering by several weeks. It was concluded that complementary interaction between Vrn-1 and Ppd-D1a active alleles imparted super/very-early flowering habit to spring wheats. The early and late flowering wheat varieties showed differences in flowering time between short day and long day conditions. The flowering time in Vrn-1 Ppd-D1a genotypes was hastened by higher temperatures under long day conditions. The ambient air temperature and photoperiod parameters for flowering in spring wheat were estimated at 25°C and 12 h, respectively.

  5. Complete Androgen Insensitivity Syndrome: A Rare Case of Disorder of Sex Development

    Directory of Open Access Journals (Sweden)

    Alfonsa Pizzo

    2013-01-01

    Full Text Available Androgen Insensitivity Syndrome (AIS could be considered as a disease that causes resistance to androgens actions, influencing both the morphogenesis and differentiation of the body structures, and systems in which this hormone exerts its effects. It depends on an X-linked mutations in the Androgen Receptor (AR gene that express a variety of phenotypes ranging from male infertility to completely normal female external genitalia. The clinical phenotypes of AIS could vary and be classified into three categories, as complete (CAIS, partial (PAIS, and mild (MAIS forms, according to the severity of androgen resistance. We will describe a case of CAIS in a 16-year-old patient.

  6. Challenges in clinical and laboratory diagnosis of androgen insensitivity syndrome: a case report

    Directory of Open Access Journals (Sweden)

    Silva Daniela M

    2011-09-01

    Full Text Available Abstract Introduction Androgen is a generic term usually applied to describe a group of sex steroid hormones. Androgens are responsible for male sex differentiation during embryogenesis at the sixth or seventh week of gestation, triggering the development of the testes and penis in male fetuses, and are directed by the testicular determining factor: the gene SRY (sex determining region on Y chromosome located on the short arm of chromosome Y. The differentiation of male external genitalia (penis, scrotum and penile urethra occurs between the 9th and 13th weeks of pregnancy and requires adequate concentration of testosterone and the conversion of this to another more potent androgen, dihydrotestosterone, through the action of 5α-reductase in target tissues. Case presentation This report describes the case of a teenage girl presenting with a male karyotype, and aims to determine the extension of the mutation that affected the AR gene. A Caucasian girl aged 15 was referred to our laboratory for genetic testing due to primary amenorrhea. Physical examination, karyotype testing and molecular analysis of the androgen receptor were critical in making the correct diagnosis of complete androgen insensitivity syndrome. Conclusions Sex determination and differentiation depend on a cascade of events that begins with the establishment of chromosomal sex at fertilization and ends with sexual maturation at puberty, subsequently leading to fertility. Mutations affecting the AR gene may cause either complete or partial androgen insensitivity syndrome. The case reported here is consistent with complete androgen insensitivity syndrome, misdiagnosed at birth, and consequently our patient was raised both socially and educationally as a female. It is critical that health care providers understand the importance of properly diagnosing a newborn manifesting ambiguous genitalia. Furthermore, a child with a pseudohermaphrodite phenotype should always undergo adequate

  7. Antimicrobial and acetylcholinesterase inhibitory activities of Buddleja salviifolia (L.) Lam. leaf extracts and isolated compounds.

    Science.gov (United States)

    Pendota, S C; Aderogba, M A; Ndhlala, A R; Van Staden, J

    2013-07-09

    Buddleja salviifolia leaves are used for the treatment of eye infections and neurodegenerative conditions by various tribes in South Africa. This study was designed to isolate the phenolic constituents from the leaf extracts of Buddleja salviifolia and evaluate their antimicrobial and acetylcholinesterase (AChE) activities. Three phenolic compounds were isolated from the ethyl acetate fraction of a 20% aqueous methanol leaf extract of Buddleja salviifolia using Sephadex LH-20 and silica gel columns. Structure elucidation of the isolated compounds was carried out using spectroscopic techniques: mass spectrometry (ESI-TOF-MS) and NMR (1D and 2D). The extracts and isolated compounds were evaluated for antimicrobial and acetylcholinesterase activities using the microdilution technique. The bacteria used for the antimicrobial assays were Gram-positive Bacillus subtilis and Staphylococcus aureus and Gram-negative Escherichia coli and Klebsiella pneumoniae. The isolated compounds were characterized as: 4'-hydroxyphenyl ethyl vanillate (1) a new natural product, acteoside (2) and quercetin (3). The crude extract, fractions and the isolated compounds from the leaves of the plant exhibited a broad spectrum of antibacterial activity. The EtOAc fraction exhibited good activity against Bacillus subtilis and Staphylococcus aureus with MIC values ranging from 780.0 to 390.0 µg/mL. Isolated compound 2 exhibited good activity against Staphylococcus aureus with an MIC value of 62.5 µg/mL. The hexane and DCM fractions of leaves showed the best activity against Candida albicans with MIC and MFC values of 390.0 µg/mL. In the AChE inhibitory test, among the tested extracts, the hexane fraction was the most potent with an IC50 value of 107.4 µg/mL, whereas for the isolated compounds, it was compound (3) (quercetin) with an IC50 value of 66.8 µg/mL. Activities demonstrated by the extracts and isolated compounds support the ethnopharmacological use of Buddleja salviifolia against eye

  8. Acetylcholinesterase in honey bees (Apis mellifera) exposed to neonicotinoids, atrazine and glyphosate: laboratory and field experiments.

    Science.gov (United States)

    Boily, Monique; Sarrasin, Benoit; Deblois, Christian; Aras, Philippe; Chagnon, Madeleine

    2013-08-01

    In Québec, as observed globally, abnormally high honey bee mortality rates have been reported recently. Several potential contributing factors have been identified, and exposure to pesticides is of increasing concern. In maize fields, foraging bees are exposed to residual concentrations of insecticides such as neonicotinoids used for seed coating. Highly toxic to bees, neonicotinoids are also reported to increase AChE activity in other invertebrates exposed to sub-lethal doses. The purpose of this study was therefore to test if the honey bee's AChE activity could be altered by neonicotinoid compounds and to explore possible effects of other common products used in maize fields: atrazine and glyphosate. One week prior to pollen shedding, beehives were placed near three different field types: certified organically grown maize, conventionally grown maize or non-cultivated. At the same time, caged bees were exposed to increasing sub-lethal doses of neonicotinoid insecticides (imidacloprid and clothianidin) and herbicides (atrazine and glyphosate) under controlled conditions. While increased AChE activity was found in all fields after 2 weeks of exposure, bees close to conventional maize crops showed values higher than those in both organic maize fields and non-cultivated areas. In caged bees, AChE activity increased in response to neonicotinoids, and a slight decrease was observed by glyphosate. These results are discussed with regard to AChE activity as a potential biomarker of exposure for neonicotinoids.

  9. Probabilistic risk assessment of insecticide concentrations in agricultural surface waters: a critical appraisal.

    Science.gov (United States)

    Stehle, Sebastian; Knäbel, Anja; Schulz, Ralf

    2013-08-01

    Due to the specific modes of action and application patterns of agricultural insecticides, the insecticide exposure of agricultural surface waters is characterized by infrequent and short-term insecticide concentration peaks of high ecotoxicological relevance with implications for both monitoring and risk assessment. Here, we apply several fixed-interval strategies and an event-based sampling strategy to two generalized and two realistic insecticide exposure patterns for typical agricultural streams derived from FOCUS exposure modeling using Monte Carlo simulations. Sampling based on regular intervals was found to be inadequate for the detection of transient insecticide concentrations, whereas event-triggered sampling successfully detected all exposure incidences at substantially lower analytical costs. Our study proves that probabilistic risk assessment (PRA) concepts in their present forms are not appropriate for a thorough evaluation of insecticide exposure. Despite claims that the PRA approach uses all available data to assess exposure and enhances risk assessment realism, we demonstrate that this concept is severely biased by the amount of insecticide concentrations below detection limits and therefore by the sampling designs. Moreover, actual insecticide exposure is of almost no relevance for PRA threshold level exceedance frequencies and consequential risk assessment outcomes. Therefore, we propose a concept that features a field-relevant ecological risk analysis of agricultural insecticide surface water exposure. Our study quantifies for the first time the environmental and economic consequences of inappropriate monitoring and risk assessment concepts used for the evaluation of short-term peak surface water pollutants such as insecticides.

  10. Ultrathin triple-band polarization-insensitive wide-angle compact metamaterial absorber

    International Nuclear Information System (INIS)

    Shang, Shuai; Yang, Shizhong; Tao, Lu; Yang, Lisheng; Cao, Hailin

    2016-01-01

    In this study, the design, realization, and characterization of an ultrathin triple-band polarization-insensitive wide-angle metamaterial absorber are reported. The metamaterial absorber comprises a periodic array of modified six-fold symmetric snowflake-shaped resonators with strip spiral line load, which is printed on a dielectric substrate backed by a metal ground plane. It is shown that the absorber exhibits three distinct near-unity absorption peaks, which are distributed across C, X, Ku bands, respectively. Owing to the six-fold symmetry, the absorber is insensitive to the polarization of the incident radiation. In addition, the absorber shows excellent absorption performance over wide oblique incident angles for both transverse electric and transverse magnetic polarizations. Simulated surface current and field distributions at the three absorption peaks are demonstrated to understand the absorption mechanism. Particularly, the absorption modes come from the fundamental and high-order dipole resonances. Furthermore, the experimental verification of the designed absorber is conducted, and the measured results are in reasonable agreement with the simulated ones. The proposed ultrathin (∼0.018λ 0 , λ 0 corresponding to the lowest peak absorption frequency) compact (0.168λ 0 ×0.168λ 0 corresponding to the area of a unit cell) absorber enables potential applications such as stealth technology, electromagnetic interference and spectrum identification.

  11. A two-stage extraction procedure for insensitive munition (IM) explosive compounds in soils.

    Science.gov (United States)

    Felt, Deborah; Gurtowski, Luke; Nestler, Catherine C; Johnson, Jared; Larson, Steven

    2016-12-01

    The Department of Defense (DoD) is developing a new category of insensitive munitions (IMs) that are more resistant to detonation or promulgation from external stimuli than traditional munition formulations. The new explosive constituent compounds are 2,4-dinitroanisole (DNAN), nitroguanidine (NQ), and nitrotriazolone (NTO). The production and use of IM formulations may result in interaction of IM component compounds with soil. The chemical properties of these IM compounds present unique challenges for extraction from environmental matrices such as soil. A two-stage extraction procedure was developed and tested using several soil types amended with known concentrations of IM compounds. This procedure incorporates both an acidified phase and an organic phase to account for the chemical properties of the IM compounds. The method detection limits (MDLs) for all IM compounds in all soil types were regulatory risk-based Regional Screening Level (RSL) criteria for soil proposed by the U.S. Army Public Health Center. At defined environmentally relevant concentrations, the average recovery of each IM compound in each soil type was consistent and greater than 85%. The two-stage extraction method decreased the influence of soil composition on IM compound recovery. UV analysis of NTO established an isosbestic point based on varied pH at a detection wavelength of 341 nm. The two-stage soil extraction method is equally effective for traditional munition compounds, a potentially important point when examining soils exposed to both traditional and insensitive munitions. Copyright © 2016 Elsevier Ltd. All rights reserved.

  12. A flow time model for melt-cast insensitive explosive process

    Energy Technology Data Exchange (ETDEWEB)

    Guillemin, Jean-Philippe; Brunet, Luc [Nexter Munitions, 7 Route de Guerry, 18023 Bourges Cedex (France); Bonnefoy, Olivier; Thomas, Gerard [Ecole Nationale Superieure des Mines de Saint-Etienne, Centre SPIN/LPMG, UMR CNRS 5148, 158 Cours Fauriel, 42023 Saint-Etienne Cedex 2 (France)

    2007-06-15

    Diphasic flows of concentrated suspensions of melt-cast insensitive explosives exhibit specific rheological properties. In order to limit the handling of pyrotechnical products presenting a risk with respect to the mechanical and thermal shocks, a lot of work has been undertaken for many years in the civil engineering sector. The objective of this study is to propose a predictive model of the flow time of a concentrated suspension through a nozzle located at the bottom of a tank. Similar to our industrial process, the suspension is made out of insensitive energetic materials and flows under gravity. Experimental results are compared to three models (Quemada, Krieger-Dougherty, and Mooney) predicting the viscosity {mu} of a suspension as a function of the solid volume fraction {phi}, the maximum packing density {phi}{sub m} and the viscosity {mu}{sub 0} of the interstitial liquid. De Larrard's model is used to calculate {phi}{sub m}. The value of viscosity measured for the pure liquid is close to the one predicted by the Bernoulli theorem, where liquids are considered as incompressible and inviscid. Finally, it was found that the Quemada's model gives a fair agreement between predictions and experiments. (Abstract Copyright [2007], Wiley Periodicals, Inc.)

  13. Insensitive high-energy energetic structural material of tungsten-polytetrafluoroethylene-aluminum composites

    Directory of Open Access Journals (Sweden)

    Liu Wang

    2015-11-01

    Full Text Available Energetic structural material is a kind of materials that are inert under normal conditions but could produce exothermic chemical reaction when subjected to impact. This report shows a kind of energetic structural material of tungsten (W-polytetrafluoroethylene (PTFE-aluminum (Al with density of 4.12 g/cm3, excellent ductility and dynamic compressive strength of 96 MPa. Moreover, 50W-35PTFE-15Al (wt% can exhibit a high reaction energy value of more than 2 times of TNT per unit mass and 5 times of TNT per unit volume, respectively, but with excellent insensitivity compared with traditional explosives. Under thermal conditions, the W-PTFE-Al composite can keep stable at 773 K. Under impact loading, when the strain rate up to ∼4820 s−1 coupled with the absorbed energy per unit volume of 120 J/cm3, deflagration occurs and combustion lasts for 500 μs. During impact compressive deformation, the PTFE matrix is elongated into nano-fibers, thus significantly increases the reaction activity of W-PTFE-Al composites. The nano-fiber structure is necessary for the reaction of W-PTFE-Al composites. The formation of PTFE nano-fibers must undergo severe plastic deformation, and therefore the W-PTFE-Al composites exhibit excellent insensitivity and safety. Furthermore, the reaction mechanisms of W-PTFE-Al composites in argon and in air are revealed.

  14. Identification of genetically diverse genotypes for photoperiod insensitivity in soybean using RAPD markers.

    Science.gov (United States)

    Singh, R K; Bhatia, V S; Yadav, Sanjeev; Athale, Rashmi; Lakshmi, N; Guruprasad, K N; Chauhan, G S

    2008-10-01

    Most of the Indian soybean varieties were found to be highly sensitive to photoperiod, which limits their cultivation in only localized area. Identification of genetically diverse source of photoperiod insensitive would help to broaden the genetic base for this trait. Present study was undertaken with RAPD markers for genetic diversity estimation in 44 accessions of soybean differing in response to photoperiod sensitivity. The selected twenty-five RAPD primers produced a total of 199 amplicons, which generated 89.9 % polymorphism. The number of amplification products ranged from 2 to 13 for different primers. The polymorphism information content ranged from 0.0 for monomorphic loci to 0.5 with an average of 0.289. Genetic diversity between pairs of genotypes was 37.7% with a range of 3.9 to 71.6%. UPGMA cluster analysis placed all the accessions of soybean into four major clusters. No discernable geographical patterns were observed in clustering however; the smaller groups corresponded well with pedigree. Mantel's test (r = 0.915) indicates very good fit for clustering pattern. Two genotypes, MACS 330 and 111/2/1939 made a very divergent group from other accessions of soybean and highly photoperiod insensitive that may be potential source for broadening the genetic base of soybean for this trait.

  15. OM4 bend insensitive multi-mode fibers’ usefulness for MCM integration

    International Nuclear Information System (INIS)

    Guzowski, Bartłomiej; Lisik, Zbigniew; Tosik, Grzegorz; Ciupa, Emilia

    2012-01-01

    Highlights: ► The influence of high temperature exposure on OM4 fibers’ mechanical properties. ► Researching OM4 class fibers for use in innovative Optical Multi Chip Module. ► The influence of bending at a very small radius, up to 2 mm, on MM fibers. - Abstract: For future generations of electronic systems, a severe bottleneck is expected on the interconnection level and the use of optical interconnection is considered as one of the most promising solutions in this matter. Recent progress in fiber development resulted in new generation of optical fibers that are bend insensitive. This makes them ideal for Multi Chip Module (MCM) application. This paper focuses on OM4 bend insensitive multi-mode fibers’ usefulness for MCM integration, particularly the investigation of MM fiber loss is presented, which is influenced by bend diameter and the fiber's mechanical performance under influence of high temperature (400 °C–1000 °C adequate to MCM production process).

  16. Divalent phosphate is a counterion for carboxyatractyloside-insensitive adenine nucleotide transport in rat liver mitochondria

    International Nuclear Information System (INIS)

    Nosek, M.T.; Aprille, J.R.

    1986-01-01

    Unidirectional, carboxyatractyloside(CAT)-insensitive adenine nucleotide (AdN) fluxes have been studied in isolated rat liver mitochondria (mito). Previous work has shown that ATP x Mg transport in one direction is coupled to ATP x Mg or P/sub i/ transport in the opposite direction. The purpose of this study was to determine whether divalent HPO 4 2- or monovalent H 2 PO 4 - is the transported phosphate species. The authors used the monofluorophosphate (PO 3 F 2- ) and difluorophosphate (PO 2 F 2 - ) analogues as potential counterions forAdN efflux. After a preincubation on ice with 14 C-ADP to label the matrix AdN, efflux was measured at 30 0 C, pH 7.4, in 225mM sucrose, 10mM KCl, 5mM MgCl 2 , 5mM glutamate, 5mM malate, 10mM Tris, 0.5mM P/sub i/, 1mM ATP, and 5μM CAT. With no other additions efflux was -0.62 +/- 0.20 nmole/minute/mg protein. The data supports the hypothesis that divalent but not monovalent phosphate can act as a counterion for ATPx Mg transport over this CAT-insensitive carrier

  17. A Robust, Gravity-Insensitive, High-Temperature Condenser for Water Recovery

    Science.gov (United States)

    Chen, Weibo; Conboy, Thomas; Ewert, Michael

    2016-01-01

    Regenerative life support systems are vital for NASA's future long-duration human space exploration missions. A Heat Melt Compactor (HMC) system is being developed by NASA to dry and compress trash generated during space missions. The resulting water vapor is recovered and separated from the process gas flow by a gravity-insensitive condenser. Creare is developing a high-temperature condenser for this application. The entire condenser is constructed from metals that have excellent resistance to chemical attack from contaminants and is suitable for high-temperature operation. The metal construction and design configuration also offer greatest flexibility for potential coating and regeneration processes to reduce biofilm growth and thus enhancing the reliability of the condenser. The proposed condenser builds on the gravity-insensitive phase separator technology Creare developed for aircraft and spacecraft applications. This paper will first discuss the design requirements for the condenser in an HMC system that will be demonstrated on the International Space Station (ISS). Then, it will present the overall design of the condenser and the preliminary thermal test results of a subscale condenser. Finally, this paper will discuss the predicted performance of the full-size condenser and the development plan to mature the technology and enhance its long-term reliability for a flight system.

  18. Overproduction of alpha chains provides a proton-insensitive component to the bluefish hemoglobin system.

    Science.gov (United States)

    Bonaventura, Celia; Godette, Gerald; Stevens, Robert; Brenowitz, Michael; Henkens, Robert

    2005-12-09

    Expression of alpha and beta chains and their post-translational assembly into alpha(2)beta(2) tetramers is fundamental to the formation and function of most vertebrate hemoglobins. There is a strong evolutionary bias that favors expression of equal amounts of the two types of chains, because cooperativity, pH sensitivity, and anionic control of function occurs only for the alpha(2)beta(2) tetramers. Remarkably, an over-production of alpha chains, as in the pathological condition known as beta thalassemia in humans, is adaptive rather than pathological in the bluefish hemoglobin system. The thalassemia of the bluefish is a novel means of providing for oxygen uptake and delivery when low pH conditions incapacitate the highly pH-sensitive Root effect hemoglobins of the fish. Although fish often have pH-insensitive along with highly pH-sensitive hemoglobins, having pH-insensitive alpha chain monomers in circulation is an unusual structural variation. The role of bluefish alpha chains in oxygen transport is enabled by their remarkably lower oxygen affinity relative to human alpha chains. This is the first reported case of a thalassemic condition that is maintained in a species as an adaptive advantage.

  19. Update Review and Clinical Presentation in Congenital Insensitivity to Pain and Anhidrosis

    Directory of Open Access Journals (Sweden)

    L. M. Pérez-López

    2015-01-01

    Full Text Available Introduction. Congenital insensitivity to pain and anhidrosis (CIPA or hereditary sensory and autonomic neuropathy type IV is an extremely rare syndrome. Three clinical findings define the syndrome: insensitivity to pain, impossibility to sweat, and mental retardation. This pathology is caused by a genetic mutation in the NTRK1 gene, which encodes a tyrosine receptor (TrkA for nerve growth factor (NGF. Methods. The consultation of a child female in our center with CIPA and a tibia fracture in pseudoarthrosis encouraged us to carefully review literature and examine the therapeutic possibilities. A thorough review of literature published in Pubmed was done about CIPA and other connected medical issues mentioned in the paper. Conclusions. The therapeutic approach of CIPA remains unclear. The preventive approach remains the only possible treatment of CIPA. We propose two new important concepts in the therapeutic approach for these patients: (1 early surgical treatment for long bone fractures to prevent pseudoarthrosis and to allow early weight bearing, decreasing the risk of further osteopenia, and (2 bisphosphonates to avoid the progression of osteopenia and to reduce the number of consecutive fractures.

  20. Inositol metabolism in WRK-1 cells. Relationship of hormone-sensitive to -insensitive pools of phosphoinositides

    International Nuclear Information System (INIS)

    Monaco, M.E.

    1987-01-01

    Previous studies have indicated the existence of two separate pools of phosphoinositides in WRK-1 cells; one is labile and hormone-sensitive with respect to turnover, while the other is stable. Hormonal stimulation results in a rapid increase in 32 Pi incorporation into the sensitive pool, while in the absence of hormone, incorporation of 32 Pi into this pool is slow. Results are quite different when [ 3 H]inositol is the precursor utilized. Incorporation of [ 3 H]inositol into hormone-sensitive phosphoinositides is not stimulated in the presence of hormone, suggesting entry of this exogenous precursor into the cycle by a route other than the resynthetic phase of the cycle. Furthermore, failure of hormone to induce loss of [ 3 H]phosphoinositide in pulse-chase experiments in the absence of lithium suggests reutilization of the [ 3 H]inositol moiety generated by phosphodiesteratic cleavage of hormone-sensitive phosphoinositide. Time course studies indicate that the relative rates of incorporation of [ 3 H]inositol into sensitive and insensitive phosphoinositide remain constant from 2 to 24 h. Several factors are capable of increasing [ 3 H]inositol incorporation into hormone-insensitive phosphoinositide including vasopressin, calcium ionophores, and manganese. On the other hand, vasopressin treatment appears to decrease incorporation of [ 3 H]inositol into the hormone-sensitive pool, probably by shifting the equilibrium between phosphoinositides and inositol phosphates, since the decrease in radioactivity observed in the phosphoinositides is equaled by the increase observed in that in the inositol phosphates