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Liana M Matson, Hilary S McCarren, C Linn Cadieux, Douglas M Cerasoli, John H McDonough
Genetics likely play a role in various responses to nerve agent exposure, as genetic background plays an important role in behavioral, neurological, and physiological responses to environmental stimuli. Mouse strains or selected lines can be used to identify susceptibility based on background genetic features to nerve agent exposure. Additional genetic techniques can then be used to identify mechanisms underlying resistance and sensitivity, with the ultimate goal of developing more effective and targeted therapies...
November 4, 2017: Toxicology
Hai-Jian Huang, Jia-Bao Lu, Qiao Li, Yan-Yuan Bao, Chuan-Xi Zhang
The planthoppers are piercing-sucking pests that continuously inject saliva into host plants using specialized stylets. However, knowledge on the constituent and function of planthopper saliva proteins was still limited. In this study, the transcriptomic and proteomic approach were adopted to characterize the composition of salivary glands and their secreted saliva in three planthoppers, respectively. Gene repertoires of salivary glands in brown planthopper (Nilaparvata lugens, BPH), white-backed planthopper (Sogatella furcifera, WBPH) and small brown planthopper (Laodelphax striatellus, SBPH) were very similar, which actively involved in protein synthesis and energy metabolism...
November 3, 2017: Journal of Proteomics
Hong Pan, Linyan Huang, Yi Li, Xumei Zhou, Yuanfu Lu, Fuguo Shi
Arecoline, a predominant alkaloid in areca nut, shows several pharmacological and toxicological effects. In present study, a sensitive and accurate liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and fully validated for quantification of arecoline in rat plasma. Importantly, our group found that arecoline was highly unstable in rat plasma samples, which brought challenges to accurately quantify in vivo. The hydrolysis of ester moiety of arecoline by carboxylesterases was responsible for its instability, and arecoline was hydrolyzed to arecaidine...
October 14, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
ChuanShan Zou, ChunHe Lv, YaJun Wang, ChuanWang Cao, GuoCai Zhang
Based on the broad spectrum of its biological activities, Chelidonium majus has been studied extensively in the medical field. However, few studies have focused on the insecticidal activity of C. majus, and the precise mechanism of its insecticidal activity. In the present study, larvicidal activity and insecticidal mechanism of C. majus on Lymantria dispar were investigated using bioassays, in vitro and in vivo enzyme activity assays, determination of the nutritional index, and gene transcription analysis...
October 2017: Pesticide Biochemistry and Physiology
Marvelous Sungirai, Samantha Baron, Doreen Zandile Moyo, Patrick De Clercq, Christine Maritz-Olivier, Maxime Madder
Acaricide resistance is one of the greatest threats towards the successful control of vector ticks worldwide. Communal farmers of Zimbabwe use amitraz as the most common acaricide with occasional usage of pyrethroids and organophosphates. As a strategy towards developing an effective acaricide resistance management system in Zimbabwe, screening was done by genotyping Rhipicephalus microplus tick populations using molecular markers associated with resistance to these chemicals. The frequency of the mutant allele for the octopamine/tyramine receptor marker associated with amitraz resistance was high (0...
November 2, 2017: Ticks and Tick-borne Diseases
Salomé Martínez Morcillo, Maria Chiara Perego, Jorge Vizuete, Francesca Caloni, Cristina Cortinovis, Luis Eusebio Fidalgo, Ana López-Beceiro, María Prado Míguez, Francisco Soler, Marcos Pérez-López
Over the last years, cholinesterase (ChE) and carboxylesterase (CbE) activities have been increasingly used in environmental biomonitoring to detect the exposure to anticholinesterase insecticides such as organophosphorates (OPs) and carbamates (CBs). The aim of this study was to determine ChE and CbE enzymatic activities present in liver and muscle of yellow-legged gulls (Larus michahellis), a seabird species considered suitable to monitor environmental pollution. In order to provide reference data for further biomonitoring studies, the influence of different factors, such as gender, age, sampling mode, and tissue, was considered in the present study...
November 2, 2017: Environmental Science and Pollution Research International
Kona Madhavinadha Prasad, Kamaraju Raghavendra, Vaishali Verma, Poonam Sharma Velamuri, Veena Pande
BACKGROUND & OBJECTIVES: Increase in prevalence and intensity of insecticide-resistance in vectors of vector-borne diseases is a major threat to sustainable disease control; and, for their effective management, studies on resistance mechanisms are important to come out with suitable strategies. Esterases are major class of detoxification enzymes in mosquitoes, which confers protection against insecticides in causing resistance. This study was aimed at biochemical characterization of esterases responsible for malathion resistance in Anopheles stephensi mosquitoes, along with its validation through biochemical techniques and native-PAGE assays...
July 2017: Journal of Vector Borne Diseases
Manli Ma, Haihong Jia, Xuepei Cui, Na Zhai, Hongfang Wang, Xingqi Guo, Baohua Xu
Carboxylesterases (CarEs) play vital roles in metabolising different physiologically important endogenous compounds and in detoxifying various harmful exogenous compounds in insects. Multiple studies of CarEs have focused on pesticide metabolism in insects, while few studies have aimed to identify CarE functions in oxidative resistance, particularly in Apis cerana cerana. In this study, we isolated a carboxylesterase gene, esterase FE4, from Apis cerana cerana and designated it towards an exploration of its roles as an antioxidant and in detoxification...
October 30, 2017: Biochimie
Sandeep Kondakala, Jung Hwa Lee, Matthew K Ross, George E Howell
The prevalence of obesity is increasing at an alarming rate in the United States with 36.5% of adults being classified as obese. Compared to normal individuals, obese individuals have noted pathophysiological alterations which may alter the toxicokinetics of xenobiotics and therefore alter their toxicities. However, the effects of obesity on the toxicity of many widely utilized pesticides has not been established. Therefore, the present study was designed to determine if the obese phenotype altered the toxicity of the most widely used organophosphate (OP) insecticide, chlorpyrifos (CPS)...
October 31, 2017: Toxicology and Applied Pharmacology
Mirna Velki, Henriette Meyer-Alert, Thomas-Benjamin Seiler, Henner Hollert
The zebrafish as a test organism enables the investigation of effects on a wide range of biological levels from molecular level to the whole-organism level. The use of fish embryos represents an attractive model for studies aimed at understanding toxic mechanisms and the environmental risk assessment of chemicals. In the present study, a zebrafish (Danio rerio) in vivo model was employed in order to assess the effects of two commonly used pesticides, the insecticide diazinon and the herbicide diuron, on zebrafish early life stages...
October 28, 2017: Aquatic Toxicology
Kim Francis McClure, David W Piotrowski, Donna Petersen, Liuqing Wei, Jun Xiao, Allyn T Londregan, Adam Kamlet, Anne-Marie Dechert-Schmitt, Brian Raymer, Roger B Ruggeri, Daniel Canterbury, Chris Limberakis, Spiros Liras, Paul DaSilva-Jardine, Robert G Dullea, Paula M Loria, Benjamin Reidich, Christopher T Salatto, Heather Eng, Emi Kimoto, Karen Atkinson, Amanda King-Ahmad, Dennis Scott, Kevin Beaumont, Jeffrey R Chabot, Michael Bolt, Kevin Maresca, Kenneth Dahl, Ryosuke Arakawa, Akihiro Takano, Christer Halladin
Targeting of the human ribosome is an unprecedented therapeutic modality with a genome-wide selectivity challenge. Herein we describe a liver-targeted drug candidate that inhibits ribosomal synthesis of PCSK9, a lipid regulator considered undruggable by small molecules. Key to the concept was the identification of pharmacologically active zwitterions designed to be retained in the liver. Oral delivery of the poorly permeable zwitterions was achieved via prodrugs susceptible to cleavage by carboxylesterase 1...
October 26, 2017: Angewandte Chemie
Duarte Gouveia, Arnaud Chaumot, Aurore Charnot, Christine Almunia, Adeline François, Lionel Navarro, Jean Armengaud, Arnaud Salvador, Olivier Geffard
As a proof of principle, a Selected Reaction Monitoring (SRM) mass spectrometry-based methodology was applied to the simultaneous quantification of dozens of protein biomarkers in caged amphipods (Gammarus fossarum). We evaluated the suitability of the methodology to assess complex field contaminations through its application in the framework of a regional river monitoring network. Thanks to the high throughput acquisition of biomarker levels in G. fossarum exposed in four reference and thirteen contaminated sites, we analyzed the individual responses of 38 peptides reporting for 25 proteins of interest in 170 organisms...
October 25, 2017: Environmental Science & Technology
Kai Lu, Ying Wang, Xia Chen, Zhichao Zhang, Yue Li, Wenru Li, Qiang Zhou
The widespread and extensive application of insecticides have promoted the development of resistance in the brown planthopper Nilaparvata lugens (Stål), one of the most important rice pests in Asia. To better understand the underlying molecular mechanisms of metabolic resistance to insecticides, a chlorpyrifos-resistant (CR) strain of N. lugens was selected and its possible resistance mechanism was investigated. Synergistic tests using carboxylesterases (CarEs) inhibitor triphenyl phosphate (TPP) decreased the resistance of N...
December 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
Sean D Kodani, Morgane Barthélemy, Shizuo G Kamita, Bruce Hammock, Christophe Morisseau
Carboxylesterases are well known for their role in the metabolism of xenobiotics. However, recent studies have also implicated carboxylesterases in regulating a number of physiological processes including metabolic homeostasis and macrophage development, underlying the need to quantify them individually. Unfortunately, current methods for selectively measuring the catalytic activity of individual carboxylesterases are not sufficiently sensitive to support many biological studies. In order to develop a more sensitive and selective method to measure the activity of human carboxylesterase 1 (hCE1), we generated and tested novel substrates with a fluorescent aminopyridine leaving group...
October 18, 2017: Analytical Biochemistry
Guodong Zhu, Yin Luo, Ming Xue, Haipeng Zhao, Xia Sun, Xinhui Wang
Bradysia odoriphaga Yang et Zhang, the Chinese chive root maggot, is a devastating pest of agricultural plants causing significant losses in vegetable crops, edible mushrooms, and humus. To determine the effects of feeding on different host plants and diets on the life parameters of B. odoriphaga and its tolerance to stressful conditions, we analyzed the life-table data of B. odoriphaga reared on Chinese chive (Allium hookeri), Welsh onion (Allium fistulosum), garlic (Allium sativum), oyster mushroom (Pleurotus ostreatus), and humus and assayed its tolerance to heat and insecticides...
October 17, 2017: Journal of Economic Entomology
Antonio J Pazos, Pablo Ventoso, Roi Martínez-Escauriaza, M Luz Pérez-Parallé, Juan Blanco, Juan C Triviño, José L Sánchez
Bivalve molluscs are filter feeding species that can accumulate biotoxins in their body tissues during harmful algal blooms. Amnesic Shellfish Poisoning (ASP) is caused by species of the diatom genus Pseudo-nitzschia, which produces the toxin domoic acid. The Mytilus galloprovincialis digestive gland transcriptome was de novo assembled based on the sequencing of 12 cDNA libraries, six obtained from control mussels and six from mussels naturally exposed to domoic acid-producing diatom Pseudo-nitzschia australis...
October 12, 2017: Toxicon: Official Journal of the International Society on Toxinology
Zhiping Liu, Qiang Zhang, Xuan Wu, Wei Yu, Shengquan Guo
Paederus fuscipes, a health pest, causes dermatitis linearis in humans. Wintergreen oil exhibits optimal insecticidal activity against P. fuscipes. However, the insecticidal mechanism remains unclear not only in P. fuscipes but also in other pests. In this study, we explored the insecticidal mechanism of wintergreen oil in terms of its effect on the activity of acetylcholinesterase (AChE) enzyme and detoxifying enzymes (carboxylesterase, glutathione-S-transferase, and mixed function oxidase); such effect was studied by fumigation both in vivo and in vitro in P...
October 4, 2017: Journal of Medical Entomology
Mikko Neuvonen, E Katriina Tarkiainen, Aleksi Tornio, Päivi Hirvensalo, Tuija Tapaninen, Maria Paile-Hyvärinen, Matti K Itkonen, Mikko T Holmberg, Vesa Kärjä, Ville T Männistö, Pertti J Neuvonen, Jussi Pihlajamäki, Janne T Backman, Mikko Niemi
Several single nucleotide variations (SNVs) affect carboxylesterase 1 (CES1) activity, but the effects of genetic variants on CES1 gene expression have not been systematically investigated. Therefore, our aim was to investigate effects of genetic variants on CES1 gene expression in two independent whole blood sample cohorts of 192 (discovery) and 88 (replication) healthy volunteers and in a liver sample cohort of 177 patients. Furthermore, we investigated possible effects of the found variants on clopidogrel pharmacokinetics (n=106) and pharmacodynamics (n=46) in healthy volunteers, who had ingested a single 300 mg or 600 mg dose of clopidogrel...
October 8, 2017: Basic & Clinical Pharmacology & Toxicology
Galina F Makhaeva, Sofya V Lushchekina, Natalia P Boltneva, Olga G Serebryakova, Elena V Rudakova, Alexey A Ustyugov, Sergey O Bachurin, Alexander V Shchepochkin, Oleg N Chupakhin, Valery N Charushin, Rudy J Richardson
We investigated the inhibitory activity of 4 groups of novel acridine derivatives against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and carboxylesterase (CaE) using the methods of enzyme kinetics and molecular docking. Antioxidant activity of the compounds was determined using the 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS(+)) radical decolorization assay as their ability to scavenge free radicals. Analysis of the esterase profiles and antiradical activities of the acridine derivatives showed that 9-aryl(heteroaryl)-N-methyl-9,10-dihydroacridines have a high radical-scavenging activity but low potency as AChE and BChE inhibitors, whereas 9-aryl(heteroaryl)-N-methyl-acridinium tetrafluoroborates effectively inhibit cholinesterases but do not exhibit antiradical activity...
November 1, 2017: Bioorganic & Medicinal Chemistry
Paul Hermant, Damien Bosc, Catherine Piveteau, Ronan Gealageas, BaoVy Lam, Cyril Ronco, Matthieu Roignant, Hasina Tolojanahary, Ludovic Jean, Pierre-Yves Renard, Mohamed Lemdani, Marilyne Bourotte, Adrien Herledan, Corentin Bedart, Alexandre Biela, Florence Leroux, Benoit Deprez, Rebecca Deprez-Poulain
Hydroxamic acids are outstanding zinc chelating groups that can be used to design potent and selective metalloenzyme inhibitors in various therapeutic areas. Some hydroxamic acids display a high plasma clearance resulting in poor in vivo activity, though they may be very potent compounds in vitro. We designed a 57-member library of hydroxamic acids to explore the structure-plasma stability relationships in these series and to identify which enzyme(s) and which pharmacophores are critical for plasma stability...
October 24, 2017: Journal of Medicinal Chemistry
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