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https://www.readbyqxmd.com/read/28929747/the-structure-of-an-insecticide-sequestering-carboxylesterase-from-the-disease-vector-culex-quinquefasciatus-what-makes-an-enzyme-a-good-insecticide-sponge
#1
Davis Henry Hopkins, Nicholas J Fraser, Peter D Mabbitt, Paul D Carr, John G Oakeshott, Colin J Jackson
Carboxylesterase (CBE)-mediated metabolic resistance to organophosphate and carbamate insecticides is a major problem for the control of insect disease vectors, such as the mosquito. The most common mechanism involves overexpression of CBEs that bind to the insecticide with high affinity, thereby sequestering them before they can interact with their target. However, the absence of any structure for an insecticide-sequestering CBE limits our understanding of the molecular basis for this process. We present the first structure of a CBE involved in sequestration, Cqestβ21, from the mosquito disease vector, Culex quinquefasciatus...
September 20, 2017: Biochemistry
https://www.readbyqxmd.com/read/28927428/current-status-of-insecticide-resistance-among-malaria-vectors-in-kenya
#2
Benyl M Ondeto, Christopher Nyundo, Luna Kamau, Simon M Muriu, Joseph M Mwangangi, Kiambo Njagi, Evan M Mathenge, Horace Ochanda, Charles M Mbogo
BACKGROUND: Insecticide resistance has emerged as one of the major challenges facing National Malaria Control Programmes in Africa. A well-coordinated national database on insecticide resistance (IRBase) can facilitate the development of effective strategies for managing insecticide resistance and sustaining the effectiveness of chemical-based vector control measures. The aim of this study was to assemble a database on the current status of insecticide resistance among malaria vectors in Kenya...
September 19, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/28910412/transcriptional-responses-in-the-hepatopancreas-of-eriocheir-sinensis-exposed-to-deltamethrin
#3
Zongying Yang, Yiliu Zhang, Yingying Jiang, Fengjiao Zhu, Liugen Zeng, Yulan Wang, Xiaoqing Lei, Yi Yao, Yujie Hou, Liangqing Xu, Chunxian Xiong, Xianle Yang, Kun Hu
Deltamethrin is an important pesticide widely used against ectoparasites. Deltamethrin contamination has resulted in a threat to the healthy breeding of the Chinese mitten crab, Eriocheir sinensis. In this study, we investigated transcriptional responses in the hepatopancreas of E. sinensis exposed to deltamethrin. We obtained 99,087,448, 89,086,478, and 100,117,958 raw sequence reads from control 1, control 2, and control 3 groups, and 92,094,972, 92,883,894, and 92,500,828 raw sequence reads from test 1, test 2, and test 3 groups, respectively...
2017: PloS One
https://www.readbyqxmd.com/read/28898947/soil-enzyme-dynamics-in-chlorpyrifos-treated-soils-under-the-influence-of-earthworms
#4
Juan C Sanchez-Hernandez, J Notario Del Pino, Yvan Capowiez, Christophe Mazzia, Magali Rault
Earthworms contribute, directly and indirectly, to contaminant biodegradation. However, most of bioremediation studies using these annelids focus on pollutant dissipation, thus disregarding the health status of the organism implied in bioremediation as well as the recovery of indicators of soil quality. A microcosm study was performed using Lumbricus terrestris to determine whether earthworm density (2 or 4individuals/kg wet soil) and the time of exposure (1, 2, 6, 12, and 18wk) could affect chlorpyrifos persistence in soil initially treated with 20mg active ingredientkg(-1) wet soil...
September 8, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28884626/in-silico-and-empirical-approaches-toward-understanding-the-structural-adaptation-of-the-alkaline-stable-lipase-kv1-from-acinetobacter-haemolyticus
#5
Kalaivani Batumalaie, Mohamed Faraj Edbeib, Naji Arafat Mahat, Fahrul Huyop, Roswanira Abdul Wahab
Interests in Acinetobacter haemolyticus lipases are showing an increasing trend concomitant with growth of the enzyme industry and the widening search for novel enzymes and applications. Here, we present a structural model that reveals the key catalytic residues of lipase KV1 from A. haemolyticus. Homology modeling of the lipase structure was based on the structure of a carboxylesterase from the archaeon Archaeoglobus fulgidus as the template, which has a sequence that is 58% identical to that of lipase KV1...
September 8, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28860055/novel-and-environmental-friendly-approach-impact-of-neem-azadirachta-indica-gum-nano-formulation-ngnf-on-helicoverpa-armigera-hub-and-spodoptera-litura-fab
#6
Chinnaperumal Kamaraj, Pachiyappan Rajiv Gandhi, Gandhi Elango, Sengodan Karthi, Ill-Min Chung, Govindsamy Rajakumar
The future of this study was to prepare a natural pesticide which will not harm the environment and yet control pests. Neem gum nano formulation (NGNF), a novel biopesticide prepared from the Neem gum extract (Azadirachta indica) (NGE) was evaluated for its antifeedant, larvicidal and pupicidal activities against Helicoverpa armigera (Hub.) and Spodoptera litura (Fab.) at 100ppm. The NGNF showed significant (100%) antifeedant, larvicidal and pupicidal activities against H. armigera and S. litura. The LC50 values of 10...
August 28, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28852982/toxicological-effects-of-chemical-constituents-from-piper-against-the-environmental-burden-aedes-aegypti-liston-and-their-impact-on-non-target-toxicity-evaluation-against-biomonitoring-aquatic-insects
#7
Prabhakaran Vasantha-Srinivasan, Annamalai Thanigaivel, Edward-Sam Edwin, Athirstam Ponsankar, Sengottayan Senthil-Nathan, Selvaraj Selin-Rani, Kandaswamy Kalaivani, Wayne B Hunter, Veeramuthu Duraipandiyan, Naif Abdullah Al-Dhabi
Dengue is the most rapidly spreading mosquito-borne viral disease in the world. The mosquito, Aedes aegypti, also spreads Yellow fever, Chikungunya, and Zika virus. As the primary vector for dengue, Ae. aegypti now occurs in over 20 countries and is a serious concern with reports of increasing insecticide resistance. Developing new treatments to manage mosquitoes are needed. Formulation of crude volatile oil from Piper betle leaves (Pb-CVO) was evaluated as a potential treatment which showed larvicidal, ovipositional, and repellency effects...
August 29, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28838926/a-comprehensive-functional-assessment-of-carboxylesterase-1-nonsynonymous-polymorphisms
#8
Xinwen Wang, Nada Rida, Jian Shi, Audrey Wu, Barry Bleske, Hao-Jie Zhu
Carboxylesterase 1 (CES1) is the predominant human hepatic hydrolase responsible for the metabolism of many clinically important medications. CES1 expression and activity vary markedly among individuals; and genetic variation is a major contributing factor to CES1 interindividual variability. In the present study, we comprehensively examined the functions of CES1 nonsynonymous single nucleotide polymorphisms (nsSNPs) and haplotypes using transfected cell lines and individual human liver tissues. The 20 candidate variants include CES1 nsSNPs with a minor allele frequency (MAF) > 0...
August 24, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28821439/effect-of-alcohol-on-skin-permeation-and-metabolism-of-an-ester-type-prodrug-in-yucatan-micropig-skin
#9
Makiko Fujii, Rieko Ohara, Azusa Matsumi, Kayoko Ohura, Naoya Koizumi, Teruko Imai, Yoshiteru Watanabe
We studied the effect that three alcohols, ethanol (EA), propanol (PA), and isopropanol (IPA), have on the skin permeation of p-hydroxy benzoic acid methyl ester (HBM), a model ester-type prodrug. HBM was applied to Yucatan micropig skin in a saturated phosphate buffered solution with or without 10% alcohol, and HBM and related materials in receptor fluid and skin were determined with HPLC. In the absence of alcohol, p-hydroxy benzoic acid (HBA), a metabolite of HBM, permeated the skin the most. The three alcohols enhanced the penetration of HBM at almost the same extent...
August 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28820941/a-photoactivatable-probe-for-super-resolution-imaging-of-enzymatic-activity-in-live-cells
#10
Elias A Halabi, Zacharias Thiel, Nils Trapp, Dorothea Pinotsi, Pablo Rivera-Fuentes
A dual-activatable, fluorogenic probe was developed to sense esterase activity with single-molecule resolution. Without enzymatic pre-activation, the diazoindanone-based probe has an electron-poor core and, upon irradiation, undergoes Wolff rearrangement to give a ring-expanded xanthene core that is nonemissive. If the probe is pre-activated by carboxylesterases, the tricyclic core becomes electron-rich, and the photoinduced Wolff rearrangement produces a highly emissive rhodol dye. Live-cell and solution studies confirmed the selectivity of the probe and revealed that the photoactivated dye does not diffuse away from the original location of activation because the intermediate ketene forms a covalent bond with surrounding macromolecules...
September 5, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28819233/biology-physiology-and-gene-expression-of-grasshopper-oedaleus-asiaticus-exposed-to-diet-stress-from-plant-secondary-compounds
#11
Xunbing Huang, Jingchuan Ma, Xinghu Qin, Xiongbing Tu, Guangchun Cao, Guangjun Wang, Xiangqun Nong, Zehua Zhang
We studied the role of plant primary and secondary metabolites in mediating plant-insect interactions by conducting a no-choice single-plant species field experiment to compare the suitability, enzyme activities, and gene expression of Oedaleus asiaticus grasshoppers feeding on four host and non-host plants with different chemical traits. O. asiaticus growth showed a positive relationship to food nutrition content and a negative relationship to secondary compounds content. Grasshopper amylase, chymotrypsin, and lipase activities were positively related to food starch, crude protein, and lipid content, respectively...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28817718/elevated-carboxylesterase-activity-contributes-to-the-lambda-cyhalothrin-insensitivity-in-quercetin-fed-helicoverpa-armigera-h%C3%A3-bner
#12
Chengyu Chen, Ying Liu, Xueyan Shi, Nicolas Desneux, Peng Han, Xiwu Gao
Quercetin as one of the key plant secondary metabolite flavonol is ubiquitous in terrestrial plants. In this study, the decrease in sensitivity to lambda-cyhalothrin was observed in quercetin-fed Helicoverpa armigera larvae. In order to figure out the mechanisms underlying the decreased sensitivity of H. armigera larvae to lambda-cyhalothrin by quercetin induction, the changes in carboxylesterase activity and in-vitro hydrolytic metabolic capacity to lambda-cyhalothrin were examined. The LC50 value of quercetin-fed H...
2017: PloS One
https://www.readbyqxmd.com/read/28817486/overcoming-clopidogrel-resistance-three-promising-novel-antiplatelet-drugs-developed-in-china
#13
Hong-Guang Xie, Yu-Meng Jia, Ting Tai, Jin-Zi Ji
Clopidogrel is one of the most frequently prescribed drugs worldwide; however, the presence of clopidogrel resistance and high susceptibility to genetic variations and drug interactions are facilitating the development of other antiplatelet drugs. To overcome clopidogrel resistance, several promising clopidogrel analogues have been developed in China, such as vicagrel (and its deuterated analogues), PLD-301, and W1. These novel chemical analogues are all characterized by much faster and more efficient bioconversion to clopidogrel thiolactone (or 2-oxo-clopidogrel, the precursor of clopidogrel active metabolite) in the intestine than clopidogrel through bypassing the first-step P450-mediated oxidation of clopidogrel in the liver...
August 4, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28817314/role-of-geraniol-against-lead-acetate-mediated-hepatic-damage-and-their-interaction-with-liver-carboxylesterase-activity-in-rats
#14
Ahmet Ozkaya, Zafer Sahin, Muslum Kuzu, Yavuz Selim Saglam, Mustafa Ozkaraca, Mirac Uckun, Ertan Yologlu, Veysel Comakli, Ramazan Demirdag, Semra Yologlu
In this study, the effect of geraniol (50 mg/kg for 30 d), a natural antioxidant and repellent/antifeedant monoterpene, in a rat model of lead acetate-induced (500 ppm for 30 d) liver damage was evaluated. Hepatic malondialdehyde increased in the lead acetate group. Reduced glutathione unchanged, but glutathione S-transferase, glutathione reductase, as well as carboxylesterase activities decreased in geraniol, lead acetate and geraniol + lead acetate groups. 8-OhDG immunoreactivity, mononuclear cell infiltrations and hepatic lead concentration were lower in the geraniol + lead acetate group than the lead acetate group...
August 17, 2017: Archives of Physiology and Biochemistry
https://www.readbyqxmd.com/read/28805379/cellular-transport-of-esculin-and-its-acylated-derivatives-in-caco-2-cell-monolayers-and-their-antioxidant-properties-in-vitro
#15
Mengmeng Zhang, Xuan Xin, Furao Lai, Xiaoyuan Zhang, Xiaofeng Li, Hui Wu
Esculin has many pharmacological effects, but these are difficult to observe after oral administration owing to poor lipid solubility. In our previous study, five acylated derivatives with different acyl chain lengths (EA, EP, EO, EL, and EM) were synthesized to improve the lipophilicity of esculin. In this study, the bioavailability and antioxidant activity of the five derivatives were investigated. The logP of esculin, EA, EP, EO, EL, and EM were -1.1 ± 0.1, -0.3 ± 0.14, 0.1 ± 0.17, 1.6 ± 0.09, 2.4 ± 0...
August 30, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28803225/carboxylesterase-1a2-encoding-gene-with-increased-transcription-and-potential-rapid-drug-metabolism-in-asian-populations
#16
Henrik Berg Rasmussen, Majbritt Busk Madsen, Yassine Kamal Lyauk, Peter Riis Hansen, Timothy Hughes
The carboxylesterase 1 gene (CES1) encodes a hydrolase implicated in the metabolism of commonly used drugs. CES1A2, a hybrid of CES1 and a CES1-like pseudogene, has a promoter that is weak in most individuals. However, some individuals harbor a promoter haplotype of this gene with two overlapping Sp1 sites that confer significantly increased transcription potentially leading to rapid drug metabolism. This CES1A2 haplotype has previously been reported to be common among Asians. Using polymerase chain reaction followed by sequencing, the present study examined variation in the promoter and 5' untranslated region of CES1A2 in 120 Han Chinese and 120 Japanese people enrolled in the 1000 Genomes Project...
August 14, 2017: Drug Metabolism and Personalized Therapy
https://www.readbyqxmd.com/read/28799241/functional-characterization-of-carboxylesterase-gene-mutations-involved-in-aphis-gossypii-resistance-to-organophosphate-insecticides
#17
Y-H Gong, G-M Ai, M Li, X-Y Shi, Q-Y Diao, X-W Gao
Carboxylesterases (CarEs) play an important role in detoxifying insecticides in insects. Over-expression and structural modification of CarEs have been implicated in the development of organophosphate (OP) insecticide resistance in insects. A previous study identified four nonsynonymous mutations (resulting in four amino acid residue substitutions) in the open reading frame of the carboxylesterase gene of resistant cotton aphids compared to the omethoate susceptible strain, which has possibly influenced the development of resistance to omethoate (a systemic OP insecticide)...
August 11, 2017: Insect Molecular Biology
https://www.readbyqxmd.com/read/28794466/a-family-of-archaea-like-carboxylesterases-preferentially-expressed-in-the-symbiotic-phase-of-the-mychorrizal-fungus-tuber-melanosporum
#18
Davide Cavazzini, Guido Grossi, Elisabetta Levati, Francesca Vallese, Barbara Montanini, Angelo Bolchi, Giuseppe Zanotti, Simone Ottonello
An increasing number of esterases is being revealed by (meta) genomic sequencing projects, but few of them are functionally/structurally characterized, especially enzymes of fungal origin. Starting from a three-member gene family of secreted putative "lipases/esterases" preferentially expressed in the symbiotic phase of the mycorrhizal fungus Tuber melanosporum ("black truffle"), we show here that these enzymes (TmelEST1-3) are dimeric, heat-resistant carboxylesterases capable of hydrolyzing various short/medium chain p-nitrophenyl esters...
August 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28782481/rational-approaches-design-strategies-structure-activity-relationship-and-mechanistic-insights-for-esterase-inhibitors
#19
Harbinder Singh, Jatinder Vir Singh, Navdeep Kaur, Mohit Sanduja, Gurpreet Singh, Preet Mohinder Singh Bedi, Sahil Sharma
BACKGROUND: Esterase is an enzyme that splits esters into an acid and alcohol. Varieties of esterases are present in human body to control diverse set of cellular processes and execute their specific functions. It can be seen that any increase in metabolites produced by these enzymes lead to severe pathological conditions like Alzheimer disease, hypercholesterolemia etc. OBJECTIVE: Numerous esterase inhibitors have been developed and reported by the researchers around the globe, but not systematically summarized yet...
August 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28775293/effect-of-carboxylesterase-1-s75n-on-clopidogrel-therapy-among-acute-coronary-syndrome-patients
#20
Fei-Yan Xiao, Jian-Quan Luo, Min Liu, Bi-Lian Chen, Shan Cao, Zhao-Qian Liu, Hong-Hao Zhou, Gan Zhou, Wei Zhang
Carboxylesterase 1 (CES1) hydrolyzes the prodrug clopidogrel to an inactive carboxylic acid metabolite. The effects of CES1 S75N (rs2307240,C>T) on clopidogrel response among 851 acute coronary syndrome patients who came from the north, central and south of China were studied. The occurrence ratios of each endpoint in the CC group were significantly higher than in the CT + TT group for cerebrovascular events (14% vs 4.8%, p < 0.001, OR = 0.31), acute myocardial infarction (15.1% vs 6.1%, p < 0...
August 3, 2017: Scientific Reports
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