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https://www.readbyqxmd.com/read/28639420/the-pharmacokinetics-of-enalapril-in-relation-to-ces1-genotype-in-healthy-danish-volunteers
#1
Claus Stage, Gesche Jürgens, Louise Schow Guski, Ragnar Thomsen, Ditte Bjerre, Laura Ferrero-Miliani, Yassine Kamal Lyauk, Henrik Berg Rasmussen, Kim Dalhoff
The present study investigated the influence of variations in the carboxylesterase 1 gene (CES1) on the pharmacokinetics of enalapril. Forty-three healthy, Danish, Caucasian volunteers representing different pre-defined genotypes each received 10 mg of enalapril. At specified time points, plasma concentrations of enalapril and the active metabolite enalaprilat were measured. The volunteers were divided into six different groups according to their genetic profile of CES1: Group 1 (controls, n=16) with two CES1 copies without non-synonymous SNPs in the exons; group 2 (n=5) with four copies of CES1; group 3 (n=6) harbouring the G143E polymorphism; group 4 (n=2) with three CES1 copies and increased transcriptional activity of the duplication (CES1A2); group 5 (n=4) harbouring the CES1A1c variant; and group 6 (n=10) with three CES1 copies and the common promoter with low transcriptional activity of the duplication...
June 21, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28619281/metabolism-of-ko143-an-abcg2-inhibitor
#2
Ke Liu, Junjie Zhu, Yixian Huang, Chaoyue Li, Jie Lu, Madhav Sachar, Song Li, Xiaochao Ma
The ATP-binding cassette sub-family G member 2 (ABCG2) plays an important role in modulating drug disposition and endobiotic homeostasis. KO143 is a potent and relatively selective ABCG2 inhibitor. We found that the metabolic stability of KO143 was very poor in human liver microsomes (HLM). Our further studies illustrated that the tert-butyl ester group in KO143 can be rapidly hydrolyzed and removed by carboxylesterase 1. This metabolic pathway was confirmed as a major pathway of KO143 metabolism in both HLM and mice...
March 6, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28618362/exposure-of-larvae-to-thiamethoxam-affects-the-survival-and-physiology-of-the-honey-bee-at-post-embryonic-stages
#3
Daiana Antonia Tavares, Claudia Dussaubat, André Kretzschmar, Stephan Malfitano Carvalho, Elaine C M Silva-Zacarin, Osmar Malaspina, Géraldine Bérail, Jean-Luc Brunet, Luc P Belzunces
Under laboratory conditions, the effects of thiamethoxam were investigated in larvae, pupae and emerging honey bees after exposure at larval stages with different concentrations in the food (0.00001 ng/μL, 0.001 ng/μL and 1.44 ng/μL). Thiamethoxam reduced the survival of larvae and pupae and consequently decreased the percentage of emerging honey bees. Thiamethoxam induced important physiological disturbances. It increased acetylcholinesterase (AChE) activity at all developmental stages and increased glutathione-S-transferase (GST) and carboxylesterase para (CaEp) activities at the pupal stages...
June 12, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28615636/autotransporter-domain-dependent-enzymatic-analysis-of-a-novel-extremely-thermostable-carboxylesterase-with-high-biodegradability-towards-pyrethroid-pesticides
#4
Xianghai Cai, Wei Wang, Lin Lin, Dannong He, Gang Huang, Yaling Shen, Wei Wei, Dongzhi Wei
The EstPS1 gene, which encodes a novel carboxylesterase of Pseudomonas synxantha PS1 isolated from oil well-produced water, was cloned and sequenced. EstPS1 has an open reading frame of 1923 bp and encodes the 640-amino acid carboxylesterase (EstPS1), which contains an autotransporter (AT) domain (357-640 amino acids). Homology analysis revealed that EstPS1 shared the highest identity (88%) with EstA from Pseudomonas fluorescens A506 (NCBI database) and belonged to the carboxylesterase family (EC 3.1.1.1). The optimum pH and temperature of recombinant EstPS1 were found to be 8...
June 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28595288/does-resistance-to-buprofezin-improve-heat-and-cold-tolerance-of-laodelphax-striatellus-hemiptera-delphacidae
#5
Yongteng Li, Yueliang Zhang, Xiangdong Liu, Huifang Guo
There is ample evidence that insecticide resistance causes fitness costs and benefits in pests, while the impact of insecticide resistance on thermotolerance of pests is mostly unclear. The Laodelphax striatellus (Fallén), is an important rice insect pest, which has developed resistance to buprofezin in China. Here, we investigated differences in heat tolerance and cold tolerance among L. striatellus lines with variable buprofezin resistance. The lethal time for 50% of the individuals to die (LT50) at 40 °C increased with an increase in buprofezin resistance level, whereas both the survival rate under -22 °C and the supercooling point of planthoppers did not differ significantly between resistant and susceptible strains...
June 8, 2017: Environmental Entomology
https://www.readbyqxmd.com/read/28590363/ethanol-interactions-with-dexmethylphenidate-and-dl-methylphenidate-spheroidal-oral-drug-absorption-systems-in-healthy-volunteers
#6
Hao-Jie Zhu, Kennerly S Patrick, Arthur B Straughn, Owen T Reeves, Hilary Bernstein, Jian Shi, Heather J Johnson, Joshua M Knight, Aaron T Smith, Robert J Malcolm, John S Markowitz
BACKGROUND/PURPOSE: Ethanol coadministered with immediate-release dl-methylphenidate (dl-MPH) or dexmethylphenidate (d-MPH) significantly increases the geomean maximum plasma concentration (Cmax) of d-MPH 22% and 15%, respectively, and elevates overall drug exposure and psychostimulant effects. We asked the question: Are these ethanol-MPH interactions based more fundamentally on (1) inhibition of postabsorption d-MPH metabolism or (2) acceleration of MPH formulation gastric dissolution by ethanol in the stomach? This was investigated using the pulsatile, distinctly biphasic, spheroidal oral drug absorption systems of dl-MPH and d-MPH...
June 5, 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28587099/a-transcriptome-survey-spanning-life-stages-and-sexes-of-the-harlequin-bug-murgantia-histrionica
#7
Michael E Sparks, Joshua H Rhoades, David R Nelson, Daniel Kuhar, Jason Lancaster, Bryan Lehner, Dorothea Tholl, Donald C Weber, Dawn E Gundersen-Rindal
The harlequin bug, Murgantia histrionica (Hahn), is an agricultural pest in the continental United States, particularly in southern states. Reliable gene sequence data are especially useful to the development of species-specific, environmentally friendly molecular biopesticides and effective biolures for this insect. Here, mRNAs were sampled from whole insects at the 2nd and 4th nymphal instars, as well as sexed adults, and sequenced using Illumina RNA-Seq technology. A global assembly of these data identified 72,540 putative unique transcripts bearing high levels of similarity to transcripts identified in other taxa, with over 99% of conserved single-copy orthologs among insects being detected...
May 25, 2017: Insects
https://www.readbyqxmd.com/read/28580548/development-of-an-eco-friendly-mosquitocidal-agent-from-alangium-salvifolium-against-the-dengue-vector-aedes-aegypti-and-its-biosafety-on-the-aquatic-predator
#8
Annamalai Thanigaivel, Prabhakaran Vasantha-Srinivasan, Edward-Sam Edwin, Athirstam Ponsankar, Selvaraj Selin-Rani, Muthiah Chellappandian, Kandaswamy Kalaivani, Sengottayan Senthil-Nathan, Giovanni Benelli
Plant extracts with their enriched chemical constituents have established potential alternative mosquito control agents. In this research, we developed an eco-friendly mosquitocidal agent from Alangium salvifolium leaves against the dengue and Zika virus vector Aedes aegypti and we investigated its biosafety on the mosquito aquatic predator Toxorhynchites splendens. Results showed that the methanolic extract of A. salvifolium leaves was composed by eight main compounds, with major peak area for hexadecenoic acid (21...
June 4, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28578994/synthesis-molecular-docking-and-biological-activity-of-polyfluoroalkyl-dihydroazolo-5-1-c-1-2-4-triazines-as-selective-carboxylesterase-inhibitors
#9
Evgeny V Shchegol'kov, Galina F Makhaeva, Natalia P Boltneva, Sofya V Lushchekina, Olga G Serebryakova, Elena V Rudakova, Nadezhda V Kovaleva, Yanina V Burgart, Victor I Saloutin, Oleg N Chupakhin, Sergey O Bachurin, Rudy J Richardson
To search for effective and selective inhibitors of carboxylesterase (CaE), a series of 7-hydroxy-7-polyfluoroalkyl-4,7-dihydroazolo[5,1-c][1,2,4]triazines has been synthesized. Their inhibitory activity against acetylcholinesterase, butyrylcholinesterase, and CaE were investigated using the methods of enzyme kinetics and molecular docking. It was shown that the tested compounds are reversible selective CaE inhibitors of mixed type. Elongation of the polyfluoroalkyl substituent and the presence of an ester, preferably the ethoxycarbonyl group, enhance inhibitory activity toward CaE...
May 20, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28578775/corrigendum-to-functional-and-immunohistochemical-characterization-of-cceae3a-a-carboxylesterase-associated-with-temephos-resistance-in-the-major-arbovirus-vectors-aedes-aegypti-and-ae-albopictus-insect-biochem-mol-biol-74-july-2016-61-67
#10
Linda Grigoraki, Vassileia Balabanidou, Christos Meristoudis, Antonis Miridakis, Hilary Ranson, Luc Swevers, John Vontas
No abstract text is available yet for this article.
June 2017: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28566216/molecular-quantitative-assay-for-esterase-mediated-organophosphate-resistance-in-rhipicephalus-microplus
#11
Luciana Gatto Brito, Loui de Oliveira Nery, Fabio da Silva Barbieri, Maribel E Funes Huacca, Soraya Dos Santos Pereira, Renata Reis da Silva, Carla Celedônio de Freitas Fernanades, Márcia Cristina de Sena Oliveira
The use of pesticides is the main tool to control infestations of the cattle tick Rhipicephalus microplus, and organophosphate (OP) is one of the most used compounds for this purpose. Carboxylesterases (ChEs) are targets for OP pesticides in arthropods, and acetylcholinesterase 2 (AChE2) and esterase 1 (EST1) are metabolic enzymes involved in the xenobiotic detoxification process. The increase in the synthesis of these enzymes can be detected by the quantitative polymerase chain reaction (qPCR) assay, which was used to identify cattle tick populations resistant to OP pesticides...
May 19, 2017: Ticks and Tick-borne Diseases
https://www.readbyqxmd.com/read/28556457/the-new-insight-into-foregut-functions-of-xenobiotic-detoxification-in-the-cockroach-periplaneta-americana
#12
Jian-Hua Zhang, Song Zhang, Yuan-Xue Yang, Yi-Xi Zhang, Ze-Wen Liu
The physiological functions of insect foregut, especially in xenobiotic detoxification, are scarcely reported because of the unimportance in appearance and insufficient molecular information. The cockroach Periplaneta americana, an entomological model organism, provides perfect material to study physiological functions of foregut tissue due to its architectural feature. Through Illumina sequencing of foregut tissue from P. americana individuals (control) or insects treated with cycloxaprid, as novel neonicotinoid insecticide, 54 193 166 clean reads were obtained and further assembled into 53 853 unigenes with an average length of 366 bp...
May 26, 2017: Insect Science
https://www.readbyqxmd.com/read/28547891/large-scale-gene-expression-reveals-different-adaptations-of-hyalopterus-persikonus-to-winter-and-summer-host-plants
#13
Na Cui, Peng-Cheng Yang, Kun Guo, Le Kang, Feng Cui
Host alternation, an obligatory seasonal shifting between host plants of distant genetic relationship, has had significant consequences for the diversification and success of the superfamily of aphids. However, the underlying molecular mechanism remains unclear. In this study, the molecular mechanism of host alternation was explored through a large-scale gene expression analysis of the mealy aphid Hyalopterus persikonus on winter and summer host plants. More than four times as many unigenes of the mealy aphid were significantly upregulated on summer host Phragmites australis than on winter host Rosaceae plants...
June 2017: Insect Science
https://www.readbyqxmd.com/read/28541740/controlling-aedes-albopictus-and-culex-pipiens-pallens-using-silver-nanoparticles-synthesized-from-aqueous-extract-of-cassia-fistula-fruit-pulp-and-its-mode-of-action
#14
Hatem Fouad, Li Hongjie, Dawood Hosni, Jiqian Wei, Ghulam Abbas, Hassan Ga'al, Mo Jianchu
Mosquitoes act as key vector for transmission of devastating parasites and pathogens which affect millions of people globally. In this research, the green synthesis of silver nanoparticles of Cassia fistula fruit pulp as an innovative and operative tool against vector mosquitoes is presented. Silver nanoparticles were characterized by a series of techniques including Fourier transform infrared spectroscopy, Transmission Electron Microscope and confirmed by Scanning Electron Microscope, UV-Vis spectrophotometry and X-ray diffraction...
May 25, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28538100/enzymatic-hydrolysis-of-polyester-thin-films-at-the-nanoscale-effects-of-polyester-structure-and-enzyme-active-site-accessibility
#15
Michael Thomas Zumstein, Daniela Rechsteiner, Nicolas Roduner, Veronika Perz, Doris Ribitsch, Georg M Guebitz, Hans-Peter E Kohler, Kristopher McNeill, Michael Sander
Biodegradable polyesters have a large potential to replace persistent polymers in numerous applications and to thereby reduce the accumulation of plastics in the environment. Ester hydrolysis by extracellular carboxylesterases is considered the rate-limiting step in polyester biodegradation. In this work, we systematically investigated the effects of polyester and carboxylesterase structure on the hydrolysis of nanometer-thin polyester films using a quartz-crystal microbalance with dissipation monitoring. Hydrolyzability increased with increasing polyester-chain flexibility as evidenced from differences in the hydrolysis rates and extents of aliphatic polyesters varying in the length of their dicarboxylic acid unit and of poly(butylene adipate co-terephthalate) (PBAT) polyesters varying in their terephthalate-to-adipate ratio by Rhizopus oryzae lipase and Fusarium solani cutinase...
May 24, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28536421/assessment-of-tissue-specific-accumulation-elimination-and-toxic-effects-of-dichlorodiphenyltrichloroethanes-ddts-in-carp-through-aquatic-food-web
#16
Shanshan Di, Ruiquan Liu, Zhongnan Tian, Cheng Cheng, Li Chen, Wenjun Zhang, Zhiqiang Zhou, Jinling Diao
Microcosms containing DDT spiked-sediment, Tubifex tubifex and carp (Cyprinus carpio) were constructed to simulate a freshwater system. The accumulation, elimination and toxic effects of DDT (p,p'-DDT, o,p'-DDT), and its metabolites DDD (p,p'-DDD, o,p'-DDD) and DDE (p,p'-DDE, o,p'-DDE) were studied in T. tubifex and carp. Tissue/organ distributions of DDTs were also investigated in carp. The bioaccumulation and elimination of DDT differed in T. tubifex, carp and its tissues/organs. Unimodal or bimodal distributions were observed, and the concentrations of DDT metabolites (DDD and p,p'-DDE) increased over time...
May 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28532270/predominant-contributions-of-carboxylesterase-1-and-2-in-hydrolysis-of-anordrin-in-humans
#17
Jinfang Jiang, Xiaoyan Chen, Dafang Zhong
1. Anordrin (2α, 17α-diethynyl-A-nor-5α-androstane-2β, 17β-diol diproprionate) is post-coital contraceptive drug that is on the market in China for more than 30 years. This study aims to elucidate enzymes involved in anordrin hydrolysis, and to evaluate the significant role of carboxylesterases in anordrin hydrolysis in humans. 2. Human liver and intestinal microsomes, recombinant human carboxylesterase were selected as enzyme sources. In human liver microsomes, intrinsic clearance was 684 ± 83 μL/min/mg protein, which was considerably higher than the value of intestine microsomes (94...
June 7, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28531881/first-in-man-dose-escalation-and-pharmacokinetic-study-of-cap7-1-a-novel-prodrug-of-etoposide-in-adults-with-refractory-solid-tumours
#18
U Keilholz, L Rohde, P Mehlitz, M Knoedler, A Schmittel, V Kümmerlen, K Klinghammer, P Treasure, M Lassus, G Steventon, M Machacek, N Utku
AIM: An open-label, phase I dose-escalation trial was performed in adult patients with various solid cancers to identify the maximum tolerated dose (MTD), to assess the safety, pharmacokinetic profile and anti-tumour activity of the new prodrug CAP7.1. The prodrug is converted to its active moiety etoposide via carboxylesterases in selective cells leading to a better tolerability and higher efficacy in therapeutic resistance cells and children with refractory neuroblastoma. PATIENTS AND METHODS: Eligible adult patients with advanced, refractory, solid malignancies received CAP7...
May 19, 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/28525556/transcriptome-of-the-gsh-depleted-lens-reveals-changes-in-detoxification-and-emt-signaling-genes-transport-systems-and-lipid-homeostasis
#19
Jeremy A Whitson, Xiang Zhang, Mario Medvedovic, Jenny Chen, Zongbo Wei, Vincent M Monnier, Xingjun Fan
Purpose: To understand the effects of glutathione (GSH)-deficiency on genetic processes that regulate lens homeostasis and prevent cataractogenesis. Methods: The transcriptome of lens epithelia and fiber cells was obtained from C57BL/6 LEGSKO (lens GSH-synthesis knockout) and buthionine sulfoximine (BSO)-treated LEGSKO mice and compared to C57BL/6 wild-type mice using RNA-Seq. Transcriptomic data were confirmed by qPCR and Western blot/ELISA on a subset of genes...
May 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28475833/imaging-and-detection-of-carboxylesterase-in-living-cells-and-zebrafish-pretreated-with-pesticides-by-a-new-near-infrared-fluorescence-off-on-probe
#20
Dongyu Li, Zhao Li, Weihua Chen, Xingbin Yang
A new near-infrared fluorescence off-on probe was developed and applied to fluorescence imaging of carboxylesterase in living HepG-2 cells and zebrafish pretreated with pesticides (carbamate, organophosphorus, and pyrethroid). The probe was readily prepared by connecting (4-acetoxybenzyl)oxy as a quenching and recognizing moiety to a stable hemicyanine skeleton that can be formed via the decomposition of IR-780. The fluorescence off-on response of the probe to carboxylesterase is based on the enzyme-catalyzed spontaneous hydrolysis of the carboxylic ester bond, followed by a further fragmentation of the phenylmethyl unit and thereby the fluorophore release...
May 24, 2017: Journal of Agricultural and Food Chemistry
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