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carboxylesterase

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https://www.readbyqxmd.com/read/28438337/carboxylesterase-activities-in-chondrichthyans-of-the-western-mediterranean-sea
#1
David Nos, Joan Navarro, Claudio Barría, Montserrat Solé
No abstract text is available yet for this article.
April 21, 2017: Marine Pollution Bulletin
https://www.readbyqxmd.com/read/28437488/the-novel-carboxylesterase-1-variant-c-662a-g-may-decrease-the-bioactivation-of-oseltamivir-in-humans
#2
Jaeseong Oh, SeungHwan Lee, Howard Lee, Joo-Youn Cho, Seo Hyun Yoon, In-Jin Jang, Kyung-Sang Yu, Kyoung Soo Lim
BACKGROUND: Human carboxylesterase 1 (CES1) is a serine esterase that hydrolyses various exogenous and endogenous compounds including oseltamivir, a prodrug used to treat influenza. A novel CES1 c.662A>G single nucleotide polymorphism (SNP) was predicted to decrease CES1 enzymatic activity in an in silico analysis. This study evaluated the effect of the c.662A>G SNP on the pharmacokinetics (PK) of oseltamivir in humans. METHODS: A single oral dose of oseltamivir at 75 mg was administered to 20 healthy subjects, 8 heterozygous c...
2017: PloS One
https://www.readbyqxmd.com/read/28435140/biowaiver-monographs-for-immediate-release-solid-oral-dosage-forms-enalapril
#3
REVIEW
Roger K Verbeeck, Isadore Kanfer, Raimar Löbenberg, Bertil Abrahamsson, Rodrigo Cristofoletti, D W Groot, Peter Langguth, James E Polli, Alan Parr, Vinod P Shah, Mehul Mehta, Jennifer B Dressman
Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhibitor enalaprilat. Enalapril as the maleate salt is shown to be highly soluble, but only 60 to 70% of an orally administered dose of enalapril is absorbed from the gastrointestinal tract into the enterocytes...
April 20, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435029/activity-of-carboxylesterases-glutathione-s-transferase-and-monooxygenase-on-rhipicephalus-microplus-exposed-to-fluazuron
#4
Fabrício Nascimento Gaudêncio, Guilherme Marcondes Klafke, Vinícius Menezes Tunholi-Alves, Thaís Paes Ferreira, Cristiane Nunes Coelho, Adivaldo Henrique da Fonseca, Isabele da Costa Angelo, Jairo Pinheiro
The objective of this study was to assess the effect of the exposure to fluazuron on the activity of common pesticide detoxification enzyme groups in the cattle tick (Rhipicephalus microplus). Engorged females of a susceptible strain (POA) and a resistant strain (Jaguar) were exposed in vitro to fluazuron and their eggs and larvae were used to compare the activities of the general esterases, mixed-function oxidases (MFO) and glutathione-S-transferase (GST). The results showed significant elevation in MFO contents and esterases activity in the resistant strain when compared with the susceptible strain, in eggs and larvae respectively...
April 20, 2017: Parasitology International
https://www.readbyqxmd.com/read/28433595/effects-of-chlorpyrifos-on-soil-carboxylesterase-activity-at-an-aggregate-size-scale
#5
Juan C Sanchez-Hernandez, Marco Sandoval
The impact of pesticides on extracellular enzyme activity has been mostly studied on the bulk soil scale, and our understanding of the impact on an aggregate-size scale remains limited. Because microbial processes, and their extracellular enzyme production, are dependent on the size of soil aggregates, we hypothesized that the effect of pesticides on enzyme activities is aggregate-size specific. We performed three experiments using an Andisol to test the interaction between carboxylesterase (CbE) activity and the organophosphorus (OP) chlorpyrifos...
April 20, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28428009/effect-of-methylparaben-in-artemia-franciscana
#6
Amparo Comeche, María Martín-Villamil, Yolanda Pico, Inma Varó
In this study, the toxicity of methylparaben (MeP) an emerging contaminant, was analyzed in the sexual species Artemia franciscana, due to its presence in coastal areas and marine saltworks in the Mediterranean region. The acute toxicity (24h-LC50) of MeP in nauplii was tested and its chronic effect (9days) evaluated by measuring survival and growth under two sublethal concentrations (0.0085 and 0.017mg/L). Also, the effect on several key enzymes involved in: antioxidant defences (catalase (CAT) and gluthathion-S-transferase (GST)), neural activity (cholinesterase (ChE)) and xenobiotic biotransformation (carboxylesterase (CbE), was assessed after 48h under sublethal exposure...
April 17, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28416547/simulating-intestinal-transporter-and-enzyme-activity-in-a-physiologically-based-pharmacokinetic-model-for-tenofovir-disoproxil-fumarate
#7
Darren M Moss, P Domanico, M Watkins, S Park, R Randolph, S Wring, J Hobson, S Rannard, M Siccardi, A Owen
Tenofovir disoproxil fumarate (TDF), a prodrug of tenofovir, has oral bioavailability (25%) limited by intestinal transport (p-glycoprotein), and intestinal degradation (carboxylesterase).….
April 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28396528/human-enterocytes-as-an-in-vitro-model-for-the-evaluation-of-intestinal-drug-metabolism-characterization-of-drug-metabolizing-enzyme-activities-of-cryopreserved-human-enterocytes-from-twenty-four-donors
#8
Ming-Chih David Ho, Nick Ring, Kirsten Amaral, Utkarsh Doshi, Albert Li
We report here successful isolation and cryopreservation of enterocytes from human small intestine. The enterocytes were isolated by enzyme digestion of the intestinal lumen followed by partial purification via differential centrifugation. The enterocytes were cryopreserved directly after isolation without culturing to maximize retention of in vivo drug metabolizing enzyme activities. Post-thaw viability of the cryopreserved enterocytes was consistently over 80% based on trypan blue exclusion. Cryopreserved enterocytes pooled from 8 donors (4 male and 4 female) were evaluated for their metabolism of 14 pathway-selective substrates: CYP1A2 (phenacetin hydroxylation), CYP2A6 (coumarin 7-hydroxylation), CYP2B6 (bupropion hydroxylation), CYP2C8 (paclitaxel 6α-hydroxylation), CYP2C9 (diclofenac 4-hydroxylation), CYP2C19 (s-mephenytoin 4-hydroxylation), CYP2D6 (dextromethorphan hydroxylation), CYP2E1 (chlorzoxazone 6-hydroxylation), CYP3A4 (midazolam 1'-hydroxylation and testosterone 6β-hydroxylation), CYP2J2 (astemizole O-demethylation), UDP-glucuronosyltransferase (UGT; 7-hydroxycoumarin glucuronidation), sulfotransferase (SULT; 7-hydroxycoumarin sulfation), and carboxylesterase 2 (CES2; irinotecan hydrolysis) activities...
April 10, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28394886/carboxylesterase-gene-amplifications-associated-with-insecticide-resistance-in-aedes-albopictus-geographical-distribution-and-evolutionary-origin
#9
Linda Grigoraki, Dimitra Pipini, Pierrick Labbé, Alexandra Chaskopoulou, Mylene Weill, John Vontas
BACKGROUND: Aedes albopictus is one of the most invasive human disease vectors. Its control has been largely based on insecticides, such as the larvicide temephos. Temephos resistance has been associated with the up-regulation, through gene amplification, of two carboxylesterase (CCE) genes closely linked on the genome, capable of sequestering and metabolizing temephos oxon, the activated form of temephos. PRINCIPAL FINDINGS: Here, we investigated the occurrence, geographical distribution and origin of the CCE amplicon in Ae...
April 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28393686/impact-of-salt-concentration-and-ph-on-surface-charged-residues-controlling-protein-association-pathways-in-carboxylesterase-estgta2
#10
Jessica K Moisan, Fatma Meddeb-Mouelhi, David M Charbonneau, Marc Beauregard
Understanding the relationship between enzymatic stability and the amino acid sequence encoding such enzymes is of utmost importance. Here we thoroughly characterized the behavior of the carboxylesterase EstGtA2 from Geobacillus thermodenitrificans during thermal denaturation at different pH with various salt concentrations. EstGtA2 was characterized by circular dichroism regarding conformation and thermal stability, by dynamic light scattering for detection of association/aggregation, by enzymatic assays for activity, and by monitoring the impact of heat treatments on activity...
April 4, 2017: Protein and Peptide Letters
https://www.readbyqxmd.com/read/28382676/natural-genomic-amplification-of-cholinesterase-genes-in-animals
#11
REVIEW
Arnaud Chatonnet, Nicolas Lenfant, Pascale Marchot, Murray E Selkirk
Tight control of the concentration of acetylcholine at cholinergic synapses requires precise regulation of the number and state of the acetylcholine receptors, and of the synthesis and degradation of the neurotransmitter. In particular, the cholinesterase activity has to be controlled exquisitely. In the genome of the first experimental models used (man, mouse, zebrafish and drosophila), there are only one or two genes coding for cholinesterases, whereas there are more genes for their closest relatives the carboxylesterases...
April 5, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28379972/the-novel-nematicide-wact-86-interacts-with-aldicarb-to-kill-nematodes
#12
Andrew R Burns, Rachel Bagg, May Yeo, Genna M Luciani, Michael Schertzberg, Andy G Fraser, Peter J Roy
Parasitic nematodes negatively impact human and animal health worldwide. The market withdrawal of nematicidal agents due to unfavourable toxicities has limited the available treatment options. In principle, co-administering nematicides at lower doses along with molecules that potentiate their activity could mitigate adverse toxicities without compromising efficacy. Here, we screened for new small molecules that interact with aldicarb, which is a highly effective treatment for plant-parasitic nematodes whose toxicity hampers its utility...
April 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28365764/transcriptome-analysis-and-identification-of-major-detoxification-gene-families-and-insecticide-targets-in-grapholita-molesta-busck-lepidoptera-tortricidae
#13
Yanqiong Guo, Yanping Chai, Lijun Zhang, Zhiguo Zhao, Ling-Ling Gao, Ruiyan Ma
The oriental fruit moth, Grapholita molesta (Busck) (Lepidoptera: Tortricidae), is an important pest of most stone and pome fruits and causes serious damage to the fruit industry worldwide. This insect pest has been primarily controlled through the application of insecticides; as a result, G. molesta has developed resistance to many different types of insecticides. To identify detoxification genes, we have, de novo, sequenced the transcriptome of G. molesta (Lepidoptera: Tortricidae) and yielded 58,970 unigenes of which 26,985 unigenes matched to known proteins...
January 1, 2017: Journal of Insect Science
https://www.readbyqxmd.com/read/28364223/remarkable-reactivity-of-alkoxide-acetato-bridged-binuclear-copper-ii-complex-as-artificial-carboxylesterase
#14
Bin Xu, Weidong Jiang, Xiaoqiang Liu, Fuan Liu, Zheng Xiang
Bromo-containing binuclear Schiff base copper(II) complex, Cu2L(OAc), with an alkoxo/acetato-bridged moiety was employed as a model of carboxylesterases to promote the hydrolytic cleavage of p-nitrophenyl picolinate (PNPP). Furthermore, the reactivity of a mononuclear complex (CuHL) was evaluated for comparing it with that of binuclear one. The results reveal that the as-prepared binuclear Cu2L(OAc) efficiently accelerated the hydrolysis of PNPP, giving rise to excess four orders of magnitude rate enhancement in contrast to the un-catalyzed reaction...
March 31, 2017: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/28351975/long-noncoding-mirna-gene-represses-wheat-%C3%AE-diketone-waxes
#15
Daiqing Huang, J Allan Feurtado, Mark A Smith, Leah K Flatman, Chushin Koh, Adrian J Cutler
The cuticle of terrestrial plants functions as a protective barrier against many biotic and abiotic stresses. In wheat and other Triticeae, β-diketone waxes are major components of the epicuticular layer leading to the bluish-white glaucous trait in reproductive-age plants. Glaucousness in durum wheat is controlled by a metabolic gene cluster at the WAX1 (W1) locus and a dominant suppressor INHIBITOR of WAX1 (Iw1) on chromosome 2B. The wheat D subgenome from progenitor Aegilops tauschii contains W2 and Iw2 paralogs on chromosome 2D...
April 11, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28345025/optimization-of-a-neural-stem-cell-mediated-carboxylesterase-irinotecan-gene-therapy-for-metastatic-neuroblastoma
#16
Margarita Gutova, Leanne Goldstein, Marianne Metz, Anahit Hovsepyan, Lyudmila G Tsurkan, Revathiswari Tirughana, Lusine Tsaturyan, Alexander J Annala, Timothy W Synold, Zesheng Wan, Robert Seeger, Clarke Anderson, Rex A Moats, Philip M Potter, Karen S Aboody
Despite improved survival for children with newly diagnosed neuroblastoma (NB), recurrent disease is a significant problem, with treatment options limited by anti-tumor efficacy, patient drug tolerance, and cumulative toxicity. We previously demonstrated that neural stem cells (NSCs) expressing a modified rabbit carboxylesterase (rCE) can distribute to metastatic NB tumor foci in multiple organs in mice and convert the prodrug irinotecan (CPT-11) to the 1,000-fold more toxic topoisomerase-1 inhibitor SN-38, resulting in significant therapeutic efficacy...
March 17, 2017: Molecular Therapy Oncolytics
https://www.readbyqxmd.com/read/28334183/comparative-transcriptional-analysis-of-the-host-specialized-aphids-aphis-gossypii-hemiptera-aphididae
#17
Yuan-Chen Zhang, Hai-Xia Lei, Ning-Hui Miao, Xiang-Dong Liu
Host specialization is an ubiquitous character in aphid populations. Many polyphagous aphid populations usually consist of several subpopulations that have strong fidelity to a specific host or a subset of host range. Host specialization is an evolutional result of food habit of insects. However, genetic basis and molecular mechanism of host specialization are still unclear. In this study, we presented a comparative analysis on global gene expression profiles of three lineages of Aphis gossypii Glover: cotton-specialized (CO), cucurbit-specialized (CU), and CU reared on cowpea (CU-cowpea), using RNA-Seq method...
April 1, 2017: Journal of Economic Entomology
https://www.readbyqxmd.com/read/28334129/transcriptional-responses-of-detoxification-genes-to-four-plant-allelochemicals-in-aphis-gossypii
#18
Fen Li, Kang-Sheng Ma, Ping-Zhuo Liang, Xue-Wei Chen, Ying Liu, Xi-Wu Gao
Aphis gossypii Glover (Hemiptera: Aphididae) can damage a variety of agricultural crops, so it is very important for cotton aphids to evolve adaptive mechanisms to various allelochemicals from host plants. Our results aim to provide a fundamental and rich resource for exploring aphid functional genes in A. gossypii. A transcriptome data set and five expression profile data sets of A. gossypii samples were analyzed by Illumina sequencing platform. In total, 53,763,866 reads were assembled into 1,963,516 contigs and 28,555 unigenes...
April 1, 2017: Journal of Economic Entomology
https://www.readbyqxmd.com/read/28331290/effects-of-dexamethasone-coadministered-with-oseltamivir-on-the-pharmacokinetics-of-oseltamivir-in-healthy-volunteers
#19
Kyungho Jang, Min-Kyoung Kim, Jaeseong Oh, SeungHwan Lee, Joo-Youn Cho, Kyung-Sang Yu, Tai Kiu Choi, Sang-Hyuk Lee, Kyoung Soo Lim
PURPOSE: Oseltamivir is widely used in the treatment and prophylaxis of influenza A and B viral infections. It is ingested as an oral prodrug that is rapidly metabolized by carboxylesterase 1 (CES1) to its active form, oseltamivir carboxylate. Dexamethasone is also used in the treatment of acute respiratory distress syndrome, a severe complication of influenza; however, its influence on the pharmacokinetics (PK) of oseltamivir is controversial. The aim of this study was to investigate the effects of coadministering oseltamivir and dexamethasone on the PK of oseltamivir in healthy volunteers...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28318508/effects-of-novel-brominated-flame-retardant-tbph-and-its-metabolite-tbmehp-on-human-vascular-endothelial-cells-implication-for-human-health-risks
#20
Ping Xiang, Rong-Yan Liu, Hong-Jie Sun, Yun-Wen Yang, Xin-Yi Cui, Lena Q Ma
As a replacement for polybrominated diphenyl ethers, bis-(2-ethylhexyl) tetrabromophthalate (TBPH) is widely used as a novel flame retardant and has been detected in many environmental matrix including human blood. TBPH can be metabolized into mono-(2-ethyhexyl) tetrabromophthalate (TBMEHP) by carboxylesterase. However, their adverse effects on human vascular endothelium and their potential impacts on human cardiovascular disease are unknown. In this study, their adverse effects and associated molecular mechanisms on human vascular endothelial cells (HUVECs) were investigated...
March 16, 2017: Environmental Research
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