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carboxylesterase

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https://www.readbyqxmd.com/read/28213320/comparative-analysis-of-mosquito-diptera-culicidae-aedes-aegypti-liston-responses-to-the-insecticide-temephos-and-plant-derived-essential-oil-derived-from-piper-betle-l
#1
Prabhakaran Vasantha-Srinivasan, Sengottayan Senthil-Nathan, Athirstam Ponsankar, Annamalai Thanigaivel, Edward-Sam Edwin, Selvaraj Selin-Rani, Muthiah Chellappandian, Venkatraman Pradeepa, Jalasteen Lija-Escaline, Kandaswamy Kalaivani, Wayne B Hunter, Veeramuthu Duraipandiyan, Naif Abdullah Al-Dhabi
Resistance to treatments with Temephos or plant derived oil, Pb-CVO, between a field collected Wild Strain (WS) and a susceptible Laboratory Strain (LS) of Ae. aegypti were measured. The Temephos (0.1mg/L) showed the greatest percentage of mosquito mortality compared to Pb-CVO (1.5mg/L) in LS Ae. aegypti. However, WS Ae. aegypti was not significantly affected by Temephos (0.1mg/L) treatment compare to the Pb-CVO (1.5mg/L). However, both strains (LS and WS) when treated with Pb-CVO (1.5mg/L) displayed steady larval mortality rate across all instars...
February 14, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28197946/alterations-in-the-skin-of-labeo-rohita-exposed-to-an-azo-dye-eriochrome-black-t-a-histopathological-and-enzyme-biochemical-investigation
#2
Ayan Srivastava, Neeraj Verma, Arup Mistri, Brijesh Ranjan, Ashwini Kumar Nigam, Usha Kumari, Swati Mittal, Ajay Kumar Mittal
Histopathological changes and alterations in the activity of certain metabolic and antioxidant enzymes were analyzed in the head skin of Labeo rohita, exposed to sublethal test concentrations of the azo dye, Eriochrome black T for 4 days, using 24 h renewal bioassay method. Hypertrophied epithelial cells, increased density of mucous goblet cells, and profuse mucous secretion at the surface were considered to protect the skin from toxic impact of the azo dye. Degenerative changes including vacuolization, shrinkage, decrease in dimension, and density of club cells with simultaneous release of their contents in the intercellular spaces were associated to plug them, preventing indiscriminate entry of foreign matter...
February 15, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28187780/levels-of-insecticide-resistance-to-deltamethrin-malathion-and-temephos-and-associated-mechanisms-in-aedes-aegypti-mosquitoes-from-the-guadeloupe-and-saint-martin-islands-french-west-indies
#3
Daniella Goindin, Christelle Delannay, Andric Gelasse, Cédric Ramdini, Thierry Gaude, Frédéric Faucon, Jean-Philippe David, Joël Gustave, Anubis Vega-Rua, Florence Fouque
BACKGROUND: In the Guadeloupe and Saint Martin islands, Aedes aegypti mosquitoes are the only recognized vectors of dengue, chikungunya, and Zika viruses. For around 40 years, malathion was used as a mosquito adulticide and temephos as a larvicide. Since the European Union banned the use of these two insecticide molecules in the first decade of the 21st century, deltamethrin and Bacillus thuringiensis var. israelensis are the remaining adulticide and larvicide, respectively, used in Guadeloupe...
February 10, 2017: Infectious Diseases of Poverty
https://www.readbyqxmd.com/read/28163251/overexpression-of-carboxylesterase-contributes-to-the-attenuation-of-cyanotoxin-microcystin-lr-toxicity
#4
Shota Takumi, Tai Shimono, Satoshi Ikema, Yuki Hotta, Petros K Chigwechokha, Kazuhiro Shiozaki, Yasumasa Sugiyama, Mitsuru Hashimoto, Tatsuhiko Furukawa, Masaharu Komatsu
Microcystin-LR is a hepatotoxin produced by several cyanobacteria. Its toxicity is mainly due to a inhibition of protein phosphatase, PP1 and PP2A. Previously, we used a cell line stably expressing uptake transporter for microcystin-LR, OATP1B3 (HEK293-OATP1B3 cells). In this study, to determine whether overexpression of carboxylesterase (CES), which degrades ester-group and amide-group, attenuates the cytotoxicity of microcystin-LR, we generated the HEK293-OATP1B3/CES2 double-transfected cells. HEK293-OATP1B3/CES2 cells showed high hydrolysis activity of p-nitrophenyl acetate (PNPA), which is an authentic substrate for esterase...
February 3, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28146010/novel-procedure-with-improved-resolution-and-specificity-for-amplification-and-differentiation-of-variants-of-the-gene-encoding-carboxylesterase-1
#5
Ditte Bjerre, Henrik B Rasmussen
Carboxylesterase 1 (CES1) is implicated in the metabolism of several commonly used drugs and other xenobiotics. The gene encoding this enzyme, CES1, is duplicated in some individuals. The original gene copy is called CES1A1. The duplicated version, CES1A2, is a hybrid of CES1A1 and the CES1-related pseudogene, CES1P1. Variants of CES1A2 with a weak and a strong promoter, respectively, have been reported. In addition, there are chimeric subtypes of CES1A1 that contain a segment of CES1P1. Collectively, this represents challenges to the genotyping of CES1 that previous procedures have had difficulties in solving, frequently leading to loss of specificity and inaccurate genotyping...
January 31, 2017: Pharmacogenetics and Genomics
https://www.readbyqxmd.com/read/28140733/integrated-metabonomic-proteomic-studies-on-blood-enrichment-effects-of-angelica-sinensis-on-a-blood-deficiency-mice-model
#6
Yongli Hua, Wangling Yao, Peng Ji, Yanming Wei
CONTEXT: Angelica sinensis (Oliv.) Diels (Umbelliferae) (AS) is a well-known Traditional Chinese Medicine (TCM) that enriches and regulates the blood. OBJECTIVE: An integrated metabonomic and proteomic method was developed and applied to study the blood enrichment effects and mechanisms of AS on blood deficiency (BD) mouse model. MATERIALS AND METHODS: Forty mice were randomly divided into the control, BD, High-dose of AS (ASH), Middle-dose of AS (ASM), and Low-dose of AS (ASL) groups...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28139840/novel-genetic-variants-in-carboxylesterase-1-predict-severe-early-onset-capecitabine-related-toxicity
#7
Seid Hamzic, Dominic Kummer, Sophie Milesi, David Mueller, Markus Joerger, Stefan Aebi, Ursula Amstutz, Carlo R Largiadèr
An important concern with the anticancer drug capecitabine (Cp), an oral prodrug of 5-fluorouracil, are dose-limiting adverse effects, in particular hand-foot syndrome (HFS) and diarrhea. Here, we evaluated the association of genetic variability in all enzymes of the Cp-activation pathway to 5-fluorouracil with Cp-related early-onset toxicity in 144 patients receiving Cp. We identified a haplotype encompassing five variants in the carboxylesterase 1 (CES1) gene region including an expression quantitative trait locus (Haplotype A3: ORadditive =2...
January 31, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28128444/suppression-of-carboxylesterases-by-imatinib-mediated-by-the-downregulation-of-pregnane-x-receptor
#8
Wenjing Luo, Yu Xin, Xia Zhao, Feng Zhang, Changqing Liu, Hongwei Fan, Tao Xi, Jing Xiong
BACKGROUND AND PURPOSE: Imatinib mesylate (IM) is first-line anti-chronic myeloid leukemia (CML) therapy as a specific inhibitor of BCR-ABL tyrosine kinase. IM in combination with other drugs has been widely applied in CML treatment, thus the influence of IM on drug metabolism enzymes (DMEs) is crucial to be understood in suggesting rational drug administration. Carboxylesterases (CESs) are important enzymes catalyzing hydrolytic biotransformation and play vital roles in the metabolism of numerous clinical drugs...
January 27, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28126414/recent-progress-in-the-discovery-of-natural-inhibitors-against-human-carboxylesterases
#9
REVIEW
Dan-Dan Wang, Li-Wei Zou, Qiang Jin, Jie Hou, Guang-Bo Ge, Ling Yang
Mammalian carboxylesterases (CEs) are important serine hydrolases catalyzing the hydrolysis of ester- or amide-containing compounds into the corresponding alcohols and carboxylic acids. In human, two primary carboxylesterases including hCE1 and hCE2 have been identified and extensively studied in the past decade. hCE1 is known to play crucial roles in the metabolism of a wide variety of endogenous esters, clinical drugs and insecticides, while hCE2 plays a key role in the metabolic activation of anticancer agents including irinotecan and capecitabine...
January 23, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28114328/pyrethroid-resistance-in-malaysian-populations-of-dengue-vector-aedes-aegypti-is-mediated-by-cyp9-family-of-cytochrome-p450-genes
#10
Intan H Ishak, Basile Kamgang, Sulaiman S Ibrahim, Jacob M Riveron, Helen Irving, Charles S Wondji
BACKGROUND: Dengue control and prevention rely heavily on insecticide-based interventions. However, insecticide resistance in the dengue vector Aedes aegypti, threatens the continued effectiveness of these tools. The molecular basis of the resistance remains uncharacterised in many endemic countries including Malaysia, preventing the design of evidence-based resistance management. Here, we investigated the underlying molecular basis of multiple insecticide resistance in Ae. aegypti populations across Malaysia detecting the major genes driving the metabolic resistance...
January 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28112927/selective-inhibitors-of-human-liver-carboxylesterase-based-upon-a-%C3%AE-lapachone-scaffold-novel-reagents-for-reaction-profiling
#11
M Jason Hatfield, Jingwen Chen, Ellie M Fratt, Liying Chi, John C Bollinger, Randall J Binder, John Bowling, Janice L Hyatt, Jerrod Scarborough, Cynthia Jeffries, Philip M Potter
Carboxylesterases (CE) are ubiquitous enzymes that are responsible for the metabolism of xenobiotics, including drugs such as irinotecan and oseltamivir. Inhibition of CEs significantly modulates the efficacy of such agents. We report here that β-lapachone is a potent, reversible CE inhibitor with Ki values in the nanomolar range. A series of amino and phenoxy analogues have been synthesized and while the former are very poor inhibitors, the latter compounds are highly effective in modulating CE activity. Our data demonstrate that tautomerism of the amino derivatives to the imino forms likely accounts for their loss in biological activity...
January 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28105534/construction-of-a-novel-lipolytic-fusion-biocatalyst-gdest-lip-for-industrial-application
#12
Renata Gudiukaite, Mikas Sadauskas, Audrius Gegeckas, Vilius Malunavicius, Donaldas Citavicius
The gene encoding esterase (GDEst-95) from Geobacillus sp. 95 was cloned and sequenced. The resulting open reading frame of 1497 nucleotides encoded a protein with calculated molecular weight of 54.7 kDa, which was classified as a carboxylesterase with an identity of 93-97% to carboxylesterases from Geobacillus bacteria. This esterase can be grouped into family VII of bacterial lipolytic enzymes, was active at broad pH (7-12) and temperature (5-85 °C) range and displayed maximum activity toward short acyl chain p-nitrophenyl (p-NP) esters...
January 19, 2017: Journal of Industrial Microbiology & Biotechnology
https://www.readbyqxmd.com/read/28099843/human-carboxylesterase-2-reverses-obesity-induced-diacylglycerol-accumulation-and-glucose-intolerance
#13
Maxwell A Ruby, Julie Massart, Devon M Hunerdosse, Milena Schönke, Jorge C Correia, Sharon M Louie, Jorge L Ruas, Erik Näslund, Daniel K Nomura, Juleen R Zierath
Serine hydrolases are a large family of multifunctional enzymes known to influence obesity. Here, we performed activity-based protein profiling to assess the functional level of serine hydrolases in liver biopsies from lean and obese humans in order to gain mechanistic insight into the pathophysiology of metabolic disease. We identified reduced hepatic activity of carboxylesterase 2 (CES2) and arylacetamide deacetylase (AADAC) in human obesity. In primary human hepatocytes, CES2 knockdown impaired glucose storage and lipid oxidation...
January 17, 2017: Cell Reports
https://www.readbyqxmd.com/read/28077333/molecular-cloning-characterization-and-expression-analysis-of-two-juvenile-hormone-esterase-like-carboxylesterase-cdnas-in-chinese-mitten-crab-eriocheir-sinensis
#14
Yu Xu, Muzi Zhao, Yanfei Deng, Yuanjie Yang, Xuguang Li, Quanping Lu, Jiachun Ge, Jianlin Pan, Zhiqiang Xu
Precise regulation of methyl farnesoate (MF) titer is of prime importance throughout the crustacean life-cycle. Although the synthetic pathway of MF is well-documented, little is known about its degradation and recycling in crustaceans. Juvenile hormone esterase-like (JHE-like) carboxylesterase (CXE) is a key enzyme in MF degradation, thus playing a significant role in regulating the MF titer. We identified and characterized two cDNAs, Es-CXE1 and Es-CXE2, encoding JHE-like CXEs in Chinese mitten crab. Full-length cDNAs of Es-CXE1 and Es-CXE2 encode proteins composed of 584 and 597 amino acids, respectively, both of which contain a typical carboxylesterase domain...
March 2017: Comparative Biochemistry and Physiology. Part B, Biochemistry & Molecular Biology
https://www.readbyqxmd.com/read/28067292/design-of-a-15-n-molecular-unit-to-achieve-long-retention-of-hyperpolarized-spin-state
#15
Hiroshi Nonaka, Masashi Hirano, Yuki Imakura, Yoichi Takakusagi, Kazuhiro Ichikawa, Shinsuke Sando
Nuclear hyperpolarization is a phenomenon that can be used to improve the sensitivity of magnetic resonance molecular sensors. However, such sensors typically suffer from short hyperpolarization lifetime. Herein we report that [(15)N, D14]trimethylphenylammonium (TMPA) has a remarkably long spin-lattice relaxation time (1128 s, 14.1 T, 30 °C, D2O) on its (15)N nuclei and achieves a long retention of the hyperpolarized state. [(15)N, D14]TMPA-based hyperpolarized sensor for carboxylesterase allowed the highly sensitive analysis of enzymatic reaction by (15)N NMR for over 40 min in phophate-buffered saline (H2O, pH 7...
January 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28058522/identification-and-characterization-of-a-novel-carboxylesterase-fpbh-that-hydrolyzes-aryloxyphenoxypropionate-herbicides
#16
Chenghong Wang, Jiguo Qiu, Youjian Yang, Jinwei Zheng, Jian He, Shunpeng Li
OBJECTIVE: To identify and characterize a novel aryloxyphenoxypropionate (AOPP) herbicide-hydrolyzing carboxylesterase from Aquamicrobium sp. FPB-1. RESULTS: A carboxylesterase gene, fpbH, was cloned from Aquamicrobium sp. FPB-1. The gene is 798 bp long and encodes a protein of 265 amino acids. FpbH is smaller than previously reported AOPP herbicide-hydrolyzing carboxylesterases and shares only 21-35% sequence identity with them. FpbH was expressed in Escherichia coli BL21(DE3) and the product was purified by Ni-NTA affinity chromatography...
January 5, 2017: Biotechnology Letters
https://www.readbyqxmd.com/read/28046150/increased-expressions-of-genes-and-proteins-involved-in-mitochondrial-oxidation-and-antioxidant-pathway-in-adipose-tissue-of-pigs-selected-for-a-low-residual-feed-intake
#17
I Louveau, A Vincent, S Tacher, H Gilbert, F Gondret
Adipose tissue is a primary sensor for nutrient availability and regulates many functions including feed intake and energy homeostasis. This study was undertaken to determine the molecular responses of adipose tissue to differences in feed intake and feed efficiency. Subcutaneous adipose tissue was collected from two lines of pigs divergently selected for residual feed intake (RFI), a measure of feed efficiency defined as the difference between actual and expected feed intake, and from a subset of high-RFI pigs that were feed-restricted at the level of the voluntary feed intake of low-RFI pigs during the growing-finishing period...
December 2016: Journal of Animal Science
https://www.readbyqxmd.com/read/28044227/a-novel-versatile-family-iv-carboxylesterase-exhibits-high-stability-and-activity-in-a-broad-ph-spectrum
#18
Amélie Dukunde, Dominik Schneider, Mingji Lu, Silja Brady, Rolf Daniel
OBJECTIVES: To investigate the properties of a novel metagenome-derived member of the hormone-sensitive lipase family of lipolytic enzymes. RESULTS: A forest soil metagenome-derived gene encoding an esterase (Est06) belonging to the hormone-sensitive lipase family of lipolytic enzymes was subcloned, heterologously expressed and characterized. Est06 is a polypeptide of 295 amino acids with a molecular mass of 31 kDa. The deduced protein sequence shares 61% similarity with a hypothetical protein from the marine symbiont Candidatus Entotheonella sp...
January 2, 2017: Biotechnology Letters
https://www.readbyqxmd.com/read/28007454/comparative-study-of-hydrolytic-metabolism-of-dimethyl-phthalate-dibutyl-phthalate-and-di-2-ethylhexyl-phthalate-by-microsomes-of-various-rat-tissues
#19
Hitomi Ozaki, Kazumi Sugihara, Yoko Watanabe, Kyoko Moriguchi, Naoto Uramaru, Tomomichi Sone, Shigeru Ohta, Shigeyuki Kitamura
Phthalates are used in food packaging, and are transferred to foods as contaminants. In this study, we examined the hydrolytic metabolism of dimethyl phthalate (DMP), dibutyl phthalate (DBP) and di(2-ethylhexyl) phthalate (DEHP) by rat tissue microsomes. We found that carboxylesterase and lipase contribute differently to these activities. When DMP, DBP and DEHP were incubated with rat liver microsomes, DBP was most effectively hydrolyzed to the phthalate monoester, followed by DMP, and the activity toward DEHP was marginal...
February 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/27998705/in%C3%A2-vitro-in%C3%A2-vivo-extrapolation-of-intestinal-availability-for-carboxylesterase-substrates-using-portal-vein-cannulated-monkey
#20
Patrick E Trapa, Kevin Beaumont, Karen Atkinson, Heather Eng, Amanda King-Ahmad, Dennis O Scott, Tristan S Maurer, Li Di
Prediction of intestinal availability (FaFg) of carboxylesterase (CES) substrates is of critical importance in designing oral prodrugs with optimal properties, projecting human pharmacokinetics and dose, and estimating drug-drug interaction potentials. A set of ester prodrugs were evaluated using in vitro permeability (parallel artificial membrane permeability assay and Madin-Darby canine kidney cell line-low efflux) and intestinal stability (intestine S9) assays, as well as in vivo portal vein-cannulated cynomolgus monkey...
December 18, 2016: Journal of Pharmaceutical Sciences
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