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carboxylesterase

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https://www.readbyqxmd.com/read/28731595/identification-of-carboxylesterase-genes-associated-with-pyrethroid-resistance-in-the-malaria-vector-anopheles-sinensis-diptera-culicidae
#1
Xue-Mei Wu, Bo-Ying Xu, Feng-Ling Si, Jianyong Li, Zhen-Tian Yan, Zheng-Wen Yan, Xiu He, Bin Chen
BACKGROUND: Carboxylesterases (CCEs) are one of three large detoxification enzyme families. Some CCEs are active on synthetic insecticides with ester structures. Anopheles sinensis is an important malaria vector in eastern Asia. This study identified and characterized the CCE genes in the An. sinensis genome and determined CCE genes associated with pyrethroid resistance using RNA-seq and RT-qPCR, in An. sinensis from Anhui, Chongqing, and Yunnan in China. RESULTS: Fifty-seven putative CCEs were identified and placed into 3 classes, 12 subfamilies and 14 clades through phylogenetics and homology analyses...
July 21, 2017: Pest Management Science
https://www.readbyqxmd.com/read/28719874/combined-effects-of-temperature-and-clomazone-gamit-%C3%A2-on-oxidative-stress-responses-and-b-esterase-activity-of-physalaemus-nattereri-leiuperidae-and-rhinella-schneideri-bufonidae-tadpoles
#2
Juliane Silberschmidt Freitas, Andreia Arantes Felício, Fabrício Barreto Teresa, Eduardo Alves de Almeida
Temperature is an important factor influencing the toxicity of chemicals in aquatic environments. Neotropical tadpoles experience large temperature fluctuations in their habitats and many species are distributed in areas impacted by agriculture. This study evaluated the effects caused by the exposure to clomazone (Gamit(®)) at different temperatures (28, 32 and 36 °C) on biochemical stress responses and esterase activities in Physalaemus nattereri and Rhinella schneideri tadpoles. Results evidenced that temperature modulates the effects of clomazone on biochemical response of tadpoles...
July 14, 2017: Chemosphere
https://www.readbyqxmd.com/read/28713276/structure-activity-relationships-of-pentacyclic-triterpenoids-as-potent-and-selective-inhibitors-against-human-carboxylesterase-1
#3
Li-Wei Zou, Tong-Yi Dou, Ping Wang, Wei Lei, Zi-Miao Weng, Jie Hou, Dan-Dan Wang, Yi-Ming Fan, Wei-Dong Zhang, Guang-Bo Ge, Ling Yang
Human carboxylesterase 1 (hCE1), one of the most important serine hydrolases distributed in liver and adipocytes, plays key roles in endobiotic homeostasis and xenobiotic metabolism. This study aimed to find potent and selective inhibitors against hCE1 from phytochemicals and their derivatives. To this end, a series of natural triterpenoids were collected and their inhibitory effects against human carboxylesterases (hCEs) were assayed using D-Luciferin methyl ester (DME) and 6,8-dichloro-9,9-dimethyl-7-oxo-7,9-dihydroacridin-2-yl benzoate (DDAB) as specific optical substrate for hCE1, and hCE2, respectively...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28711984/clarithromycin-co-administration-does-not-increase-irinotecan-cpt-11-toxicity-in-colorectal-cancer-patients
#4
Katsuya Makihara, Sayaka Nakamura, Kazuyo Miyagi, Hiroyuki Ueno, Izumi Nakata
PURPOSE: Irinotecan (CPT-11) is used to treat advanced colorectal cancer. The drug is activated by carboxylesterases and rendered inactive by CYP3A4. Recently, the efficacy of combining CPT-11 and anti-epidermal growth factor receptor (EGFR) agents was confirmed in patients with KRAS wild-type metastatic colorectal cancer. Clarithromycin (CAM) is a strong CYP3A inhibitor often used to prevent rash associated with anti-EGFR therapy. The objective of this study was to evaluate the risk of increased neutropenia and diarrhea in combining CPT-11 and CAM...
July 15, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28697978/functional-characterization-of-bdb1-a-well-conserved-carboxylesterase-among-tephritid-fruit-flies-associated-with-malathion-resistance-in-bactrocera-dorsalis-hendel
#5
Luo-Luo Wang, Xue-Ping Lu, Guy Smagghe, Li-Wei Meng, Jin-Jun Wang
There are many evidences that insect carboxylesterase possess important physiological roles in xenobiotic metabolism and are implicated in the detoxification of organophosphate (OP) insecticides. Despite the ongoing resistance development in the oriental fruit fly, Bactrocera dorsalis (Hendel), the molecular basis of carboxylesterase and its ability to confer OP resistance remain largely obscure. This study was initiated to provide a better understanding of carboxylesterase-mediated resistance mechanism in a tephritid pest fly...
July 8, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28677105/carboxylesterases-in-lipid-metabolism-from-mouse-to-human
#6
REVIEW
Jihong Lian, Randal Nelson, Richard Lehner
Mammalian carboxylesterases hydrolyze a wide range of xenobiotic and endogenous compounds, including lipid esters. Physiological functions of carboxylesterases in lipid metabolism and energy homeostasis in vivo have been demonstrated by genetic manipulations and chemical inhibition in mice, and in vitro through (over)expression, knockdown of expression, and chemical inhibition in a variety of cells. Recent research advances have revealed the relevance of carboxylesterases to metabolic diseases such as obesity and fatty liver disease, suggesting these enzymes might be potential targets for treatment of metabolic disorders...
July 4, 2017: Protein & Cell
https://www.readbyqxmd.com/read/28667306/crystal-structure-of-pelagibacterium-halotolerans-pe8-new-insight-into-its-substrate-binding-pattern
#7
Ying-Yi Huo, Suhua Li, Jing Huang, Zhen Rong, Zhao Wang, Zhengyang Li, Rui Ji, Siyun Kuang, Heng-Lin Cui, Jixi Li, Xue-Wei Xu
Lysophospholipase_carboxylesterase (LPCE) has highly conserved homologs in many diverse species ranging from bacteria to humans, as well as substantial biological significance and potential therapeutic implications. However, its biological function and catalytic mechanism remain minimally investigated because of the lack of structural information. Here, we report the crystal structure of a bacterial esterase PE8 belonging to the LPCE family. The crystal structure of PE8 was solved with a high resolution of 1...
June 30, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28664339/metabolite-profiling-of-carbamazepine-and-ibuprofen-in-solea-senegalensis-bile-using-high-resolution-mass-spectrometry
#8
Jaume Aceña, Sandra Pérez, Peter Eichhorn, Montserrat Solé, Damià Barceló
The widespread occurrence of pharmaceuticals in the aquatic environment has raised concerns about potential adverse effects on exposed wildlife. Very little is currently known on exposure levels and clearance mechanisms of drugs in marine fish. Within this context, our research was focused on the identification of main metabolic reactions, generated metabolites, and caused effects after exposure of fish to carbamazepine (CBZ) and ibuprofen (IBU). To this end, juveniles of Solea senegalensis acclimated to two temperature regimes of 15 and 20 °C for 60 days received a single intraperitoneal dose of these drugs...
June 29, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28660514/monitoring-of-organic-pollutants-in-marine-environment-by-semipermeable-membrane-devices-and-mussels-accumulation-and-biochemical-responses
#9
Oya S Okay, Burak Karacık, Abbas Güngördü, Atilla Yılmaz, Nazmi C Koyunbaba, Sevil D Yakan, Bernhard Henkelmann, Karl-Werner Schramm, Murat Ozmen
This study involves the monitoring of organic pollutants using transplanted mussels (Mytilus galloprovincialis) as bioindicator organisms and semipermeable membrane devices (SPMDs) as passive samplers. Mussels and SPMDs were deployed to marinas, shipyards and shipbreaking yards on the coastal area of Turkey and retrieved after 60 days. Polycyclic aromatic hydrocarbons (PAH), polychlorinated biphenyls (PCB) and organochlorine pesticide (OCP) compounds were analysed with high-resolution GC-MS. Total PAH concentrations in SPMDs and mussels ranged from 200 to 4740 ng g sampler(-1) and from 7...
June 28, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28647840/interaction-of-ferulic-acid-with-glutathione-s-transferase-and-carboxylesterase-genes-in-the-brown-planthopper-nilaparvata-lugens
#10
Jun Yang, Xiao-Qin Sun, Shu-Ying Yan, Wen-Jun Pan, Mao-Xin Zhang, Qing-Nian Cai
Plant phenolics are crucial defense phytochemicals against herbivores and glutathione S-transferase (GST) and carboxylesterase (CarE) in herbivorous insects are well-known detoxification enzymes for such xenobiotics. To understand relationship between a plant phenolic and herbivore GST or CarE genes, we evaluated the relationship between a rice phenolic ferulic acid and resistance to brown planthopper (BPH, Nilaparvata lugens), and investigated the interaction of ferulic acid with GST or CarE genes in BPH. The results indicate that ferulic acid content in tested rice varieties was highly associated with resistance to BPH...
June 24, 2017: Journal of Chemical Ecology
https://www.readbyqxmd.com/read/28647665/comparative-metabolism-of-ddao-benzoate-in-liver-microsomes-from-various-species
#11
Hong-Ying Ma, Jia-Da Yang, Jie Hou, Li-Wei Zou, Qiang Jin, Da-Cheng Hao, Jing Ning, Guang-Bo Ge, Ling Yang
DDAB (6,8-dichloro-9,9-dimethyl-7-oxo-7,9-dihydroacridin-2-yl benzoate) is a newly developed near-infrared fluorescent probe for human carboxylesterase 2 (hCE2), exhibiting high specificity and good reactivity for real-time monitoring the enzymatic activities of hCE2 in complex biological systems. In order to explore the applicability of DDAB in commonly used animal species, the interspecies difference in DDAB hydrolysis was carefully investigated by using liver microsomes from human and five experimental animals including mouse, rat, dog, minipig and monkey...
June 21, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28639420/the-pharmacokinetics-of-enalapril-in-relation-to-ces1-genotype-in-healthy-danish-volunteers
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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...
August 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
#18
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
#19
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
#20
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
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