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Y K Lyauk, C Stage, T K Bergmann, L Ferrero-Milliani, D Bjerre, R Thomsen, K P Dalhoff, H B Rasmussen, G Jürgens
The aim of this study was to identify demographic and genetic factors that significantly affect methylphenidate (MPH) pharmacokinetics (PK), and may help explain interindividual variability and further increase the safety of MPH. d-MPH plasma concentrations, demographic covariates, and carboxylesterase 1 (CES1) genotypes were gathered from 122 healthy adults and analyzed using nonlinear mixed effects modeling. The structural model that best described the data was a two-compartment disposition model with absorption transit compartments...
October 18, 2016: Clinical and Translational Science
Toby Fountain, Mark Ravinet, Richard Naylor, Klaus Reinhardt, Roger K Butlin
The rapid evolution of insecticide resistance remains one of the biggest challenges in the control of medically and economically important pests. Insects have evolved a diverse range of mechanisms to reduce the efficacy of the commonly used classes of insecticides and finding the genetic basis of resistance is a major aid to management. In a previously unstudied population, we performed an F2 resistance mapping cross for the common bed bug, Cimex lectularius, for which insecticide resistance is increasingly widespread...
October 12, 2016: G3: Genes—Genomes—Genetics
Hafiz Azhar Ali Khan, Waseem Akram
Developing resistance management strategies for eco-friendly insecticides is essential for the management of insect pests without harming the environment. Cyromazine is a biorational insecticide with very low mammalian toxicity. Resistance to cyromazine has recently been reported in house flies from Punjab, Pakistan. In order to propose a resistance management strategy for cyromazine, experiments were planned to study risk for resistance development, possibility of cross-resistance and bio-chemical mechanisms...
October 8, 2016: Chemosphere
Sofía Otero, Gisela Kristoff
Organophosphate insecticides (OPs) continue to be an important class of agrochemicals used in modern agriculture worldwide. Even though these pesticides persist in the environment for a relatively short time, they show a high acute toxicity that may represent a serious hazard for wildlife. Sub-lethal effects on non-target species are a focus in pest management programs and should be used as biomarkers. Cholinesterases (ChEs) are the most used biomarker of OP exposure in vertebrate and invertebrate species. However, the combined monitoring of ChE and carboxylesterase (CE) activities may provide a more useful indication of exposure and effect of the organisms...
October 6, 2016: Aquatic Toxicology
Tian Tao, Xi Xie, Mingxin Liu, Qinghua Jiang, Dongfa Zhu
The sesquiterpenoid methyl farnesoate (MF) is the unepoxidized form of insect juvenile hormone (JH) III, and is considered an equivalent of JH in crustaceans. Degradation of MF is similar to that of JH which occurs through ester hydrolysis by specific carboxylesterases (CXEs). In this study, the full-length cDNAs of two JH esterase-like CXEs were cloned from the swimming crab, Portunus trituberculatus. The predicted amino acid sequences of the two PtCXEs contain the conserved motifs including catalytic triad and oxyanion hole, which are the hallmark of the CXE family proteins...
October 5, 2016: Comparative Biochemistry and Physiology. Part B, Biochemistry & Molecular Biology
Miao Xie, Na-Na Ren, Yan-Chun You, Wei-Jun Chen, Qi-Sheng Song, Min-Sheng You
BACKGROUND: Carboxylesterases (CarEs) are involved in metabolic detoxification of dietary and environmental xenobiotics in insects. However, due to the complexity of the protein family, the involvement of CarEs in insecticide metabolism in Plutella xylostella has not been fully elucidated. This study aimed to characterize two CarE genes and assess their potential roles in response to chlorpyrifos in P. xylostella. RESULTS: Synergistic test showed that triphenyl phosphate decreased the resistance of the 3(rd) -instar larvae to chlorpyrifos...
September 22, 2016: Pest Management Science
Jarrad K Baker, Sara M Long, Kathryn L Hassell, Vincent J Pettigrove, Marthe M Gagnon
Port Phillip Bay, Australia, is a large semi-closed bay with over four million people living in its catchment basin. The Bay receives waters from the Yarra River which drains the city of Melbourne, as well as receiving the discharges of sewage treatment plants and petrochemical and agricultural chemicals. A 1999 study demonstrated that fish inhabiting Port Phillip Bay showed signs of effects related to pollutant exposure despite pollution management practices having been implemented for over a decade. To assess the current health status of the fish inhabiting the Bay, a follow up survey was conducted in 2015...
2016: PloS One
Lai Peng, Stephanie Piekos, Grace L Guo, Xiao-Bo Zhong
The expression of phase-I drug metabolizing enzymes in liver changes dramatically during postnatal liver maturation. Farnesoid X receptor (FXR) is critical for bile acid and lipid homeostasis in liver. However, the role of FXR in regulating ontogeny of phase-I drug metabolizing genes is not clear. Hence, we applied RNA-sequencing to quantify the developmental expression of phase-I genes in both Fxr-null and control (C57BL/6) mouse livers during development. Liver samples of male C57BL/6 and Fxr-null mice at 6 different ages from prenatal to adult were used...
September 2016: Acta Pharmaceutica Sinica. B
Ya-Jing Liu, Shi-Yang Li, Jie Hou, Yan-Fang Liu, Dan-Dan Wang, Yong-Shan Jiang, Guang-Bo Ge, Xin-Miao Liang, Ling Yang
White Mulberry Root-bark (WMR) is an edible Chinese herbal used for the treatment of inflammation, nephritis and asthma. This study aimed to investigate the inhibitory effects of ethanol extract from WMR against human carboxylesterase 2 (hCE2), as well as to identity and character natural hCE2 inhibitors in this herbal. Our results demonstrated that the ethanol extract of WMR displayed potent inhibitory effects against hCE2, while three major bioactive constitutes in WMR were identified on the basis of LC fingerprinting combined with activity-based screening of LC fractions...
October 1, 2016: Fitoterapia
Qingqi Lin, Siyuan Chen, Yuanqing Chao, Xiongfei Huang, Shizhong Wang, Rongliang Qiu
Uptake and accumulation by plants is a significant pathway in the migration and transformation of phthalate esters (PAEs) in the environment. However, limited information is available on the mechanisms of PAE metabolism in plants. Here, we investigated the metabolism of di-n-butyl phthalate (DnBP), one of the most frequently detected PAEs, in pumpkin (Cucurbita moschata) seedlings via a series of hydroponic experiments with an initial concentration of 10 mg L(-1). DnBP hydrolysis occurred primarily in the root, and two of its metabolites, mono-n-butyl phthalate (MnBP) and phthalic acid (PA), were detected in all plant tissues...
September 30, 2016: Environmental Pollution
Taiji Nomura
Plants have evolved secondary metabolite biosynthetic pathways of immense rich diversity. The genes encoding enzymes for secondary metabolite biosynthesis have evolved through gene duplication followed by neofunctionalization, thereby generating functional diversity. Emerging evidence demonstrates that some of those enzymes catalyze reactions entirely different from those usually catalyzed by other members of the same family; e.g. transacylation catalyzed by an enzyme similar to a hydrolytic enzyme. Tuliposide-converting enzyme (TCE), which we recently discovered from tulip, catalyzes the conversion of major defensive secondary metabolites, tuliposides, to antimicrobial tulipalins...
October 4, 2016: Bioscience, Biotechnology, and Biochemistry
Qiongqiong Zhou, Wenjuan Sun, Xiyan Liu, Xiliang Wang, Yuncai Xiao, Dingren Bi, Jingdong Yin, Deshi Shi
AIM: Pig liver carboxylesterase (PLE) gene sequences in GenBank are incomplete, which has led to difficulties in studying the genetic structure and regulation mechanisms of gene expression of PLE family genes. The aim of this study was to obtain and analysis of complete gene sequences of PLE family by screening from a Rongchang pig BAC library and third-generation PacBio gene sequencing. METHODS: After a number of existing incomplete PLE isoform gene sequences were analysed, primers were designed based on conserved regions in PLE exons, and the whole pig genome used as a template for Polymerase chain reaction (PCR) amplification...
2016: PloS One
A M Attademo, J C Sanchez-Hernandez, R C Lajmanovich, P M Peltzer, C Junges
An outdoor microcosm was performed with tadpoles (Rhinella arenarum) exposed to 125μgL(-1) chlorpyrifos and fed two types of food, i.e., lettuce (Lactuca sativa) and a formulated commercial pellet. Acetylcholinesterase (AChE) and carboxylesterase (CbE) activities were measured in liver and intestine after 10 days of pesticide exposure. Non-exposed tadpoles fed lettuce had an intestinal AChE activity almost two-fold higher than that of pellet-fed tadpoles. No significant differences were observed, however, in liver AChE activity between diets...
September 21, 2016: Ecotoxicology and Environmental Safety
Karl Emil Nelveg-Kristensen, Peter Bie, Laura Ferrero, Ditte Bjerre, Niels E Bruun, Martin Egfjord, Henrik B Rasmussen, Peter R Hansen
BACKGROUND: Variation in the carboxylesterase 1 gene (CES1) may contribute to the efficacy of ACEIs. Accordingly, we examined the impact of CES1 variants on plasma angiotensin II (ATII)/angiotensin I (ATI) ratio in patients with congestive heart failure (CHF) that underwent ACEI dose titrations. Five of these variants have previously been associated with drug response or increased CES1 expression, i.e., CES1 copy number variation, the variant of the duplicated CES1 gene with high transcriptional activity, rs71647871, rs2244613, and rs3815583...
2016: PloS One
Jiekai Yu, Xiaofen Li, Chenhan Zhong, Dan Li, Xiaohui Zhai, Wangxiong Hu, Cheng Guo, Ying Yuan, Shu Zheng
Proteins, as executives of genes' instructions, are responsible for cellular phenotypes. Integratingproteomics with gene microarray, we conducted this study to identify potential protein biomarkers of colorectal cancer (CRC). Isobaric tags with related and absolute quantitation (iTRAQ) labeling mass spectrometry (MS) was applied to screen and identify differentially expressed proteins between paired CRC and adjacent normal mucosa. Meanwhile, Affymetrix U133plus2.0 microarrays were used to perform gene microarray analysis...
September 20, 2016: Oncotarget
Sung S Choi, Kichul Yoon, Seon-A Choi, Seung-Bin Yoon, Seung U Kim, Hong J Lee
Advanced pancreatic cancer is one of the most lethal malignant human diseases lacking effective treatment. Its extremely low survival rate necessitates development of novel therapeutic approach. Human neural stem cells (NSCs) are known to have tumor-tropic effect. We genetically engineered them to express rabbit carboxyl esterase (F3.CE), which activates prodrug CPT-11(irinotecan) into potent metabolite SN-38. We found significant inhibition of the growth of BxPC3 human pancreatic cancer cell line in vitro by F3...
September 21, 2016: Oncotarget
Kayoko Ohura, Hikaru Nishiyama, Saori Saco, Keisuke Kurokawa, Teruko Imai
Caco-2 cells predominantly express human carboxylesterase 1 (hCE1), unlike the human intestine which predominantly expresses human carboxylesterase 2 (hCE2). Transport experiments using Caco-2 cell monolayers often lead to mis-estimation of the intestinal absorption of prodrugs because of this difference, as prodrugs designed to increase the bioavailability of parent drugs are made to be resistant to hCE2 in the intestine, so that they can be hydrolyzed by hCE1 in the liver. In the present study, we tried to establish a new Caco-2 subclone, with a similar pattern of carboxylase expression to human intestine, to enable a more accurate estimation of the intestinal absorption of prodrugs...
September 16, 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Xingyue Li, Qizhi Liu, Edwin E Lewis, Eustachio Tarasco
Entomopathogenic nematodes (EPNs) of the genera Steinernema and Heterorhabditis are lethal parasites of many insect species. To investigate defensive mechanisms towards EPNs in relation to antioxidative and detoxifying enzymes, we chose Tenebrio molitor (Coleoptera: Tenebrionidae) as experimental insect. We studied the activity changes of superoxide dismutases (SODs), peroxidases (PODs), and catalases (CATs), as well as tyrosinase (TYR), acetylcholinesterase (AChE), carboxylesterase (CarE), and glutathione S-transferase (GSTs) for 40 h in T...
September 9, 2016: Parasitology Research
Jian Shi, Xinwen Wang, Jenny-Hoa Nguyen, Barry E Bleske, Yan Liang, Li Liu, Hao-Jie Zhu
The oral anticoagulant prodrug dabigatran etexilate (DABE) is sequentially metabolized by intestinal carboxylesterase 2 (CES2) and hepatic carboxylesterase 1 (CES1) to form its active metabolite dabigatran (DAB). A recent genome-wide association study reported that the CES1 single nucleotide polymorphisms (SNPs) rs2244613 and rs8192935 were associated with lower DAB plasma concentrations in the Randomized Evaluation of Long-term Anticoagulation Therapy (RE-LY) study participants. In addition, gender differences in exposure to DAB were observed in clinical studies...
November 1, 2016: Biochemical Pharmacology
M Basij, K Talebi, M Ghadamyari, V Hosseininaveh, S A Salami
Nine Bemisia tabaci (Gennadius) populations were collected from different regions of Iran. In all nine populations, only one biotype (B biotype) was detected. Susceptibilities of these populations to imidacloprid and acetamiprid were assayed. The lethal concentration 50 values (LC50) for different populations showed a significant discrepancy in the susceptibility of B. tabaci to imidacloprid (3.76 to 772.06 mg l(-1)) and acetamiprid (4.96 to 865 mg l(-1)). The resistance ratio of the populations ranged from 9...
September 2, 2016: Neotropical Entomology
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