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https://www.readbyqxmd.com/read/28334183/comparative-transcriptional-analysis-of-the-host-specialized-aphids-aphis-gossypii-hemiptera-aphididae
#1
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...
February 17, 2017: Journal of Economic Entomology
https://www.readbyqxmd.com/read/28334129/transcriptional-responses-of-detoxification-genes-to-four-plant-allelochemicals-in-aphis-gossypii
#2
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...
February 17, 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
#3
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
#4
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
https://www.readbyqxmd.com/read/28285137/functional-analysis-of-carboxylesterase-in-human-induced-pluripotent-stem-cell-derived-enterocytes
#5
Tomoki Kabeya, Wakana Matsumura, Takahiro Iwao, Masakiyo Hosokawa, Tamihide Matsunaga
Human carboxylesterase (CES) is a key esterase involved in the metabolism and biotransformation of drugs. Hydrolysis activity in the human small intestine is predominantly mediated by CES2A1 rather than CES1A. In drug development studies, Caco-2 cells are commonly used as a model to predict drug absorption in the human small intestine. However, the expression patterns of CES2A1 and CES1A in Caco-2 cells differ from those in the human small intestine. There are also species-specific differences in CES expression patterns between human and experimental animals...
April 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28281384/transport-properties-of-valsartan-sacubitril-and-its-active-metabolite-lbq657-as-determinants-of-disposition
#6
Imad Hanna, Natalya Alexander, Matthew H Crouthamel, John Davis, Adrienne Natrillo, Phi Tran, Arpine Vapurcuyan, Bing Zhu
1. The potential for drug-drug interactions of LCZ696 (a novel, crystalline complex comprising sacubitril and valsartan) was investigated in vitro. 2. Sacubitril was shown to be a highly permeable P-glycoprotein (P-gp) substrate and was hydrolyzed to the active anionic metabolite LBQ657 by human carboxylesterase 1 (CES1b and 1c). The multidrug resistance-associated protein 2 (MRP2) was shown to be capable of LBQ657 and valsartan transport that contributes to the elimination of either compound. 3. LBQ657 and valsartan were transported by OAT1, OAT3, OATP1B1 and OATP1B3, whereas no OAT- or OATP-mediated sacubitril transport was observed...
March 10, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28272521/activity-screening-of-environmental-metagenomic-libraries-reveals-novel-carboxylesterase-families
#7
Ana Popovic, Tran Hai, Anatoly Tchigvintsev, Mahbod Hajighasemi, Boguslaw Nocek, Anna N Khusnutdinova, Greg Brown, Julia Glinos, Robert Flick, Tatiana Skarina, Tatyana N Chernikova, Veronica Yim, Thomas Brüls, Denis Le Paslier, Michail M Yakimov, Andrzej Joachimiak, Manuel Ferrer, Olga V Golyshina, Alexei Savchenko, Peter N Golyshin, Alexander F Yakunin
Metagenomics has made accessible an enormous reserve of global biochemical diversity. To tap into this vast resource of novel enzymes, we have screened over one million clones from metagenome DNA libraries derived from sixteen different environments for carboxylesterase activity and identified 714 positive hits. We have validated the esterase activity of 80 selected genes, which belong to 17 different protein families including unknown and cyclase-like proteins. Three metagenomic enzymes exhibited lipase activity, and seven proteins showed polyester depolymerization activity against polylactic acid and polycaprolactone...
March 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28257192/enzyme-instructed-assembly-and-disassembly-processes-for-targeting-downregulation-in-cancer-cells
#8
Zhaoqianqi Feng, Huaimin Wang, Rong Zhou, Jie Li, Bing Xu
Cancer cells differ from normal cells in both gain of functions (i.e., upregulation) and loss of functions (i.e., downregulation). While it is common to suppress gain of function for chemotherapy, it remains challenging to target downregulation in cancer cells. Here we show the combination of enzyme-instructed assembly and disassembly to target downregulation in cancer cells by designing peptidic precursors as the substrates of both carboxylesterases (CESs) and alkaline phosphatases (ALPs). The precursors turn into self-assembling molecules to form nanofibrils upon dephosphorylation by ALP, but CES-catalyzed cleavage of the ester bond on the molecules results in disassembly of the nanofibrils...
March 13, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28254583/insecticide-susceptibility-status-and-major-detoxifying-enzymes-activity-in-aedes-albopictus-skuse-vector-of-dengue-and-chikungunya-in-northern-part-of-west-bengal-india
#9
Minu Bharati, Dhiraj Saha
Mosquitoes belonging to Aedes genus, Aedes aegypti and Aedes albopictus transmit many globally important arboviruses including Dengue (DENV) and Chikungunya (CHIKV). Vector control with the use of insecticide remains the suitable method of choice to stop the transmission of these diseases. However, vector control throughout the world is failing to achieve its target results because of the worldwide development of insecticide resistance in mosquitoes. To assess the insecticide susceptibility status of Aedes albopictus from northern part of West Bengal, the susceptibility of eight different Aedes albopictus populations were tested against a commonly used larvicide (temephos) and some adulticides (malathion, deltamethrin and lambda cyhalothrin) along with the major insecticide detoxifying enzymes' activity in them...
February 27, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28246253/association-between-statin-use-and-ischemic-stroke-or-major-hemorrhage-in-patients-taking-dabigatran-for-atrial-fibrillation
#10
Tony Antoniou, Erin M Macdonald, Zhan Yao, Simon Hollands, Tara Gomes, Mina Tadrous, Muhammad M Mamdani, David N Juurlink
BACKGROUND: Dabigatran etexilate is a prodrug whose absorption is opposed by intestinal P-glycoprotein and which is converted by carboxylesterase to its active form, dabigatran. Unlike other statins, simvastatin and lovastatin are potent inhibitors of P-glycoprotein and carboxylesterase, and might either increase the risk of hemorrhage with dabigatran etexilate or decrease its effectiveness. METHODS: We conducted 2 population-based, nested case-control studies involving Ontario residents 66 years of age and older who started dabigatran etexilate between May 1, 2012, and Mar...
January 9, 2017: CMAJ: Canadian Medical Association Journal, Journal de L'Association Medicale Canadienne
https://www.readbyqxmd.com/read/28245791/24-epibrassinolide-stimulates-imidacloprid-detoxification-by-modulating-the-gene-expression-of-brassica-juncea-l
#11
Anket Sharma, Sharad Thakur, Vinod Kumar, Anup Kumar Kesavan, Ashwani Kumar Thukral, Renu Bhardwaj
BACKGROUND: Pesticides cause oxidative stress to plants and their residues persist in plant parts, which are a major concern for the environment as well as human health. Brassinosteroids (BRs) are known to protect plants from abiotic stress conditions including pesticide toxicity. The present study demonstrated the effects of seed-soaking with 24-epibrassinolide (EBR) on physiological responses of 10-day old Brassica juncea seedlings grown under imidacloprid (IMI) toxicity. RESULTS: In the seedlings raised from EBR-treated seeds and grown under IMI toxicity, the contents of hydrogen peroxide (H2O2) and superoxide anion (O(...
February 28, 2017: BMC Plant Biology
https://www.readbyqxmd.com/read/28242322/assessment-of-the-inhibitory-effects-of-pyrethroids-against-human-carboxylesterases
#12
Wei Lei, Dan-Dan Wang, Tong-Yi Dou, Jie Hou, Liang Feng, Heng Yin, Qun Luo, Jie Sun, Guang-Bo Ge, Ling Yang
Pyrethroids are broad-spectrum insecticides that widely used in many countries, while humans may be exposed to these toxins by drinking or eating pesticide-contaminated foods. This study aimed to investigate the inhibitory effects of six commonly used pyrethroids against two major human carboxylesterases (CES) including CES1 and CES2. Three optical probe substrates for CES1 (DME, BMBT and DMCB) and a fluorescent probe substrate for CES2 (DDAB) were used to characterize the inhibitory effects of these pyrethroids...
February 24, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28238946/involvement-of-pregnane-x-receptor-in-the-suppression-of-carboxylesterases-by-metformin-in-vivo-and-in-vitro-mediated-by-the-activation-of-ampk-and-jnk-signaling-pathway
#13
Enfang Shan, Zhu Zhu, Shuangcheng He, Dongbao Chu, Dinghao Ge, Yunran Zhan, Wei Liu, Jian Yang, Jing Xiong
Type 2 diabetes mellitus (T2D) is a complex metabolic disorder requiring polypharmacy treatment in clinic, with metformin being widely used antihyperglycemic drug. However, the mechanisms of metformin as a perpetrator inducing potential drug-drug interactions and adverse drug reactions are scarcely known to date. Carboxylesterases (CESs) are major hydrolytic enzymes highly expressed in the liver, including mouse carboxylesterase 1d (Ces1d) and Ces1e. In the present study, experiments are designed to investigate the effects and mechanisms of metformin on Ces1d and Ces1e in vivo and in vitro...
February 24, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28237806/chemical-composition-and-insecticidal-property-of-myrsine-stolonifera-koidz-walker-family-myrsinaceae-on-musca-domestica-diptera-muscidae
#14
Xue Gui Wang, Qian Li, Su Rong Jiang, Pei Li, Ji Zhi Yang
Musca domestica is one of the most important pests of human health, and has developed strong resistance to many chemicals used for its control. One important approach for creating new pesticides is the exploration of novel compounds from plants. During a wide screening of plants with insecticidal properties that grow in southern China, we found that the methanolic extracts of Myrsine stolonifera had insecticidal activity against the adults of M. domestica. However, the insecticidal constituents and mechanisms of the M...
February 22, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28237465/human-and-soil-exposure-during-mechanical-chlorpyrifos-myclobutanil-and-copper-oxychloride-application-in-a-peach-orchard-in-argentina
#15
Giselle Berenstein, Soledad Nasello, Érica Beiguel, Pedro Flores, Johanna Di Schiena, Silvana Basack, Enrique A Hughes, Anita Zalts, Javier M Montserrat
The objective of this study was to measure the impact of the mechanized chlorpyrifos, copper oxychloride and myclobutanil application in a small peach orchard, on humans (operators, bystanders and residents) and on the productive soil. The mean Potential Dermal Exposure (PDE) of the workers (tractor drivers) was 30.8mL·h(-1)±16.4mL·h(-1), with no specific pesticide distribution on the laborers body. Although the Margin of Safety (MOS) factor for the application stage were above 1 (safe condition) for myclobutanil and cooper oxycloride it was below 1 for chlorpyrifos...
May 15, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28230321/disruption-of-genes-involved-in-corvet-complex-leads-to-enhanced-secretion-of-heterologous-carboxylesterase-only-in-protease-deficient-pichia-pastoris
#16
Lukas Marsalek, Clemens Gruber, Friedrich Altmann, Markus Aleschko, Diethard Mattanovich, Brigitte Gasser, Verena Puxbaum
The methylotrophic yeast Pichia pastoris (Komagataella spp.) is a popular microbial host for the production of recombinant proteins. Previous studies have shown that mis-sorting to the vacuole can be a bottleneck during production of recombinant secretory proteins in yeast, however, no information was available for P. pastoris. In this work we have therefore generated vps (vacuolar protein sorting) mutant strains disrupted in genes involved in the CORVET tethering complex at the early stages of endosomal sorting...
February 23, 2017: Biotechnology Journal
https://www.readbyqxmd.com/read/28228413/determination-of-human-hepatic-cyp2c8-and-cyp1a2-age-dependent-expression-to-support-human-health-risk-assessment-for-early-ages
#17
Gina Song, Xueying Sun, Ronald N Hines, D Gail McCarver, Brian G Lake, Thomas G Osimitz, Moire R Creek, Harvey J Clewell, Miyoung Yoon
Predicting age-specific metabolism is important for evaluating age-related drug and chemical sensitivity. Multiple cytochrome P450s (CYP) and carboxylesterase (CES) enzymes are responsible for human pyrethroid metabolism. Complete ontogeny data for each enzyme is needed to support in vitro to in vivo extrapolation (IVIVE). This study was designed to determine age-dependent human hepatic CYP2C8 expression, for which only limited ontogeny data are available, and to further define CYP1A2 ontogeny. CYP2C8 and 1A2 protein levels were measured by quantitative Western blotting using liver microsomal samples prepared from 222 subjects with ages ranging from 8 weeks gestation to 18 years after birth...
February 22, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28218815/glycoengineering-of-esterase-activity-through-metabolic-flux-based-modulation-of-sialic-acid
#18
Mohit Mathew, Elaine Tan, Jason W Labonte, Shivam Shah, Christopher T Saeui, Lingshu Liu, Rahul Bhattacharya, Patawut Bovonratwet, Jeffrey J Gray, Kevin Yarema
This report describes the metabolic glycoengineering (MGE) of intracellular esterase activity in human colon cancer (LS174T) and Chinese hamster ovary (CHO) cells. In silico analysis of the carboxylesterases CES1 and CES2 suggested that these enzymes are modified with sialylated N-glycans, which are proposed to stabilize the active multimeric forms of these enzymes. This premise was supported by treating cells with butanolylated ManNAc to increase sialylation, which in turn increased esterase activity. By contrast, hexosamine analogs not targeted to sialic acid biosynthesis (e...
February 20, 2017: Chembiochem: a European Journal of Chemical Biology
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
#19
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 20, 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
#20
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
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