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Human carboxylesterase

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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
#1
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
#2
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...
March 8, 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
#3
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/28245791/24-epibrassinolide-stimulates-imidacloprid-detoxification-by-modulating-the-gene-expression-of-brassica-juncea-l
#4
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
#5
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/28237806/chemical-composition-and-insecticidal-property-of-myrsine-stolonifera-koidz-walker-family-myrsinaceae-on-musca-domestica-diptera-muscidae
#6
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
#7
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/28228413/determination-of-human-hepatic-cyp2c8-and-cyp1a2-age-dependent-expression-to-support-human-health-risk-assessment-for-early-ages
#8
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
#9
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/28126414/recent-progress-in-the-discovery-of-natural-inhibitors-against-human-carboxylesterases
#10
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...
March 2017: Fitoterapia
https://www.readbyqxmd.com/read/28112927/selective-inhibitors-of-human-liver-carboxylesterase-based-on-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 (CEs) 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 although the former are very poor inhibitors, the latter compounds are highly effective in modulating CE activity...
February 7, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28099843/human-carboxylesterase-2-reverses-obesity-induced-diacylglycerol-accumulation-and-glucose-intolerance
#12
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/27998705/in%C3%A2-vitro-in%C3%A2-vivo-extrapolation-of-intestinal-availability-for-carboxylesterase-substrates-using-portal-vein-cannulated-monkey
#13
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
https://www.readbyqxmd.com/read/27986599/development-of-a-novel-formulation-that-improves-preclinical-bioavailability-of-tenofovir-disoproxil-fumarate
#14
Melynda E Watkins, Steve Wring, Ryan Randolph, Seonghee Park, Kendall Powell, Lissa Lutz, Michelle Nowakowski, Ram Ramabhadran, Paul L Domanico
Tenofovir disoproxil fumarate (TDF), the bisphosphonate ester prodrug of tenofovir (TFV), has poor bioavailability due to intestinal degradation and efflux transport. Reformulation using U.S. Food and Drug Administration-approved esterase and efflux inhibitors to increase oral bioavailability could provide lower dose alternatives and reduce costs for patients with HIV in resource-limited settings. Inhibition of mucosal and intracellular esterases was studied in human and rat intestinal extracts (S9), where TDF was protected by the carboxylesterase inhibitor bis-para-nitrophenylphosphate, the ester mix EM1, and the generally recognized-as-safe (GRAS) excipient propylparaben...
March 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27895113/age-dependent-absolute-abundance-of-hepatic-carboxylesterases-ces1-and-ces2-by-lc-ms-ms-proteomics-application-to-pbpk-modeling-of-oseltamivir-in-vivo-pharmacokinetics-in-infants
#15
Mikael Boberg, Marc Vrana, Aanchal Mehrotra, Robin E Pearce, Andrea Gaedigk, Deepak Kumar Bhatt, J Steven Leeder, Bhagwat Prasad
The age-dependent absolute protein abundance of carboxylesterase (CES) 1 and CES2 in human liver was investigated and applied to predict infant pharmacokinetics (PK) of oseltamivir. The CES absolute protein abundance was determined by liquid chromatography-tandem mass spectrometry proteomics in human liver microsomal and cytosolic fractions prepared from tissue samples obtained from 136 pediatric donors and 35 adult donors. Two surrogate peptides per protein were selected for the quantification of CES1 and CES2 protein abundance...
February 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27881673/sortilin-1-modulates-hepatic-cholesterol-lipotoxicity-in-mice-via-functional-interaction-with-liver-carboxylesterase-1
#16
Jibiao Li, Yifeng Wang, David J Matye, Hemantkumar Chavan, Partha Krishnamurthy, Feng Li, Tiangang Li
The liver plays a key role in cholesterol metabolism. Impaired hepatic cholesterol homeostasis causes intracellular free cholesterol accumulation and hepatocyte injury. Sortilin 1 (SORT1) is a lysosomal trafficking receptor that was identified by genome-wide association studies (GWAS) as a novel regulator of cholesterol metabolism in humans. Here we report that SORT1 deficiency protected against cholesterol accumulation-induced liver injury and inflammation in mice. Using an LC-MS/MS-based proteomics approach, we identified liver carboxylesterase 1 (CES1) as a novel SORT1-interacting protein...
January 6, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27831961/nomenclature-for-alleles-of-the-human-carboxylesterase-1-gene
#17
Henrik B Rasmussen, Majbritt B Madsen, Peter R Hansen
No abstract text is available yet for this article.
November 9, 2016: Pharmacogenetics and Genomics
https://www.readbyqxmd.com/read/27800573/pharmacokinetic-modeling-and-monte-carlo-simulation-to-predict-interindividual-variability-in-human-exposure-to-oseltamivir-and-its-active-metabolite-ro-64-0802
#18
Mototsugu Ito, Hiroyuki Kusuhara, Atsushi Ose, Tsunenori Kondo, Kazunari Tanabe, Hideki Nakayama, Shigeru Horita, Takuya Fujita, Yuichi Sugiyama
Oseltamivir (Tamiflu®) is a prodrug of Ro 64-0802, a selective inhibitor of influenza virus neuraminidase. There is a possible relationship between oseltamivir treatment and neuropsychiatric adverse events; although this has not been established, close monitoring is recommended on the prescription label. The objective of this study was to predict interindividual variability of human exposure to oseltamivir and its active metabolite Ro 64-0802. By leveraging mathematical models and computations, physiological parameters in virtual subjects were generated with population means and coefficient of variations collected from the literature or produced experimentally...
January 2017: AAPS Journal
https://www.readbyqxmd.com/read/27771568/effect-of-surfactant-in-mitigating-cadmium-oxide-nanoparticle-toxicity-implications-for-mitigating-cadmium-toxicity-in-environment
#19
Sricharani Rao Balmuri, Uthra Selvaraj, Vadivel Vinod Kumar, Savarimuthu Philip Anthony, Aristides Michael Tsatsakis, Kirill Sergeevich Golokhvast, Thiagarajan Raman
Cadmium (Cd), classified as human carcinogen, is an extremely toxic heavy metal pollutant, and there is an increasing environmental concern for cadmium exposure through anthropogenic sources including cigarette smoke. Though Cd based nanoparticles such as cadmium oxide (CdO) are being widely used in a variety of clinical and industrial applications, the toxicity of CdO nanoparticles has not been well characterized. Herein we report the toxicity of CdO nanoparticles employing zebrafish as a model. Two different CdO nanoparticles were prepared, calcination of Cd(OH)2 without any organic molecule (CdO-1) and calcination of Cd-citrate coordination polymer (CdO-2), to evaluate and compare the toxicity of these two different CdO nanoparticles...
January 2017: Environmental Research
https://www.readbyqxmd.com/read/27702666/identification-and-characterization-of-naturally-occurring-inhibitors-against-human-carboxylesterase-2-in-white-mulberry-root-bark
#20
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...
December 2016: Fitoterapia
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