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https://www.readbyqxmd.com/read/28532270/predominant-contributions-of-carboxylesterase-1-and-2-in-hydrolysis-of-anordrin-in-humans
#1
Jinfang Jiang, Xiaoyan Chen, Dafang Zhong
1. Anordrin (2α, 17α-diethynyl-A-nor-5α-androstane-2β, 17β-diol diproprionate) is post-coital contraceptive drug that is on the market in China for more than 30 years. This study aims to elucidate enzymes involved in anordrin hydrolysis, and to evaluate the significant role of carboxylesterases in anordrin hydrolysis in humans. 2. Human liver and intestinal microsomes, recombinant human carboxylesterase were selected as enzyme sources. In human liver microsomes, intrinsic clearance was 684 ± 83 μL/min/mg protein, which was considerably higher than the value of intestine microsomes (94...
May 22, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28531881/first-in-man-dose-escalation-and-pharmacokinetic-study-of-cap7-1-a-novel-prodrug-of-etoposide-in-adults-with-refractory-solid-tumours
#2
U Keilholz, L Rohde, P Mehlitz, M Knoedler, A Schmittel, V Kümmerlen, K Klinghammer, P Treasure, M Lassus, G Steventon, M Machacek, N Utku
AIM: An open-label, phase I dose-escalation trial was performed in adult patients with various solid cancers to identify the maximum tolerated dose (MTD), to assess the safety, pharmacokinetic profile and anti-tumour activity of the new prodrug CAP7.1. The prodrug is converted to its active moiety etoposide via carboxylesterases in selective cells leading to a better tolerability and higher efficacy in therapeutic resistance cells and children with refractory neuroblastoma. PATIENTS AND METHODS: Eligible adult patients with advanced, refractory, solid malignancies received CAP7...
May 19, 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/28525556/transcriptome-of-the-gsh-depleted-lens-reveals-changes-in-detoxification-and-emt-signaling-genes-transport-systems-and-lipid-homeostasis
#3
Jeremy A Whitson, Xiang Zhang, Mario Medvedovic, Jenny Chen, Zongbo Wei, Vincent M Monnier, Xingjun Fan
Purpose: To understand the effects of glutathione (GSH)-deficiency on genetic processes that regulate lens homeostasis and prevent cataractogenesis. Methods: The transcriptome of lens epithelia and fiber cells was obtained from C57BL/6 LEGSKO (lens GSH-synthesis knockout) and buthionine sulfoximine (BSO)-treated LEGSKO mice and compared to C57BL/6 wild-type mice using RNA-Seq. Transcriptomic data were confirmed by qPCR and Western blot/ELISA on a subset of genes...
May 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28475833/imaging-and-detection-of-carboxylesterase-in-living-cells-and-zebrafish-pretreated-with-pesticides-by-a-new-near-infrared-fluorescence-off-on-probe
#4
Dongyu Li, Zhao Li, Weihua Chen, Xingbin Yang
A new near-infrared fluorescence off-on probe was developed and applied to fluorescence imaging of carboxylesterase in living HepG-2 cells and zebrafish pretreated with pesticides (carbamate, organophosphorus, and pyrethroid). The probe was readily prepared by connecting (4-acetoxybenzyl)oxy as a quenching and recognizing moiety to a stable hemicyanine skeleton that can be formed via the decomposition of IR-780. The fluorescence off-on response of the probe to carboxylesterase is based on the enzyme-catalyzed spontaneous hydrolysis of the carboxylic ester bond, followed by a further fragmentation of the phenylmethyl unit and thereby the fluorophore release...
May 16, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28473993/salvia-miltiorrhiza-roots-against-cardiovascular-disease-consideration-of-herb-drug-interactions
#5
REVIEW
Feng Chen, Li Li, Dan-Dan Tian
Salvia miltiorrhiza root (Danshen) is widely used in Asia for its cardiovascular benefits and contains both hydrophilic phenolic acids and lipophilic tanshinones, which are believed to be responsible for its therapeutic efficacy. This review summarized the effects of these bioactive components from S. miltiorrhiza roots on pharmacokinetics of comedicated drugs with mechanic insights regarding alterations of protein binding, enzyme activity, and transporter activity based on the published data stemming from both in vitro and in vivo human studies...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28473326/reduced-carboxylesterase-1-is-associated-with-endothelial-injury-in-methamphetamine-induced-pulmonary-arterial-hypertension
#6
Mark E Orcholski, Artyom Khurshudyan, Elya A Shamskhou, Ke Yuan, Ian Y Chen, Sean D Kodani, Christophe Morisseau, Bruce D Hammock, Ellen M Hong, Ludmila Alexandrova, Tero-Pekka Alastalo, Gerald Berry, Roham T Zamanian, Vinicio A de Jesus Perez
Pulmonary arterial hypertension is a complication of methamphetamine use (METH-PAH) but the pathogenic mechanisms are unknown. Given that cytochrome P450 2D6 (CYP2D6) and carboxylesterase 1 (CES1) are involved in metabolism of METH and other amphetamine-like compounds, we postulated that loss of function variants could contribute to METH-PAH. While no difference in CYP2D6 expression was seen by lung immunofluorescence, CES1 expression was significantly reduced in endothelium of METH-PAH microvessels. Mass spectrometry analysis showed that healthy pulmonary microvascular endothelial cells (PMVECs) have the capacity to both internalize and metabolize METH...
May 4, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28460306/acute-toxicity-and-esterase-response-to-carbaryl-exposure-in-two-different-populations-of-amphipods-hyalella-curvispina
#7
Olga Liliana Anguiano, Melina Vacca, María Emilia Rodriguez Araujo, Mónica Montagna, Andrés Venturino, Ana Ferrari
During the last years, a carbaryl insecticide was extensively applied in the valley of Río Negro and Neuquén, North Patagonia Argentina, to manage codling moths (Cydia pomonella), the main pest of pear and apple trees. In this study carbaryl susceptibility and B-esterase activity from both insecticide-exposed and non-exposed field populations of amphipods Hyalella curvispina were studied. Two subpopulations, one susceptible to carbaryl (LC50=213±7.5μg/L carbaryl) and one resistant to it (LC50=14,663±2379μg/L carbaryl), were found in the agricultural area selected in this study...
April 19, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28456306/characterization-and-establishment-of-a-reference-deltamethrin-and-cypermethrin-resistant-tick-line-ivri-iv-of-rhipicephalus-boophilus-microplus
#8
Srikant Ghosh, Snehil Gupta, K G Ajith Kumar, Anil Kumar Sharma, Sachin Kumar, Gaurav Nagar, Rinesh Kumar, Souvik Paul, Ashutosh Fular, Gajanan Chigure, Abhijit Nandi, H V Manjunathachar, Aquil Mohammad, M R Verma, B C Saravanan, Debdatta Ray
The problem of ticks and tick borne diseases is a global threat and growing reports of resistance to commonly used insecticides further aggravated the condition and demands for country specific resistance monitoring tools and possible solutions of the problem. Establishment of standard reference is prerequisite for development of monitoring tools. For studying possible role of different mechanisms involved in development of resistance in Rhipicephalus (Boophilus) microplus population and to develop newer drug to manage the problem of resistance, a deltamethrin exposed and selected tick colony, referred to as IVRI-IV, was characterized using reference susceptible IVRI-I tick line as control...
May 2017: Pesticide Biochemistry and Physiology
https://www.readbyqxmd.com/read/28438337/carboxylesterase-activities-in-chondrichthyans-of-the-western-mediterranean-sea
#9
David Nos, Joan Navarro, Claudio Barría, Montserrat Solé
No abstract text is available yet for this article.
April 21, 2017: Marine Pollution Bulletin
https://www.readbyqxmd.com/read/28437488/the-novel-carboxylesterase-1-variant-c-662a-g-may-decrease-the-bioactivation-of-oseltamivir-in-humans
#10
Jaeseong Oh, SeungHwan Lee, Howard Lee, Joo-Youn Cho, Seo Hyun Yoon, In-Jin Jang, Kyung-Sang Yu, Kyoung Soo Lim
BACKGROUND: Human carboxylesterase 1 (CES1) is a serine esterase that hydrolyses various exogenous and endogenous compounds including oseltamivir, a prodrug used to treat influenza. A novel CES1 c.662A>G single nucleotide polymorphism (SNP) was predicted to decrease CES1 enzymatic activity in an in silico analysis. This study evaluated the effect of the c.662A>G SNP on the pharmacokinetics (PK) of oseltamivir in humans. METHODS: A single oral dose of oseltamivir at 75 mg was administered to 20 healthy subjects, 8 heterozygous c...
2017: PloS One
https://www.readbyqxmd.com/read/28435140/biowaiver-monographs-for-immediate-release-solid-oral-dosage-forms-enalapril
#11
REVIEW
Roger K Verbeeck, Isadore Kanfer, Raimar Löbenberg, Bertil Abrahamsson, Rodrigo Cristofoletti, D W Groot, Peter Langguth, James E Polli, Alan Parr, Vinod P Shah, Mehul Mehta, Jennifer B Dressman
Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhibitor enalaprilat. Enalapril as the maleate salt is shown to be highly soluble, but only 60 to 70% of an orally administered dose of enalapril is absorbed from the gastrointestinal tract into the enterocytes...
April 20, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435029/activity-of-carboxylesterases-glutathione-s-transferase-and-monooxygenase-on-rhipicephalus-microplus-exposed-to-fluazuron
#12
Fabrício Nascimento Gaudêncio, Guilherme Marcondes Klafke, Vinícius Menezes Tunholi-Alves, Thaís Paes Ferreira, Cristiane Nunes Coelho, Adivaldo Henrique da Fonseca, Isabele da Costa Angelo, Jairo Pinheiro
The objective of this study was to assess the effect of the exposure to fluazuron on the activity of common pesticide detoxification enzyme groups in the cattle tick (Rhipicephalus microplus). Engorged females of a susceptible strain (POA) and a resistant strain (Jaguar) were exposed in vitro to fluazuron and their eggs and larvae were used to compare the activities of the general esterases, mixed-function oxidases (MFO) and glutathione-S-transferase (GST). The results showed significant elevation in MFO contents and esterases activity in the resistant strain when compared with the susceptible strain, in eggs and larvae respectively...
April 20, 2017: Parasitology International
https://www.readbyqxmd.com/read/28433595/effects-of-chlorpyrifos-on-soil-carboxylesterase-activity-at-an-aggregate-size-scale
#13
Juan C Sanchez-Hernandez, Marco Sandoval
The impact of pesticides on extracellular enzyme activity has been mostly studied on the bulk soil scale, and our understanding of the impact on an aggregate-size scale remains limited. Because microbial processes, and their extracellular enzyme production, are dependent on the size of soil aggregates, we hypothesized that the effect of pesticides on enzyme activities is aggregate-size specific. We performed three experiments using an Andisol to test the interaction between carboxylesterase (CbE) activity and the organophosphorus (OP) chlorpyrifos...
August 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28428009/effect-of-methylparaben-in-artemia-franciscana
#14
Amparo Comeche, María Martín-Villamil, Yolanda Pico, Inma Varó
In this study, the toxicity of methylparaben (MeP) an emerging contaminant, was analyzed in the sexual species Artemia franciscana, due to its presence in coastal areas and marine saltworks in the Mediterranean region. The acute toxicity (24h-LC50) of MeP in nauplii was tested and its chronic effect (9days) evaluated by measuring survival and growth under two sublethal concentrations (0.0085 and 0.017mg/L). Also, the effect on several key enzymes involved in: antioxidant defences (catalase (CAT) and gluthathion-S-transferase (GST)), neural activity (cholinesterase (ChE)) and xenobiotic biotransformation (carboxylesterase (CbE), was assessed after 48h under sublethal exposure...
April 17, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28416547/simulating-intestinal-transporter-and-enzyme-activity-in-a-physiologically-based-pharmacokinetic-model-for-tenofovir-disoproxil-fumarate
#15
Darren M Moss, P Domanico, M Watkins, S Park, R Randolph, S Wring, J Hobson, S Rannard, M Siccardi, A Owen
Tenofovir disoproxil fumarate (TDF), a prodrug of tenofovir, has oral bioavailability (25%) limited by intestinal transport (p-glycoprotein), and intestinal degradation (carboxylesterase).….
April 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28396528/human-enterocytes-as-an-in-vitro-model-for-the-evaluation-of-intestinal-drug-metabolism-characterization-of-drug-metabolizing-enzyme-activities-of-cryopreserved-human-enterocytes-from-twenty-four-donors
#16
Ming-Chih David Ho, Nick Ring, Kirsten Amaral, Utkarsh Doshi, Albert Li
We report here successful isolation and cryopreservation of enterocytes from human small intestine. The enterocytes were isolated by enzyme digestion of the intestinal lumen followed by partial purification via differential centrifugation. The enterocytes were cryopreserved directly after isolation without culturing to maximize retention of in vivo drug metabolizing enzyme activities. Post-thaw viability of the cryopreserved enterocytes was consistently over 80% based on trypan blue exclusion. Cryopreserved enterocytes pooled from 8 donors (4 male and 4 female) were evaluated for their metabolism of 14 pathway-selective substrates: CYP1A2 (phenacetin hydroxylation), CYP2A6 (coumarin 7-hydroxylation), CYP2B6 (bupropion hydroxylation), CYP2C8 (paclitaxel 6α-hydroxylation), CYP2C9 (diclofenac 4-hydroxylation), CYP2C19 (s-mephenytoin 4-hydroxylation), CYP2D6 (dextromethorphan hydroxylation), CYP2E1 (chlorzoxazone 6-hydroxylation), CYP3A4 (midazolam 1'-hydroxylation and testosterone 6β-hydroxylation), CYP2J2 (astemizole O-demethylation), UDP-glucuronosyltransferase (UGT; 7-hydroxycoumarin glucuronidation), sulfotransferase (SULT; 7-hydroxycoumarin sulfation), and carboxylesterase 2 (CES2; irinotecan hydrolysis) activities...
April 10, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28394886/carboxylesterase-gene-amplifications-associated-with-insecticide-resistance-in-aedes-albopictus-geographical-distribution-and-evolutionary-origin
#17
Linda Grigoraki, Dimitra Pipini, Pierrick Labbé, Alexandra Chaskopoulou, Mylene Weill, John Vontas
BACKGROUND: Aedes albopictus is one of the most invasive human disease vectors. Its control has been largely based on insecticides, such as the larvicide temephos. Temephos resistance has been associated with the up-regulation, through gene amplification, of two carboxylesterase (CCE) genes closely linked on the genome, capable of sequestering and metabolizing temephos oxon, the activated form of temephos. PRINCIPAL FINDINGS: Here, we investigated the occurrence, geographical distribution and origin of the CCE amplicon in Ae...
April 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28393686/impact-of-salt-concentration-and-ph-on-surface-charged-residues-controlling-protein-association-pathways-in-carboxylesterase-estgta2
#18
Jessica K Moisan, Fatma Meddeb-Mouelhi, David M Charbonneau, Marc Beauregard
Understanding the relationship between enzymatic stability and the amino acid sequence encoding such enzymes is of utmost importance. Here we thoroughly characterized the behavior of the carboxylesterase EstGtA2 from Geobacillus thermodenitrificans during thermal denaturation at different pH with various salt concentrations. EstGtA2 was characterized by circular dichroism regarding conformation and thermal stability, by dynamic light scattering for detection of association/aggregation, by enzymatic assays for activity, and by monitoring the impact of heat treatments on activity...
April 4, 2017: Protein and Peptide Letters
https://www.readbyqxmd.com/read/28382676/natural-genomic-amplification-of-cholinesterase-genes-in-animals
#19
REVIEW
Arnaud Chatonnet, Nicolas Lenfant, Pascale Marchot, Murray E Selkirk
Tight control of the concentration of acetylcholine at cholinergic synapses requires precise regulation of the number and state of the acetylcholine receptors, and of the synthesis and degradation of the neurotransmitter. In particular, the cholinesterase activity has to be controlled exquisitely. In the genome of the first experimental models used (man, mouse, zebrafish and drosophila), there are only one or two genes coding for cholinesterases, whereas there are more genes for their closest relatives the carboxylesterases...
April 5, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28379972/the-novel-nematicide-wact-86-interacts-with-aldicarb-to-kill-nematodes
#20
Andrew R Burns, Rachel Bagg, May Yeo, Genna M Luciani, Michael Schertzberg, Andy G Fraser, Peter J Roy
Parasitic nematodes negatively impact human and animal health worldwide. The market withdrawal of nematicidal agents due to unfavourable toxicities has limited the available treatment options. In principle, co-administering nematicides at lower doses along with molecules that potentiate their activity could mitigate adverse toxicities without compromising efficacy. Here, we screened for new small molecules that interact with aldicarb, which is a highly effective treatment for plant-parasitic nematodes whose toxicity hampers its utility...
April 2017: PLoS Neglected Tropical Diseases
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