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https://www.readbyqxmd.com/read/29345044/preclinical-characterisation-of-absorption-distribution-metabolism-and-excretion-properties-of-tak-063
#1
Kimio Tohyama, Miyako Sudo, Akio Morohashi, Suguru Kato, Junzo Takahashi, Yoshihiko Tagawa
TAK-063 is currently being developed to treat schizophrenia. In this study, we investigated the absorption, distribution, metabolism and excretion (ADME) properties of TAK-063 using several paradigms. Following oral administration of TAK-063 at 0.3 mg/kg, bioavailability of TAK-063 was 27.4% in rats and 49.5% in dogs with elimination half-lives of 3.1 hr in rats and 3.7 hr in dogs. TAK-063 is a highly permeable compound without P-glycoprotein (P-gp) or breast cancer resistance protein substrate liability and can be readily absorbed into systemic circulation via the intestine...
January 17, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29343296/quantitative-method-for-analysis-of-six-anticoagulant-rodenticides-in-faeces-applied-in-a-case-with-repeated-samples-from-a-dog
#2
Kristin Opdal Seljetun, Elin Eliassen, Ritva Karinen, Lars Moe, Vigdis Vindenes
BACKGROUND: Accidental poisoning with anticoagulant rodenticides is not uncommon in dogs, but few reports of the elimination kinetics and half-lives in this species have been published. Our objectives were to develop and validate a new method for the quantification of anticoagulant rodenticides in canine blood and faeces using reversed phase ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) and apply the method on a case of anticoagulant rodenticide intoxication...
January 17, 2018: Acta Veterinaria Scandinavica
https://www.readbyqxmd.com/read/29341233/fate-uptake-and-distribution-of-nanoencapsulated-pesticides-in-soil-earthworm-systems-implications-for-environmental-risk-assessment
#3
Mohd Anuar Mohd Firdaus, Annika Agatz, Mark E Hodson, Omar S A Al-Khazrajy, Alistair B A Boxall
Nanopesticides are novel plant protection products offering numerous benefits. As nanoparticles behave differently from dissolved chemicals, environmental risks of these materials could differ from conventional pesticides. Here we used soil-earthworm systems to compare the fate and uptake of analytical grade bifenthrin to that of bifenthrin in traditional and nano-encapsulated formulations. Apparent sorption coefficients for bifenthrin in the nano-treatments were up to 3.8 times lower than in the non-nano treatments whereas dissipation half-lives of the nano-treatments were up to two time longer...
January 17, 2018: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/29339289/characterization-of-two-extracellular-%C3%AE-glucosidases-produced-from-the-cellulolytic-fungus-aspergillus-sp-ydj216-and-their-potential-applications-for-the-hydrolysis-of-flavone-glycosides
#4
Jong Min Oh, Jae Pil Lee, Seung Cheol Baek, Seul Gi Kim, Yang Do Jo, Jungho Kim, Hoon Kim
A cellulolytic fungus YDJ216 was isolated from a compost and identified as an Aspergillus sp. strain. Two extracellular β-glucosidases, BGL1 and BGL2, were purified using ultrafiltration, ammonium sulfate fractionation, and High-Q chromatography. Molecular masses of BGL1 and BGL2 were estimated to be 97 and 45 kDa, respectively, by SDS-PAGE. The two enzymes eluted as one peak at 87 kDa by Sephacryl S-200 chromatography, and located at similar positions in a zymogram after intact gel electrophoresis, suggesting BGL1 and BGL2 might be monomeric and dimeric, respectively...
January 12, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29337462/-antiretroviral-treatments-towards-simplified-regimens
#5
Olivier Nawej Tshikung, Alexandra Calmy
The chronicity of HIV infection and the use of antiretroviral therapy among all individuals living with HIV necessitate new treatment strategies. Alternatives to lifelong tri-therapy treatment are under investigation with the aim to improve the quality of life of patients. New therapies with longer half-lives or « biological » treatments are also under study in clinical trials in order to develop streamlined maintenance strategies. These simplified therapies represent the near future of HIV management both with regards to less toxic molecules and a change in the traditional dogma of tri-therapy, including the daily dose thanks to the possibility of dosage only on certain weekdays or via molecules under development with a long duration of action...
January 10, 2018: Revue Médicale Suisse
https://www.readbyqxmd.com/read/29336565/appearances-of-fukushima-daiichi-nuclear-power-plant-derived-137cs-in-coastal-waters-around-japan-results-from-marine-monitoring-off-nuclear-power-plants-and-facilities-1983-2016
#6
Hyoe Takata, Masashi Kusakabe, Naohiko Inatomi, Takahito Ikenoue
Monitoring of 137Cs in seawater in coastal areas around Japan between 1983 and 2016 yielded new insights into the sources and transport of Fukushima Daiichi Nuclear Power Plant (FDNPP)-derived 137Cs, particularly along the west coast of Japan. Before the FDNPP accident (1983-2010), the activity concentrations of 137Cs, mainly from fallout, were decreasing exponentially. Effective 137Cs half-lives in surface seawater ranged from 15.6 to 18.4 yr. After the FDNPP accident (March 2011) 137Cs activity concentrations in seawater off Fukushima and neighboring prefectures immediately increased...
January 16, 2018: Environmental Science & Technology
https://www.readbyqxmd.com/read/29334019/chemical-stabilization-of-polymers-implications-for-dermal-exposure-to-additives
#7
N Bartsch, M Girard, L Schneider, V Van De Weijgert, A Wilde, O Kappenstein, B Vieth, C Hutzler, A Luch
Technical benefits of additives in polymers stand in marked contrast to their associated health risks. Here, a multi-analyte method based on gas chromatography coupled to tandem mass spectrometry (GC-MS/MS) was developed to quantify polymer additives in complex matrices such as low-density polyethylene (LDPE) and isolated human skin layers after dermal exposure ex vivo. That way both technical aspects and dermal exposure were investigated. The effects of polymer additivation on the material were studied using the example of LDPE...
January 15, 2018: Journal of Environmental Science and Health. Part A, Toxic/hazardous Substances & Environmental Engineering
https://www.readbyqxmd.com/read/29333858/mineral-and-base-catalyzed-hydrolysis-of-organophosphate-flame-retardants-a-potential-major-fate-controlling-sink-in-soil-and-aquatic-environments
#8
Yida Fang, Erin Kim, Timothy J Strathmann
The ubiquitous occurrence of organophosphate flame retardants (OPFRs) in aquatic and soil environments poses significant risks to human health and ecosystems. Here, we report on the hydrolysis of six OPFRs and three structural analogues in the absence and presence of metal (hydr)oxide minerals. Eight of the target compounds showed marked degradation in alkaline solutions (pH 9-12) with half-lives ranging from 0.02 - 170 d. Kinetics follow a second-order rate law with apparent rate constants for base-catalyzed hydrolysis (kB) ranging from 0...
January 15, 2018: Environmental Science & Technology
https://www.readbyqxmd.com/read/29333740/pharmacokinetics-disposition-and-plasma-concentrations-of-dimethyl-sulfoxide-dmso-in-the-horse-following-topical-oral-and-intravenous-administration
#9
L R Soma, M A Robinson, Y You, R C Boston, J Rudy
Compartmental models were used to investigate the pharmacokinetics of intravenous (i.v.), oral (p.o.), and topical (TOP) administration of dimethyl sulfoxide (DMSO). The plasma concentration-time curve following a 15-min i.v. infusion of DMSO was described by a two-compartment model. Median and range of alpha (t1/2α ) and beta (t1/2β ) half-lives were 0.029 (0.026-0.093) and 14.1 (6.6-16.4) hr, respectively. Plasma concentration-time curves of DMSO following p.o. and TOP administration were best described by one-compartment absorption and elimination models...
January 14, 2018: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29329837/the-fate-and-enantioselective-behavior-of-zoxamide-during-wine-making-process
#10
Xinglu Pan, Fengshou Dong, Na Liu, Youpu Cheng, Jun Xu, Xingang Liu, Xiaohu Wu, Zenglong Chen, Yongquan Zheng
The fate of zoxamide and its enantiomers were evaluated in detail during wine-making process. The enantiomers of zoxamide were separated and determined by ultra-high-performance liquid chromatography coupled with tandem mass spectrometry (UHPLC-MS/MS) after each processing procedure including washing, peeling, fermentation and clarification. Significant enantioselectivity was observed in all three treatments with the half-lives of R-zoxamide and S-zoxamide estimated to be 45.6 and 52.9 h in Group A, 45.0 and 52...
May 15, 2018: Food Chemistry
https://www.readbyqxmd.com/read/29327491/dissipation-pre-harvest-interval-estimation-and-dietary-risk-assessment-of-carbosulfan-dimethoate-and-their-relevant-metabolites-in-greenhouse-cucumber-cucumis-sativus-l
#11
Yue Geng, Linjie Jiang, Yanwei Zhang, Zeying He, Lu Wang, Yi Peng, Yuehua Wang, Xiaowei Liu, Yaping Xu
BACKGROUND: The dissipation behavior, pre-harvest interval estimation, and dietary risk assessment of carbosulfan, dimethoate, and their relevant metabolites were investigated in greenhouse cucumber in Tianjin, northern China, to ensure raw consumption safety. RESULTS: Carbosulfan was metabolized to carbofuran, dibutylamine, 3-hydroxycarbofuran, 3-ketocarbofuran as well as dimethoate was degraded to omethoate in cucumber fruits and leaves. The dissipation of carbosulfan, carbofuran, 3-hydroxycarbofuran, and dimethoate fitted first-order kinetics well with R2 ranged from 0...
January 12, 2018: Pest Management Science
https://www.readbyqxmd.com/read/29321979/improvement-of-aspergillus-flavus-saponin-hydrolase-thermal-stability-and-productivity-via-immobilization-on-a-novel-carrier-based-on-sugarcane-bagasse
#12
Hala A Amin, Francesco Secundo, Hassan Amer, Faten A Mostafa, Wafaa A Helmy
Soyasapogenol B (SB) is known to have many biological activities such as hepatoprotective, anti-inflammatory, anti-mutagenic, antiviral and anticancer activities. Enzymatic conversion of soyasaponins to SB was carried out using saponin hydrolase (SH) extracted from Aspergillus flavus. The partially purified enzyme was immobilized on different carriers by physical adsorption, covalent binding or entrapment. Among the investigated carriers, Eupergit C and sugarcane bagasse (SCB) activated by DIC and NHS were the most suitable two carriers for immobilization (the immobilized forms recovered 46...
March 2018: Biotechnology Reports
https://www.readbyqxmd.com/read/29320205/heavy-atom-secondary-kinetic-isotope-effect-on-h-tunneling
#13
André Kristopher Eckhardt, Dennis Gerbig, Peter R Schreiner
Although frequently employed, heavy atom kinetic isotope effects (KIE) have not been reported for quantum mechanical tunneling reactions. Here we examine the secondary KIE through 13C substitution of the carbene atom in methylhydroxycarbene (H3C-C̈-OH) in its [1,2]H tunneling shift reaction to acetaldehyde (H3C-CHO). Our study employs matrix isolation IR spectroscopy in various inert gases and quantum chemical computations. Depending on the choice of the matrix host gas the KIE varies within a range of 1.0 in xenon and 1...
January 10, 2018: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/29318653/pharmacokinetic-pharmacodynamic-modelling-of-neutrophil-response-to-g-csf-in-healthy-subjects-and-patients-with-chemotherapy-induced-neutropenia
#14
Murad Melhem, Isabelle Delor, Juan Jose Pérez-Ruixo, John Harrold, Andrew Chow, Liviawati Wu, Philippe Jacqmin
AIM: The objective of this study was to use pharmacokinetic-pharmacodynamic modelling to characterize the effects of chemotherapy on the granulopoietic system and to predict the absolute neutrophil counts (ANCs) for patients with chemotherapy-induced neutropenia (CIN) treated with filgrastim and pegfilgrastim. METHODS: Data were extracted from 10 phase 1-3 studies conducted in 110 healthy adults and 618 adult and 52 paediatric patients on chemotherapy following administration of filgrastim or pegfilgrastim...
January 9, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29316515/the-body-burden-and-thyroid-disruption-in-lizards-eremias-argus-living-in-benzoylurea-pesticides-contaminated-soil
#15
Jing Chang, Jitong Li, Weiyu Hao, Huili Wang, Wei Li, Baoyuan Guo, Jianzhong Li, Yinghuan Wang, Peng Xu
Dermal exposure is regarded as a potentially significant but understudied route for pesticides uptake in terrestrial reptiles. In this study, a native Chinese lizard was exposed to control, diflubenzuron or flufenoxuron contaminated soil (1.5 mg kg-1) for 35 days. Tissue distribution, liver lesions, thyroid hormone levels and transcription of most target genes were examined. The half-lives of diflubenzuron and flufenoxuron in the soil were 118.9 and 231.8 days, respectively. The accumulation of flufenoxuron in the liver, brain, kidney, heart, plasma and skin (1...
January 4, 2018: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/29314286/the-impact-of-kidney-donor-profile-index-kdpi-on-delayed-graft-function-and-transplant-outcomes-a-single-center-analysis
#16
Tiffany J Zens, Juan S Danobeitia, Glen Leverson, Peter J Chlebeck, Laura J Zitur, Robert R Redfield, Anthony M D'Alessandro, Scott Odorico, Dixon B Kaufman, Luis A Fernandez
INTRODUCTION: Renal transplant outcomes result from a combination of factors. Traditionally, donor factors were summarized by classifying kidneys as extended criteria or standard criteria. In 2014, the nomenclature changed to describe donor factors with the kidney donor profile index (KDPI). We aim to evaluate the relationship between KDPI and delayed graft function, and the impact KDPI on transplant outcomes for both donor after cardiac death (DCD) and donor after brain death (DBD) ...
January 3, 2018: Clinical Transplantation
https://www.readbyqxmd.com/read/29311084/intrapulmonary-pharmacokinetics-of-relebactam-a-novel-%C3%AE-lactamase-inhibitor-dosed-in-combination-with-imipenem-cilastatin-in-healthy-subjects
#17
Matthew L Rizk, Elizabeth G Rhee, Patricia A Jumes, Mark H Gotfried, Tian Zhao, Eric Mangin, Sheng Bi, Cynthia M Chavez-Eng, Zufei Zhang, Joan R Butterton
This Phase I study assessed the intrapulmonary pharmacokinetic profiles of relebactam (MK-7655), a novel ß-lactamase inhibitor, and imipenem. Sixteen healthy subjects received 250 mg relebactam with 500 mg imipenem/cilastatin, given IV every 6 hours for 5 doses, and were randomized to bronchoscopy/broncho-alveolar lavage at 0.5, 1, 1.5, or 3 hours after the last dose (4 subjects per time point). Both drugs penetrated the epithelial lining fluid (ELF) to a similar degree, with profiles similar in shape to the corresponding plasma profiles and apparent terminal half-lives in plasma and ELF, respectively, of 1...
January 8, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29306199/effect-of-composting-and-soil-type-on-dissipation-of-veterinary-antibiotics-in-land-applied-manures
#18
Chaoqi Chen, Partha Ray, Katharine F Knowlton, Amy Pruden, Kang Xia
The objective of this study was to determine the fate of commonly used veterinary antibiotics in their naturally excreted form when manure-based amendments are applied to soil. Beef cattle were administered sulfamethazine, tylosin, and chlortetracycline and dairy cows were treated with pirlimycin. The resulting manure was composted for 42 d under static or turned conditions and applied at agronomic N rates to sandy, silt, and silty clay loam soils and compared with amendment with corresponding raw manures in sacrificial microcosms over a 120-day period...
December 26, 2017: Chemosphere
https://www.readbyqxmd.com/read/29304529/passivating-injured-endothelium-with-kinexins-in-thrombolytic-therapy
#19
Yunn-Hwa Ma, Chao-Wei Huang, Chih-Jen Wen, Yi-Ching Lu, Shiaw-Pyng Wey, Tze-Chein Wun
Without conjunctive administration of an anticoagulant, endothelial injury-induced thrombosis is resistant to thrombolysis and prone to re-thrombosis. We hypothesized that co-delivery of recombinant tissue plasminogen activator (rtPA) with annexin V-containing anticoagulants that specifically target the injured endothelium may passivate the thrombogenic elements of the vascular injury site and enhance rtPA-induced thrombolysis. In this study, the effects of conjunctive administration of Kinexins (Kunitz inhibitor-annexin V fusion proteins) with rtPA on thrombolysis were determined in vitro and in vivo...
January 2018: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/29301968/engineering-posttranslational-proofreading-to-discriminate-nonstandard-amino-acids
#20
Aditya M Kunjapur, Devon A Stork, Erkin Kuru, Oscar Vargas-Rodriguez, Matthieu Landon, Dieter Söll, George M Church
Incorporation of nonstandard amino acids (nsAAs) leads to chemical diversification of proteins, which is an important tool for the investigation and engineering of biological processes. However, the aminoacyl-tRNA synthetases crucial for this process are polyspecific in regard to nsAAs and standard amino acids. Here, we develop a quality control system called "posttranslational proofreading" to more accurately and rapidly evaluate nsAA incorporation. We achieve this proofreading by hijacking a natural pathway of protein degradation known as the N-end rule, which regulates the lifespan of a protein based on its amino-terminal residue...
January 4, 2018: Proceedings of the National Academy of Sciences of the United States of America
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