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https://www.readbyqxmd.com/read/28736501/design-of-radioiodinated-pharmaceuticals-structural-features-affecting-metabolic-stability-towards-in-vivo-deiodination
#1
REVIEW
Lorenzo Cavina, Dion van der Born, Peter H M Klaren, Martin C Feiters, Otto C Boerman, Floris P J T Rutjes
Radioiodinated pharmaceuticals are convenient tracers for clinical and research investigations because of the relatively long half-lives of radioactive iodine isotopes (i.e., (123)I, (124)I, and (131)I) and the ease of their chemical insertion. Their application in radionuclide imaging and therapy may, however, be hampered by poor in vivo stability of the C-I bond. After an overview of the use of iodine in biology and nuclear medicine, we present here a survey of the catabolic pathways for iodinated xenobiotics, including their biodistribution, accumulation, and biostability...
June 30, 2017: European Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28735541/photoresponsive-foams-generated-by-a-rigid-surfactant-derived-from-dehydroabietic-acid
#2
Lan Lei, Danhua Xie, Binglei Song, Jianzhong Jiang, Xiaomei Pei, Zhenggang Cui
Innovation in the structure of surfactants is crucial to the construction of a surfactant-based system with intriguing properties. With dehydroabietic acid as a starting material, a nearly totally rigid azobenzene surfactant (R-azo-Na) was synthesized. The trans-R-azo-Na formed stable foams with half-lives of 636, 656, 976, and 872 min for 0.3, 1, 2, and 4 mmol∙L-1 aqueous solutions, respectively. Under UV light irradiation, a fast collapse of the foams was observed, showing an in situ response. The excellent foam stability of trans-R-azo-Na leads to the extremely high photoresponsive efficiency...
July 22, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28730290/a-phase-i-study-to-investigate-the-metabolism-excretion-and-pharmacokinetics-of-14-c-fruquintinib-a-novel-oral-selective-vegfr-inhibitor-in-healthy-chinese-male-volunteers
#3
Sufeng Zhou, Feng Shao, Zhaoqiang Xu, Lu Wang, Ke Jin, Lijun Xie, Juan Chen, Yun Liu, Hongwen Zhang, Ning Ou
PURPOSE: Fruquintinib (HMPL-013) is a novel, potent, and highly selective tyrosine kinase inhibitor targeting the vascular endothelial growth factor receptors (1, 2 and 3). This study was conducted to investigate the metabolism, excretion, and pharmacokinetics of HMPL-013 after a single oral dose to healthy Chinese men. METHODS: Six subjects were administrated an oral suspension containing 5 mg of (14)C-labeled HMPL-013 (100 μCi) in a fasted state. Blood and excreta samples were collected at the designated time points or intervals for pharmacokinetics and radiometric analyses...
July 20, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28727998/enrichment-of-endogenous-fractalkine-and-anti-inflammatory-cells-via-aptamer-functionalized-hydrogels
#4
Syed Faaiz Enam, Jack R Krieger, Tarun Saxena, Brian E Watts, Claire E Olingy, Edward A Botchwey, Ravi V Bellamkonda
Early recruitment of non-classical monocytes and their macrophage derivatives is associated with augmented tissue repair and improved integration of biomaterial constructs. A promising therapeutic approach to recruit these subpopulations is by elevating local concentrations of chemoattractants such as fractalkine (FKN, CX3CL1). However, delivering recombinant or purified proteins is not ideal due to their short half-lives, suboptimal efficacy, immunogenic potential, batch variabilities, and cost. Here we report an approach to enrich endogenous FKN, obviating the need for delivery of exogenous proteins...
July 10, 2017: Biomaterials
https://www.readbyqxmd.com/read/28727453/formation-of-developmentally-toxic-phenanthrene-metabolite-mixtures-by-mycobacterium-sp-elw1
#5
Jill E Schrlau, Amber L Kramer, Anna Chlebowski, Lisa Truong, Robert L Tanguay, Staci L Massey Simonich, Lewis Semprini
Mycobacterium sp. ELW1 co-metabolically degraded up to 1.8 μmol of phenanthrene (PHE) in ∼48 h, and hydroxyphenanthrene (OHPHE) metabolites, including 1-hydroxyphenanthrene (1-OHPHE), 3-hydroxyphenanthrene (3-OHPHE), 4-hydroxyphenanthrene (4-OHPHE), 9-hydroxyphenanthrene (9-OHPHE), 9,10-dihydroxyphenanthrene (1,9-OHPHE), and trans-9,10-dihydroxy-9,10-dihydrophenanthrene (trans-9,10-OHPHE), were identified and quantified over time. The monooxygenase responsible for co-metabolic transformation of PHE was inhibited by 1-octyne...
July 20, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28726397/potential-releases-of-129-i-236-u-and-pu-isotopes-from-the-fukushima-dai-ichi-nuclear-power-plants-to-the-ocean-during-2013-to-2015
#6
Núria Casacuberta, Marcus Christl, Ken O Buesseler, YikSze Lau, Christof Vockenhuber, Maxi Castrillejo, Hans-Arno Synal, Pere Masque
After the Fukushima Dai-ichi Nuclear accident, many efforts were put into the determination of the presence of (137)Cs, (134)Cs, (131)I and other gamma-emitting radionuclides in the ocean, but minor work was done regarding the monitoring of less volatile radionuclides, pure beta-ray emitters or simply radionuclides with very long half-lives. In this study we document the temporal evolution of (129)I, (236)U and Pu isotopes ((239)Pu and (240)Pu) in seawater sampled during four different cruises performed 2, 3 and 4 years after the accident, and compare the results to (137)Cs collected at the same stations and depths...
July 20, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28724104/fate-characterization-of-benzene-kresoxim-methyl-a-strobilurin-fungicide-in-different-aerobic-soils
#7
Jinhao Zhao, Likun Wang, Jingli Cheng, Wei Wang, Qingfu Ye
Benzene kresoxim-methyl (BKM) is a promising broad-spectrum strobilurin fungicide widely used to control fungal pathogens in crops. However, information on its environmental fate is limited. To broaden our understanding of this fungicide's kinetic fate in aerobic soils, we labeled BKM with C on its benzoate ring and used ultralow-level liquid scintillation counting coupled with high-performance liquid chromatography analysis. Results show that degradation, mineralization, and bound residue (BR) formation of BKM was controlled by soil type and microbial community composition...
May 2017: Journal of Environmental Quality
https://www.readbyqxmd.com/read/28724091/effect-of-environmental-conditions-on-the-degradation-of-florasulam-in-typical-soils-of-northern-china
#8
Wangcang Su, Hongle Xu, Hongdan Hao, Renhai Wu, Hengliang Wang, Chuantao Lu
The widespread use of florasulam in China makes residues from this herbicide in soil a serious concern due to their potential to pollute the soil environment and groundwater. Accelerating the degradation of these residues will reduce their pollution potential. In this study, we investigated the degradation and adsorption of florasulam in four typical soils in northern China and examined the degradation of florasulam in Inceptisols at different temperatures, soil moisture contents, and pH values, as well as the influence of microorganisms and the use of organic matter and biogas slurry as soil amendments...
May 2017: Journal of Environmental Quality
https://www.readbyqxmd.com/read/28722197/simultaneous-determination-and-method-validation-of-difenoconazole-propiconazole-and-pyraclostrobin-in-pepper-and-soil-by-lc-ms-ms-in-field-trial-samples-from-three-provinces-china
#9
Kunming Zheng, Banghua Meng, Sizhuo Wu, Haizhen Zhang, Fei Wang, Ying Cui, Song Zeng, Kankan Zhang, Deyu Hu
A liquid chromatography-electrospray ionization tandem mass spectrometry method was developed for simple and accurate detection of the fungicides difenoconazole, propiconazole and pyraclostrobin in peppers and soil. Three fungicides residues were extracted from samples by acetonitrile, cleaned up by dispersive solid phase extraction before instrumental analysis. The accuracy and precision of the method were evaluated by conducting intra- and inter-day recovery experiment. The limits of quantification and detection of difenoconazole, propiconazole and pyraclostrobin in pepper and soil were 0...
July 19, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28719879/four-types-of-attenuation-of-phenol-and-cresols-in-microcosms-under-simulated-marine-conditions-a-kinetic-study
#10
Yuejie Wang, Fanping Meng, Yufei Lin, Weiyan Duan, Qunqun Liu
Phenol, o-cresol, m-cresol, and p-cresol were selected to conduct microcosm experiments to examine their attenuation under simulated marine conditions, aiming at estimating natural attenuation and the contribution of oxidation, photolysis, biodegradation, and volatilisation to total attenuation of phenol and three cresols in the marine environment. The development of attenuation in microcosms showed the relevance of the pseudo-first-order kinetic for all phenols. The half-lives of phenol, o-cresol, m-cresol, and p-cresol attenuation under optimal conditions were 7...
July 11, 2017: Chemosphere
https://www.readbyqxmd.com/read/28719664/predicting-the-protein-half-life-in-tissue-from-its-cellular-properties
#11
Mahbubur Rahman, Rovshan G Sadygov
Protein half-life is an important feature of protein homeostasis (proteostasis). The increasing number of in vivo and in vitro studies using high throughput proteomics provide estimates of the protein half-lives in tissues and cells. However, protein half-lives in cells and tissues are different. Due to the resource requirements for researching tissues, more data is available from cellular studies than tissues. We have designed a multivariate linear model for predicting protein half-life in tissue from its cellular properties...
2017: PloS One
https://www.readbyqxmd.com/read/28715785/prenatal-exposure-estimation-of-bpa-and-dehp-using-integrated-external-and-internal-dosimetry-a-case-study
#12
M A Martínez, J Rovira, R Prasad Sharma, M Nadal, M Schuhmacher, V Kumar
Prenatal exposure to Endocrine disruptors (EDs), such as Bisphenol A (BPA) and di (2-ethylhexyl) phthalate (DEHP), has been associated with obesity and diabetes diseases in childhood, as well as reproductive, behavioral and neurodevelopment problems. The aim of this study was to estimate the prenatal exposure to BPA and DEHP through food consumption for pregnant women living in Tarragona County (Spain). Probabilistic calculations of prenatal exposure were estimated by integrated external and internal dosimetry modelling, physiologically based pharmacokinetic (PBPK) model, using a Monte-Carlo simulation...
July 14, 2017: Environmental Research
https://www.readbyqxmd.com/read/28714475/acylated-heptapeptide-binds-albumin-with-high-affinity-and-application-as-tag-furnishes-long-acting-peptides
#13
Alessandro Zorzi, Simon J Middendorp, Jonas Wilbs, Kaycie Deyle, Christian Heinis
The rapid renal clearance of peptides in vivo limits this attractive platform for the treatment of a broad range of diseases that require prolonged drug half-lives. An intriguing approach for extending peptide circulation times works through a 'piggy-back' strategy in which peptides bind via a ligand to the long-lived serum protein albumin. In accordance with this strategy, we developed an easily synthesized albumin-binding ligand based on a peptide-fatty acid chimera that has a high affinity for human albumin (Kd=39 nM)...
July 17, 2017: Nature Communications
https://www.readbyqxmd.com/read/28710810/putative-binding-sites-for-mir-125-family-mirnas-in-the-mouse-lfng-3-utr-affect-transcript-expression-in-the-segmentation-clock-but-mir-125a-5p-is-dispensable-for-normal-somitogenesis
#14
Kanu Wahi, Sophia Friesen, Vincenzo Coppola, Susan E Cole
BACKGROUND: In vertebrate embryos, a "segmentation clock" times somitogenesis. Clock-linked genes, including Lunatic fringe (Lfng), exhibit cyclic expression in the presomitic mesoderm (PSM), with a period matching the rate of somite formation. The clock period varies widely across species, but the mechanisms that underlie this variability are not clear. The half-lives of clock components are proposed to influence the rate of clock oscillations, and are tightly regulated in the PSM. Interactions between Lfng and mir-125a-5p in the embryonic chicken PSM promote Lfng transcript instability, but the conservation of this mechanism in other vertebrates has not been tested...
July 14, 2017: Developmental Dynamics: An Official Publication of the American Association of Anatomists
https://www.readbyqxmd.com/read/28706991/multiplexed-gene-control-reveals-rapid-mrna-turnover
#15
Antoine Baudrimont, Sylvia Voegeli, Eduardo Calero Viloria, Fabian Stritt, Marine Lenon, Takeo Wada, Vincent Jaquet, Attila Becskei
The rates of mRNA synthesis and decay determine the mRNA expression level. The two processes are under coordinated control, which makes the measurements of these rates challenging, as evidenced by the low correlation among the methods of measurement of RNA half-lives. We developed a minimally invasive method, multiplexed gene control, to shut off expression of genes with controllable synthetic promoters. The method was validated by measuring the ratios of the nascent to mature mRNA molecules and by measuring the half-life with endogenous promoters that can be controlled naturally or through inserting short sequences that impart repressibility...
July 2017: Science Advances
https://www.readbyqxmd.com/read/28705956/rapid-recovery-gene-downregulation-during-excess-light-stress-and-recovery-in-arabidopsis
#16
Peter Alexander Crisp, Diep Ganguly, Aaron B Smith, Kevin D Murray, Gonzalo M Estavillo, Iain R Searle, Ethan Ford, Ozren Bogdanović, Ryan Lister, Justin O Borevitz, Steven R Eichten, Barry J Pogson
Stress recovery may prove to be a promising approach to increase plant performance, and theoretically, mRNA instability may facilitate faster recovery. Transcriptome (RNA-seq, qPCR, sRNA-seq, PARE) and methylome profiling during repeated excess-light stress and recovery was performed at intervals as short as three minutes. We demonstrate that 87% of the stress-upregulated mRNAs analysed exhibit very rapid recovery. For instance, HSP101 abundance declined two-fold every 5.1 minutes. We term this phenomenon Rapid Recovery Gene Downregulation (RRGD), whereby mRNA abundance rapidly decreases promoting transcriptome resetting...
July 13, 2017: Plant Cell
https://www.readbyqxmd.com/read/28704661/direct-and-indirect-photolysis-of-seven-micropollutants-in-secondary-effluent-from-a-wastewater-lagoon
#17
Yufei Wang, Felicity A Roddick, Linhua Fan
The photodegradation of seven micropollutants commonly found in municipal wastewater, namely caffeine, carbamazepine, diuron, simazine, sulfamethoxazole, triclosan and 2,4-D, was investigated in pure water and secondary effluent to understand the direct and indirect photolysis of these compounds under natural sunlight irradiation. Sulfamethoxazole and triclosan were readily photodegraded with half-lives of 5.8 and 1.8 h, respectively, whilst the others were relatively resistant towards sunlight irradiation...
June 29, 2017: Chemosphere
https://www.readbyqxmd.com/read/28700897/a-systematic-comparison-of-clinically-viable-nanomedicines-targeting-hmg-coa-reductase-in-inflammatory-atherosclerosis
#18
Amr Alaarg, Max L Senders, Aida Varela-Moreira, Carlos Pérez-Medina, Yiming Zhao, Jun Tang, Francois Fay, Thomas Reiner, Zahi A Fayad, Wim E Hennink, Josbert M Metselaar, Willem J M Mulder, Gert Storm
Atherosclerosis is a leading cause of worldwide morbidity and mortality whose management could benefit from novel targeted therapeutics. Nanoparticles are emerging as targeted drug delivery systems in chronic inflammatory disorders. To optimally exploit nanomedicines, understanding their biological behavior is crucial for further development of clinically relevant and efficacious nanotherapeutics intended to reduce plaque inflammation. Here, three clinically relevant nanomedicines, i.e., high-density lipoprotein ([S]-HDL), polymeric micelles ([S]-PM), and liposomes ([S]-LIP), that are loaded with the HMG-CoA reductase inhibitor simvastatin [S], were evaluated in the apolipoprotein E-deficient (Apoe(-/-)) mouse model of atherosclerosis...
July 9, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28697876/pharmacokinetics-of-the-anti-androgenic-drug-flutamide-in-healthy-stallions
#19
Francisco Javier Mendoza, Juan Manuel Serrano-Rodriguez, Antonio Buzon-Cuevas, Alejandro Perez-Ecija
Alternatives to surgical castration are necessary for controlling the sexual behaviour of stallions with breeding potential in training and competition. Flutamide is a potent selective non-steroidal androgen receptor competitive antagonist that has been used in human beings as an anti-androgenic drug. In this study, the pharmacokinetics and bioavailability of flutamide and its main active metabolite, 2-hydroflutamide, were determined in seven healthy mature stallions. Single doses of flutamide (1mg/kg intravenously, 1mg/kg orally in fasted horses, 5mg/kg orally in fasted horses and 5mg/kg orally in fed horses) were administered randomly at intervals of 2 weeks...
June 2017: Veterinary Journal
https://www.readbyqxmd.com/read/28693443/association-of-benzodiazepine-and-z-drug-use-with-the-risk-of-hospitalisation-for-fall-related-injuries-among-older-people-a-nationwide-nested-case-control-study-in-taiwan
#20
Nan-Wen Yu, Pei-Jung Chen, Hui-Ju Tsai, Chih-Wan Huang, Yu-Wen Chiu, Wen-Ing Tsay, Jui Hsu, Chia-Ming Chang
BACKGROUND: Non-benzodiazepine hypnotics (Z-drugs) are advocated to be safer than benzodiazepines (BZDs). This study comprehensively investigated the association of BZD and Z-drug usage with the risk of hospitalisation for fall-related injuries in older people. METHODS: This study used the Taiwan National Health Insurance Database with a nested matched case-control design. We identified 2238 elderly patients who had been hospitalised for fall-related injuries between 2003 and 2012...
July 11, 2017: BMC Geriatrics
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