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https://www.readbyqxmd.com/read/29035714/biodegradation-of-triclosan-in-diatom-navicula-sp-kinetics-transformation-products-toxicity-evaluation-and-the-effects-of-ph-and-potassium-permanganate
#1
Tengda Ding, Kunde Lin, Mengting Yang, Lianjun Bao, Juying Li, Bo Yang, Jay Gan
Triclosan (TCS) is one of the most widely used pharmaceutically active compounds and frequently detected in treated wastewater and the impacted aquatic environment. However, the fate and toxicity of TCS in aquatic organisms is poorly known, including in particular the potential for the formation of incomplete biological transformation products. In this study, TCS posed high toxic effects (e.g., growth inhibition and damage of photosynthesis) to typical freshwater diatom Navicula sp., with the 24h and 72h EC50 values of 173...
September 21, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/29032526/micro-pollutants-in-sediment-samples-in-the-middle-danube-region-serbia-occurrence-and-risk-assessment
#2
Biljana D Škrbić, Kiwao Kadokami, Igor Antić, Grigorije Jovanović
This is the first comprehensive study on the occurrence of 940 semi-volatile organic compounds including sterols, polycyclic aromatic hydrocarbons (PAHs), polychlorinated biphenyls (PCBs), pesticides, plasticizers, and other emerging compounds in 10 river and canal sediments collected in northern Serbia. For quantification of investigated compounds GC-MS-MS (selected reaction monitoring) and GC-MS (using both selected ion monitoring and total ion monitoring) methods were used. The number of detected compounds was in the range of 85-117, while the sum of the concentrations varied from 959 μg/kg dry-wt to 84,445 μg/kg dry-wt...
October 14, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29032447/evaluation-and-calibration-of-high-throughput-predictions-of-chemical-distribution-to-tissues
#3
Robert G Pearce, R Woodrow Setzer, Jimena L Davis, John F Wambaugh
Toxicokinetics (TK) provides critical information for integrating chemical toxicity and exposure assessments in order to determine potential chemical risk (i.e., the margin between toxic doses and plausible exposures). For thousands of chemicals that are present in our environment, in vivo TK data are lacking. The publicly available R package "httk" (version 1.8, named for "high throughput TK") draws from a database of in vitro data and physico-chemical properties in order to run physiologically-based TK (PBTK) models for 553 compounds...
October 14, 2017: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/29031440/removal-of-antibiotics-in-a-parallel-plate-thin-film-photocatalytic-reactor-process-modeling-and-evolution-of-transformation-by-products-and-toxicity
#4
Can Burak Özkal, Zacharias Frontistis, Maria Antonopoulou, Ioannis Konstantinou, Dionissios Mantzavinos, Süreyya Meriç
Photocatalytic degradation of sulfamethoxazole (SMX) antibiotic has been studied under recycling batch and homogeneous flow conditions in a thin-film coated immobilized system namely parallel-plate (PPL) reactor. Experimentally designed, statistically evaluated with a factorial design (FD) approach with intent to provide a mathematical model takes into account the parameters influencing process performance. Initial antibiotic concentration, UV energy level, irradiated surface area, water matrix (ultrapure and secondary treated wastewater) and time, were defined as model parameters...
October 2017: Journal of Environmental Sciences (China)
https://www.readbyqxmd.com/read/29031071/discovery-of-thienopyrrolotriazine-derivatives-to-protect-mitochondrial-function-against-a%C3%AE-induced-neurotoxicity
#5
TaeHun Kim, Woo Seung Son, Mohammad Neaz Morshed, Ashwini M Londhe, Seo Yun Jung, Jong-Hyun Park, Woo-Kyu Park, Sang Min Lim, Ki Duk Park, Sung Jin Cho, Kyu-Sung Jeong, Jiyoun Lee, Ae Nim Pae
Recovery of mitochondrial dysfunction has gained increasing attention as an alternative therapeutic strategy for Alzheimer's disease (AD). Recent studies suggested that the 18 kDa mitochondrial translocator protein (TSPO) has the potential to serve as a drug target for the treatment of AD. In this study, we generated a structure-based pharmacophore model and virtually screened a commercial library, identifying SVH07 as a virtual hit, which contained a tricyclic core structure, thieno[2',3':4,5]pyrrolo[1,2-d][1,2,4]triazine group...
September 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29030269/the-importance-of-inclusion-of-kinetic-information-in-the-extrapolation-of-high-to-low-concentrations-for-human-limit-setting
#6
Liesbeth Geraets, Marco J Zeilmaker, Peter M J Bos
Human health risk assessment of inhalation exposures generally includes a high-to-low concentration extrapolation. Although this is a common step in human risk assessment, it introduces various uncertainties. One of these uncertainties is related to the toxicokinetics. Many kinetic processes such as absorption, metabolism or excretion can be subject to saturation at high concentration levels. In the presence of saturable kinetic processes of the parent compound or metabolites, disproportionate increases in internal blood or tissue concentration relative to the external concentration administered may occur resulting in nonlinear kinetics...
October 10, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/29029183/evaluation-of-the-constituents-of-vetiver-oil-against-anopheles-minimus-diptera-culicidae-a-malaria-vector-in-thailand
#7
Rungarun Tisgratog, Chutipong Sukkanon, John P Grieco, Unchalee Sanguanpong, Kamlesh R Chauhan, Joel R Coats, Theeraphap Chareonviriyaphap
The development of resistance by mosquitoes to current synthetic compounds has resulted in reduced effectiveness of prevention and control methods worldwide. An alternative nonchemical based control tools are needed to be evaluated particularly plant-derived essential oils. Several components of vetiver oil have been documented as insect repellents. However, detailed knowledge of those components action against insect remains unknown. In this study, behavioral response of Anopheles minimus to four constituents of vetiver oil (valencene, terpinen-4-ol, isolongifolene, vetiverol) was evaluated by using the high-throughput screening assay system...
October 6, 2017: Journal of Medical Entomology
https://www.readbyqxmd.com/read/29027716/cytotoxicity-of-group-5-transition-metal-ditellurides-mte2-m-v-nb-ta
#8
Martin Pumera
Much research effort has been put in to study layered compounds with transition metal dichalcogenides (TMDs) being one of the most studied compounds. Due to their extraordinary properties such as excellent electrochemical properties, tuneable band gaps and low shear resistance due to weak van der Waals interactions between layers, TMDs have been found to have a wide application such as electrocatalyst for hydrogen evolution reactions, supercapacitors, biosensors, field-effect transistors (FETs), photovoltaic and lubricant additives...
October 13, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29027085/two-new-cytotoxic-stilbenoid-dimers-isolated-from-cajanus-cajan
#9
Nenling Zhang, Xiangchun Shen, Xiaofei Jiang, Jiazhong Cai, Xiaoling Shen, Yingjie Hu, Samuel X Qiu
Two new stilbenoid dimers, cajanstilbenoids A (1) and B (2), were isolated from the leaves of Cajanus cajan. Planar structures of these compounds were verified by NMR (1D and 2D) and high-resolution electrospray ionization mass spectroscopy (HR-ESI-MS). Absolute configurations were assigned by comparing experimental and calculated electronic CD values. The cytotoxicity of 1 and 2 against human hepatoma (HepG2), human breast adenocarcinoma (MCF-7), and human lung cancer (A549) cells were evaluated in vitro. Compound 1 showed strong cytotoxicity against all the tested cell lines (IC50 values: 2...
October 12, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/29026857/repellency-effect-of-essential-oils-of-some-native-plants-and-synthetic-repellents-against-human-flea-pulex-irritans-siphonaptera-pulicidae
#10
Mohammad Bagher Ghavami, Fahimeh Poorrastgoo, Behrooz Taghiloo, Jamshid Mohammadi
BACKGROUND: Fleas are important vectors of human and animal disease, and control measures for protection against their bites and flea-borne diseases are necessary. METHODS: The essential oils (EOs) of four native medicinal plants, Ziziphora tenuiore, Myrtus communis, Achillea wilhelmsii and Mentha piperita were isolated by hydrodistillation technique and analyzed by GC-MC. The repellent activity of EOs and synthetic compounds, DEET and permethrin, were assayed on human subjects against field collected fleas...
March 2017: Journal of Arthropod-borne Diseases
https://www.readbyqxmd.com/read/29026428/evaluation-of-the-physiological-activity-of-venom-from-the-eurasian-water-shrew-neomys-fodiens
#11
Krzysztof Kowalski, Paweł Marciniak, Grzegorz Rosiński, Leszek Rychlik
BACKGROUND: Animal toxins can have medical and therapeutic applications. Principally, toxins produced by insects, arachnids, snakes and frogs have been characterized. Venomous mammals are rare, and their venoms have not been comprehensively investigated. Among shrews, only the venom of Blarina brevicauda has been analysed so far, and blarina toxin has been proven to be its main toxic component. It is assumed that Neomys fodiens employs its venom to hunt larger prey. However, the toxic profile, properties and mode of action of its venom are largely unknown...
2017: Frontiers in Zoology
https://www.readbyqxmd.com/read/29024910/leishmanicidal-and-cytotoxic-activity-of-hederagenin-bistriazolyl-derivatives
#12
Diego Rodríguez-Hernández, Luiz C A Barbosa, Antonio J Demuner, Amalyn Nain-Perez, Sebastião R Ferreira, Ricardo T Fujiwara, Raquel M de Almeida, Lucie Heller, René Csuk
Aiming to obtain new potent leishmanicidal and cytotoxic compounds from natural sources, the triterpene hederagenin was converted into several new 1,2,3-triazolyl derivatives tethered at C-23 and C-28. For this work hederagenin was isolated from fruits of Sapindus saponaria and reacted with propargyl bromide to afford as a major product bis-propargylic derivative 1 in 74%. Submitting this compound to Huisgen 1,3-dipolar cycloaddition reactions with several azides afforded the derivatives 2-19 with yields in the range of 40-87%...
September 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29024886/a-case-study-to-identify-priority-cytostatic-contaminants-in-hospital-effluents
#13
A Olalla, N Negreira, M López de Alda, D Barceló, Y Valcárcel
This study analyses the presence of 17 cytostatic agents from seven different groups, based on their different mechanisms of action, in the effluent from a medium-sized hospital located in eastern Spain. Analysis of the compounds found in the effluents studied involved solidphase extraction (SPE) coupled on-line to a high performance liquid chromatograph tandem mass spectrometer (HPLC-MS/MS). The environmental risk of the compounds studied was then assessed by calculating the hazard quotient (HQ), combining the measured environmental concentrations (MECs) with dose-response data based on the predicted no effect concentrations (PNECs)...
September 28, 2017: Chemosphere
https://www.readbyqxmd.com/read/29024789/in-vitro-pharmacological-characterization-of-the-bispyridinium-non-oxime-compound-mb327-and-its-2-and-3-regioisomers
#14
K V Niessen, T Seeger, S Rappenglück, T Wein, G Höfner, K T Wanner, H Thiermann, F Worek
The primary toxic mechanism of organophosphorus compounds, i.e. nerve agents or pesticides, is based on the irreversible inhibition of acetylcholinesterase. In consequence of the impaired hydrolysis, the neurotransmitter acetylcholine accumulates in cholinergic synapses and disturbs functional activity of nicotinic and muscarinic acetylcholine receptors by overstimulation and subsequent desensitization. The resulting cholinergic syndrome will become acute life-threatening, if not treated adequately. The current standard treatment, consisting of administration of a competitive mAChR antagonist (e...
October 9, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/29024685/cardiac-pathologic-findings-in-three-unusual-cases-of-sudden-cardiac-death-related-to-anorexiant-drugs
#15
Ornella Leone, Valentina Agostini, Alberto Foà, Bruna Cerbelli, Cira Rosaria Tiziana di Gioia, Mariarosaria Aromatario, Costantino Ciallella, Joaquin Lucena, Giulia d'Amati
Amphetamine congeners can be prescribed as anorexiant drugs, despite their potential side effects, including cardiac toxicity. However, the morphologic features of cardiac damage related to protracted use of these compounds are unknown. We provide a detailed description of cardiac autopsy findings in three cases of sudden death associated with protracted use of high-doses of phendimetrazine and/or phenylpropanolamine or bupropion prescribed as anorexiants, in association with other compounds. The main cardiac findings were similar in all three cases: i) mild-moderate hypertrophy of the left ventricle and/or the septum; ii) myocardial non-ischemic scarring (mid-mural and/or sub-epicardial) appearing as discrete foci or with a band/like morphology; iii) mild-moderate intramural small vessel disease, in absence of significant epicardial coronary artery stenosis; iv) acute/recent inflammatory lesions consistent with toxic myocarditis...
October 9, 2017: Human Pathology
https://www.readbyqxmd.com/read/29023751/the-use-of-factorial-design-to-evaluate-the-oxidation-of-oils-containing-different-types-of-omega-3-fatty-acids
#16
Thamyris Dias Fabiano Agnes, Gabriela Grassmann Roschel, Inar Alves Castro
N3 FA promote beneficial effects on cardiovascular diseases, but they are highly susceptible to oxidation, which leads to the formation of potentially toxic secondary products. In this study, the antioxidant capacity of natural compounds (sinapic acid and rutin) was evaluated using an accelerated model to oxidize the oils. Five inducers (Temperature, Fe(2+) , AAPH, Ascorbyl palmitate and AMVN) were combined in a factorial design to accelerate the oxidation of three oils (flaxseed, echium and fish) containing different sources of n3 FA...
October 11, 2017: Journal of the Science of Food and Agriculture
https://www.readbyqxmd.com/read/29023131/direct-synthesis-of-acyl-fluorides-from-carboxylic-acids-with-the-bench-stable-solid-reagent-me4n-scf3
#17
Thomas Scattolin, Kristina Deckers, Franziska Schoenebeck
A convenient, highly efficient, and selective transformation of aliphatic and aromatic carboxylic acids to acyl fluorides is reported. In contrast to established approaches that require toxic or volatile additives and base and reaction control (i.e., cooling, slow addition), this protocol allows for a straightforward access to various R-COF entities upon direct reaction with the bench-stable, solid reagent (Me4N)SCF3 at room temperature. The method is base- and additive-free, compatible with late-stage synthetic applications, high functional group tolerance, and facile target compound purification via filtration...
October 12, 2017: Organic Letters
https://www.readbyqxmd.com/read/29023104/quantitative-evaluation-of-cisplatin-uptake-in-sensitive-and-resistant-individual-cells-by-single-cell-icp-ms-sc-icp-ms
#18
Mario Corte Rodríguez, Roberto Álvarez-Fernández García, Elisa Blanco Gonzalez, Jorg Bettmer, Maria Montes-Bayon
One of the main limitations to the Pt-therapy in cancer is the development of associated drug resistance that can be associated to a significant reduction of the intracellular platinum concentration. Thus, intracellular Pt concentration could be considered as a biomarker of cisplatin resistance. In this work, an alternative method to address intracellular Pt concentration in individual cells is explored to permit the evaluation of different cell models and/or alternative therapies in a relatively fast way. For this aim, total Pt analysis in single cells has been implemented using a total consumption nebulizer coupled to inductively coupled plasma mass spectrometric detection (ICP-MS)...
October 12, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/29022758/pharmacokinetic-profiling-of-conjugated-therapeutic-oligonucleotides-a-high-throughput-method-based-upon-serial-blood-microsampling-coupled-to-peptide-nucleic-acid-hybridization-assay
#19
Bruno M D C Godinho, James W Gilbert, Reka A Haraszti, Andrew H Coles, Annabelle Biscans, Loic Roux, Mehran Nikan, Dimas Echeverria, Matthew Hassler, Anastasia Khvorova
Therapeutic oligonucleotides, such as small interfering RNAs (siRNAs), hold great promise for the treatment of incurable genetically defined disorders by targeting cognate toxic gene products for degradation. To achieve meaningful tissue distribution and efficacy in vivo, siRNAs must be conjugated or formulated. Clear understanding of the pharmacokinetic (PK)/pharmacodynamic behavior of these compounds is necessary to optimize and characterize the performance of therapeutic oligonucleotides in vivo. In this study, we describe a simple and reproducible methodology for the evaluation of in vivo blood/plasma PK profiles and tissue distribution of oligonucleotides...
October 12, 2017: Nucleic Acid Therapeutics
https://www.readbyqxmd.com/read/29022620/transferring-mixtures-of-chemicals-from-sediment-to-a-bioassay-using-silicone-based-passive-sampling-and-dosing
#20
Lukas Mustajärvi, Ann-Kristin Eriksson-Wiklund, Elena Gorokhova, Annika Jahnke, Anna Sobek
Environmental mixtures of chemicals consist of a countless number of compounds with unknown identity and quantity. Yet, chemical regulation is mainly built around the assessment of single chemicals. Existing frameworks for assessing the toxicity of mixtures require that both the chemical composition and quantity are known. Quantitative analyses of the chemical composition of environmental mixtures are however extremely challenging and resource-demanding. Bioassays may therefore serve as a useful approach for investigating the combined toxicity of environmental mixtures of chemicals in a cost-efficient and holistic manner...
October 12, 2017: Environmental Science. Processes & Impacts
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