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https://www.readbyqxmd.com/read/28549369/safety-analysis-of-occupational-exposure-of-healthcare-workers-to-residual-contaminations-of-cytotoxic-drugs-using-fmeca-security-approach
#1
Laetitia Minh Mai Le, Delphine Reitter, Sophie He, Franck Té Bonle, Amélie Launois, Diane Martinez, Patrice Prognon, Eric Caudron
Handling cytotoxic drugs is associated with chemical contamination of workplace surfaces. The potential mutagenic, teratogenic and oncogenic properties of those drugs create a risk of occupational exposure for healthcare workers, from reception of starting materials to the preparation and administration of cytotoxic therapies. The Security Failure Mode Effects and Criticality Analysis (FMECA) was used as a proactive method to assess the risks involved in the chemotherapy compounding process. FMECA was carried out by a multidisciplinary team from 2011 to 2016...
May 22, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28549345/a-novel-synthetic-derivative-of-quercetin-8-trifluoromethyl-3-5-7-3-4-o-pentamethyl-quercetin-inhibits-bladder-cancer-growth-by-targeting-the-ampk-mtor-signaling-pathway
#2
Ting Tao, Caimei He, Jun Deng, Yanjun Huang, Qiongli Su, Mei Peng, Meiling Yi, Kwame Oteng Darko, Hui Zou, Xiaoping Yang
Quercetin is a naturally existing compound and shows attractive anticancer properties for a variety of solid tumors including glioma, bladder cancer, hepatocellular carcinoma, breast cancer, hematological malignancies and prostate carcinoma. However, these anticancer properties have not been clinically approved due to unclear mechanistic information and its low bioactivity. In our previous study, we elucidated that quercetin activates AMPK pathway which is the major mechanism for its unique anticancer effect in bladder cancer...
May 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28549334/molecular-insight-into-specific-14-3-3-modulators-inhibitors-and-stabilisers-of-protein-protein-interactions-of-14-3-3
#3
Alwin M Hartman, Anna K H Hirsch
The 14-3-3 protein family is implicated in several diseases and biological processes. Several recent reviews have summarised knowledge on certain aspects of 14-3-3 proteins, ranging from a historic overview to the structure, function and regulation. This review focuses on the structures and molecular recognition of the modulators by the 14-3-3 proteins, and small modifications of certain modulators are proposed where cocrystal structures have been reported. Our analysis opens up possibilities for the optimisation of the reported compounds...
April 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28549324/salinity-and-sensitivity-to-endocrine-disrupting-chemicals-a-comparison-of-reproductive-endpoints-in-small-bodied-fish-exposed-under-different-salinities
#4
Thijs Bosker, Giacomo Santoro, Steven D Melvin
The influence of salinity on toxicity outcomes has been demonstrated for various contaminants, but has received limited attention for endocrine disrupting chemicals (EDCs). Short-term laboratory tests using small-bodied fish are an important tool for evaluating impacts of EDCs on reproduction. Tests have been developed for both freshwater and estuarine/marine species, providing an opportunity to assess whether concentrations at which small-bodied fish respond to EDCs may be influenced by salinity. We conducted a semi-quantitative review of short-term laboratory tests with small-bodied fish exposed to EDCs, including 59 studies under freshwater conditions (7 species) and 23 studies conducted under saline conditions (5 species)...
May 16, 2017: Chemosphere
https://www.readbyqxmd.com/read/28549321/studies-on-free-radical-scavenging-cancer-cell-antiproliferation-and-calf-thymus-dna-interaction-of-schiff-bases
#5
Cleiton M da Silva, Marina M Silva, Fabiano S Reis, Ana Lúcia T G Ruiz, João E de Carvalho, Josué C C Santos, Isis M Figueiredo, Rosemeire B Alves, Luzia V Modolo, Ângelo de Fátima
Thirty-nine Schiff bases were synthesized by performing microwave-assisted condensation of the corresponding aldehydes and aromatic amines. Their reactive nitrogen species (RNS) scavenging activity and inhibitory effects against cancer cell growth were then subsequently investigated. Additionally, the interaction between the calf thymus DNA (ctDNA) and selected Schiff bases was evaluated using fluorescence spectroscopy, and their binding parameters were determined. The yields of the various compounds ranged from moderate to excellent (43-99%) after only a 2-min reaction...
May 17, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28549311/reaction-of-diazepam-and-related-benzodiazepines-with-chlorine-kinetics-transformation-products-and-in-silico-toxicological-assessment
#6
Inmaculada Carpinteiro, Rosario Rodil, José Benito Quintana, Rafael Cela
In this work, the reaction of four benzodiazepines (diazepam, oxazepam, nordazepam and temazepam) during water chlorination was studied by means of liquid chromatography-quadrupole-time of flight-mass spectrometry (LC-QTOF-MS). For those compounds that showed a significant degradation, i.e. diazepam, oxazepam and nordazepam, parameters affecting to the reaction kinetics (pH, chlorine and bromide level) were studied in detail and transformation products were tentatively identified. The oxidation reactions followed pseudofirst-order kinetics with rate constants in the range of 1...
May 3, 2017: Water Research
https://www.readbyqxmd.com/read/28549272/acute-toxicity-of-emerging-atmospheric-pollutants-from-wood-lignin-due-to-biomass-burning
#7
Maryline Pflieger, Ana Kroflič
Guaiacol (2-methoxyphenol) is an important atmospheric pollutant. It is the major component of wood lignin and is essentially emitted to the atmosphere during biomass burning. Its aging in the tropospheric aqueous phase leads to the generation of the following ring-retaining transformation products, also during nighttime: 4-nitroguaiacol, 6-nitroguaiacol, and dinitroguaiacol. This study presents the first toxicological data of guaiacol and its nitro derivatives and reveals their harmful potential for the ecosystem...
May 15, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/28549265/facile-screening-of-potential-xenoestrogens-by-an-estrogen-receptor-based-reusable-optical-biosensor
#8
Lanhua Liu, Xiaohong Zhou, Yun Lu, Didi Shan, Bi Xu, Miao He, Hanchang Shi, Yi Qian
The apparent increase in hormone-induced cancers and disorders of the reproductive tract has led to a growing demand for new technologies capable of screening xenoestrogens. We reported an estrogen receptor (ER)-based reusable fiber biosensor for facile screening estrogenic compounds in environment. The bioassay is based on the competition of xenoestrogens with 17β-estradiol (E2) for binding to the recombinant receptor of human estrogen receptor α (hERα) protein, leaving E2 free to bind to fluorophore-labeled anti-E2 monoclonal antibody...
May 18, 2017: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/28549262/passive-sampling-of-wastewater-as-a-tool-for-the-long-term-monitoring-of-community-exposure-illicit-and-prescription-drug-trends-as-a-proof-of-concept
#9
J A Baz-Lomba, Christopher Harman, Malcolm Reid, Kevin V Thomas
A passive sampling device, the Polar Organic Chemical Integrative Sampler (POCIS), was calibrated in-situ over a 4-week period in Oslo (Norway) for 10 illicit drugs and pharmaceuticals with the goal of developing an approach for monitoring long-term wastewater drug loads. The calibrations were performed in triplicate using three different overlapping calibration sets under changing environmental conditions that allowed the uncertainty of the sampling rates to be evaluated. All 10 compounds exhibited linear uptake kinetics and provided sampling rates of between 0...
May 20, 2017: Water Research
https://www.readbyqxmd.com/read/28549213/binding-of-copper-and-cisplatin-to-atox1-is-mediated-by-glutathione-through-the-formation-of-metal-sulfur-clusters
#10
Nataliya V Dolgova, Corey Yu, John P Cvitkovic, Miroslav Hodak, Kurt Nienaber, Kelly Lynn Summers, Julien Cotelesage, Jerzy Bernholc, George A Kaminski, Ingrid J Pickering, Graham N George, Oleg Y Dmitriev
Copper is an essential nutrient required for many biological processes involved in primary metabolism, but free cop-per is toxic due to its ability to catalyze formation of free radicals. To prevent toxic effects, in the cell copper is bound to proteins and low molecular weight compounds, such as glutathione, at all times. The widely used chemotherapy agent cisplatin is known to bind to copper-transporting proteins, including copper chaperone Atox1. Cisplatin interac-tions with Atox1 and other copper transporters are linked to cancer resistance to platinum-based chemotherapy...
May 26, 2017: Biochemistry
https://www.readbyqxmd.com/read/28549212/synthesis-of-four-monoterpene-derived-organosulfates-and-their-quantification-in-atmospheric-aerosol-samples
#11
Yuchen Wang, Jingyun Ren, X H Hilda Huang, Rongbiao Tong, Jian Zhen Yu
Monoterpenes, a major class of biogenic volatile organic compounds, are known to produce oxidation products that further react with sulfate to form organosulfates. The accurate quantification of monoterpene-derived organosulfates (OSs) is necessary for quantifying this controllable aerosol source; however, it has been hampered by a lack of authentic standards. Here we report a unified synthesis strategy starting from the respective monoterpene through Upjohn dihydroxylation or Sharpless asymmetric dihydroxylation followed by mono-sulfation with sulfur trioxide-pyridine complex...
May 26, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28548971/allergic-contact-dermatitis-in-preservatives-current-standing-and-future-options
#12
Gustavo Deza, Ana M Giménez-Arnau
PURPOSE OF REVIEW: Preservatives are well known skin sensitizers and represent one of the main causes of contact allergy. The purpose of this article is to review the current state of contact sensitization induced by preservatives and point future alternatives for products' preservation. RECENT FINDINGS: Isothiazolinones currently are the most common preservatives responsible of contact allergy in Europe and in the United States, and although some regulatory interventions have been taken place, the current contact allergy outbreak is not yet under control...
May 25, 2017: Current Opinion in Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28548960/severe-hypertriglyceridemia-due-to-two-novel-loss-of-function-lipoprotein-lipase-gene-mutations-c310r-e396v-in-a-chinese-family-associated-with-recurrent-acute-pancreatitis
#13
Yu Lun, Xiaofang Sun, Ping Wang, Jingwei Chi, Xu Hou, Yangang Wang
Lipoprotein lipase (LPL) is widely expressed in skeletal muscles, cardiac muscles as well as adipose tissue and involved in the catabolism of triglyceride. Herein we have systematically characterized two novel loss-of-function mutations in LPL from a Chinese family in which afflicted members were manifested by severe hypertriglyceridemia and recurrent pancreatitis. DNA sequencing revealed that the proband was a heterozygote carrying a novel c.T928C (p.C310R) mutation in exon 6 of the LPL gene. Another member of the family was detected to be a compound heterozygote who along with the c...
May 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28548956/dalbinol-a-rotenoid-from-amorpha-fruticosa-l-exerts-anti-proliferative-activity-by-facilitating-%C3%AE-catenin-degradation-in-hepatocellular-carcinoma-cells
#14
Xiaohui Zhu, Xin Wu, Jing Cheng, Hongbo Liao, Xiaoqing Di, Lili Li, Rong Li, Yanfang Zhou, Xiangning Zhang
Hepatocellular carcinoma (HCC) is a highly malignant tumor, and the main cause of treatment failure is malignant proliferation. Aberrations in Wnt/β-catenin signaling are associated with HCC development. Despite the improvements in overall survival made over the past decade from the advent of molecularly targeted therapies, these treatments do not have efficacy in all patients with different pathogeneses. Therefore, there is a demand for novel chemotherapeutic agents for HCC. To this end, we built a natural compound library and screened out a rotenoid named dalbinol from the seeds of Amorpha fruticosa L...
May 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28548955/exploring-brusatol-as-a-new-anti-pancreatic-cancer-adjuvant-biological-evaluation-and-mechanistic-studies
#15
Zheng Lu, Zheng-Quan Lai, Albert W N Leung, Po Sing Leung, Zhao-Shen Li, Zhi-Xiu Lin
Pancreatic cancer is highly resistant to chemotherapeutic agents and is known to have a poor prognosis. The development of new therapeutic entities is badly needed for this deadly malignancy. In this study, we demonstrated for the first time that brusatol, a natural quassinoid isolated from a Chinese herbal medicine named Bruceae Fructus, possessed potent cytotoxic effect against different pancreatic adenocarcinoma cell lines. Its anti-pancreatic cancer effect was comparable to that of the first-line chemotherapeutic agents such as gemcitabine and 5-fluorouracil, with a more favorable safety profile...
May 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28548853/a-series-of-fluorescent-and-colorimetric-chemodosimeters-for-selective-recognition-of-cyanide-based-on-fret-mechanism
#16
Ying-Xi Hua, Yongliang Shao, Ya-Wen Wang, Yu Peng
A series of fluorescence "turn-on" probes (PY, AN, NA, B1 and B2) have been developed and successfully applied to detect cyanide anions based on Michael-addition reaction and FRET mechanism. These probes demonstrated good selectivity, high sensitivity and very fast recognition for CN-. Especially, the fluorescence response of probe NA finished within 3 seconds. Low LODs (down to 63 nM) are also obtained in these probes with remarkable fluorescence enhancement factors. In addition, fluorescence colors of these probes turned to blue, yellow or orange upon sensing CN-...
May 26, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28548851/celastrofurans-a-g-dihydro-%C3%AE-agarofurans-from-the-australian-rainforest-vine-celastrus-subspicata-and-their-inhibitory-effect-on-leucine-transport-in-prostate-cancer-cells
#17
Mario Wibowo, Qian Wang, Jeff Holst, Jonathan M White, Andreas Hofmann, Rohan A Davis
Seven new dihydro-β-agarofurans, celastrofurans A-G (1-7), along with two known secondary metabolites, 9β-benzoyloxy-1α-furoyloxydihydro-β-agarofuran (8) and (1R,2R,4R,5S,7R,9S,10R)-2-acetoxy-9-benzoyloxy-1-furoyloxydihydro-β-agarofuran (9), were obtained from the leaves of the Australian rainforest vine, Celastrus subspicata. The structures of the new compounds were determined by detailed spectroscopic (1D/2D NMR) and MS data analysis. The absolute configurations of compounds 1-4 were defined by ECD and single-crystal X-ray diffraction studies...
May 26, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28548850/highly-enantioselective-copper-and-iron-catalyzed-intramolecular-cyclopropanation-of-indoles
#18
Huan Xu, Li Yi-Pan, Yan Cai, Guo-Peng Wang, Shou-Fei Zhu, Qi-Lin Zhou
We report the first intramolecular enantioselective cyclopropa-nation of indoles, which was accomplished in good to high yield (up to 94%) with excellent enantioselectivity (up to >99.9% ee) by using copper or iron complexes of chiral spiro bisoxa-zolines as catalysts. This reaction is a straightforward, efficient method for constructing polycyclic compounds with an all-carbon quaternary chiral center at the 3-position of the indole skeleton, a core structure shared by numerous natural products and bioactive compounds...
May 26, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28548846/ambient-size-distributions-and-lung-deposition-of-aerosol-dithiothreitol-measured-oxidative-potential-a-contrast-between-soluble-and-insoluble-particles
#19
Ting Fang, Linghan Zeng, Dong Gao, Vishal Verma, Aleksandr B Stefaniak, Rodney J Weber
Ambient particulate matter (PM) may upset redox homeostasis leading to oxidative stress and adverse health effects. Size distributions of water-insoluble and water-soluble OP^DTT (dithiothreitol assay, measure of oxidative potential per air volume) are reported for a road-side and urban site. The average water-insoluble fractions were 23% and 51%, and 37% and 39% for fine and coarse mode at the road-side and urban site, respectively, measured during different periods. Water-soluble OP^DTT was unimodal peaked near 1-2...
May 26, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28548834/subtly-modulating-glycogen-synthase-kinase-3-%C3%AE-allosteric-inhibitors-development-and-their-potential-for-the-treatment-of-chronic-diseases
#20
Valle Palomo, Daniel I Pérez, Carlos Roca, Cara Anderson, Natalia Rodriguez-Muela, Concepción Pérez, Jose A Morales-Garcia, Julio A Reyes, Nuria E Campillo, Ana M Pérez-Castillo, Lee L Rubin, Lubov T Timchenko, Carmen Gil, Ana Martínez
Glycogen synthase kinase 3 β (GSK-3β) is a central target in several unmet diseases. To increase the specificity of GSK-3β inhibitors in chronic treatments we are developing small molecules allowing subtle modulation of GSK-3β activity. Design synthesis, structure-activity relationships and binding mode of quinoline-3-carbohydrazide derivatives as allosteric modulators of GSK-3β are here presented. Furthermore, we show how allosteric binders may overcome the β-catenin side effects associated to strong GSK-3β inhibition...
May 26, 2017: Journal of Medicinal Chemistry
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