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https://www.readbyqxmd.com/read/28334528/why-prodrugs-and-propesticides-succeed
#1
John E Casida
What are the advantages of bioactivation in optimizing drugs and pesticides? Why are there so many prodrugs and propesticides? These questions are examined here by considering compounds selected on the basis of economic value or market success. The 100 major drugs and 90 major pesticides are divided into ones acting directly and those definitely or possibly requiring bioactivation. Established or candidate prodrugs accounted for 19% of the total drug sales with corresponding values of 20, 37 and 17% for proinsecticides, proherbicides and profungicides...
March 23, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28304351/the-preparation-and-identification-of-a-monoclonal-antibody-against-citrinin-and-the-development-of-detection-via-indirect-competitive-elisa
#2
Shimuye Kalayu Yirga, Sumei Ling, Yanling Yang, Jun Yuan, Shihua Wang
Citrinin (CTN) is a hepato-nephrotoxic mycotoxin produced by fungi genera of Aspergillus, Monauscus, and Penicillium. CTN contaminates grains, fruits, juices and vegetables, and causes various toxic effects to humans and animals. It has small molecular weight, which is non-immunogenic to animals. Thus, CTN was conjugated to bovine serum albumin (BSA) and ovalbumin (OVA), respectively, by amide bonds using 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) and N-hydroxysuccinimide (NHS). Mice were immunized with CTN-BSA conjugates, and spleen cells of the immunized mice were fused with Sp2/0 myeloma cells to obtain 21H27 hybriodoma cell...
March 17, 2017: Toxins
https://www.readbyqxmd.com/read/28289994/determination-of-rhodamine-b-in-food-samples-by-fe3o4-ionic-liquids-%C3%AE-cyclodextrin-cross-linked-polymer-solid-phase-extraction-coupled-with-fluorescence-spectrophotometry
#3
Almojtaba AbdAlkhalig Ahmed Bakheet, Xia Shi Zhu
Fe3O4@Ionic liquids β-cyclodextrin polymer(Fe3O4@ mono-6- deoxy-6- (1-ethyl- imidazolium)-β-cyclodextrin iodide polymer, ILs-β-CDCP) was prepared. A novel method based on Fe3O4@ILs-β-CDCP solid phase extraction coupled with fluorescence spectrophotometry for Rhodamine B (RhB) determination, was investigated. Results were shown that RhB was adsorbed on Fe3O4@ILs-β-CDCP and eluted with sodium dodecyl sulfate (SDS) (1.0%) rapidly. Different parameters, such as pH, adsorption time and volume, eluent volume and time were studied...
March 13, 2017: Journal of Fluorescence
https://www.readbyqxmd.com/read/28272346/a-greener-quick-and-comprehensive-extraction-approach-for-lc-ms-of-multiple-mycotoxins
#4
Andreas Breidbach
In food/feed control, mycotoxin analysis is often still performed "one analyte at a time". Here a method is presented which aims at making mycotoxin analysis environmentally friendlier through replacing acetonitrile by ethyl acetate and reducing chemical waste production by analyzing four mycotoxins together, forgoing sample extract clean-up, and minimizing solvent consumption. For this, 2 g of test material were suspended in 8 mL water and 16 mL ethyl acetate were added. Extraction was accelerated through sonication for 30 min and subsequent addition of 8 g sodium sulfate...
March 7, 2017: Toxins
https://www.readbyqxmd.com/read/28242546/characterization-and-evaluation-of-bioactive-polyphenolic-constituents-from-zanthoxylum-armatum-dc-a-traditionally-used-plant
#5
Zulfa Nooreen, Shilpi Singh, Dhananjay Kumar Singh, Sudeep Tandon, Ateeque Ahmad, Suaib Luqman
Zanthoxylum armatum or Timoor has been used in different traditional system of medicine due to its aromatic properties and also in the treatment of cancer, diarrhea and cholera. In the present investigation, four chemically distinct compounds namely Tambulin (6), Prudomestin (7), Ombuin (8) and 3, 4, 5, 3', 4', 5'-hexahydroxydiphenyl ether (9) have been isolated and quantified from the fruits. To explore the biological activities, we have further studied the antiproliferative, antimicrobial and antioxidant efficacy...
February 24, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28167367/large-scale-synthesis-and-regioselective-protection-schemes-of-ethyl-2-azido-2-deoxy-1-thio-%C3%AE-d-cellobioside-for-preparation-of-heparin-thiodisaccharide-building-blocks
#6
Kevin Sheerin, Lorenzo Guazzelli, Stefan Oscarson
Crystalline acetylated ethyl 2-azido-2-deoxy-1-thio-α-d-cellobioside has been prepared on a multigram scale from cellobiose in an overall yield of 23% with no chromatography required and converted after deacetylation into the 4',6'-O-benzylidene and 4',6'-O-benzylidene-6-O-TBDMS protected derivatives. Applying a number of regioselective benzylation methods on these gave access to a variety of regioselectively protected derivatives, both mono-ols (2'- and 3-OH), diols (2',6-, 2',3-, and 3,6-di-OH), and triols (2',3,6- and 2',3',3-tri-OH)...
February 22, 2017: Carbohydrate Research
https://www.readbyqxmd.com/read/28152658/lc-ms-identification-and-preparative-hplc-isolation-of-frankenia-pulverulenta-phenolics-with-antioxidant-and-neuroprotective-capacities-in-pc12-cell-line
#7
Rim Ben Mansour, Megdiche Ksouri Wided, Stéphanie Cluzet, Stéphanie Krisa, Tristan Richard, Riadh Ksouri
CONTEXT: Frankenia pulverulenta L. (Frankeniaceae) is a medicinal species with carminative, analgesic and antiviral properties. However, phytochemical investigations, antioxidant and neuroprotective capacities of this plant remain unclear. OBJECTIVE: This work assesses the phenolic composition of F. pulverulenta shoot and root and evaluates their antioxidant and neuroprotective capacities. MATERIALS AND METHODS: Successive fractionation of F...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28137860/creatine-maintains-intestinal-homeostasis-and-protects-against-colitis
#8
Emre Turer, William McAlpine, Kuan-Wen Wang, Tianshi Lu, Xiaohong Li, Miao Tang, Xiaoming Zhan, Tao Wang, Xiaowei Zhan, Chun-Hui Bu, Anne R Murray, Bruce Beutler
Creatine, a nitrogenous organic acid, replenishes cytoplasmic ATP at the expense of mitochondrial ATP via the phosphocreatine shuttle. Creatine levels are maintained by diet and endogenous synthesis from arginine and glycine. Glycine amidinotransferase (GATM) catalyzes the rate-limiting step of creatine biosynthesis: the transfer of an amidino group from arginine to glycine to form ornithine and guanidinoacetate. We screened 36,530 third-generation germline mutant mice derived from N-ethyl-N-nitrosourea-mutagenized grandsires for intestinal homeostasis abnormalities after oral administration of dextran sodium sulfate (DSS)...
February 14, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28132972/a-new-desorption-method-for-removing-organic-solvents-from-activated-carbon-using-surfactant
#9
Mitsuo Hinoue, Sumiyo Ishimatsu, Yukiko Fueta, Hajime Hori
OBJECTIVES: A new desorption method was investigated, which does not require toxic organic solvents. Efficient desorption of organic solvents from activated carbon was achieved with an ananionic surfactant solution, focusing on its washing and emulsion action. METHODS: Isopropyl alcohol (IPA) and methyl ethyl ketone (MEK) were used as test solvents. Lauryl benzene sulfonic acid sodium salt (LAS) and sodium dodecyl sulfate (SDS) were used as the surfactant. Activated carbon (100 mg) was placed in a vial and a predetermined amount of organic solvent was added...
January 28, 2017: Journal of Occupational Health
https://www.readbyqxmd.com/read/28130892/development-and-validation-of-an-hplc-method-for-determination-of-thiamethoxam-and-its-metabolites-in-cotton-leaves-and-soil
#10
Gagan Jyot, Balwinder Singh
An easy and simple analytical method was standardized and validated for the estimation of residues of thiamethoxam andits metabolites in cotton. The samples were extracted with acetonitrile, water, and methanol; diluted with brine solution; partitioned into dichloromethane and ethyl acetate; dried over anhydrous sodium sulfate; and cleaned up by glass column chromatography. Final clear extracts were concentrated under vacuum and reconstituted into HPLC grade acetonitrile, and residues were estimated using an HPLC instrument equipped with a C<sub>18</sub> column and photodiode array detector system...
January 28, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28098942/biomarkers-for-the-detection-of-prenatal-alcohol-exposure-a-review
#11
REVIEW
Heidi Bager, Lars Porskjaer Christensen, Steffen Husby, Lene Bjerregaard
Alcohol exposure during pregnancy can cause adverse effects to the fetus, because it interferes with fetal development, leading to later physical and mental impairment. The most common clinical tool to determine fetal alcohol exposure is maternal self-reporting. However, a more objective and useful method is based on the use of biomarkers in biological specimens alone or in combination with maternal self-reporting. This review reports on clinically relevant biomarkers for detection of prenatal alcohol exposure (PAE)...
February 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/28079919/copper-oxide-nanoparticles-and-copper-sulphate-act-as-antigenotoxic-agents-in-drosophila-melanogaster
#12
Mohamed Alaraby, Alba Hernández, Ricard Marcos
The biological reactivity of metal and metal oxide nanomaterials is attributed to their redox properties, which would explain their pro- or anti-cancer properties depending on exposure circumstances. In this sense, copper oxide nanoparticles (CuONP) have been proposed as a potential anti-tumoral agent. The aim of this study was to assess if CuONP can exert antigenotoxic effects using Drosophila melanogaster as an in vivo model. Genotoxicity was induced by two well-known genotoxic compounds, namely potassium dichromate (PD) and ethyl methanesulfonate (EMS)...
January 12, 2017: Environmental and Molecular Mutagenesis
https://www.readbyqxmd.com/read/28069244/ultrasonic-irradiation-assisted-synthesis-of-bi2s3-nanoparticles-in-aqueous-ionic-liquid-at-ambient-condition
#13
Salomé M de la Parra-Arciniega, Nora A Garcia-Gomez, Lorena L Garza-Tovar, Domingo I García-Gutiérrez, Eduardo M Sánchez
In this work, an easy, fast and environmentally friendly method to obtain Bi2S3 nanostructures with sphere-like morphology is introduced. The promising material was successfully synthesized by a sonochemical route in 20% 1-ethyl-3-methylimidazolium ethyl sulfate [EMIM][EtSO4] ionic liquid solution (IL). Morphological studies by electron microscopy (SEM and TEM) show that the use of IL in the synthesis of Bi2S3 favors the formation of nanocrystals non-agglomerated. Micro Raman and energy dispersive X-ray spectroscopy (EDXS) were used to determine the composition and purity of the synthesized material...
May 2017: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/27995334/strategies-on-process-engineering-of-chondrocyte-culture-for-cartilage-tissue-regeneration
#14
Sarada Prasanna Mallick, Amit Rastogi, Satyavrat Tripathi, Pradeep Srivastava
The current work is an attempt to study the strategies for cartilage tissue regeneration using porous scaffold in wavy walled airlift bioreactor (ALBR). Novel chitosan, poly (L-lactide) and hyaluronic acid based composite scaffold were prepared. The scaffolds were cross-linked with 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide, N-hydroxysuccinimide and chondroitin sulfate to obtain interconnected 3D microstructure showing excellent biocompatibility, higher cellular differentiation and increased stability. The surface morphology and porosity of the scaffolds were analyzed using scanning electron microscopy (SEM) and mercury intrusion porosimeter and optimized for chondrocyte regeneration...
April 2017: Bioprocess and Biosystems Engineering
https://www.readbyqxmd.com/read/27976726/increased-levels-of-the-oxidative-stress-biomarker-8-iso-prostaglandin-f2%C3%AE-in-wastewater-associated-with-tobacco-use
#15
Yeonsuk Ryu, Emma Gracia-Lor, Richard Bade, J A Baz-Lomba, Jørgen G Bramness, Sara Castiglioni, Erika Castrignanò, Ana Causanilles, Adrian Covaci, Pim de Voogt, Felix Hernandez, Barbara Kasprzyk-Hordern, Juliet Kinyua, Ann-Kathrin McCall, Christoph Ort, Benedek G Plósz, Pedram Ramin, Nikolaos I Rousis, Malcolm J Reid, Kevin V Thomas
Wastewater analysis has been demonstrated to be a complementary approach for assessing the overall patterns of drug use by a population while the full potential of wastewater-based epidemiology has yet to be explored. F2-isoprostanes are a prototype wastewater biomarker to study the cumulative oxidative stress at a community level. In this work, 8-iso-prostaglandin F2α (8-iso-PGF2α) was analysed in raw 24 h-composite wastewater samples collected from 4 Norwegian and 7 other European cities in 2014 and 2015...
December 15, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27939663/heat-activated-persulfate-oxidation-of-methyl-and-ethyl-parabens-effect-kinetics-and-mechanism
#16
Yiqun Chen, Pinya Deng, Pengchao Xie, Ran Shang, Zongping Wang, Songlin Wang
We evaluated the degradation of methylparaben (MeP) and ethylparaben (EtP), two representative parabens, using the heat-activated persulfate system in a laboratory. Both sulfate and hydroxyl radicals contributed to the removal of the two parabens. The degradations of both MeP and EtP were improved by increasing the heating temperature or persulfate dose in accordance with a pseudo-first-order reaction model. The oxidation efficiency of parabens was found to be pH-dependent; decreasing in the order pH 5.0 > 7...
February 2017: Chemosphere
https://www.readbyqxmd.com/read/27884121/prevalence-and-risk-factors-of-intestinal-protozoan-infections-a-population-based-study-in-rural-areas-of-boyer-ahmad-district-southwestern-iran
#17
Bahador Sarkari, Ghasem Hosseini, Mohammad Hossein Motazedian, Mohammad Fararouei, Abdolali Moshfe
BACKGROUND: Parasitic infections are still a significant health problem in rural areas in developing countries including Iran. There is no recent population-based data about the prevalence of human intestinal parasites in most rural areas of Iran. The current study aimed to determine the prevalence of intestinal protozoan infection in inhabitants of rural areas of Boyer-Ahmad district, Southwestern Iran. METHODS: A total of 1025 stool samples were collected from the inhabitant of 50 randomly selected villages in Boyer-Ahmad Township...
November 25, 2016: BMC Infectious Diseases
https://www.readbyqxmd.com/read/27882327/migration-of-btex-and-biodegradation-in-shallow-underground-water-through-fuel-leak-simulation
#18
Yaping Cheng, Yudao Chen, Yaping Jiang, Lingzhi Jiang, Liqun Sun, Liuyue Li, Junyu Huang
To provide more reasonable references for remedying underground water, fuel leak was simulated by establishing an experimental model of a porous-aquifer sand tank with the same size as that of the actual tank and by monitoring the underground water. In the tank, traditional gasoline and ethyl alcohol gasoline were poured. This study was conducted to achieve better understanding of the migration and distribution of benzene, toluene, ethyl benzene, and xylene (BTEX), which are major pollutants in the underground water...
2016: BioMed Research International
https://www.readbyqxmd.com/read/27828553/simulations-of-the-water-exchange-dynamics-of-lanthanide-ions-in-1-ethyl-3-methylimidazolium-ethyl-sulfate-emim-etso4-and-water
#19
Yi-Jung Tu, Matthew J Allen, G Andrés Cisneros
The dynamics of ligand exchange on lanthanide ions is important for catalysis and organic reactions. Recent (17)O-NMR experiments have shown that water-exchange rates of lanthanide ions in water/1-ethyl-3-methylimidazolium ethyl sulfate (water/[EMIm][EtSO4]) increase as a function of increasing charge density. The trend of water-exchange rates in this solvent is opposite to that observed in water. Since the lanthanide ions and ionic liquids investigated in that work were highly charged, an advanced polarizable potential is desirable for accurate simulations...
November 9, 2016: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/27808452/spectroscopic-insight-into-the-interaction-of-bovine-serum-albumin-with-imidazolium-based-ionic-liquids-in-aqueous-solution
#20
Lakkoji Satish, Sabera Millan, Harekrushna Sahoo
The study of protein-ionic liquid interactions is very important because of the widespread use of ionic liquids as protein stabilizer in the recent years. In this work, the interaction of bovine serum albumin (BSA) with different imidazolium-based ionic liquids (ILs) such as [1-ethyl-3-methyl-imidazolium ethyl sulfate (EmimESO4 ), 1-ethyl-3-methyl-imidazolium chloride (EmimCl) and 1-butyl-3-methyl-imidazolium chloride (BmimCl)] has been investigated using different spectroscopic techniques. The intrinsic fluorescence of BSA is quenched by ILs by the dynamic mechanism...
November 3, 2016: Luminescence: the Journal of Biological and Chemical Luminescence
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