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https://www.readbyqxmd.com/read/28646690/polycyclic-aromatic-hydrocarbons-in-the-water-spm-sediment-system-from-the-middle-reaches-of-huai-river-china-distribution-partitioning-origin-tracing-and-ecological-risk-assessment
#1
Jiamei Zhang, Guijian Liu, Rujing Wang, He Huang
The polycyclic aromatic hydrocarbons (PAHs) concentrations in the water, suspended particulate matter (SPM) and sediment from the middle reaches of Huai River were analyzed by a gas chromatograph-mass spectrometer (GC-MS). The mean concentrations for the sum of 16 PAHs (∑16 PAHs) in the water, SPM and sediment were 1204 ng/L, 3192 ng/g (dry weight; dw), and 7955 ng/g (dw), respectively. Along the vertical profiles of water columns, higher ∑16 PAHs levels were seen in surface and bottom water layers and co-located SPM...
June 21, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28646659/analysis-of-recombinant-monoclonal-antibodies-in-hydrophilic-interaction-chromatography-a-generic-method-development-approach
#2
Balázs Bobály, Valentina D'Atri, Alain Beck, Davy Guillarme, Szabolcs Fekete
Hydrophilic interaction liquid chromatography (HILIC) is a well-established technique for the separation and analysis of small polar compounds. A recently introduced widepore stationary phase expanded HILIC applications to larger molecules, such as therapeutic proteins. In this paper, we present some generic HILIC conditions adapted for a wide range of FDA and EMA approved recombinant monoclonal antibody (mAb) species and for an antibody-drug conjugate (ADC). Seven approved mAbs possessing various isoelectric point (pI) and hydrophobicity as well as a cysteine conjugated ADC were used in this study...
June 15, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28646621/the-hydrophobic-side-chain-of-oseltamivir-influences-type-a-subtype-selectivity-of-neuraminidase-inhibitors
#3
Xiong Lin, Chen Qin-Hua, Li Peng, Li Chun-Lei, Yang Guang-De
Neuraminidase, which plays a critical role in the influenza virus life cycle, is a target for new therapeutic agents. The study of structure-activity relationships revealed that the C-5 position amino group of oseltamivir was pointed to 150-cavity of the neuraminidase in group-1. This cavity is important for selectivity of inhibitors against N1 versus N2 NA. A serial of influenza neuraminidase inhibitors with the oseltavimir scaffold containing lipophilic side chains at the C-5 position have been synthesized and evaluated for their influenza neuraminidase inhibitory activity and selectivity...
June 24, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28646542/reconstitution-of-low-density-lipoproteins-with-fatty-acids-for-the-targeted-delivery-of-drugs-into-cancer-cells
#4
Chunlei Zhu, Pallab Pradhan, Da Huo, Jiajia Xue, Song Shen, Krishnendu Roy, Younan Xia
Low-density lipoproteins (LDLs) represent a novel class of nanocarriers for the targeted delivery of therapeutics into aberrant cells that overexpress the LDL receptor. Here we report a facile procedure for reconstituting the hydrophobic core of LDLs with a binary fatty acid mixture. Facilitated by the tumor targeting capability of the apolipoprotein, the reconstituted, drug-loaded LDLs can effectively target cancer cells that overexpress the LDL receptor while showing minor adverse impact on normal fibroblasts...
June 24, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28646511/control-of-autoimmune-inflammation-using-liposomes-to-deliver-positive-allosteric-modulators-of-metabotropic-glutamate-receptors
#5
Joshua M Gammon, Arjun R Adapa, Christopher M Jewell
Multiple sclerosis (MS) is an autoimmune disease where myelin is incorrectly recognized as foreign and attacked by the adaptive immune system. Dendritic cells (DCs) direct adaptive immunity by presenting antigens to T cells, therefore serving as a target for autoimmune therapies. N-Phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide (PHCCC), a positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4), can promote regulatory T cells by altering cytokine secretion to bias T cell differentiation...
June 24, 2017: Journal of Biomedical Materials Research. Part A
https://www.readbyqxmd.com/read/28646405/revealing-the-importance-of-linkers-in-k-series-oxime-reactivators-for-tabun-inhibited-ache-using-quantum-chemical-docking-and-smd-studies
#6
Shibaji Ghosh, Nellore Bhanu Chandar, Kalyanashis Jana, Bishwajit Ganguly
Inhibition of acetylcholinesterase (AChE) with organophosphorus compounds has a detrimental effect on human life. Oxime K203 seems to be one of the promising reactivators for tabun-inhibited AChE than (K027, K127, and K628). These reactivators differ only in the linker units between the two pyridinium rings. The conformational analyses performed with quantum chemical RHF/6-31G* level for K027, K127, K203 and K628 showed that the minimum energy conformers have different orientations of the active and peripheral pyridinium rings for these reactivator molecules...
June 23, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28646179/herbal-medicine-yinchenhaotang-protects-against-%C3%AE-naphthylisothiocyanate-induced-cholestasis-in-rats
#7
Jingyu Yan, Guoxiang Xie, Chungeng Liang, Yiyang Hu, Aihua Zhao, Fengjie Huang, Ping Hu, Ping Liu, Wei Jia, Xiaoning Wang
Cholestasis is a clinical disorder defined as an impairment of bile flow, and that leads to toxic bile acid (BA) accumulation in hepatocytes. Here, we investigated the hepatoprotective effect of Yinchenhaotang (YCHT), a well-known formulae for the treatment of jaundice and liver disorders, against the cholestasis using the α-naphthylisothiocyanate (ANIT)-induced cholestasis in male Wistar rats. ANIT feeding induced significant cholestasis with substantially increased intrahepatic retention of hydrophobic BAs...
June 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28645658/spacer-structure-and-hydrophobicity-influences-transfection-activity-of-novel-polycationic-gemini-amphiphiles
#8
Pavel A Puchkov, Irina A Kartashova, Elena V Shmendel, Anastasya S Luneva, Nina G Morozova, Marina A Zenkova, Mikhail A Maslov
Three novel polycationic gemini amphiphiles with different spacers were developed and evaluated in terms of their physiochemical properties and transfection efficiencies. Cationic liposomes formed by these amphiphiles and the helper lipid DOPE were able to successfully condense DNA, as shown by gel mobility shift and ethidium bromide intercalation assays. Transfection activity of the liposomes was superior to Lipofectamine(®) 2000 and was dependent on spacer structure, hydrophobicity, and nucleic acid type (pDNA or siRNA)...
June 10, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28645623/identification-of-a-coumarin-based-antihistamine-as-an-anti-filoviral-entry-inhibitor
#9
Han Cheng, Adam Schafer, Veronica Soloveva, Dima Gharaibeh, Tara Kenny, Cary Retterer, Rouzbeh Zamani, Sina Bavari, Norton P Peet, Lijun Rong
Filoviruses, consisting of Ebola virus, Marburg virus and Cuevavirus, cause severe hemorrhagic fevers in humans with high mortality rates up to 90%. Currently, there is no approved vaccine or therapy available for the prevention and treatment of filovirus infection in humans. The recent 2013-2015 West African Ebola epidemic underscores the urgency to develop antiviral therapeutics against these infectious diseases. Our previous study showed that GPCR antagonists, particularly histamine receptor antagonists (antihistamines) inhibit Ebola and Marburg virus entry...
June 20, 2017: Antiviral Research
https://www.readbyqxmd.com/read/28645045/hydra-amphiphiles-using-three-heads-and-one-tail-to-influence-aggregate-formation-and-to-kill-pathogenic-bacteria
#10
Tara M Gallagher, John N Marafino, Brenden K Wimbish, Brandi Volkers, Gabriel Fitzgerald, Kristin McKenna, Jason Floyd, Nicholas T Minahan, Brenna Walsh, Kirstie Thompson, David Bruno, Monica Paneru, Sybelle Djikeng, Stephanie Masters, Suma Haji, Kyle Seifert, Kevin L Caran
Hydra amphiphiles mimic the morphology of the mythical multi-headed creatures for which they are named. Likewise, when faced with a pathogenic bacterium, some hydra derivatives are as destructive as their fabled counterparts were to their adversaries. This report focuses on eight new tricephalic (triple-headed), single-tailed amphiphiles. Each amphiphile has a mesitylene (1,3,5-trimethylbenzene) core, two benzylic trimethylammonium groups and one dimethylalkylammonium group with a linear hydrophobe ranging from short (C8H17) to ultralong (C22H45)...
June 10, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28644555/a-self-assembled-trigonal-prismatic-molecular-vessel-for-catalytic-dehydration-reactions-in-water
#11
Partha Sarathi Mukherjee, Paramita Das, Atul Kumar, Prodip Howlader
A water-soluble Pd6 trigonal prism (A) was synthesized by two-component coordination-driven self-assembly of a Pd(II) 90° acceptor with a tetraimidazole donor. As the walls of the prism are constructed by three conjugated aromatic building blocks, the confined pocket of the prism is hydrophobic. In addition to the hydrophobic cavity, large product egress windows make A an ideal molecular vessel to catalyze otherwise challenging pseudo multicomponent dehydration reactions in its confined nanospace in aqueous medium...
June 23, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28644514/polylutidines-multifunctional-surfaces-via-vapor-based-polymerization-of-substituted-pyridinophanes
#12
Joerg Lahann, Florence Bally-Le Gall, Christoph Hussal, Joshua Kramer, Kenneth Chang, Ramya Kumar, Vanessa Trouillet, Martin Nieger, Stefan Braese, Thomas Eyster, Amy Baek
We report a new class of functionalized polylutidine polymers that are prepared via chemical vapor deposition polymerization of substituted [2](1,4)benzeno[2](2,5)pyridinophanes. To prepare sufficient monomer for CVD polymerization, a new synthesis route for ethynylpyridinophane has been developed in three steps with an overall yield of 59%. Subsequent CVD polymerization yielded well-defined films of poly(2,5-lutidinylene-co-p-xylylene) and poly(4-ethynyl-2,5-lutidinylene-co-p-xylylene). All polymers were characterized by IRRAS, ellipsometry, contact angle and XPS...
June 23, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28644501/stabilizing-amyloid-%C3%AE-peptide-by-the-n-terminus-capture-is-capable-of-preventing-and-eliminating-amyloid-%C3%AE-oligomers
#13
Gesi Wen, Daoyuan Chen, Wenjing Qin, Binhua Zhou, Youqiao Wang, Ziyi Liu, Jun Du, Qiang Zhou, Junmin Quan, Xianzhang Bu
Elimination of amyloid-β (Aβ) oligomers remains challenging. We describe here a novel strategy to prevent and eliminate the Aβ oligomers from either the early aggregation or the fibril dissolution pathway by targeting the flexible N-terminus, but not the widely investigated hydrophobic segment, with a rationally designed cyclopeptide.
June 23, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28644385/ch-%C3%AF-interactions-in-carbohydrate-recognition
#14
REVIEW
Vojtěch Spiwok
Many carbohydrate-binding proteins contain aromatic amino acid residues in their binding sites. These residues interact with carbohydrates in a stacking geometry via CH/π interactions. These interactions can be found in carbohydrate-binding proteins, including lectins, enzymes and carbohydrate transporters. Besides this, many non-protein aromatic molecules (natural as well as artificial) can bind saccharides using these interactions. Recent computational and experimental studies have shown that carbohydrate-aromatic CH/π interactions are dispersion interactions, tuned by electrostatics and partially stabilized by a hydrophobic effect in solvated systems...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644051/brief-overview-of-nanoparticulate-therapy-in-cancer
#15
Rajesh R Wakaskar
Nanoparticles govern an all-important role, in this day and age, in determining the tissue distribution of either hydrophobic or hydrophilic anti-cancer drugs by encapsulating them or by covalent attachment. The whole purpose is to systematically improve upon the existing anti-tumor efficacy of these drugs. Selective delivery of these chemotherapeutic agents to the compromised or diseased tissue is the key to avoid any potential toxicity problems. Certain types of nanoparticles, through various mechanisms such as active targeting or reversing multi-drug resistance, display immense potential in adding to the existing anti-tumor efficacy profile...
June 23, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/28643710/postoperative-posterior-capsular-striae-and-the-posterior-capsular-opacification-in-patients-implanted-with-two-types-of-intraocular-lens-material
#16
Rajesh Subhash Joshi
AIM: To evaluate the incidence of postoperative posterior capsular striae (PCS) and its influence on posterior capsular opacification (PCO) in patients implanted with two types of lens material. SETTING: Tertiary eye care center in central rural India. STUDY DESIGN: A prospective, observational, nonrandomized study. MATERIALS AND METHODS: The study included 1247 patients having age-related cataract scheduled for removal by phacoemulsification technique and implantation of hydrophilic or hydrophobic intraocular lens (IOL)...
June 2017: Indian Journal of Ophthalmology
https://www.readbyqxmd.com/read/28643379/tuning-the-inter-nanofibril-interaction-to-regulate-the-morphology-and-function-of-peptide-dna-co-assembled-viral-mimics
#17
Rong Ni, Ying Chau
The ability to tune the inter-subunit interaction within the virus capsid may be critical to assembly and biological function. This process has been extended here with peptide/DNA co-assembled viral mimics. The resulting co-assemblies, formed and stabilized by both DNA-peptide nanofibril and peptide nanofibril-nanofibril interactions, have been tuned through hydrophobic packing interactions of the peptide sequences. By strengthening peptide side chain complementarity and/or elongating the peptide chain (from 4 to 8 residues), we report strengthening the inter-nanofibril interaction to create stable nanococoons with high gene transfection efficacy...
June 22, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28643367/facile-one-pot-synthesis-of-functional-giant-polymeric-vesicles-controlled-by-oscillatory-chemistry
#18
Bishnu Bastakoti, Juan Perez-Mercader
We introduce a novel application of an oscillatory chemical reaction to the synthesis of block copolymers. The Belousov-Zhabotinsky (B-Z) reaction is coupled with the polymerization of an amphiphilic block copolymer. Radicals generated in the B-Z reaction initiate the polymerization between a polyethylene glycol (PEG) macro reversible addition-fragmentation chain transfer agent and butyl acrylate monomers. The growth of the hydrophobic block on PEG undergoes self-assembly to form spherical micelles. The nanoscale micelles transform into submicron vesicles and grow to giant vesicles as a consequence of the oscillatory behavior of the B-Z reaction...
June 22, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28642943/aqueous-dispersions-of-nanostructures-formed-through-the-self-assembly-of-iminolipids-with-exchangeable-hydrophobic-termini
#19
Wen Li, Daryl McManus, Han Liu, Cinzia Casiraghi, Simon J Webb
The addition of amines to an aldehyde surfactant, which was designed to be analogous to didodecyldimethylammonium bromide, gave exchangeable "iminolipids" that self-assembled to give stable aqueous dispersions of nano-sized vesicles. For example, sonication of suspensions of the n-hexylamine-derived iminolipid gave vesicles 50 to 200 nm in diameter that could encapsulate a water-soluble dye. The iminolipids could undergo dynamic exchange with added amines, and the resulting equilibrium constants (Krel) were quantified by (1)H NMR spectroscopy...
June 23, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28642787/mutational-signatures-are-critical-for-proper-estimation-of-purifying-selection-pressures-in-cancer-somatic-mutation-data-when-using-the-dn-ds-metric
#20
Jimmy Van den Eynden, Erik Larsson
Large cancer genome sequencing initiatives have led to the identification of cancer driver genes based on signals of positive selection in somatic mutation data. Additionally, the identification of purifying (negative) selection has the potential to identify essential genes that may be of therapeutic interest. The most widely used way of quantifying selection pressures in protein-coding genes is the dN/dS metric, which compares non-synonymous to synonymous substitution rates. In this study, we examine whether and how this metric is influenced by the mutational processes that have been active during tumor evolution...
2017: Frontiers in Genetics
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