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Kristen Healy
The goal of this study was to evaluate the use of stable isotope labeled compounds to better understand factors influencing energy turnover in larval Culex quinquefasciatus (Say; Diptera: Culicidae). Three isotope labeled compounds were evaluated in this study, including 15N-labeled potassium nitrate, 13C-labeled glucose, and 13C-labeled leucine. Conditions were first optimized in the laboratory to determine the most appropriate concentration of isotope, as well as the half-life of enrichment. Once optimum conditions were established we used standard equations to predict and determine temperature and density-dependent energy turnover rates...
March 14, 2018: Journal of Medical Entomology
Deepak Reddy Gade, Amareswararao Makkapati, Rajesh Babu Yarlagadda, Godefridus J Peters, B S Sastry, V V S Rajendra Prasad
Overexpression of P-glycoprotein (P-gp) leads to the emergence of multidrug resistance (MDR) in cancer treatment. Acridones have the potential to reverse MDR and sensitize cells. In the present study, we aimed to elucidate the chemosensitization potential of acridones by employing various molecular modelling techniques. Pharmacophore modeling was performed for the dataset of chemosensitizing acridones earlier proved for cytotoxic activity against MCF7 breast cancer cell line. Gaussian-based QSAR studies also performed to predict the favored and disfavored region of the acridone molecules...
February 24, 2018: Computational Biology and Chemistry
Cassandra Rauert, Mahiba Shoieb, Jasmin K Schuster, Anita Eng, Tom Harner
Poly- and per-fluoroalkyl substances (PFAS) and volatile methyl siloxanes (VMS) were monitored at 21 sites in the Global Atmospheric Passive Sampling (GAPS) Network. Atmospheric concentrations previously reported from 2009 were compared to concentrations measured at these sites in 2013 and 2015, to assess trends over 7 years of monitoring. Concentrations of the fluorotelomer alcohols (FTOHs) and fluorinated sulfonamides and sulfonamidoethanols (FOSAs and FOSEs) were stable at these sites from 2009 to 2015 with no significant difference (p > 0...
March 13, 2018: Environmental Pollution
Masafumi Yoshinaga, Hiromasa Ninomiya, M M Aeorangajeb Al Hossain, Makoto Sudo, Anwarul Azim Akhand, Nazmul Ahsan, Md Abdul Alim, Md Khalequzzaman, Machiko Iida, Ichiro Yajima, Nobutaka Ohgami, Masashi Kato
Chromium (Cr) pollution caused by wastewater from tanneries is a worldwide environmental problem. To develop a countermeasure, we performed a comprehensive study using Hazaribagh, the tannery area in Dhaka City, Bangladesh, as a model. Our environmental monitoring indicated that the soluble form of Cr, but not barium or arsenic, in Buriganga River is derived from Hazaribagh. Our chemical analysis next showed that Cr, the primary pollutant in canal water at Hazaribagh, consisted of ≤0.7 μM hexavalent Cr [Cr(VI)] and ≤1705 μM trivalent Cr [Cr(III)]...
March 5, 2018: Chemosphere
Gregory D Bowden, Kirkwood M Land, Roberta M O'Connor, Heather M Fritz
The apicomplexan parasite Sarcocystis neurona is the primary etiologic agent of equine protozoal myeloencephalitis (EPM), a serious neurologic disease of horses. Many horses in the U.S. are at risk of developing EPM; approximately 50% of all horses in the U.S. have been exposed to S. neurona and treatments for EPM are 60-70% effective. Advancement of treatment requires new technology to identify new drugs for EPM. To address this critical need, we developed, validated, and implemented a high-throughput screen to test 725 FDA-approved compounds from the NIH clinical collections library for anti-S...
February 16, 2018: International Journal for Parasitology, Drugs and Drug Resistance
Claudia Bello, Jianfei Bai, Bartosz K Zambron, Pilar Elías-Rodríguez, Consuelo Gajate, Inmaculada Robina, Irene Caffa, Michele Cea, Fabrizio Montecucco, Alessio Nencioni, Aimable Nahimana, Dominique Aubry, Caroline Breton, Michel A Duchosal, Faustino Mollinedo, Pierre Vogel
We have synthesized a wide array of structurally related amphiphilic compounds, containing a functionalized pyrrolidine polar group coupled to different ether-linked hydrocarbon chains, to generate novel structures with antitumor activity. These newly synthesized amphiphilic pyrrolidine-derived compounds were classified in three different sub-libraries regarding the number of hydroxyl groups substituting the pyrrolidine moiety at C3 and C4. Pyrrolidine compounds with one or none hydroxyl groups showed a potent cell killing activity against pancreatic cancer cells, but they lacked selectivity for tumor cells...
March 2, 2018: European Journal of Medicinal Chemistry
Silvia Salerno, Aída Nelly García-Argáez, Elisabetta Barresi, Sabrina Taliani, Francesca Simorini, Concettina La Motta, Giorgio Amendola, Stefano Tomassi, Sandro Cosconati, Ettore Novellino, Federico Da Settimo, Anna Maria Marini, Lisa Dalla Via
Inhibition of angiogenesis via blocking vascular endothelial growth factor receptor (VEGFR) signaling pathway emerged as an established approach in anticancer therapy. So far, many monoclonal antibodies and ATP-competitive small molecule inhibitors have been clinically validated and approved. In this study, structure-activity relationships (SAR) within the 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidine class of kinase inhibitors were further refined by the synthesis and biological evaluation of new compounds 1-21 featuring different substitution patterns on the pendant phenyl moiety, combined with H, OCH3 , or Cl at 8-position...
March 7, 2018: European Journal of Medicinal Chemistry
Asmaa E Kassab, Ehab M Gedawy
As we are interested in synthetizing biologically active leads with dual anticancer and antibacterial activity, we adopted biology oriented drug synthesis (BIODS) strategy to synthesize a series of novel ciprofloxacin (CP) hybrids. The National Cancer Institute (USA) selected seventeen newly synthesized compounds for anticancer evaluation against 59 different human tumor cell lines. Five compounds 3e, 3f, 3h, 3o and 3p were further studied through determination of IC50 values against the most sensitive cancer cell lines...
March 9, 2018: European Journal of Medicinal Chemistry
M Kulik, D Kołodyńska, A Bayramov, A Drozdziel, A Olejniczak, J Żuk
The surfaces of (100) GaAs were irradiated with In+ ions. The implanted samples were isobaric annealed at 800°C and then of dielectric function, the surface atomic concentrations of atoms and also the chemical composition of the near surface layers in these implanted semiconductor samples were obtained. The following investigation methods were used: spectroscopic ellipsometry (SE), Rutherford backscattering spectrometry analyses (RBSA) and X-ray photoelectron spectroscopy (XPS) in the study of the above mentioned quantities, respectively...
February 12, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
María S Islas, Juan J Martínez Medina, Oscar E Piro, Gustavo A Echeverría, Evelina G Ferrer, Patricia A M Williams
Coumarins (2H-chromen-2-one) are oxygen-containing heterocyclic compounds that belong to the benzopyranones family. In this work we have synthesized different coordination complexes with coumarin-3-carboxylic acid (HCCA), o-phenanthroline (phen) and zinc(II). In the reported [Zn(CCA)2 (H2 O)2 ] complex, coumarin-3-carboxylate (CCA) is acting as a bidentate ligand while in the two prepared complexes, [Zn(phen)3 ]CCA(NO3 ) (obtained as a single crystal) and [Zn(CCA)2 phen].4H2 O, CCA is acting as a counterion of the complex cation [Zn(phen)3 ]+2 or coordinated to the metal center along with phen, respectively...
March 7, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
A Garbout, M Férid
Considering the features in changing the structure and properties of rare earth titanates pyrochlores, the substituted Dy2 Ti2 O7 may be very attractive for various applications. Effect of Sm and Y substitution on the structural properties of Dy2 Ti2 O7 ceramic was established. These ceramics were prepared by solid-state reaction and characterized by X-ray diffraction and Raman spectroscopy. Both analysis show that YDyTi2 O7 with the pyrochlore structure is obtained after heating at 1400°C, but SmDyTi2 O7 has already formed after sintering at 1200°C...
March 10, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Gillian A Ryan, Sarah M Nicholson, John J Morrison
Vaginal birth after caesarean (VBAC) delivery remains a controversial topic, and one for which there is a lack of robust data to guide clinicians and parturients regarding their best option for mode of delivery in a subsequent pregnancy. In many developed countries the trend observed in recent years is that of progressively reduced VBAC rates, and hence increased use of elective repeat caesarean section (ERCS). This factor has contributed, more than any other, to the disproportionately high caesarean section (CS) rates in many countries...
March 7, 2018: European Journal of Obstetrics, Gynecology, and Reproductive Biology
Alberto Gil de la Fuente, Joanna Godzien, Mariano Fernández López, Francisco J Rupérez, Coral Barbas, Abraham Otero
CEU Mass Mediator (CMM) is an on-line tool for aiding researchers when performing metabolite annotation. Its database is comprised of 279,318 real compounds integrated from several metabolomic databases including Human Metabolome Database (HMDB), KEGG and LipidMaps and 672,042 simulated compounds from MINE. In addition, CMM scores the annotations which matched the query parameters using 122 rules based on expert knowledge. This knowledge, obtained from the Centre for Metabolomics and Bioanalysis (CEMBIO) and from a literature review, enables CMM expert system to automatically extract evidence to support or refute the annotations by checking relationships among them...
February 23, 2018: Journal of Pharmaceutical and Biomedical Analysis
Hilal Ahmad Parray, Jameel Lone, Jong Pil Park, Jang Won Choi, Jong Won Yun
OBJECTIVE: The aim of this study was to explore the browning and antioxidative effects of magnolol in 3T3-L1 adipocytes, as recruitment of beige-like adipocytes (browning) by natural compounds is being considered as a promising strategy to fight against obesity. METHODS: Magnolol-induced browning effect was evaluated by determining the expression levels of specific marker genes and proteins using real-time polymerase chain reaction and immunoblotting, respectively...
February 5, 2018: Nutrition
Shelley HuaLei Zhang, Stephan E Maier, Lawrence P Panych
PURPOSE: Magnetic resonance spectroscopic imaging (MRSI), under low-spatial resolution settings, often suffers signal contamination from neighboring voxels due to ringing artifacts. Spatial localization can be improved by constraining the point-spread-function (PSF). Here the effectiveness of the two-dimensional PSF-Choice technique in providing improved spatial localization for MRSI is demonstrated. THEORY AND METHODS: The PSF-Choice technique constrains the PSF to a desired shape by manipulating the weighting of RF excitation pulse throughout phase-encode steps...
March 3, 2018: Journal of Magnetic Resonance
Samuel Mesihää, Ilpo Rasanen, Ilkka Ojanperä
Gas chromatography (GC) hyphenated with nitrogen chemiluminescence detection (NCD) and quadrupole time-of-flight mass spectrometry (QTOFMS) was applied for the first time to the quantitative analysis of new psychoactive substances (NPS) in urine, based on the N-equimolar response of NCD. A method was developed and validated to estimate the concentrations of three metabolites of the common stimulant NPS α-pyrrolidinovalerophenone (α-PVP) in spiked urine samples, simulating an analysis having no authentic reference standards for the metabolites and using the parent drug instead for quantitative calibration...
February 27, 2018: Forensic Science International
Ya'nan Liu, Na Liu, Yuning Chen, Weifeng Zhang, Ruixiang Qu, Qingdong Zhang, Tzungyu-Shih, Lin Feng, Yen Wei
Food waste water is one of the most urgent environmental problems for the close connection between food and our daily life. Herein, we use a simple hydrothermal method to prepare a highly efficient catalyst-CeO2 /Co3 O4 compound on the stainless steel mesh, aiming for food waste water treatment. Possessing the superhydrophilic property and catalytic ability under ultraviolet light, CeO2 /Co3 O4 coated mesh has successfully processed three representative contaminants in food wastewater, which are soybean oil (food oil), AR (food dye) and VA (food flavor) simultaneously with an one-step filtration...
March 9, 2018: Water Research
Julianne Teresa Djordjevic, Sophie Lev
Invasive fungal diseases pose a serious threat, and new drugs are urgently needed. In this issue of Cell Chemical Biology, Pries et al. (2018) identified benzamide- and picolinamide-based small-molecule inhibitors with antifungal properties, including some active against pathogenic Candida species. These compounds target an essential component of the fungal secretion machinery, suggesting a new approach to antifungal development.
March 15, 2018: Cell Chemical Biology
Meryem Lehbili, Abdulmagid Alabdul Magid, Ahmed Kabouche, Laurence Voutquenne-Nazabadioko, Hamid Morjani, Dominique Harakat, Zahia Kabouche
Eight undescribed triterpenoid saponins, scabiostellatosides A-H, together with three known compounds were isolated from the whole plant of Scabiosa stellata L. Their structures were established by spectroscopic analyses (1D, 2D-NMR and HRESIMS) and chemical methods. Scabiostellatosides A-H were evaluated for their cytotoxicity against human fibrosarcoma cell line (HT1080). Scabiostellatoside F, a heptasaccharide derivative of oleanolic acid, exhibited moderate cytotoxicity against HT1080 cell line with IC50 value of 12...
March 12, 2018: Phytochemistry
Jared T Hammill, Daniel C Scott, Jaeki Min, Michele C Connelly, Gloria Holbrook, Fangyi Zhu, Amy Matheny, Lei Yang, Bhuvanesh Singh, Brenda A Schulman, R Kiplin Guy
We previously discovered and validated a class of piperidinyl ureas that regulate defective in cullin neddylation 1 (DCN1)-dependent neddylation of cullins. Here, we report preliminary structure-activity relationship studies aimed at advancing our high-throughput screen hit into a tractable tool compound for dissecting the effects of acute DCN1-UBE2M inhibition on the NEDD8/cullin pathway. Structure-enabled optimization led to a 100-fold increase in biochemical potency and modestly increased solubility and permeability as compared to our initial hit...
March 16, 2018: Journal of Medicinal Chemistry
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