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Danielle Oliveira Dos Anjos, Eliomara Sousa Sobral Alves, Vinicius Tomaz Gonçalves, Sheila Suarez Fontes, Mateus Lima Nogueira, Ana Márcia Suarez-Fontes, João Batista Neves da Costa, Fabricio Rios-Santos, Marcos André Vannier-Santos
Natural products comprise valuable sources for new antiparasitic drugs. Here we tested the effects of a novel β-lapachone derivative on Trypanosoma cruzi parasite survival and proliferation and used microscopy and cytometry techniques to approach the mechanism(s) underlying parasite death. The selectivity index determination indicate that the compound trypanocidal activity was over ten-fold more cytotoxic to epimastigotes than to macrophages or splenocytes. Scanning electron microscopy analysis revealed that the R72 β-lapachone derivative affected the T...
October 12, 2016: International Journal for Parasitology, Drugs and Drug Resistance
Vasanthanathan Poongavanam, Jacob Kongsted
The high rate of drug resistance as well as the complex biochemical process of the parasite reproduction cycle makes development of new drugs for malaria a very important but challenging task. Falcipain 2 (FL2) and Falcipain 3 (FL3) are the major cysteine protease enzymes that play a central role in providing essential amino acids for the parasite's protein biosynthesis through the hemoglobin hydrolysis process. Selective inhibition of these enzymes is considered as a promising chemotherapeutic target. In the present investigation, the highly efficient linear interaction energy (LIE) method has been parameterized for binding affinity predictions and assessed with a set of 244 compounds for FL2 and FL3 inhibition...
June 26, 2016: Journal of Molecular Graphics & Modelling
Abdulkadir Kocak, Ismail Erol, Muslum Yildiz, Hatice Can
Developing small compound based drugs targeting the β-secretase (BACE) enzyme is one of the most promising strategies in treatment of the Alzheimer's disease. As the enzyme shows the activity based on the acid-base reaction at a very narrow pH range, the protonation state of aspartic acids with the residue number 32 and 228 (Asp32 and Asp228), which forms the active site dyad, along with the protonation state of the ligand (substrate or inhibitor) play very critical role in interactions between the ligand and enzyme...
October 17, 2016: Journal of Molecular Graphics & Modelling
Mostafa M Ghorab, Mansour S Alsaid, Ghada H Al-Ansary, Ghada A Abdel-Latif, Dalal A Abou El Ella
Twenty novel chromene derivatives carrying different sulfonamide moieties (3-22) were designed and synthesized. All the newly prepared compounds were evaluated for their in vitro anticancer activity against breast cancer cell line (T47D). Most of the synthesized compounds showed good to moderate activity (IC50 = 8.8-108.9 μM), where compound 16 (IC50 = 8.8 μM) exhibited higher activity compared to doxorubicin (IC50 = 9.8 μM). In order to determine the mechanism of the anticancer activity in T47D cells, the effect of the most potent compounds (5-8, 11-14, and 16-18) on the aromatase activity was tested...
October 13, 2016: European Journal of Medicinal Chemistry
R Tafer, M Sleiman, A Boulkamh, C Richard
The photolysis of aqueous 5-chlorosalicylic acid (ClSA) and dihydroxybenzoic acid (DHBA), its main photoproduct, was studied to determine the extent of degradation caused by simulated solar light. Photoproducts identification was achieved using high resolution LC-MS and GC-MS. About 40 photoproducts from C19 to C1 were characterized, including a dihydroxycyclopentadienic acid, a ring contraction photoproduct, and numerous carbonyls and carboxylic acid derivatives that were detected thanks to derivatization...
October 15, 2016: Water Research
Yan Li, Mourad Harir, Marianna Lucio, Michael Gonsior, Boris P Koch, Philippe Schmitt-Kopplin, Norbert Hertkorn
Deciphering the molecular codes of dissolved organic matter (DOM) improves our understanding of its role in the global element cycles and its active involvement in ecosystem services. This study demonstrates comprehensive characterization of DOM by an initial polarity-based stepwise solid phase extraction (SPE) with single methanol elution of the cartridges, but separate collection of equal aliquots of eluate. The reduction of molecular complexity in the individual DOM fractions attenuates intermolecular interactions and substantially increases the disposable resolution of any structure selective characterization...
October 14, 2016: Water Research
Philippe Glorennec, Jean-Paul Lucas, Anne-Camille Mercat, Alain-Claude Roudot, Barbara Le Bot
Children are exposed to toxic metals and metalloids via their diet and environment. Our objective was to assess the aggregate chronic exposure of children aged 3-6years, living in France, to As, Cd, Cr, Cu, Mn, Pb, Sb, Sr, and V present in diet, tap water, air, soil and floor dust in the years 2007-2009. Dietary data came from the French Total Diet Study, while concentrations in residential tap water, soil and indoor floor dust came from the 'Plomb-Habitat' nationwide representative survey on children's lead exposure at home...
October 19, 2016: Environment International
Yanjun Liu, Yanting Liu, Hao Li, Xindi Fu, Hanwen Guo, Ruihong Meng, Wenjing Lu, Ming Zhao, Hongtao Wang
Aromatic compounds (ACs) emitted from landfills have attracted a lot of attention of the public due to their adverse impacts on the environment and human health. This study assessed the health risk impacts of the fugitive ACs emitted from the working face of a municipal solid waste (MSW) landfill in China. The emission data was acquired by long-term in-situ samplings using a modified wind tunnel system. The uncertainty of aromatic emissions is determined by means of statistics and the emission factors were thus developed...
October 19, 2016: Environment International
Limin Xiang, Yihai Wang, Xiaomin Yi, Xiangjiu He
Phytochemical investigations of the rhizome of Tupistra chinensis led to the isolation of ten new furostanol saponins along with fourteen known spirostanols. Their chemical structures were elucidated on the basis of spectroscopic and chemical methods, including IR, NMR, MS, and GC analyses. The antiproliferative effects against FaDu and Detroit 562 cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7 were assayed for all the isolated compounds...
October 19, 2016: Steroids
Alexandra Kodadová, Zuzana Vitková, Jarmila Oremusová, Petra Herdová, Anton Ťažký, Peter Mikuš
This work was aimed at a progressive formulation of drugs into chitosan hydrogels. It was taken into consideration that a therapeutic effect of the drugs could be enhanced by a combination of natural compounds with chemical (synthetic) drugs. In this work, sage essential oil (SEO) bicyclic monoterpenes with antiflogistic, antiseptic, and antimycotic properties were combined with terbinafine (TB) having a strong antimycotic activity. Detail optimization of the hydrogel-drugs composition (SEO monoterpenes, TB, chitosan, and polysorbate 80 concentrations), based on permeation experiment and UV absorption/GC-MS analysis of permeated species (eucalyptol, camphor, borneol, thujone, TB) in dialysates, was made...
October 22, 2016: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
Friardi Ismed, Françoise Lohézic-Le Dévéhat, Isabelle Rouaud, Solenn Ferron, Amri Bakhtiar, Joël Boustie
The phytochemical study of Stereocaulon montagneanum harvested in Sumatra (Indonesia) led to the isolation of 11 known compounds including two metabolites not previously described in the genus Stereocaulon, peristictic acid (8) and menegazziaic acid (10). The complete 1H and 13C NMR spectral assignments of stictic acid derivatives are reported with some revisions. Five depsidones belonging to the stictic acid chemosyndrome were superoxide anion scavengers as potent as ascorbic acid and with no toxicity on two human cell lines...
October 22, 2016: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
Guaraci D Cordeiro, Mardiore Pinheiro, Stefan Dötterl, Isabel Alves-Dos-Santos
Bees are the most important diurnal pollinators of angiosperms. In several groups of bees a nocturnal/crepuscular habit was developed, yet, little is known about their role in pollination and whether some plants are adapted specifically to these bees. We used a multidisciplinary approach to investigate the reproductive biology and to understand the role of nocturnal/crepuscular bees in pollination of Campomanesia phaea (Myrtaceae), popularly named cambuci. We studied the floral biology and the breeding system of C...
October 22, 2016: Plant Biology
Patrick R Arsenault, Daisheng Song, Marian Bergkamp, Andrew M Ravaschiere, Bradleigh E Navalsky, Paul M Lieberman, Frank S Lee
The Prolyl Hydroxylase Domain protein (PHD):Hypoxia Inducible Factor (HIF) pathway is the main pathway by which changes in oxygen concentration are transduced to changes in gene expression. In mammals, there are three PHD paralogues, and PHD2 has emerged as a particularly critical one for regulating HIF target genes such as ERYTHROPOIETIN (EPO), which controls red cell mass and hematocrit. PHD2 is distinctive among the three PHDs in that it contains an N-terminal MYND type zinc finger. We have proposed that this zinc finger binds a Pro-Xaa-Leu-Glu (PXLE) motif found in proteins of the HSP90 pathway to facilitate HIF-α hydroxylation...
October 22, 2016: Chembiochem: a European Journal of Chemical Biology
Jingzhao Xia, Guoqiang Yang, Ruijing Zhuge, Yangang Liu, Wanbin Zhang
An iridium-catalyzed asymmetric hydrogenation of unfunctionalized exocyclic C=C bonds was achieved using an axially flexible chiral phosphine-oxazoline ligand, providing the desired (S)-1-benzyl-2,3-dihydro-1H-indene products with up to 98% ee. This represents the first general hydrogenation of unfunctionalized exocyclic olefins with the highest selectivity reported thus far. The additive acetate ion plays an important role in the reaction's high enantioselectivity. The chiral product can be further transformed to key intermediates required for the synthesis of an important insecticide and a drug compound...
October 22, 2016: Chemistry: a European Journal
N Kantaria, I Pantsulaia, I Andronikashvili, G Simonia
This investigation differentiates types of essential hypertension in a Georgian population as well as describes endogenous cardiotonic steroids in salt-sensitive and salt-resistant subjects. This case control study included 185 subjects: 94 cases with stage 1 essential hypertension (JNC7) naïve to antihypertensive treatment, and 91 controls. A salt-sensitivity test was used to dichotomize case and control groups into salt-sensitive and salt-resistant subgroups. Blood and urine samples were obtained to categorize participants as consuming high and low salt diets...
September 2016: Georgian Medical News
N Kantaria, I Pantsulaia, I Andronikashvili, G Simonia
It has been known that salt-sensitivity of blood pressure is defined genetically as well as can be developed secondary to either decreased renal function or by influence of other environmental factors. The aim of the study was to evaluate the possible mechanism for the development of salt-sensitive essential hypertension in the population of Georgia. The Case-Control study included 185 subjects, 94 cases with Essential Hypertension stage I (JNC7) without prior antihypertensive treatment, and 91 controls. Salt-sensitivity test was used to divide both case and control groups into salt-sensitive (n=112) and salt-resistant (n=73) subgroups...
September 2016: Georgian Medical News
Akiko Asada, Takahiro Doi, Takaomi Tagami, Akihiro Takeda, Yoshiyuki Sawabe
N-(1-adamantyl)-1-pentyl-1H-indazole-3-carboxamide (APINACA) and N-(1-adamantyl)-1-pentyl-1H-indole-3-carboxamide (APICA) are carboxamide-type synthetic cannabinoids comprising indazole/indole-3-carboxylic acid and adamantan-1-amine moieties. However, in the case of compounds like APINACA or APICA, adamantyl positional isomers exist, wherein either adamantan-1-amine or adamantan-2-amine is present. These adamantyl positional isomers have not been reported in previous studies, and no analytical data are available yet...
October 21, 2016: Drug Testing and Analysis
Omar Santana-Méridas, Azucena González-Coloma, Maria Fe Andrés, Veroniki P Vidali, Moschos G Polissiou, Athanasios C Kimbaris
Essential oils from Greek Mentha species showed different chemical compositions for two populations of M. pulegium, characterized by piperitone and pulegone. M. spicata essential oil was characterized by endocyclic piperitenone epoxide, piperitone epoxide, and carvone. The bioactivities of these essential oils and their components have been tested against insect pests (Leptinotarsa decemlineata, Spodoptera littoralis and Myzus persicae), root-knot nematodes (Meloydogine javanica) and plants (Lactuca sativa, Lolium perenne, Solanum lycopersicum)...
October 21, 2016: Chemistry & Biodiversity
Sachin C Sarode, Gargi S Sarode, Rahul Anand, Shankargouda Patil, Hemant Unadkat
BACKGROUND: The aim of the present study was to find out the efficacy of WhatsApp application for obtaining second opinion on histopathological diagnosis in oral pathology practice. METHODS: A total of 247 cases comprising of 34 different oral pathologies were photomicrographed using smartphone cameras through compound microscopes and sent for second opinion diagnosis (SOD) to 20 different oral pathologists using WhatsApp. RESULTS: Out of 4795 (97...
October 22, 2016: Journal of Oral Pathology & Medicine
Hong Shang, Subramaniam Sukumar, Cornelius von Morze, Robert A Bok, Irene Marco-Rius, Adam Kerr, Galen D Reed, Eugene Milshteyn, Michael A Ohliger, John Kurhanewicz, Peder E Z Larson, John M Pauly, Daniel B Vigneron
PURPOSE: Balanced steady-state free precession (bSSFP) sequences can provide superior signal-to-noise ratio efficiency for hyperpolarized (HP) carbon-13 ((13) C) magnetic resonance imaging by efficiently utilizing the nonrecoverable magnetization, but managing their spectral response is challenging in the context of metabolic imaging. A new spectrally selective bSSFP sequence was developed for fast imaging of multiple HP (13) C metabolites with high spatiotemporal resolution. THEORY AND METHODS: This novel approach for bSSFP spectral selectivity incorporates optimized short-duration spectrally selective radiofrequency pulses within a bSSFP pulse train and a carefully chosen repetition time to avoid banding artifacts...
October 21, 2016: Magnetic Resonance in Medicine: Official Journal of the Society of Magnetic Resonance in Medicine
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