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Chemical biology

K Anand, C Tiloke, A Phulukdaree, B Ranjan, A Chuturgoon, S Singh, R M Gengan
The biosynthesis of nanostructured biopalladium nanoparticles (PdNPs) from an aqueous solution of crystalline palladium acetate is reported. For the synthesised PdNPs in solution, an agroforest biomass waste petal of Moringa oleifera derived bis-phthalate was used as natural reducing and biocapping agents. Continuous absorption in the UV region and subsequent brown colour change confirmed the formation of PdNPs. A strong surface plasmon peak for PdNPs occurred at 460nm. PdNPs were characterized by SEM with EDX, FTIR, TEM and DLS...
September 29, 2016: Journal of Photochemistry and Photobiology. B, Biology
Meghan L M Fuzzen, Leslie M Bragg, Gerald R Tetreault, Paulina A Bahamonde, Rajiv N Tanna, Charles J Bennett, Mark E McMaster, Mark R Servos
Municipal wastewater effluent (MWWE) and its constituents, such as chemicals of emerging concern, pose a potential threat to the sustainability of fish populations by disrupting key endocrine functions in aquatic organisms. While studies have demonstrated changes in biological markers of exposure of aquatic organisms to groups of chemicals of emerging concern, the variability of these markers over time has not been sufficiently described in wild fish species. The aim of this study was to assess the spatial and temporal variability of biological markers in response to MWWE exposure and to test the consistency of these responses between seasons and among years...
2016: PloS One
Tae Soup Shim, Zaki G Estephan, Zhaoxia Qian, Jacob H Prosser, Su Yeon Lee, David M Chenoweth, Daeyeon Lee, So-Jung Park, John C Crocker
Active materials that respond to physical and chemical stimuli can be used to build dynamic micromachines that lie at the interface between biological systems and engineered devices. In principle, the specific hybridization of DNA can be used to form a library of independent, chemically driven actuators for use in such microrobotic applications and could lead to device capabilities that are not possible with polymer- or metal-layer-based approaches. Here, we report shape changing films that are powered by DNA strand exchange reactions with two different domains that can respond to distinct chemical signals...
October 24, 2016: Nature Nanotechnology
Michael J Waring, Huawei Chen, Alfred A Rabow, Graeme Walker, Romel Bobby, Scott Boiko, Rob H Bradbury, Rowena Callis, Edwin Clark, Ian Dale, Danette L Daniels, Austin Dulak, Liz Flavell, Geoff Holdgate, Thomas A Jowitt, Alexey Kikhney, Mark McAlister, Jacqui Méndez, Derek Ogg, Joe Patel, Philip Petteruti, Graeme R Robb, Matthew B Robers, Sakina Saif, Natalie Stratton, Dmitri I Svergun, Wenxian Wang, David Whittaker, David M Wilson, Yi Yao
Proteins of the bromodomain and extraterminal (BET) family, in particular bromodomain-containing protein 4 (BRD4), are of great interest as biological targets. BET proteins contain two separate bromodomains, and existing inhibitors bind to them monovalently. Here we describe the discovery and characterization of probe compound biBET, capable of engaging both bromodomains simultaneously in a bivalent, in cis binding mode. The evidence provided here was obtained in a variety of biophysical and cellular experiments...
October 24, 2016: Nature Chemical Biology
Jin Xu, Xia-Fei Wang, Peng Chen, Fang-Tao Liu, Shuai-Chao Zheng, Hui Ye, Ming-He Mo
The vast majority of lepidopterans, about 90%, are moths. Some moths, particularly their caterpillars, are major agricultural and forestry pests in many parts of the world. However, some other members of moths, such as the silkworm Bombyx mori, are famous for their economic value. Fire et al. in 1998 initially found that exogenous double-stranded RNA (dsRNA) can silence the homolog endogenous mRNA in organisms, which is called RNA interference (RNAi). Soon after, the RNAi technique proved to be very promising not only in gene function determination but also in pest control...
October 19, 2016: Genes
Ali Ghanchi
On Friday, November 13, 2015, Paris was subjected to a multiple terrorist attack that caused widespread carnage. Although French emergency planning, response, and resilience procedures (Plan Blanc) anticipated crisis management of a major incident, these had to be adapted to the local context of Pitié-Salpêtrière University Teaching Hospital. Health care workers had undergone Plan Blanc training and exercises and it was fortunate that such a drill had occurred on the morning of the attack. The procedures were observed to work well because this type of eventuality had been fully anticipated, and staff performance exceeded expectations owing to prior in-depth training and preparations...
October 2016: Disaster Medicine and Public Health Preparedness
Niloofar Eslahi, Marjan Abdorahim, Abdolreza Arash Simchi
Stimuli responsive hydrogels (SRHs) are attractive bio-scaffolds for tissue engineering. The structural similarity of SRHs to the extracellular matrix (ECM) of many tissues offers great advantages for a minimally invasive tissue repair. Among various potential applications of SRHs, cartilage regeneration has attracted significant attention. The repair of cartilage damage is challenging in orthopedics owing to its low repair capacity. Recent advances include development of injectable hydrogels to minimize invasive surgery with nanostructured features and rapid stimuli-responsive characteristics...
October 24, 2016: Biomacromolecules
Heinrich Krobath, Tao Chen, Hue Sun Chan
Volumetric properties of proteins bear directly on their biological functions in hyperbaric environments and are useful in general as a biophysical probe. To gain insight into conformation-dependent protein volume, we developed an implicit-solvent atomic chain model that transparently embodies two physical origins of volume. First, a fundamental geometric term capturing the van der Waals volume of the protein and the particulate, finite-size nature of the water molecules, modeled together by the volume encased by the protein's molecular surface...
October 24, 2016: Biochemistry
Paolo Cifani, Alex Kentsis
Given superior analytical features, mass spectrometry proteomics is well suited for the basic investigation and clinical diagnosis of human disease. Modern mass spectrometry enables detailed functional characterization of the pathogenic biochemical processes, as achieved by accurate and comprehensive quantification of proteins and their regulatory chemical modifications. Here, we describe how high-accuracy mass spectrometry in combination with high-resolution chromatographic separations can be leveraged to meet these analytical requirements in a mechanism-focused manner...
October 24, 2016: Proteomics
Giulia Morgese, Lucca Trachsel, Matteo Romio, Mohammad Divandari, Shivaprakash N Ramakrishna, Edmondo M Benetti
The cyclic polymer topology strongly alters the interfacial, physico-chemical properties of polymer brushes, when compared to the linear counterparts. In this study, we especially concentrated on poly-2-ethyl-2-oxazoline (PEOXA) cyclic and linear grafts assembled on titanium oxide surfaces by the "grafting-to" technique. The smaller hydrodynamic radius of ring PEOXAs favors the formation of denser brushes with respect to linear analogs. Denser and more compact cyclic brushes generate a steric barrier that surpasses the typical entropic shield by a linear brush...
October 24, 2016: Angewandte Chemie
Kyung Suk Lee, Lucy E Lee, Erel Levine
Small animals such as the roundworm C. elegans are excellent models for studying bacterial infection and host response, as well as for genetic and chemical screens. A key methodology is the killing assay, in which the number of surviving animals is tracked as a function of the time post infection. This is a labor-intensive procedure, prone to human error and subjective choices, and often involves undesired perturbation to the animals and their environment. In addition, the survival of animals is just one aspect of a multi-dimensional complex biological process...
October 24, 2016: Scientific Reports
Jonghoon Kim, Jinjoo Jung, Jaeyoung Koo, Wansang Cho, Won Seok Lee, Chanwoo Kim, Wonwoo Park, Seung Bum Park
Diversity-oriented synthesis (DOS) can provide a collection of diverse and complex drug-like small molecules, which is critical in the development of new chemical probes for biological research of undruggable targets. However, the design and synthesis of small-molecule libraries with improved biological relevance as well as maximized molecular diversity represent a key challenge. Herein, we employ functional group-pairing strategy for the DOS of a chemical library containing privileged substructures, pyrimidodiazepine or pyrimidine moieties, as chemical navigators towards unexplored bioactive chemical space...
October 24, 2016: Nature Communications
Susanna Piluso, Al Halifa Soultan, Jennifer Patterson
BACKGROUND: Polymer-based systems are attractive in drug delivery and regenerative medicine due to the possibility of tailoring their properties and functions to a specific application. METHODS: The present review provides several examples of molecularly engineered polymer systems, including stimuli responsive polymers and supramolecular polymers. RESULTS: The advent of controlled polymerization techniques has enabled the preparation of polymers with controlled molecular weight and well-defined architecture...
October 21, 2016: Current Pharmaceutical Design
Marcello Locatelli, Gokhan Zengin, Ahmet Uysal, Simone Carradori, Elisa De Luca, Giuseppe Bellagamba, Abdurrahman Aktumsek, Irina Lazarova
The current study was carried out to evaluate multicomponent pattern, biological and enzymatic activities of seven Asphodeline taxa root extracts as useful ingredients, due to the fact that these plants are commonly used as traditional food supplements in Turkish regions. The extracts were characterized for free anthraquinones and phenolics to obtain a specific chemical fingerprint useful for quality control. These analyzes were coupled to biological and enzymatic activities in order to obtain comprehensive information of the natural product...
October 24, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Emilie Evain-Bana, Lucie Schiavo, Christophe Bour, Don Antoine Lanfranchi, Simone Berardozzi, Francesca Ghirga, Denyse Bagrel, Bruno Botta, Gilles Hanquet, Mattia Mori
The cell division cycle 25 phosphatases (CDC25A, B, and C; E.C. are key regulator of the cell cycle in human cells. Their aberrant expression has been associated with the insurgence and development of various types of cancer, and with a poor clinical prognosis. Therefore, CDC25 phosphatases are a valuable target for the development of small molecule inhibitors of therapeutic relevance. Here, we used an integrated strategy mixing organic chemistry with biological investigation and molecular modeling to study novel quinonoid derivatives as CDC25 inhibitors...
October 23, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Teddy Stephen Ehianeta, Stéphane Laval, Biao Yu
Mangiferin (2C-β-d-glucopyranosyl-1,3,6,7-tetrahydroxyxanthone) is a xanthone C-glycoside occurring in many plant species. Composed of a glucose unit C1→2 linked to a 1,3,6,7-tetrahydroxyxanthone aglycone, mangiferin exhibits a wide range of biological activities, which recently renewed its interest as a potential pharmacophore. Mangiferin is mainly isolated after extraction procedures from natural sources alongside with its isoforms isomangiferin, homomangiferin, and neomangiferin. However, enzymatic and chemical approaches have been developed to access these phytochemicals, which address the challenging construction of the C-glycosidic linkage...
September 10, 2016: BioFactors
Eliza de Oliveira Cardoso, Bruno José Conti, Karina Basso Santiago, Fernanda Lopes Conte, Lucas Pires Garcia Oliveira, Rodrigo Tavanelli Hernandes, Marjorie de Assis Golim, José Maurício Sforcin
OBJECTIVES: Propolis is a natural product with a complex chemical composition. Its isolated compounds exert biological activities; however, its synergistic effects are unknown. The involvement of phenolic acids (caffeic - Caf, dihydrocinnamic - Cin and p-coumaric - Cou) alone or in combination was investigated in the action of propolis in human monocytes. METHODS: Cell viability was analysed by MTT assay; TNF-α, IL-6 and IL-10 production by enzyme-linked immunosorbent assay (ELISA); cell markers expression by flow cytometry; colony-forming units were counted to assess the microbicidal activity; and H2 O2 production was analysed by colorimetric assay...
October 24, 2016: Journal of Pharmacy and Pharmacology
Michelle Maclean, John G Anderson, Scott J MacGregor, Tracy White, Chintamani D Atreya
Bacterial contamination of injectable stored biological fluids such as blood plasma and platelet concentrates preserved in plasma at room temperature is a major health risk. Current pathogen reduction technologies (PRT) rely on the use of chemicals and/or ultraviolet light, which affects product quality and can be associated with adverse events in recipients. 405 nm violet-blue light is antibacterial without the use of photosensitizers and can be applied at levels safe for human exposure, making it of potential interest for decontamination of biological fluids such as plasma...
2016: Journal of Blood Transfusion
Boris Pinchuk, Thorsten von Drathen, Viktoria Opel, Christian Peifer
Dabrafenib (Tafinlar) was approved in 2013 by the FDA as a selective single agent treatment for patients with BRAF(V600E) mutation-positive advanced melanoma. One year later, a combination of dabrafenib and trametinib was used for treatment of BRAF(V600E/K) mutant metastatic melanoma. In the present study, we report on hitherto not described photosensitivity of dabrafenib both in organic and aqueous media. The half-lives for dabrafenib degradation were determined. Moreover, we revealed photoinduced chemical conversion of dabrafenib to its planar fluorescent derivative dabrafenib_photo 2...
October 13, 2016: ACS Medicinal Chemistry Letters
Alejandra Prieto-Davó, Tiago Dias, Sofia E Gomes, Sara Rodrigues, Yessica Parera-Valadez, Pedro M Borralho, Florbela Pereira, Cecilia M P Rodrigues, Ilda Santos-Sanches, Susana P Gaudêncio
Marine-derived actinomycetes have demonstrated an ability to produce novel compounds with medically relevant biological activity. Studying the diversity and biogeographical patterns of marine actinomycetes offers an opportunity to identify genera that are under environmental pressures, which may drive adaptations that yield specific biosynthetic capabilities. The present study describes research efforts to explore regions of the Atlantic Ocean, specifically around the Madeira Archipelago, where knowledge of the indigenous actinomycete diversity is scarce...
2016: Frontiers in Microbiology
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