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https://www.readbyqxmd.com/read/28429292/preparation-of-chloramphenicol-amino-acid-combinations-exhibiting-enhanced-dissolution-rates-and-reduced-drug-induced-oxidative-stress
#1
Vanesa B Sterren, Virginia Aiassa, Claudia Garnero, Yamila Garro Linck, Ana K Chattah, Gustavo A Monti, Marcela R Longhi, Ariana Zoppi
Chloramphenicol is an old antibiotic agent that is re-emerging as a valuable alternative for the treatment of multidrug-resistant pathogens. However, it exhibits suboptimal biopharmaceutical properties and toxicity profiles. In this work, chloramphenicol was combined with essential amino acids (arginine, cysteine, glycine, and leucine) with the aim of improving its dissolution rate and reduce its toxicity towards leukocytes. The chloramphenicol/amino acid solid samples were prepared by freeze-drying method and characterized in the solid state by using Fourier transform infrared spectroscopy, powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and solid-state nuclear magnetic resonance...
April 20, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28425152/nmr-structures-and-molecular-dynamics-simulation-of-hylin-a1-peptide-analogs-interacting-with-micelles
#2
Edson Crusca, Amanda Souza Câmara, Carolina Oliveira Matos, Reinaldo Marchetto, Eduardo Maffud Cilli, Luciano Morais Lião, Aline Lima de Oliveira
Antimicrobial peptides are recognized candidates with pharmaceutical potential against epidemic emerging multi-drug resistant bacteria. In this study, we use nuclear magnetic resonance spectroscopy and molecular dynamics simulations to determine the unknown structure and evaluate the interaction with dodecylphosphatidylcholine (DPC) and sodium dodecylsulphate (SDS) micelles with three W(6) -Hylin-a1 analogs antimicrobial peptides (HyAc, HyK, and HyD). The HyAc, HyK, and HyD bound to DPC micelles are all formed by a unique α-helix structure...
April 20, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28423670/invasive-fusobacterium-nucleatum-activates-beta-catenin-signaling-in-colorectal-cancer-via-a-tlr4-p-pak1-cascade
#3
Yongyu Chen, Yan Peng, Jiahui Yu, Ting Chen, Yaxin Wu, Lei Shi, Qing Li, Jiao Wu, Xiangsheng Fu
The underlying mechanism of Fusobacterium nucleatum (Fn) in the carcinogenesis of colorectal cancer (CRC) is poorly understood. Here, we examined Fn abundance in CRC tissues, as well as β-catenin, TLR4 and PAK1 protein abundance in Fn positive and Fn negative CRCs. Furthermore, we isolated a strain of Fn (F01) from a CRC tissue and examined whether Fn (F01) infection of colon cancer cells activated β-catenin signaling via the TLR4/P-PAK1/P-β-catenin S675 cascade. Invasive Fn was abundant in 62.2% of CRC tissues...
March 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28416656/effect-of-cholesterol-on-the-molecular-structure-and-transitions-in-a-clinical-grade-lung-surfactant-extract
#4
Jenny Marie Andersson, Carl Grey, Marcus Larsson, Tiago Mendes Ferreira, Emma Sparr
The lipid-protein film covering the interface of the lung alveolar in mammals is vital for proper lung function and its deficiency is related to a range of diseases. Here we present a molecular-level characterization of a clinical-grade porcine lung surfactant extract using a multitechnique approach consisting of [Formula: see text]-[Formula: see text] solid-state nuclear magnetic spectroscopy, small- and wide-angle X-ray scattering, and mass spectrometry. The detailed characterization presented for reconstituted membranes of a lung extract demonstrates that the molecular structure of lung surfactant strongly depends on the concentration of cholesterol...
April 17, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28415422/synthesis-and-characterization-of-redox-sensitive-heparin-%C3%AE-sitosterol-micelles-their-application-as-carriers-for-the-pharmaceutical-agent-doxorubicin-and-investigation-of-their-antimetastatic-activities-in-vitro
#5
Tilahun Ayane Debele, Shewaye Lakew Mekuria, Hsieh-Chih Tsai
Although there are several clinical attempts to treat tumors at the primary site, only few therapies can inhibit the spread of metastatic cancers. In this study, we synthesized redox-sensitive heparin-β-sitosterol micelles that show antimetastatic activity. Proton nuclear magnetic resonance and Fourier transform infrared analyses confirmed the formation of bioreducible heparin-β-sitosterol (bHSC) conjugates, whereas dynamic light scattering was used to measure the particle size and zeta potential. Both 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and flow cytometry assays confirmed the low toxicity of the synthesized micelles...
June 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28401469/bioactive-amento-flavone-isolated-from-cassia-fistula-l-leaves-exhibits-therapeutic-efficacy
#6
M Srividhya, H Hridya, V Shanthi, K Ramanathan
Novel natural compounds endowed with sound bioactivities are currently the utmost need as leads toward drug discovery. For the first time, here, we report the presence of Amentoflavone (biflavonoid) in the leaves of Cassia fistula L. Structural characterization was carried out using ultraviolet-visible spectrophotometer, Fourier transform infrared, nuclear magnetic resonance, and thin-layer chromatography. The isolated compound was further evaluated for its bioactivity. The compound demonstrated moderate cytotoxicity in liver carcinoma (HepG2) cells, and the comparative analysis for the standard and normal compound has also been validated...
May 2017: 3 Biotech
https://www.readbyqxmd.com/read/28396564/structural-analysis-of-the-glucocorticoid-receptor-ligand-binding-domain-in-complex-with-triamcinolone-acetonide-and-a-fragment-of-the-atypical-coregulator-shp
#7
Emily R Weikum, Denise C Okafor, Emma H D'Agostino, Jennifer K Colucci, Eric A Ortlund
The synthetic glucocorticoids (GCs) dexamethasone, mometasone furoate, and triamcinolone acetonide have been pharmaceutical mainstays to treat chronic inflammatory diseases. These drugs bind to the glucocorticoid receptor (GR), a ligand- activated transcription factor and member of the nuclear receptor superfamily. GR is widely recognized as a therapeutic target for its ability to counter pro-inflammatory signaling. Despite the popularity of GCs in the clinic, long-term use leads to numerous side effects, driving the need for new and improved drugs with less off-target pharmacology...
April 10, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28393270/mitochondrial-dna-variants-in-colorectal-carcinogenesis-drivers-or-passengers
#8
REVIEW
Edoardo Errichiello, Tiziana Venesio
INTRODUCTION: Mitochondrial DNA alterations have widely been reported in many age-related degenerative diseases and tumors, including colorectal cancer. In the past few years, the discovery of inter-genomic crosstalk between nucleus and mitochondria has reinforced the role of mitochondrial DNA variants in perturbing this essential signaling pathway and thus indirectly targeting nuclear genes involved in tumorigenic and invasive phenotype. FINDINGS: Mitochondrial dysfunction is currently considered a crucial hallmark of carcinogenesis as well as a promising target for anticancer therapy...
April 9, 2017: Journal of Cancer Research and Clinical Oncology
https://www.readbyqxmd.com/read/28393216/cancer-induced-cardiac-cachexia-pathogenesis-and-impact-of-physical-activity-review
#9
Yassine Belloum, Françoise Rannou-Bekono, François B Favier
Cachexia is a wasting syndrome observed in many patients suffering from several chronic diseases including cancer. In addition to the progressive loss of skeletal muscle mass, cancer cachexia results in cardiac function impairment. During the severe stage of the disease, patients as well as animals bearing cancer cells display cardiac atrophy. Cardiac energy metabolism is also impeded with disruption of mitochondrial homeostasis and reduced oxidative capacity, although the available data remain equivocal. The release of inflammatory cytokines by tumor is a key mechanism in the initiation of heart failure...
May 2017: Oncology Reports
https://www.readbyqxmd.com/read/28390998/on-the-use-of-positron-counting-for-radio-assay-in-nuclear-pharmaceutical-production
#10
D Maneuski, F Giacomelli, C Lemaire, S Pimlott, A Plenevaux, J Owens, V O'Shea, A Luxen
Current techniques for the measurement of radioactivity at various points during PET radiopharmaceutical production and R&D are based on the detection of the annihilation gamma rays from the radionuclide in the labelled compound. The detection systems to measure these gamma rays are usually variations of NaI or CsF scintillation based systems requiring costly and heavy lead shielding to reduce background noise. These detectors inherently suffer from low detection efficiency, high background noise and very poor linearity...
March 24, 2017: Applied Radiation and Isotopes
https://www.readbyqxmd.com/read/28382686/methylparaben-induced-decrease-in-collagen-production-and-viability-of-cultured-human-dermal-fibroblasts
#11
Natalia Majewska, Ilona Zaręba, Arkadiusz Surażyński, Anna Galicka
Parabens owing to their many advantageous properties are widely applied in cosmetics, food products and pharmaceuticals. However, recent research results have shown that they possess the ability to accumulate in the human body and exert many adverse effects. In this study, the impact of methylparaben (MP) as the most frequently used preservative in cosmetics, on human dermal fibroblasts and collagen production was evaluated. In cells treated with 0.01, 0.03 and 0.05% MP a dose-dependent decrease in collagen biosynthesis was revealed, which was positively correlated with the activity of prolidase responsible for the recovery of proline...
April 6, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/28363028/spectroscopic-investigation-of-the-formation-and-disruption-of-hydrogen-bonds-in-pharmaceutical-semicrystalline-dispersions
#12
Tu Van Duong, Gunter Reekmans, Akkaladevi Venkatesham, Arthur Van Aerschot, Peter Adriaensens, Jan Van Humbeeck, Guy Van den Mooter
We recently found that indomethacin (IMC) can effectively act as a powerful crystallization inhibitor for polyethylene glycol 6000 (PEG) despite the fact that the absence of interactions between the drug and the carrier in the solid state was reported in the literature. However, in the present study, we investigate the possibility of drug-carrier interactions in the liquid state to explain the polymer crystallization inhibition effect of IMC. We also aim to discover other potential PEG crystallization inhibitors...
April 11, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28359887/preparation-and-characterization-of-aminoethyl-hydroxypropyl-starch-modified-with-collagen-peptide
#13
Huigao Wen, Jin Hu, Hongyu Ge, Shengqiong Zou, Yao Xiao, Ya Li, Han Feng, Lihong Fan
The preparation of aminoethyl hydroxypropyl starch collagen peptide (AEHPS-COP) was via an enzyme-catalyzed reaction between amino groups in aminoethyl hydroxypropyl starch (AEHPS) and γ-carboxamide groups in collagen peptide (COP) by using microbial transglutaminase (MTGase) as biocatalyst. As an intermediate reactant, AEHPS was synthesized from hydroxypropyl starch (HPS) and 2-chloroethylamine hydrochloride (CEH). The chemical structures of HPS, AEHPS and AEHPS-COP were characterized by Fourier transform infrared spectroscopy (FT-IR) and (13)C nuclear magnetic resonance ((13)C NMR)...
March 27, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28357920/investigation-of-the-sensitivity-of-transmission-raman-spectroscopy-for-polymorph-detection-in-pharmaceutical-tablets
#14
Hanzhou Feng, Robert W Bondi, Carl A Anderson, James K Drennen, Benoît Igne
Polymorph detection is critical for ensuring pharmaceutical product quality in drug substances exhibiting polymorphism. Conventional analytical techniques such as X-ray powder diffraction and solid-state nuclear magnetic resonance are utilized primarily for characterizing the presence and identity of specific polymorphs in a sample. These techniques have encountered challenges in analyzing the constitution of polymorphs in the presence of other components commonly found in pharmaceutical dosage forms. Laborious sample preparation procedures are usually required to achieve satisfactory data interpretability...
January 1, 2017: Applied Spectroscopy
https://www.readbyqxmd.com/read/28353211/current-status-of-stress-myocardial-perfusion-imaging-pharmaceuticals-and-radiation-exposure-in-japan-results-from-a-nationwide-survey
#15
Ryuto Otsuka, Narumi Kubo, Yosuke Miyazaki, Mio Kawahara, Jun Takaesu, Kazuki Fukuchi
BACKGROUND: Ionizing radiation generated during medical imaging procedures is a matter of concern. However, the current status of radiopharmaceutical use in stress myocardial perfusion imaging (MPI) and the radiation exposure from these radiopharmaceuticals is unknown in Japan. METHODS AND RESULTS: A nationwide survey was conducted from June through July 2016. The questionnaires on the radiopharmaceuticals used and their administered doses during stress MPI were sent to 641 nuclear medicine facilities...
March 28, 2017: Journal of Nuclear Cardiology: Official Publication of the American Society of Nuclear Cardiology
https://www.readbyqxmd.com/read/28347799/ursolic-acid-attenuates-cigarette-smoke-induced-emphysema-in-rats-by-regulating-perk-and-nrf2-pathways
#16
Lin Li, Yan Yin, Gang Hou, Dan Han, Jian Kang, Qiuyue Wang
OBJECTIVE: Ursolic acid (UA) is widely distributed in natural plants to against oxidation, virus, inflammation, tumor, and has been widely used in the pharmaceutical and cosmetics. However, its effect on emphysema of chronic obstructive pulmonary disease (COPD) is unknown. Unfolded protein response is involved in pathogenesis of COPD through PERK pathway. Nuclear erythroid-related factor 2 (Nrf2) regulates antioxidant defensive mechanism in COPD. This study was to explore effect and mechanism of UA on cigarette smoke (CS)-induced rat emphysema...
March 24, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28344580/a-perspective-on-the-development-of-plant-made-vaccines-in-the-fight-against-ebola-virus
#17
REVIEW
Sergio Rosales-Mendoza, Ricardo Nieto-Gómez, Carlos Angulo
The Ebola virus (EBOV) epidemic indicated a great need for prophylactic and therapeutic strategies. The use of plants for the production of biopharmaceuticals is a concept being adopted by the pharmaceutical industry, with an enzyme for human use currently commercialized since 2012 and some plant-based vaccines close to being commercialized. Although plant-based antibodies against EBOV are under clinical evaluation, the development of plant-based vaccines against EBOV essentially remains an unexplored area...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28339201/high-throughput-in-silico-structure-validation-and-revision-of-halogenated-natural-products-is-enabled-by-parametric-corrections-to-dft-computed-13-c-nmr-chemical-shifts-and-spin-spin-coupling-constants
#18
Andrei G Kutateladze, D Sai Reddy
Halogenated natural products constitute diverse and promising feedstock for molecular pharmaceuticals. However, their solution-structure elucidation by NMR presents several challenges, including the lack of fast methods to compute (13)C chemical shifts for carbons bearing heavy atoms. We show that parametric corrections to DFT-computed chemical shifts in conjunction with rff-computed spin-spin coupling constants allow for fast and reliable screening of a large number of reported halogenated natural products, resulting in expedient structure validation or revision...
March 24, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28332354/cyclized-oligopeptide-targeting-lrp5-6-dkk1-interaction-reduces-the-growth-of-tumor-burden-in-a-multiple-myeloma-mouse-model
#19
Bo Mi Park, Eun Jin Kim, Hee Jin Nam, Dongdong Zhang, Chu Hyun Bae, Myeongmo Kang, Heeyoun Kim, Weontae Lee, Bjarne Bogen, Sung Kil Lim
PURPOSE: Dickkopf 1 (DKK1) has been extensively investigated in mouse models of multiple myeloma, which results in osteolytic bone lesions. Elevated DKK1 levels in bone marrow plasma and serum inhibit the differentiation of osteoblast precursors. Present pharmaceutical approaches to target bone lesions are limited to antiresorptive agents. In this study, we developed a cyclized oligopeptide against DKK1-low density lipoprotein receptor-related protein (LRP) 5/6 interaction and tested the effects of the oligopeptide on tumor burden...
May 2017: Yonsei Medical Journal
https://www.readbyqxmd.com/read/28327439/an-in-silico-functional-annotation-and-screening-of-potential-drug-targets-derived-from-leishmania-spp-hypothetical-proteins-identified-by-immunoproteomics
#20
Miguel A Chávez-Fumagalli, Mônica S Schneider, Daniela P Lage, Ricardo A Machado-de-Ávila, Eduardo A F Coelho
Leishmaniasis is a parasitic disease caused by the protozoan of the Leishmania genus. While no human vaccine is available, drugs such as pentavalent antimonials, pentamidine and amphotericin B are used for treat the patients. However, the high toxicity of these pharmaceutics, the emergence of parasite resistance and/or their high cost have showed to the urgent need of identify new targets to be employed in the improvement of the treatment against leishmaniasis. In a recent immunoproteomics approach performed in the Leishmania infantum species, 104 antigenic proteins were recognized by antibodies in sera of visceral leishmaniasis (VL) dogs...
May 2017: Experimental Parasitology
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